raloxifene

Summary

Summary: A second generation selective estrogen receptor modulator (SERM) used to prevent osteoporosis in postmenopausal women. It has estrogen agonist effects on bone and cholesterol metabolism but behaves as a complete estrogen antagonist on mammary gland and uterine tissue.

Top Publications

  1. ncbi Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial
    Victor G Vogel
    Magee Womens Hospital, University of Pittsburgh School of Medicine, University of Pittsburgh, Pittsburgh, PA 15213 3221, USA
    JAMA 295:2727-41. 2006
  2. ncbi Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women
    Elizabeth Barrett-Connor
    Department of Family and Preventive Medicine, University of California, San Diego, La Jolla 92093 0607, USA
    N Engl J Med 355:125-37. 2006
  3. ncbi Molecular determinants for the tissue specificity of SERMs
    Yongfeng Shang
    Department of Adult Oncology, Dana Farber Cancer Institute, 44 Binney Street, and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    Science 295:2465-8. 2002
  4. ncbi Comparative effects of 17beta-estradiol, raloxifene and genistein on bone 3D microarchitecture and volumetric bone mineral density in the ovariectomized mice
    A Cano
    Department of Pediatrics, Obstetrics and Gynecology, University of Valencia, Valencia, Spain
    Osteoporos Int 19:793-800. 2008
  5. pmc American society of clinical oncology clinical practice guideline update on the use of pharmacologic interventions including tamoxifen, raloxifene, and aromatase inhibition for breast cancer risk reduction
    Kala Visvanathan
    Cancer Policy and Clinical Affairs, 2318 Mill Rd, Suite 800, Alexandria, VA 22314, USA
    J Clin Oncol 27:3235-58. 2009
  6. pmc Effects of the selective estrogen receptor modulator raloxifene on coronary outcomes in the Raloxifene Use for The Heart trial: results of subgroup analyses by age and other factors
    Peter Collins
    Department of Cardiology, Royal Brompton and Harefield NHS Trust and NHLI, Imperial College London, Sydney Street, London, UK
    Circulation 119:922-30. 2009
  7. ncbi The enhanced antiproliferative response to combined treatment of trichostatin A with raloxifene in MCF-7 breast cancer cells and its relevance to estrogen receptor β expression
    Zhenzhen Tu
    Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, People s Republic of China
    Mol Cell Biochem 366:111-22. 2012
  8. ncbi Selective estrogen receptor modulators (SERMS) and their roles in breast cancer prevention
    Woo Chan Park
    Lynn Sage Breast Cancer Research Program, Robert H Lurie Comprehensive Cancer Center, Olson Pavilion 8258, 303 E Chicago Avenue, Chicago, IL 60611, USA
    Trends Mol Med 8:82-8. 2002
  9. ncbi Cardioprotective effects of long-term treatment with raloxifene, a selective estrogen receptor modulator, on myocardial ischemia/reperfusion injury in ovariectomized rats
    Ming Ting Chung
    Center for Reproductive Medicine, Department of Obstetrics and Gynecology, Chi Mei Medical Center, Tainan
    Menopause 17:127-34. 2010
  10. pmc Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal
    Manal A Elsheikh
    Department of Pharmaceutics, Alexandria University, Alexandria, Egypt
    Int J Nanomedicine 7:3787-802. 2012

Research Grants

  1. Theranostic Nanomedicine for Breast Cancer Prevention and Image-Guided Therapy
    Prakash R Rai; Fiscal Year: 2011
  2. Theranostic Nanomedicine for Breast Cancer Prevention and Image-Guided Therapy
    Prakash R Rai; Fiscal Year: 2013
  3. Assessing and modifying bone quality in chronic kidney disease
    Chris Newman; Fiscal Year: 2013
  4. Estrogen receptors in benign prostatic hyperplasia
    TRISTAN MARRINER NICHOLSON; Fiscal Year: 2013
  5. Herb-Drug Glucuronidation Interactions
    Reginald F Frye; Fiscal Year: 2011
  6. The role of HDAC2 in hormone therapy resistance
    Pamela N Munster; Fiscal Year: 2013
  7. Development of BRCA1-mimetic drugs for breast cancer
    Eliot M Rosen; Fiscal Year: 2013
  8. HUMAN CYTOSOLIC SULFOTRANSFERASES
    Charles N Falany; Fiscal Year: 2013
  9. Biointeractions of antiestrogens with nitric oxide
    Gregory R J Thatcher; Fiscal Year: 2013
  10. Regulation of SULT1A1 in Human Breast
    SUSAN A KADLUBAR; Fiscal Year: 2012

Detail Information

Publications340 found, 100 shown here

  1. ncbi Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial
    Victor G Vogel
    Magee Womens Hospital, University of Pittsburgh School of Medicine, University of Pittsburgh, Pittsburgh, PA 15213 3221, USA
    JAMA 295:2727-41. 2006
    Tamoxifen is approved for the reduction of breast cancer risk, and raloxifene has demonstrated a reduced risk of breast cancer in trials of older women with osteoporosis.
  2. ncbi Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women
    Elizabeth Barrett-Connor
    Department of Family and Preventive Medicine, University of California, San Diego, La Jolla 92093 0607, USA
    N Engl J Med 355:125-37. 2006
    The effect of raloxifene, a selective estrogen-receptor modulator, on coronary heart disease (CHD) and breast cancer is not established.
  3. ncbi Molecular determinants for the tissue specificity of SERMs
    Yongfeng Shang
    Department of Adult Oncology, Dana Farber Cancer Institute, 44 Binney Street, and Department of Medicine, Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
    Science 295:2465-8. 2002
    ..The therapeutic effectiveness of SERMs such as tamoxifen and raloxifene in breast cancer depends on their antiestrogenic activity. In the uterus, however, tamoxifen is estrogenic...
  4. ncbi Comparative effects of 17beta-estradiol, raloxifene and genistein on bone 3D microarchitecture and volumetric bone mineral density in the ovariectomized mice
    A Cano
    Department of Pediatrics, Obstetrics and Gynecology, University of Valencia, Valencia, Spain
    Osteoporos Int 19:793-800. 2008
    This study assessed the effect of estradiol, raloxifene and genistein on the preservation of bone 3D-microarchitecture and volumetric bone mineral density (vBMD) in the ovariectomized mouse model...
  5. pmc American society of clinical oncology clinical practice guideline update on the use of pharmacologic interventions including tamoxifen, raloxifene, and aromatase inhibition for breast cancer risk reduction
    Kala Visvanathan
    Cancer Policy and Clinical Affairs, 2318 Mill Rd, Suite 800, Alexandria, VA 22314, USA
    J Clin Oncol 27:3235-58. 2009
    ..Vascular and vasomotor events do not persist post-treatment across all ages. In postmenopausal women, raloxifene and tamoxifen reduce the risk of ER-positive invasive BC with equal efficacy...
  6. pmc Effects of the selective estrogen receptor modulator raloxifene on coronary outcomes in the Raloxifene Use for The Heart trial: results of subgroup analyses by age and other factors
    Peter Collins
    Department of Cardiology, Royal Brompton and Harefield NHS Trust and NHLI, Imperial College London, Sydney Street, London, UK
    Circulation 119:922-30. 2009
    The Raloxifene Use for The Heart (RUTH) trial showed that raloxifene, a selective estrogen receptor modulator, had no overall effect on the incidence of coronary events in women with established coronary heart disease or coronary heart ..
  7. ncbi The enhanced antiproliferative response to combined treatment of trichostatin A with raloxifene in MCF-7 breast cancer cells and its relevance to estrogen receptor β expression
    Zhenzhen Tu
    Department of Biomedical Engineering, School of Life Science and Technology, China Pharmaceutical University, Nanjing 210009, People s Republic of China
    Mol Cell Biochem 366:111-22. 2012
    ..The well-described HDAC inhibitor, trichostatin A (TSA), and antiestrogen raloxifene were found to, respectively, inhibit E2-induced proliferation of MCF-7 breast cancer cell in a dose-responsive ..
  8. ncbi Selective estrogen receptor modulators (SERMS) and their roles in breast cancer prevention
    Woo Chan Park
    Lynn Sage Breast Cancer Research Program, Robert H Lurie Comprehensive Cancer Center, Olson Pavilion 8258, 303 E Chicago Avenue, Chicago, IL 60611, USA
    Trends Mol Med 8:82-8. 2002
    ..b>Raloxifene, a related SERM, is now available to treat osteoporosis and is also being tested as a preventive for breast ..
  9. ncbi Cardioprotective effects of long-term treatment with raloxifene, a selective estrogen receptor modulator, on myocardial ischemia/reperfusion injury in ovariectomized rats
    Ming Ting Chung
    Center for Reproductive Medicine, Department of Obstetrics and Gynecology, Chi Mei Medical Center, Tainan
    Menopause 17:127-34. 2010
    The aim of this study was to investigate the beneficial effect of long-term treatment with raloxifene (RAL), a selective estrogen receptor modulator, on myocardial ischemia/reperfusion (MI/R) injury in ovariectomized (Ovx) rats.
  10. pmc Nanoemulsion liquid preconcentrates for raloxifene hydrochloride: optimization and in vivo appraisal
    Manal A Elsheikh
    Department of Pharmaceutics, Alexandria University, Alexandria, Egypt
    Int J Nanomedicine 7:3787-802. 2012
    b>Raloxifene hydrochloride (RLX) is a selective estrogen-receptor modulator for treatment of osteoporosis and prevention of breast and endometrial cancer. By virtue of extensive presystemic clearance, RLX bioavailability is only 2%...
  11. ncbi Raloxifene, a selective estrogen receptor modulator, induces apoptosis in androgen-responsive human prostate cancer cell line LNCaP through an androgen-independent pathway
    Isaac Yi Kim
    Laboratory of Cell Regulation and Carcinogenesis, National Cancer Institute, Bethesda, Maryland 20892, USA
    Cancer Res 62:3649-53. 2002
    b>Raloxifene, a selective estrogen receptor (ER) modulator, is a mixed estrogen agonist/antagonist that has been shown to prevent osteoporosis and breast cancer in women...
  12. ncbi Selective estrogen receptor modulators decrease reactive astrogliosis in the injured brain: effects of aging and prolonged depletion of ovarian hormones
    George Barreto
    Instituto Cajal, Consejo Superior de Investigaciones Cientificas, Avenida Doctor Arce 37, E 28002 Madrid, Spain
    Endocrinology 150:5010-5. 2009
    ..In this study we assessed whether raloxifene and tamoxifen, two selective estrogen receptor modulators, have effects similar to estradiol in astrocytes...
  13. ncbi Differential effects of estradiol and raloxifene on collagen biosynthesis in cultured human skin fibroblasts
    Arkadiusz Surazynski
    Department of Medicinal Chemistry, Medical Academy of Bialystok, 15 230 Bialystok, Poland
    Int J Mol Med 12:803-9. 2003
    The dose-dependent effect of a 24 h treatment with estradiol (E(2)) (1, 2, 5, 10 nM) and raloxifene (Rx) (1, 5, 10, 20 microM) on ER alpha and ER beta mRNA expression, collagen bio-synthesis, prolidase activity, MMP-2, MMP-9, insulin-like ..
  14. ncbi Selective estrogen receptor modulators as brain therapeutic agents
    Maria Angeles Arevalo
    Instituto Cajal, CSIC, Avenida Doctor Arce 37, E 28002 Madrid, Spain
    J Mol Endocrinol 46:R1-9. 2011
    ..New SERMs with specific actions on neurons and glial cells may represent promising therapeutic tools for the brain...
  15. ncbi Neuroprotective properties of 17beta-estradiol, progesterone, and raloxifene in MPTP C57Bl/6 mice
    S Callier
    Oncology and Molecular Endocrinology Research Center, and Faculty of Pharmacy, Laval University, , QC, G1K 7P4, Canada
    Synapse 41:131-8. 2001
    ..MPTP) induced dopamine depletion in striatum of C57Bl/6 mice by 17beta-estradiol, progesterone, and raloxifene, whereas 17alpha-estradiol had no effect...
  16. ncbi Prevalence of depressive symptoms in postmenopausal women with low bone mineral density and/or prevalent vertebral fracture: results from the Multiple Outcomes of Raloxifene Evaluation (MORE) study
    Stuart L Silverman
    Cedars Sinai Medical Center, UCLA, Greater Los Angeles Veterans Administration Health System, Los Angeles, California, USA
    J Rheumatol 34:140-4. 2007
    ..To examine the prevalence of depressive symptoms in a cross-sectional study of postmenopausal women with osteoporosis with and without prevalent vertebral fracture...
  17. pmc Effects of genistein aglycone in osteoporotic, ovariectomized rats: a comparison with alendronate, raloxifene and oestradiol
    A Bitto
    Section of Pharmacology, Department of Clinical and Experimental Medicine and Pharmacology, University of Messina, Messina, Italy
    Br J Pharmacol 155:896-905. 2008
    ..To clarify this, we investigated the effects of genistein compared with alendronate, raloxifene and oestradiol in an animal model of established osteoporosis.
  18. ncbi Effects of teriparatide in postmenopausal women with osteoporosis on prior alendronate or raloxifene: differences between stopping and continuing the antiresorptive agent
    Felicia Cosman
    Helen Hayes Hospital, West Haverstraw, New York 10993, USA
    J Clin Endocrinol Metab 94:3772-80. 2009
    The aim of the study was to assess adding vs. switching to teriparatide 20 microg/d in patients on alendronate or raloxifene.
  19. ncbi Lipid, glucose and homocysteine metabolism in women treated with a GnRH agonist with or without raloxifene
    Stefano Palomba
    Department of Obstetrics and Gynaecology, University of Catanzaro Magna Graecia, Catanzaro, Italy
    Hum Reprod 19:415-21. 2004
    ..Therefore, we have evaluated the effect of a GnRH analogue, administered with or without raloxifene, on serum levels of lipoproteins, glucose, insulin and homocysteine (Hcy).
  20. ncbi Raloxifene improves vascular reactivity in pressurized septal coronary arteries of ovariectomized hamsters fed cholesterol diet
    Yau Chi Chan
    Institute of Vascular Medicine, Li Ka Shing Institute of Health Sciences, and School of Biomedical Sciences, Chinese University of Hong Kong, Hong Kong, China
    Pharmacol Res 65:182-8. 2012
    ..The impact of raloxifene therapy and cholesterol diet on myogenic constriction during estrogen deficiency is unresolved...
  21. ncbi LY353381.HCl: a novel raloxifene analog with improved SERM potency and efficacy in vivo
    M Sato
    Department of Endocrine Research, Lilly Corporate Center, Indianapolis, Indiana, USA
    J Pharmacol Exp Ther 287:1-7. 1998
    ..and lowered them to below sham levels in a dose dependent manner, with maximum efficacy similar to estrogen or raloxifene. However, LY353381.HCl was consistently more potent than raloxifene, with a half maximal efficacious dose of 0...
  22. pmc Raloxifene inhibits growth of RT4 urothelial carcinoma cells via estrogen receptor-dependent induction of apoptosis and inhibition of proliferation
    Kristi L Hoffman
    Program in Translational Biology and Molecular Medicine, Baylor College of Medicine, Houston, TX, USA
    Horm Cancer 4:24-35. 2013
    ..lines representing a variety of disease stage and grades were treated with the antiestrogens 4-hydroxytamoxifen, raloxifene, or the pure antagonist ICI 182,780...
  23. ncbi Update on raloxifene: mechanism of action, clinical efficacy, adverse effects, and contraindications
    Salvatore Gizzo
    Department of Woman and Child Health, University of Padua, Padua, Italy
    Obstet Gynecol Surv 68:467-81. 2013
    b>Raloxifene is the only selective estrogen receptor modulator approved for long-term treatment in the prevention of osteoporotic fractures and for the reduction of invasive breast cancer risk in post-menopausal women...
  24. ncbi The use of raloxifene in osteoporosis treatment
    Patrizia D'Amelio
    University of Torino, Gerontology and Bone Metabolic Disease Section, Department of Medical Sciences, Corso Bramante 88 90, 10126 Torino, Italy
    Expert Opin Pharmacother 14:949-56. 2013
    ..Osteoporosis is a common disease characterized by the occurrence of fragility fractures. Major osteoporotic fractures are associated with decreased quality of life and high costs...
  25. ncbi Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation
    Qing Chen
    Department of Drug Metabolism, Merck Research Laboratories, Rahway, New Jersey 07065, USA
    Chem Res Toxicol 15:907-14. 2002
    b>Raloxifene is a selective estrogen receptor modulator which is effective in the treatment of osteoporosis in postmenopausal women...
  26. ncbi Raloxifene reduces triple-negative breast cancer tumor growth and decreases EGFR expression
    Sebastien Taurin
    Department of Pharmacology and Toxicology, University of Otago, Adams Building, Dunedin 9016, New Zealand
    Int J Oncol 43:785-92. 2013
    ..Previous studies have suggested an effect of raloxifene, a selective estrogen receptor modulator that is independent of the estrogen receptor (ER)...
  27. ncbi A meta-analysis of the efficacy of raloxifene on all clinical and vertebral fractures and its dependency on FRAX
    John A Kanis
    WHO Collaborating Centre for Metabolic Bone Diseases, University of Sheffield, Beech Hill Road, Sheffield, UK
    Bone 47:729-35. 2010
    Multiple Outcomes of Raloxifene Evaluation (MORE), a placebo controlled phase III study of raloxifene in postmenopausal osteoporosis, showed that both doses tested (60 mg and 120 mg daily) reduced the risk of vertebral fracture...
  28. ncbi Adiponectin and leptin serum levels in osteoporotic postmenopausal women treated with raloxifene or alendronate
    Arantzazu Sebastián-Ochoa
    Endocrinology Division, Hospital Universitario San Cecilio, Granada, Spain
    Menopause 19:172-7. 2012
    ..determine adiponectin and leptin levels in osteoporotic postmenopausal women and their relationship with bone mass and bone turnover and to analyze changes on adiponectin and leptin levels after treatment with raloxifene or alendronate.
  29. ncbi Effect of raloxifene (a Selective Estrogen Receptor Modulator (SERM)) as coadjuvant to antidepressant treatment: a case report
    Judith Usall
    Sant Joan de Deu SSM, Fundació Sant Joan de Déu, Sant Boi, Barcelona
    Actas Esp Psiquiatr 39:334-6. 2011
    We report a case of a woman with a depressive disorder with partial response to antidepressant treatment. Raloxifene, a Selective Estrogen Receptor Modulator (SERM) was added to the treatment, the patient achieving complete remission of ..
  30. ncbi Oxidation of raloxifene to quinoids: potential toxic pathways via a diquinone methide and o-quinones
    Linning Yu
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, M C 781, Chicago, Illinois 60612 7231, USA
    Chem Res Toxicol 17:879-88. 2004
    b>Raloxifene was approved in 1997 by the FDA for the treatment of osteoporosis in postmenopausal women, and it is currently in clinical trials for the chemoprevention of breast cancer...
  31. ncbi Post hoc analysis of data from the Multiple Outcomes of Raloxifene Evaluation (MORE) trial on the effects of three years of raloxifene treatment on glycemic control and cardiovascular disease risk factors in women with and without type 2 diabetes
    Elizabeth Barrett-Connor
    Department of Family and Preventive Medicine, School of Medicine, University of California at San Diego, La Jolla, California 92093 0607, USA
    Clin Ther 25:919-30. 2003
    The long-term effects of the selective estrogen-receptor modulator raloxifene hydrochloride on glycemic control and markers of cardiovascular disease risk in postmenopausal women with type 2 diabetes mellitus are unknown.
  32. ncbi Efficacy of tissue-selective estrogen complex of bazedoxifene/conjugated estrogens for osteoporosis prevention in at-risk postmenopausal women
    Robert Lindsay
    Department of Medicine, Helen Hayes Hospital, West Haverstraw, New York, New York, and Columbia University, New York, New York, USA
    Fertil Steril 92:1045-52. 2009
    ..To evaluate the efficacy of the tissue-selective estrogen complex, bazedoxifene/conjugated estrogens (BZA/CE), for postmenopausal osteoporosis prevention...
  33. ncbi Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators
    B Ettinger
    Division of Research, Kaiser Permanente, Oakland, Calif 94611 5400, USA
    JAMA 282:637-45. 1999
    b>Raloxifene hydrochloride, a selective estrogen receptor modulator, prevents bone loss in postmenopausal women, but whether it reduces fracture risk in these women is not known.
  34. ncbi Effect of selective estrogen receptor modulator/raloxifene analogue on proliferation and collagen metabolism of tendon fibroblast
    Toru Irie
    Department of Orthopaedic Surgery, Hokkaido University Graduate School of Medicine, Sapporo, Japan
    Connect Tissue Res 51:179-87. 2010
    The selective estrogen receptor modulator raloxifene is therapeutically beneficial for postmenopausal connective tissue degradation, such as osteoporosis, vascular sclerosis, and dermal degradation; however, the effects of raloxifene on ..
  35. ncbi Optimising endocrine approaches for the chemoprevention of breast cancer beyond the Study of Tamoxifen and Raloxifene (STAR) trial
    V Craig Jordan
    Fox Chase Cancer Centre, 333 Cottman Avenue, Philadelphia, PA 19111, USA
    Eur J Cancer 42:2909-13. 2006
    The completion of the Study of Tamoxifen and Raloxifene (STAR) [Vogel VG, Costantino JP, Wickerham DL, et al. The Study of Tamoxifen and Raloxifene (STAR): Report of the National Surgical Adjuvant Breast and Bowel Project P-2 Trial...
  36. ncbi Bone turnover matters: the raloxifene treatment paradox of dramatic decreases in vertebral fractures without commensurate increases in bone density
    B Lawrence Riggs
    J Bone Miner Res 17:11-4. 2002
  37. ncbi Raloxifene does not affect insulin sensitivity or glycemic control in postmenopausal women with type 2 diabetes mellitus: a randomized clinical trial
    Bjorn Andersson
    University of Goteborg, S 413 45 Goteborg, Sweden
    J Clin Endocrinol Metab 87:122-8. 2002
    Little is known about the metabolic or cardiovascular effects of selective ER modulators (SERMs), such as raloxifene hydrochloride (RLX), in postmenopausal women with type 2 diabetes mellitus (DM). Therefore, the effect of RLX vs...
  38. pmc Raloxifene acutely suppresses ventricular myocyte contractility through inhibition of the L-type calcium current
    Reginald Liew
    Cardiac Medicine, National Heart and Lung Institute, Imperial College London, Dovehouse Street, London, SW3 6LY
    Br J Pharmacol 142:89-96. 2004
    1. The selective oestrogen (ER) receptor modulator, raloxifene, is widely used in the treatment of postmenopausal osteoporosis, but may also possess cardioprotective properties...
  39. ncbi Prevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifene
    Michael R McClung
    Oregon Osteoporosis Center, Portland, OR 97213, USA
    Menopause 13:377-86. 2006
    ..The objective of this study was to compare the effects of lasofoxifene with raloxifene and placebo on indices of bone health in postmenopausal women.
  40. ncbi Anti-inflammatory effect of selective estrogen receptor modulators (SERMs) in microglial cells
    T Suuronen
    Department of Neuroscience and Neurology, University of Kuopio, PO Box 1627, 70211 Kuopio, Finland
    Inflamm Res 54:194-203. 2005
    ..Our aim was to study how different SERMs modulate the inflammatory responses induced by lipopolysaccharide (LPS) or unmethylated CpG-oligonucleotides in mouse and rat microglial cells...
  41. ncbi Alendronate produces greater effects than raloxifene on bone density and bone turnover in postmenopausal women with low bone density: results of EFFECT (Efficacy of FOSAMAX versus EVISTA Comparison Trial) International
    P N Sambrook
    Institue of Bone and Joint Research, Royal North Shore Hospital, University of Sydney, St Leonards NSW, Australia
    J Intern Med 255:503-11. 2004
    Alendronate and raloxifene are antiresorptive agents with different mechanisms of action, each used to treat osteoporosis in postmenopausal women...
  42. ncbi Raloxifene, a mixed estrogen agonist/antagonist, induces apoptosis in androgen-independent human prostate cancer cell lines
    Isaac Yi Kim
    Laboratory of Cell Regulation and Carcinogenesis, National Cancer Institute NIH, Building 41, Room C629, 9000 Rockville Pike, Bethesda, MD 20892, USA
    Cancer Res 62:5365-9. 2002
    b>Raloxifene, a selective estrogen receptor (ER) modulator, is a mixed estrogen agonist/antagonist that has been shown to prevent osteoporosis and breast cancer in women...
  43. ncbi Effects of raloxifene and estradiol on hippocampal acetylcholine release and spatial learning in the rat
    Robert B Gibbs
    Department of Pharmaceutical Sciences, University of Pittsburgh School of Pharmacy, 1004 Salk Hall, Pittsburgh, PA 15261, USA
    Psychoneuroendocrinology 29:741-8. 2004
    The effects of raloxifene on acquisition of a delayed matching to position (DMP) T-maze task and on hippocampal acetylcholine release were evaluated and compared with estradiol, to determine whether raloxifene has estrogenic effects on ..
  44. ncbi Estrogen and selective estrogen receptor modulators exert neuroprotective effects and stimulate the expression of selective Alzheimer's disease indicator-1, a recently discovered antiapoptotic gene, in human neuroblast long-term cell cultures
    Susanna Benvenuti
    Endocrine Unit, Department of Clinical Physiopathology, University of Florence, Viale Pieraccini, 6, 50139 Florence, Italy
    J Clin Endocrinol Metab 90:1775-82. 2005
    ..We found that 17beta-estradiol (17betaE(2)) and the selective estrogen receptor modulators (SERMs) raloxifene and tamoxifen exerted neuroprotective effects, which were independent of cell proliferation, by increasing ..
  45. pmc Treatment of osteoporosis and reduction in risk of invasive breast cancer in postmenopausal women with raloxifene
    Seung Sang Ko
    Georgetown University Medical Center, Lombardi Comprehensive Cancer Center, Department of Oncology, 3970 Reservoir Rd N W, Washington, DC 20057, USA
    Expert Opin Pharmacother 12:657-74. 2011
    b>Raloxifene, a non-steroidal selective estrogen receptor modulator (SERM), offers a new dimension for the treatment and prevention of osteoporosis and risk reduction of invasive breast cancer in postmenopausal populations at high risk...
  46. pmc Return of chronic pelvic pain from endometriosis after raloxifene treatment: a randomized controlled trial
    Pamela Stratton
    Reproductive Biology and Medicine Branch, National Institutes of Health, Bethesda, Maryland, USA
    Obstet Gynecol 111:88-96. 2008
    To evaluate whether 6 months of raloxifene was effective in treatment of chronic pelvic pain in women with endometriosis.
  47. pmc In vivo reference point indentation reveals positive effects of raloxifene on mechanical properties following 6 months of treatment in skeletally mature beagle dogs
    Mohammad Aref
    Department of Anatomy and Cell Biology, Indiana University School of Medicine, Indianapolis, IN 46202, USA
    Bone 56:449-53. 2013
    b>Raloxifene treatment has been shown previously to positively affect bone mechanical properties following 1 year of treatment in skeletally mature dogs...
  48. pmc Combined treatment with dexamethasone and raloxifene totally abrogates osteoporosis and joint destruction in experimental postmenopausal arthritis
    Ulrika Islander
    Centre for Bone and Arthritis Research, The Sahlgrenska Academy, University of Gothenburg, Box 480, 405 30 Gothenburg, Sweden
    Arthritis Res Ther 13:R96. 2011
    ..Therefore, our aim was to investigate if addition of the selective estrogen receptor modulator raloxifene, or estradiol, could prevent loss of bone mineral density in ovariectomized and dexamethasone treated mice with ..
  49. ncbi Differential time-dependent inactivation of P450 3A4 and P450 3A5 by raloxifene: a key role for C239 in quenching reactive intermediates
    Josh T Pearson
    Department of Pharmacokinetics and Drug Metabolism, Amgen, Inc Seattle, WA 98119 3105, USA
    Chem Res Toxicol 20:1778-86. 2007
    The role of C239 as the active-site residue responsible for forming the covalent linkage with raloxifene during P450 3A4 time-dependent inactivation (TDI) was recently identified...
  50. pmc Update of the National Surgical Adjuvant Breast and Bowel Project Study of Tamoxifen and Raloxifene (STAR) P-2 Trial: Preventing breast cancer
    Victor G Vogel
    NSABP, Pittsburgh, PA 15212, USA
    Cancer Prev Res (Phila) 3:696-706. 2010
    ..The FDA approved the SERM raloxifene for breast cancer risk reduction following its demonstrated effectiveness in preventing invasive breast cancer ..
  51. pmc Evaluation of CYP2D6 and efficacy of tamoxifen and raloxifene in women treated for breast cancer chemoprevention: results from the NSABP P1 and P2 clinical trials
    Matthew P Goetz
    Department of Oncology, Mayo Clinic, Rochester, Minnesota 55905, USA
    Clin Cancer Res 17:6944-51. 2011
    ..Controversy exists regarding the association between CYP2D6 enzyme activity and tamoxifen effectiveness in the adjuvant treatment of invasive breast cancer; however, this association in the primary prevention of breast cancer is unknown...
  52. ncbi Therapeutically relevant concentrations of raloxifene dilate pressurized rat resistance arteries via calcium-dependent endothelial nitric oxide synthase activation
    Yau Chi Chan
    Institute of Vascular Medicine, Hong Kong, China
    Arterioscler Thromb Vasc Biol 30:992-9. 2010
    ..The present study aimed to examine roles of Ca(2+) influx in endothelium and endothelial nitric oxide synthase (eNOS) activation in dilatations induced by raloxifene, a second-generation SERM in myogenically active arteries.
  53. ncbi Raloxifene attenuates Pseudomonas aeruginosa pyocyanin production and virulence
    Shannan J Ho Sui
    Department of Molecular Biology and Biochemistry, Simon Fraser University, 8888 University Drive, Burnaby, BC V5A 1S6, Canada
    Int J Antimicrob Agents 40:246-51. 2012
    ..The selective oestrogen receptor modulator raloxifene, a drug currently used in the prevention of osteoporosis and/or invasive breast cancer in post-menopausal women, ..
  54. ncbi Raloxifene induces cell death and inhibits proliferation through multiple signaling pathways in prostate cancer cells expressing different levels of estrogen receptor α and β
    V Rossi
    Dipartimento di Internistica Clinica e Sperimentale, Sezione di Endocrinologia ed Andrologia Medica, Universita Federico II, Napoli, Italy
    J Cell Physiol 226:1334-9. 2011
    b>Raloxifene (RAL), a selective estrogen receptor (ER) modulator (SERM) seems to induce apoptosis in both androgen-dependent and -independent prostate cell (PC) lines via activation of ERβ and an antagonistic effect on ERα...
  55. ncbi Disposition mechanisms of raloxifene in the human intestinal Caco-2 model
    Eun Ju Jeong
    Department of Pharmaceutical Sciences, College of Pharmacy, Washington State University, Pullman, Washington 99164 6510, USA
    J Pharmacol Exp Ther 310:376-85. 2004
    The purpose of this study was to determine the mechanisms responsible for transport of raloxifene and its hydrophilic conjugates. Human intestinal Caco-2 cell culture model and Caco-2 cell lysate were used for the studies...
  56. ncbi Pharmacokinetics of raloxifene in male Wistar-Hannover rats: influence of complexation with hydroxybutenyl-beta-cyclodextrin
    Michael F Wempe
    Eastman Chemical Company, Kingsport, TN, USA
    Int J Pharm 346:25-37. 2008
    b>Raloxifene is a highly insoluble, highly metabolized serum estrogen receptor modulator approved for use in the treatment of osteoporosis...
  57. ncbi Gynecologic conditions in participants in the NSABP breast cancer prevention study of tamoxifen and raloxifene (STAR)
    Carolyn D Runowicz
    National Surgical Adjuvant Breast and Bowel Project, National Cancer Institute, Pittsburgh, PA, USA
    Am J Obstet Gynecol 205:535.e1-5. 2011
    This study reports the gynecologic conditions in postmenopausal women (intact uterus on enrollment) in the National Surgical Adjuvant Breast and Bowel Project (NSABP) study of tamoxifen and raloxifene (STAR)/P-2 trial.
  58. ncbi Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance
    Daniel C Kemp
    University of North Carolina, Curriculum of Toxicology, Chapel Hill, North Carolina, USA
    Drug Metab Dispos 30:694-700. 2002
    b>Raloxifene, a selective estrogen receptor modulator used for the treatment of osteoporosis, undergoes extensive conjugation to the 6-beta- and 4'-beta-glucuronides in vivo...
  59. ncbi Cognitive function in postmenopausal women treated with raloxifene
    K Yaffe
    Department of Psychiatry, University of California at San Francisco, 94121, USA
    N Engl J Med 344:1207-13. 2001
    ..Whether raloxifene, a selective estrogen-receptor modulator, might have similar actions is not known...
  60. ncbi Raloxifene ameliorates detrimental enzymatic and nonenzymatic collagen cross-links and bone strength in rabbits with hyperhomocysteinemia
    M Saito
    Department of Orthopaedic Surgery, Jikei University School of Medicine, Tokyo, Japan
    Osteoporos Int 21:655-66. 2010
    ..Such detrimental cross-link formation in bone was ameliorated by raloxifene (RLX) treatment.
  61. ncbi Effects of raloxifene and estradiol on bone turnover parameters in intact and ovariectomized rats
    S Canpolat
    Faculty of Medicine, Department of Physiology, Yeditepe University, Istanbul, Turkey
    J Physiol Biochem 66:23-8. 2010
    This study was designed to investigate effects of raloxifene (RLX) and estradiol on bone formation and resorption in intact and ovariectomized (ovx) rat models...
  62. ncbi Patient compliance with alendronate, risedronate and raloxifene for the treatment of osteoporosis in postmenopausal women
    J D Ringe
    Medical Department IV, Hospital Leverkusen, University of Cologne, Leverkusen, Germany
    Curr Med Res Opin 23:2677-87. 2007
    ..The aim was to investigate patient compliance with different osteoporosis medications commonly prescribed in clinical practice, to determine risk factors associated with discontinuation and to evaluate quality of life changes...
  63. ncbi Administration of raloxifene reduces sensorimotor and working memory deficits following traumatic brain injury
    Olga N Kokiko
    Restorative Neuroscience Laboratory, Department of Psychology, Southern Illinois University, Carbondale, IL 62901, USA
    Behav Brain Res 170:233-40. 2006
    ..The present study examined the effects of raloxifene, a SERM, on functional recovery after bilateral cortical contusion injury (bCCI) or sham procedure...
  64. ncbi Sulfation of raloxifene and 4-hydroxytamoxifen by human cytosolic sulfotransferases
    Josie L Falany
    Department of Pharmacology and Toxicology, 1670 University Blvd, Volker Hall G133M, University of Alabama at Birmingham, Birmingham, AL 35294, USA
    Drug Metab Dispos 34:361-8. 2006
    b>Raloxifene and 4-hydroxytamoxifen (4-OHT) are important estrogen-related drugs used in the treatment of osteoporosis and breast cancer...
  65. ncbi Difference between genomic actions of estrogen versus raloxifene in human ovarian cancer cell lines
    H Sasaki
    Department of Obstetrics and Gynecology, Osaka University Medical School, Yamadaoka, Suita, Osaka, Japan
    Oncogene 27:2737-45. 2008
    ..The molecular mechanisms of the effects of SERMs such as raloxifene on the tumor progression of epithelial ovarian cancer are also still unclear...
  66. ncbi Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women
    Janne Komi
    Hormos Medical Corporation, Turku, Finland
    Menopause 12:202-9. 2005
    To compare ospemifene and raloxifene regarding their effects on hormones, lipids, genital tract, and tolerability in postmenopausal women.
  67. ncbi Transition from estrogen-progestin to raloxifene in postmenopausal women: effect on vasomotor symptoms
    Stephen Gordon
    Women s Health and Internal Medicine, Comprehensive NeuroScience, Inc, 6065 Roswell, Suite 820, Atlanta, GA 30328, USA
    Obstet Gynecol 103:267-73. 2004
    To compare vasomotor symptoms after transition from estrogen-progestin therapy to raloxifene 60 mg/d with and without a placebo washout.
  68. ncbi Transition from estrogen therapy to raloxifene in postmenopausal women: effects on treatment satisfaction and the endometrium-a pilot study
    Susan R Davis
    Jean Hailes Foundation, Melbourne, Australia
    Menopause 11:167-75. 2004
    To compare the effects of transferring from low-dose, transdermal estrogen to raloxifene with a phase of alternate-day raloxifene therapy with or without low-dose transdermal estrogen on patient satisfaction, endometrial changes, and ..
  69. pmc Treatment with selective estrogen receptor modulators regulates myelin specific T-cells and suppresses experimental autoimmune encephalomyelitis
    Bruce F Bebo
    Neurological Sciences Institute, Oregon Health and Science University, Beaverton, Oregon, USA
    Glia 57:777-90. 2009
    ..In this study, we investigated the ability of two commercially available SERMs (tamoxifen and raloxifene) to regulate myelin specific immunity and experimental autoimmune encephalomyelitis (EAE) in mice...
  70. ncbi Raloxifene analog LY117018 enhances the regeneration of sciatic nerve in ovariectomized female mice
    R McMurray
    Department of Physiology, The Brody School of Medicine at East Carolina University, 600 Moye Blvd, Greenville, NC 27858, USA
    Brain Res 980:140-5. 2003
    ..Our study suggests that LY117018 may markedly accelerate peripheral nerve regeneration and functional recovery through activation of estrogen receptors...
  71. ncbi Effect of raloxifene after recombinant teriparatide [hPTH(1-34)] treatment in postmenopausal women with osteoporosis
    S Adami
    Riabilitazione Reumatologica, University of Verona, Valeggio s Mincio, Verona, Italy
    Osteoporos Int 19:87-94. 2008
    ..Sequential raloxifene prevented rapid bone loss at lumbar spine and further increased bone mineral density (BMD) at femoral neck, ..
  72. ncbi Effect of prior and ongoing raloxifene therapy on response to PTH and maintenance of BMD after PTH therapy
    F Cosman
    Clinical Research Center, Helen Hayes Hospital, West Haverstraw, NY 10993, USA
    Osteoporos Int 19:529-35. 2008
    Women with osteoporosis on raloxifene were randomized to 1-34hPTH + raloxifene or raloxifene alone for one year. In the PTH + raloxifene group, bone turnover increased 125-584%, spine BMD increased 9.6%, hip BMD increased 1.2-3...
  73. ncbi Incidence of invasive breast cancer in postmenopausal women after discontinuation of long-term raloxifene administration
    Victor G Vogel
    Department of Research, American Cancer Society, Atlanta, GA, USA
    Clin Breast Cancer 9:45-50. 2009
    ..women with osteoporosis had a 66% relative risk reduction for invasive breast cancer over 8 years of raloxifene therapy in the randomized, placebo-controlled 4-year MORE (Multiple Outcomes of Raloxifene Evaluation) trial and ..
  74. ncbi Raloxifene is not associated with biologically relevant changes in hot flushes in postmenopausal women for whom therapy is appropriate
    Santiago Palacios
    Instituto Palacios, Madrid, Spain
    Am J Obstet Gynecol 191:121-31. 2004
    b>Raloxifene is approved for the treatment and prevention of postmenopausal osteoporosis. Previous studies have described a raloxifene-associated increase in hot flushes, reported as adverse events...
  75. ncbi From adjuvant therapy to breast cancer prevention: BCPT and STAR
    B K Dunn
    Division of Cancer Prevention, National Cancer Institute, Bethesda, Maryland, USA
    Breast J 7:144-57. 2001
    ..b>Raloxifene, a second-generation SERM approved for the prevention of osteoporosis in postmenopausal women, displays ..
  76. ncbi Novel biodegradable polyesters. Synthesis and application as drug carriers for the preparation of raloxifene HCl loaded nanoparticles
    Dimitrios Bikiaris
    Laboratory of Organic Chemical Technology, Chemistry Department, Aristotle University of Thessaloniki, 541 24 Thessaloniki, Greece
    Molecules 14:2410-30. 2009
    b>Raloxifene HCl is a drug with poor bioavailability and poor water solubility. Furthermore nomicron pharmaceutically acceptable organic solvent has been reported before to dilute the drug...
  77. ncbi Effects of estrogen and raloxifene on neuroglia number and morphology in the hippocampus of aged female mice
    D L Lei
    Laboratory of Experimental Gerontology, Gerontology Research Center, National Institute on Aging, NIH, Baltimore, MD 21224, USA
    Neuroscience 121:659-66. 2003
    Hormone replacement therapy with the gonadal steroid estrogen or synthetic agents such as raloxifene, a selective estrogen receptor modulator, may affect cellular function in brains of postmenopausal women...
  78. ncbi Tamoxifen inhibits inward rectifier K+ 2.x family of inward rectifier channels by interfering with phosphatidylinositol 4,5-bisphosphate-channel interactions
    Daniela Ponce-Balbuena
    Unidad de Investigación Carlos Méndez del Centro Universitario de Investigaciones Biomédicas de la Universidad de Colima, Colima, Colima, Mexico
    J Pharmacol Exp Ther 331:563-73. 2009
    ..3 potassium channels that underlie cardiac I(K1). We also studied the effects of 4-hydroxytamoxifen and raloxifene. All three drugs inhibited inward rectifier K(+) 2.x (Kir2.x) family members...
  79. ncbi The selective estrogen receptor modulator raloxifene regulates osteoclast and osteoblast activity in vitro
    A Taranta
    Istituto Dermopatico dell Immacolata, Rome, Italy
    Bone 30:368-76. 2002
    b>Raloxifene is a selective estrogen receptor modulator (SERM) that prevents bone loss...
  80. ncbi The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. Multiple Outcomes of Raloxifene Evaluation
    S R Cummings
    Department of Medicine, University of California, San Francisco, USA
    JAMA 281:2189-97. 1999
    b>Raloxifene hydrochloride is a selective estrogen receptor modulator that has antiestrogenic effects on breast and endometrial tissue and estrogenic effects on bone, lipid metabolism, and blood clotting.
  81. ncbi Estrogen and raloxifene modulate leptin and its receptor in hypothalamus and adipose tissue from ovariectomized rats
    Rosaria Meli
    Department of Experimental Pharmacology, University of Naples, Italy
    Endocrinology 145:3115-21. 2004
    ..OVX) rats modification of estrogen levels or treatment with a selective estrogen receptor modulator, raloxifene (RAL), alters leptinemia and modulates leptin receptor (Ob-R) abundance in hypothalamus and white adipose tissue,..
  82. ncbi Structural modulation of reactivity/activity in design of improved benzothiophene selective estrogen receptor modulators: induction of chemopreventive mechanisms
    Bolan Yu
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL 60612, USA
    Mol Cancer Ther 6:2418-28. 2007
    The benzothiophene selective estrogen receptor modulators (SERM) raloxifene and arzoxifene are in clinical use and clinical trials for chemoprevention of breast cancer and other indications...
  83. pmc The effect of tamoxifen and raloxifene on estrogen metabolism and endometrial cancer risk
    Marian Y Williams-Brown
    Department of Obstetrics and Gynecology, University of Texas Medical Branch, Galveston, United States
    J Steroid Biochem Mol Biol 126:78-86. 2011
    ..While tamoxifen (TAM) use increases the risk of endometrial hyperplasia and malignancy, raloxifene (RAL) has neutral effects on the uterus...
  84. ncbi Effects of calcitonin, risedronate, and raloxifene on erythrocyte antioxidant enzyme activity, lipid peroxidation, and nitric oxide in postmenopausal osteoporosis
    Salih Ozgocmen
    Division of Rheumatology, Department of Physical Medicine and Rehabilitation, Faculty of Medicine, Firat University, Elazig, Turkey
    Arch Med Res 38:196-205. 2007
    ..Additionally, in vivo effects of three different anti-osteoporotic drugs, calcitonin, risedronate and raloxifene, on the erythrocyte oxidant-antioxidant status in women with PMO were also assessed.
  85. ncbi Additive effects of raloxifene and alendronate on bone density and biochemical markers of bone remodeling in postmenopausal women with osteoporosis
    Olof Johnell
    Department of Orthopaedics, Universiteitssjukhuset MAS, Malmø, Sweden
    J Clin Endocrinol Metab 87:985-92. 2002
    Both raloxifene (RLX) and alendronate (ALN) can treat and prevent new vertebral fractures, increase bone mineral density (BMD), and decrease biochemical markers of bone turnover in postmenopausal women with osteoporosis...
  86. ncbi Rationale for using raloxifene to prevent both osteoporosis and breast cancer in postmenopausal women
    Wen Ling Lee
    Division of Endocrinology and Metabolism, Department of Medicine, Chen Hsin Rehabilitation Center Taipei, Taiwan
    Maturitas 60:92-107. 2008
    ..Among these SERMs, raloxifene may be the most attractive agent based on the evidence from five recent large trials (Multiple Outcomes of ..
  87. ncbi Estradiol and raloxifene protect cultured SN4741 neurons against oxidative stress
    Eric Biewenga
    Biology Department, University of Colorado at Denver, P O Box 173364, Denver, CO 80217 3364, USA
    Neurosci Lett 373:179-83. 2005
    ..We used the clonal substantia nigra cell line SN4741 to compare the neuroprotective properties of estrogen and raloxifene against oxidative stress, and to determine whether raloxifene acted as an estrogen agonist or antagonist in this ..
  88. pmc Effect of raloxifene on stroke and venous thromboembolism according to subgroups in postmenopausal women at increased risk of coronary heart disease
    Lori Mosca
    Director, Preventive Cardiology, New York Presbyterian Hospital, 601 West 168th Street, 43, New York, NY 10032, USA
    Stroke 40:147-55. 2009
    b>Raloxifene, a selective estrogen receptor modulator, reduces risk of invasive breast cancer and osteoporosis, but the effect on risk for stroke and venous thromboembolism in different patient subgroups is not established...
  89. ncbi Raloxifene enhances vertebral mechanical properties independent of bone density
    Matthew R Allen
    Department of Anatomy and Cell Biology, MS 5035, Indiana University School of Medicine, 635 Barnhill Drive, Indianapolis, IN 46202, USA
    Bone 39:1130-5. 2006
    ..10 mg/kg/day), alendronate (ALN, 0.2 mg/kg/day), raloxifene (RAL, 0.50 mg/kg/day), or saline (VEH, 1 ml/kg/day)...
  90. ncbi Beneficial effects of raloxifene and tamoxifen in the treatment of pubertal gynecomastia
    Sarah E Lawrence
    Department of Pediatrics, University of Ottawa, Ontario, Canada
    J Pediatr 145:71-6. 2004
    ..To assess the efficacy of the anti-estrogens tamoxifen and raloxifen in the medical management of persistent pubertal gynecomastia...
  91. ncbi Biomedicine. Defining the "S" in SERMs
    Benita S Katzenellenbogen
    Department of Molecular and Integrative Physiology, University of Illinois and College of Medicine at Urbana Champaign, Urbana, IL 61801, USA
    Science 295:2380-1. 2002
  92. pmc The NSABP Study of Tamoxifen and Raloxifene (STAR) trial
    Victor G Vogel
    University of Pittsburgh Cancer Institute, Magee Womens Hospital, Pittsburgh, PA 15213 3180, USA
    Expert Rev Anticancer Ther 9:51-60. 2009
    In the Study of Tamoxifen and Raloxifene (STAR) trial, postmenopausal women at increased risk of breast cancer received either oral tamoxifen (20 mg/day) or raloxifene (60 mg/day) over 5 years...
  93. ncbi Structure-activity relationships for a family of benzothiophene selective estrogen receptor modulators including raloxifene and arzoxifene
    Cassia R Overk
    Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, 833 S Wood St, Chicago, IL 60612, USA
    ChemMedChem 2:1520-6. 2007
    ..Based on the clinical and preclinical benzothiophene SERMs, raloxifene and arzoxifene, a family of SERMs has been developed to modulate activity and oxidative lability...
  94. ncbi Raloxifene as an adjunctive treatment for postmenopausal women with schizophrenia: a double-blind, randomized, placebo-controlled trial
    Judith Usall
    Parc Sanitari Sant Joan de Déu C Antoni Pujadas, 42 Sant Boi de Llobregat 08830, Barcelona, Spain
    J Clin Psychiatry 72:1552-7. 2011
    The potential therapeutic utility of estrogens in schizophrenia is increasingly being recognized. Raloxifene, a selective estrogen receptor modulator, appears to act similarly to conjugated estrogens on dopamine and serotonin brain ..
  95. pmc Estrogen and raloxifene improve metaphyseal fracture healing in the early phase of osteoporosis. A new fracture-healing model at the tibia in rat
    E K Stuermer
    Department of Trauma Surgery, Plastic and Reconstructive Surgery, Georg August University of Goettingen, Robert Koch Str 40, 37099, Gottingen, Germany
    Langenbecks Arch Surg 395:163-72. 2010
    ..Quality and speed of fracture healing in osteoporotic fractures are crucial with regard to the outcome of patients. The question arises whether established antiosteoporotic drugs can further improve fracture healing...
  96. ncbi Randomized control study of the effects of raloxifene on serum lipids and homocysteine in older women
    V De Leo
    Department of Obstetrics and Gynecology, University of Siena, Italy
    Am J Obstet Gynecol 184:350-3. 2001
    b>Raloxifene, a selective estrogen receptor modulator, has beneficial estrogen agonist effects on bone and cardiovascular risk factors and estrogen antagonist effects on the breast and uterus...
  97. ncbi Solid state interaction of raloxifene HCl with different hydrophilic carriers during co-grinding and its effect on dissolution rate
    Anuj Garg
    Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi, India
    Drug Dev Ind Pharm 35:455-70. 2009
    ..methyl cellulose and hydroxy propyl cellulose], and Sodium Alginate) on the solid state and dissolution rate of Raloxifene hydrochloride (R-HCl)...
  98. ncbi Estrogen therapy for hereditary haemorrhagic telangiectasia (HHT): Effects of raloxifene, on Endoglin and ALK1 expression in endothelial cells
    Virginia Albiñana
    Centro de Investigaciones Biologicas, Spanish Research Council CSIC, Madrid, Spain
    Thromb Haemost 103:525-34. 2010
    ..We report preliminary results obtained with Raloxifene to treat epistaxis in postmenopausal HHT women diagnosed with osteoporosis...
  99. ncbi Transcriptional activities of estrogen receptor alpha and beta in yeast properties of raloxifene
    E Jisa
    Institute of Applied Microbiology, University of Agricultural Sciences, Vienna, Austria
    Biochem Pharmacol 62:953-61. 2001
    b>Raloxifene represents a potent compound for the prevention and treatment of osteoporosis and cardiovascular disease in postmenopausal women...
  100. ncbi Randomized, controlled study of the effects of raloxifene on high sensitivity C-reactive protein and serum lipids
    Efser Oztas
    Department of Obstetrics and Gynecology, Faculty of Medicine, Ufuk University, Ankara, Turkey
    Arch Gynecol Obstet 283:71-7. 2011
    To investigate the effects of raloxifene, on serum lipids and high-sensitivity C-reactive protein (hs-CRP) in healthy postmenopausal women.
  101. ncbi In vitro evaluation, biodistribution in rats of radiolabeled raloxifene
    Elif Bayrak
    Ege University, Institute of Nuclear Science, Department of Nuclear Applications, Bornova, 35100 Izmir, Turkey
    Appl Radiat Isot 68:33-6. 2010
    b>Raloxifene is a selective estrogen receptor modulator that produces both estrogen agonistic effects on bone and lipid metabolism and estrogen-antagonistic effects on uterine endometrium and breast tissue...

Research Grants62

  1. Theranostic Nanomedicine for Breast Cancer Prevention and Image-Guided Therapy
    Prakash R Rai; Fiscal Year: 2011
    ..The strategy is to use Chemopreventive Nanocells (CPNC) that encapsulate raloxifene, anastrazole, metformin, fenretinide and celecoxib as preventive agents with indocyanine green (ICG) as the ..
  2. Theranostic Nanomedicine for Breast Cancer Prevention and Image-Guided Therapy
    Prakash R Rai; Fiscal Year: 2013
    ..The strategy is to use Chemopreventive Nanocells (CPNC) that encapsulate raloxifene, anastrazole, metformin, fenretinide and celecoxib as preventive agents with indocyanine green (ICG) as the ..
  3. Assessing and modifying bone quality in chronic kidney disease
    Chris Newman; Fiscal Year: 2013
    ..Also, recent analyses suggest that raloxifene, a selective estrogen receptor modulator, might be a useful intervention for patients with late stage kidney ..
  4. Estrogen receptors in benign prostatic hyperplasia
    TRISTAN MARRINER NICHOLSON; Fiscal Year: 2013
    ..estrogen receptor modulators (SERMs) that target relevant ER subtypes and the clinically relevant SERMs Raloxifene and Fulvestrant...
  5. Herb-Drug Glucuronidation Interactions
    Reginald F Frye; Fiscal Year: 2011
    ..on mycophenolic acid pharmacokinetics;and 2) the effect of green tea leaf extract administration on raloxifene pharmacokinetics...
  6. The role of HDAC2 in hormone therapy resistance
    Pamela N Munster; Fiscal Year: 2013
    ..as the selective estrogen receptor down-regulator (SERD) fulvestrant, or the selective estrogen modulator (SERM) raloxifene, has had limited success beyond that achieved with tamoxifen...
  7. Development of BRCA1-mimetic drugs for breast cancer
    Eliot M Rosen; Fiscal Year: 2013
    ..a manner that is distinct from that of the selective estrogen receptor modulators (SERMs), such as Tamoxifen and Raloxifene. Thus, they may be useful by themselves, in combination with existing agents, or in cases of hormone-resistant ..
  8. HUMAN CYTOSOLIC SULFOTRANSFERASES
    Charles N Falany; Fiscal Year: 2013
    ..DHEA) can bind in both the presence and absence of PAPS, whereas bulkier substrates such as raloxifene, can bind only if PAPS in not bound...
  9. Biointeractions of antiestrogens with nitric oxide
    Gregory R J Thatcher; Fiscal Year: 2013
    ..The benzothiophene SERM (BT-SERM) raloxifene is currently the sole SERM in clinical use for postmenopausal syndrome and breast cancer chemoprevention...
  10. Regulation of SULT1A1 in Human Breast
    SUSAN A KADLUBAR; Fiscal Year: 2012
    ..catalyzes the sulfation of a host of structurally diverse endo- and xenobiotics, including tamoxifen (TAM) and raloxifene (RAL), therapeutic agents used in breast cancer prevention and adjuvant therapy...
  11. Effects of herbs on transcription and cell proliferation
    Dale Leitman; Fiscal Year: 2003
    ..recently, SERMs are becoming increasingly popular for preventing cancer, since studies found that tamoxifen and raloxifene reduce the incidence of estrogen receptor positive breast tumors...
  12. Actions of Endoxifen on the Skeleton
    Anne Gingery; Fiscal Year: 2013
    ..Present day therapies involve anti-resorptive agents such as bisphosphonates, estrogen analogs, raloxifene and calcitonin which primarily target bone resorbing osteoclasts resulting in reduced bone turnover...
  13. TRANSLATIONAL RESEARCH IN BREAST CANCER
    C Kent Osborne; Fiscal Year: 2012
    ..3) Prevention trials have shown that SERMs like tamoxifen or raloxifene can greatly reduce ER-positive but not ER-negative breast cancer in high-risk women...
  14. MECHANISM OF ACTION OF ESTROGENS AND ANTIESTROGENS
    Donald P McDonnell; Fiscal Year: 2013
    ..Indeed, drugs with these properties like the SERMs raloxifene, bazedoxifene and lazofoxifene have already been developed...
  15. Enhancing bone strength using combination drug therapy
    Matthew R Allen; Fiscal Year: 2013
    ..b>Raloxifene (RAL) minimally affects bone mass yet significantly improves material properties leading to an enhancement in ..
  16. Female Hormones and Vision
    Alvin Eisner; Fiscal Year: 2006
    ..and visual system as a result of estrogen-receptor action and to elucidate the effects of 2 SERMS, tamoxifen and raloxifene, as functions of their durations of use...
  17. A Molecular Basis for Phytoestrogen Chemoprevention
    Andrew Mesecar; Fiscal Year: 2002
    ..the only phytoestrogen-ER structure solved to date, to those of estradiol (agonist) bound to ER-alpha and Raloxifene (antagonist) bound to ER- beta, reveals that the phytoestrogen genistein induces a novel conformation in ER...
  18. MODEL FOR PELVIC FLOOR DISORDERS
    Amanda Clark; Fiscal Year: 2004
    ..Special attention will be paid to the effects of a SERM (raloxifene) as there are tow reports that experimental SERMs increase the incidence of POP...
  19. Antiestrogen Regulation of Bladder Cancer
    Carolyn Smith; Fiscal Year: 2009
    ..is expressed in multiple bladder cancer cell lines tested;3) the selective estrogen receptor modulators (SERMs), raloxifene and tamoxifen, inhibit growth of bladder cancer cell lines in vitro and 4) raloxifene and 4- hydroxytamoxifen ..
  20. REGULATION OF ESTROGEN-RESPONSIVE GENES
    ANN NARDULLI; Fiscal Year: 2007
    ..and coregutatory proteins involved in mediating the effects of estrogen and the SERMs 4-hydroxytamoxifen and raloxifene will be determined using in vivo footprinting and chromatin immunoprecipitation experiments...
  21. Hormone Replacement Therapy, SERMs & Leg Blood Flow in Postmenopausal Women
    DOUGLAS SEALS; Fiscal Year: 2007
    ..the present proposal is that HRT (transdermal estradiol) and/or a selective estrogen receptor modulator (SERM; raloxifene) will increase LBF in healthy previously estrogen deficient postmenopausal women by increasing LVC, with or ..
  22. PSYCHOBIOLOGY OF ESTROGEN RECEPTOR MODULATORS
    Mark Wilson; Fiscal Year: 2003
    ..This project will determine if the SERMs, tamoxifen and raloxifene, are E2 agonists or antagonists in the neuroendocrine regulation of behavior in female rhesus monkeys...
  23. Interactions between SERMs, soy and black cohosh
    Heather Shaw; Fiscal Year: 2007
    ..b>Raloxifene, a newer SERM, is currently widely used for treatment of osteoporosis and is in trials for breast cancer ..
  24. Interferon and Raloxifene Effects on Cancer Cells
    CHERYL ROSENFELD; Fiscal Year: 2007
    ..The University is in the process of developing a Comparative Oncology Program. The campus provides a rich mix of disciplines and a collaborative environment, in which Dr. Rosenfeld is expected to continue to thrive. ..
  25. COGNITIVE AGING: EFFECTS OF ESTRADIOL AND RALOXIFENE
    AGNES LACREUSE; Fiscal Year: 2000
    ..We will use a rhesus monkey model of human menopause to examine the effects of estradiol and the SERM raloxifene on female cognition...
  26. Selective estrogen modulators and cognition
    James Herndon; Fiscal Year: 2005
    ..This project will first determine whether the SERMs tamoxifen and raloxifene are E2 agonists or E2 antagonists in a variety of cognitive domains in Ovariectomized female rhesus monkeys...
  27. SPECIALIZED CENTER OF RESEARCH IN ISCHEMIC HEART DISEASE
    Michael Mendelsohn; Fiscal Year: 2004
    ..Infarction", a secondary prevention trial at New England Medical Center with the selective ER modulator raloxifene; Project 3: "Cardiac ER and MI: Mouse Models", studies of ventricular remodeling, arrhythmogenic changes, and ..
  28. Estrogen Receptor-beta and Prostate Function
    Shuk Mei Ho; Fiscal Year: 2004
    ..Aim 1: To identify novel (the Hanson compounds) or known (tamoxifene, ICI-182,780, and Raloxifene) estrogen-like compounds that show pronounced subtype-selective differences in ligand binding, prostatic cell ..
  29. NUCLEAR RECEPTOR COACTIVATORS AND BREAST CANCER
    Yijun Zhu; Fiscal Year: 2004
    ..B. Thimmapaya), and prevention of breast cancer using antiestrogens tamoxifen and raloxifene (Dr. C. Jordan)...
  30. SELECTIVE ESTROGEN RECEPTOR MODULATORS
    Ashraf Saeed; Fiscal Year: 1999
    ..These were, thus, classified as Selective Estrogen Receptor Modulators (SERM). One such compound, raloxifene, is already in use for the treatment of osteoporosis...
  31. Estrogen enhancement of endothelial vasodilatory factors
    Roshanak Rahimian; Fiscal Year: 2003
    ..The objective of my research is to elucidate the cellular and molecular mechanisms whereby estrogen and raloxifene, a selective estrogen receptor modulator, enhance release of endothelial vasodilatory factors (EDRF) including ..
  32. ESTROGEN AND EXERCISE--VASCULAR BENEFITS AFTER MENOPAUSE
    KIMBERLY BROWNLEY; Fiscal Year: 2004
    ..The plan is structured around a randomized placebo-controlled study of raloxifene and aerobic exercise training in hypertensive postmenopausal women. Dr...
  33. Estrogen Receptor Modulators and Dendritic Cell Function
    Susan Kovats; Fiscal Year: 2006
    ..The study of tamoxifen and raloxifene (STAR) is a current NCI breast cancer prevention trial involving treatment of women at high risk for breast ..
  34. Antiestrogenic Effects on Tumor Angiogenesis
    Kimberly Blackwell; Fiscal Year: 2006
    ..drugs include pure ER antagonists, such as ICI 182,780, and selective ER modulators (SERMs) such as raloxifene, idoxifene, clomiphene and GW 7604...
  35. Functional Genetic Tests for Breast Cancer Diagnosis
    GRANT BITTER; Fiscal Year: 2003
    ..as estrogen receptor alpha (ER) positive, and these patients are treated with tamoxifen, or the related drug raloxifene. Tamoxifen is a selective estrogen receptor modulator (SERM) that inhibits the growth of estrogen receptor-..
  36. BREAST CANCER SURVIVORS: EXERCISE AND RALOXIFENE
    Anna Schwartz; Fiscal Year: 2003
    ..innovative study will use a randomized placebo-controlled design to test the effects of (a) exercise and (b) raloxifene in postmenopausal breast cancer survivors (N=240) between 3 months and one year after completing chemotherapy on:..
  37. RALOXIFENE EFFECTS ON COGNITION IN EARLY MENOPAUSE
    MARGARET UPCHURCH; Fiscal Year: 2001
    ..effort to reduce these risks, some physicians are prescribing the selective estrogen receptor modulator (SERM) raloxifene (trade name Evista) for the prevention of osteoporosis...
  38. Estrogen receptor signaling in diabetes prevention
    Franck Mauvais Jarvis; Fiscal Year: 2005
    ..To address this issue, we propose: 1) To determine whether the SERM, raloxifene, can prevent pancreatic beta-cell destruction in vivo in diabetic rodents...
  39. FRET-based HTS Assay for Estrogen Receptor Modulators
    SID DE; Fiscal Year: 2003
    ..Knowledge of SERMs, such as Tamoxifen and Raloxifene, has led to the development of novel drugs to treat a variety of conditions...
  40. EFFICACY STUDIES OF CHEMOPREVENTIVE AGENTS IN ANIMAL MOD
    Clinton Grubbs; Fiscal Year: 2000
    ..9-cis Retinoic acid, Raloxifene, Celecoxib, Zileutin are being administered in the diet singly and in combination...
  41. Estrogen: Chrodroprotective or Destructive?
    Sally Frenkel; Fiscal Year: 2002
    ..to estrogen, we will also examine the effects on cartilage of the specific estrogen receptor modulator (SERM) raloxifene, currently used in lieu of estrogen replacement therapy as a preventive and treatment for the postmenopausal ..
  42. ESTROGEN COMPOUNDS, COGNITION & DEMENTIA IN OLDER WOMEN
    Kristine Yaffe; Fiscal Year: 2002
    ..2) To determine whether elderly women treated for four years with a new selective estrogen receptor modulator, raloxifene, have better cognitive function and less incidence of dementia than women treated with placebo, (3) To determine ..
  43. ESTROGEN RECEPTOR FORMS IN NORMAL & MALIGNANT ENDOMETRIA
    Laurel Rice; Fiscal Year: 2001
    ..The function of these variants, in response to estrogen and antiestrogens including Tamoxifen, Raloxifene, and ICI compounds, will be assessed...
  44. Understanding the SELENA trial: Estrogen in Lupus
    Betty Diamond; Fiscal Year: 2007
    ..it may be that such patients would benefit from selective estrogen receptor modulators such as tamoxifen or raloxifene or from aromatase inhibitors...
  45. RECEPTOR FUNCTION IN BREAST CANCERS WITH HIGH ER PROTEIN
    Mark Nichols; Fiscal Year: 2001
    ..However, response to endocrine therapies such as tamoxifen and raloxifene require a functional ER...
  46. MECHANISMS OF ESTROGEN MEDIATED VASOPROTECTION
    Suzanne Oparil; Fiscal Year: 1999
    ..c. or locally to the adventitial surface of the injured artery, or by the selective estrogen receptor agonist raloxifene. The effects of the selective estrogen receptor antagonist ICI-182780 will also be examined...
  47. PSYCHOSOCIAL SEQUELAE TO PREDISPOSITION GENETIC TESTING
    Jeannie Pasacreta; Fiscal Year: 2001
    ..will meet regularly with 2 investigators from the STAR trial, designed to compare the efficacy of tamoxifen and raloxifene as preventive breast cancer agents in women at increased risk...
  48. GENDER DIFFERENCES IN OSTEOPOROSIS
    Elizabeth Barrett Connor; Fiscal Year: 2002
    ....
  49. Breast Cancer Prevention by Letrozole in High Risk Women
    Carol J Fabian; Fiscal Year: 2010
    ....
  50. Endogenous/Exogenous Sex Hormones & CHD Risk Factors
    Elizabeth Barrett Connor; Fiscal Year: 2003
    ..These observations may aid in deciding whether individual women should use HRT and, if so, which regimen would provide the most benefit with the least risk. ..
  51. CHEMOPREVENTION FOR WOMEN AT HIGH RISK OF BREAST CANCER
    CAROL FABIAN; Fiscal Year: 2003
    ..The answer impacts on the entire future of breast cancer chemoprevention development efforts. ..
  52. FlaxSeed Lignan for Breast Cancer Chemoprevention
    CAROL FABIAN; Fiscal Year: 2007
    ..If positive, the results of this study will be critical to the design and implementation of a placebo-controlled Phase II prevention trial with Brevail and/or commercial flaxseed. [unreadable] [unreadable]..
  53. Outcomes of Sleep Disorders in Older Men
    Elizabeth Barrett Connor; Fiscal Year: 2007
    ..We will also supplement the bank of MrOS specimens to allow for testing of future hypotheses concerning the role of sleep in the development of age-related diseases and conditions. ..
  54. Breast Cancer Risk Biomarkers and Energy Balance
    CAROL FABIAN; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  55. CVD Predictors of Cognitive Function Trajectory over 20 Years
    Elizabeth L Barrett Connor; Fiscal Year: 2010
    ..This information is important given the aging of the population, the fact that CVD risk factors are modifiable, and because the maintenance of cognitive function is an essential component of healthy aging. ..
  56. EFFECT OF RALOXIFENE ON SALIVARY STEROIDS
    VIRGIL JORDAN; Fiscal Year: 2002
    DESCRIPTION: (Applicant's Description) Raloxifene, a chemical cousin of tamoxifen, is currently being tested as a breast cancer preventive in Study of Tamoxifen and Raloxifene (STAR) in postmenopausal, high-risk women...
  57. Pharmacogenetics of Sulfate Conjugation
    VIRGIL JORDAN; Fiscal Year: 2006
    ..These results will increase our understanding of the contribution of SULT1A1 pharmacogenetics to individual variation in response to estrogens and an important antiestrogen. ..
  58. Family Cardiac Caregiver Investigation to Evaluate Outcomes (FIT-O)
    Lori J Mosca; Fiscal Year: 2010
    ..Improved adherence to evidence-based preventive therapies could have a substantial public health benefit. ..
  59. ADAM: Androgen Deprivation vs. Antiandrogen Monotherapy
    Matthew Smith; Fiscal Year: 2004
    ..In addition, this project will provide important insights into the relative contributions of testosterone and estrogen in bone metabolism, and maintenance of muscle size and strength in older men. ..
  60. UCSF-KAISER WOMEN'S HEALTH INTERDISCIPLINARY SCHOLARSHIP
    Deborah Grady; Fiscal Year: 2004
    ..Our goal is to create a model national resource for training successful investigators in women's health. ..
  61. WHI Sex Hormone & Genetic Risk Factors for Hip Fracture
    Steven Cummings; Fiscal Year: 2005
    ..The proposed study is a very efficient approach to understanding the etiologies of hip fracture. ..
  62. QUANTITATIVE ASSOCIATION METHODS FOR GENE MAPPING
    Daniel Schaid; Fiscal Year: 2001
    ..The advantages of this proposed research, over those currently used to identify and characterize genes of complex diseases, are that it will offer a more powerful and flexible method to find these types of genes. ..