azasteroids

Summary

Summary: Steroidal compounds in which one or more carbon atoms in the steroid ring system have been substituted with nitrogen atoms.

Top Publications

  1. ncbi Effect of dutasteride on the risk of prostate cancer
    Gerald L Andriole
    Division of Urology, Washington University School of Medicine in St Louis, St Louis, MO 63110, USA
    N Engl J Med 362:1192-202. 2010
  2. ncbi Dutasteride
    Hannah C Evans
    Adis International Limited, Auckland, New Zealand
    Drugs Aging 20:905-16; discussion 917-8. 2003
  3. ncbi Improved supersaturation and oral absorption of dutasteride by amorphous solid dispersions
    In Hwan Beak
    College of Pharmacy, Chungnam National University, 220 Gung Dong, Yuseong Gu, Daejeon 305 764, Republic of Korea
    Chem Pharm Bull (Tokyo) 60:1468-73. 2012
  4. ncbi Cost-effectiveness of combination therapy for treatment of benign prostatic hyperplasia: a model based on the findings of the Combination of Avodart and Tamsulosin trial
    Truls E Bjerklund Johansen
    Urology Department, Arhus University Hospital, Arhus, Denmark
    BJU Int 109:731-8. 2012
  5. ncbi Pharmacologic basis for the enhanced efficacy of dutasteride against prostatic cancers
    Yi Xu
    Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland 21231, USA
    Clin Cancer Res 12:4072-9. 2006
  6. ncbi Effect of dutasteride on the expression of hypoxia-inducible factor-1alpha, vascular endothelial growth factor and microvessel density in rat and human prostate tissue
    Ja Hyeon Ku
    Department of Urology, Seoul National University College of Medicine, Seoul, Korea
    Scand J Urol Nephrol 43:445-53. 2009
  7. ncbi The effects of combination therapy with dutasteride and tamsulosin on clinical outcomes in men with symptomatic benign prostatic hyperplasia: 4-year results from the CombAT study
    Claus G Roehrborn
    Department of Urology, UT Southwestern Medical Center, Dallas, Texas 75390 9110, USA
    Eur Urol 57:123-31. 2010
  8. ncbi Efficacy and safety of a dual inhibitor of 5-alpha-reductase types 1 and 2 (dutasteride) in men with benign prostatic hyperplasia
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390 9110, USA
    Urology 60:434-41. 2002
  9. ncbi Differential expression of steroid 5alpha-reductase isozymes and association with disease severity and angiogenic genes predict their biological role in prostate cancer
    Kakoli Das
    Cancer Science Institute, Department of Pathology, National University Health System, National University of Singapore, 28 Medical Drive, Singapore
    Endocr Relat Cancer 17:757-70. 2010
  10. ncbi Dutasteride, the dual 5alpha-reductase inhibitor, inhibits androgen action and promotes cell death in the LNCaP prostate cancer cell line
    C B Lazier
    Department of Biochemistry and Molecular Biology, Dalhousie University, Halifax, NS, Canada
    Prostate 58:130-44. 2004

Detail Information

Publications189 found, 100 shown here

  1. ncbi Effect of dutasteride on the risk of prostate cancer
    Gerald L Andriole
    Division of Urology, Washington University School of Medicine in St Louis, St Louis, MO 63110, USA
    N Engl J Med 362:1192-202. 2010
    ..We conducted a study to determine whether dutasteride reduces the risk of incident prostate cancer, as detected on biopsy, among men who are at increased risk for the disease...
  2. ncbi Dutasteride
    Hannah C Evans
    Adis International Limited, Auckland, New Zealand
    Drugs Aging 20:905-16; discussion 917-8. 2003
    ..With the exception of gynaecomastia, incidence consistently decreased over time...
  3. ncbi Improved supersaturation and oral absorption of dutasteride by amorphous solid dispersions
    In Hwan Beak
    College of Pharmacy, Chungnam National University, 220 Gung Dong, Yuseong Gu, Daejeon 305 764, Republic of Korea
    Chem Pharm Bull (Tokyo) 60:1468-73. 2012
    ..These results suggest that amorphous solid dispersions containing Eudragit E, formed by a spray-drying process, offer enhanced supersaturation characteristics, leading to increased oral absorption of dutasteride...
  4. ncbi Cost-effectiveness of combination therapy for treatment of benign prostatic hyperplasia: a model based on the findings of the Combination of Avodart and Tamsulosin trial
    Truls E Bjerklund Johansen
    Urology Department, Arhus University Hospital, Arhus, Denmark
    BJU Int 109:731-8. 2012
    ....
  5. ncbi Pharmacologic basis for the enhanced efficacy of dutasteride against prostatic cancers
    Yi Xu
    Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, Baltimore, Maryland 21231, USA
    Clin Cancer Res 12:4072-9. 2006
    ..Therefore, the levels of expression SRD5A1 and SRD5A2 and the antiprostatic cancer growth response to finasteride, a selective SRD5A2 inhibitor, versus the dual SRD5A1 and SRD5A2 inhibitor, dutasteride, were compared...
  6. ncbi Effect of dutasteride on the expression of hypoxia-inducible factor-1alpha, vascular endothelial growth factor and microvessel density in rat and human prostate tissue
    Ja Hyeon Ku
    Department of Urology, Seoul National University College of Medicine, Seoul, Korea
    Scand J Urol Nephrol 43:445-53. 2009
    ..To evaluate the effects of dutasteride on the expression of angiogenesis markers in rat and human prostates...
  7. ncbi The effects of combination therapy with dutasteride and tamsulosin on clinical outcomes in men with symptomatic benign prostatic hyperplasia: 4-year results from the CombAT study
    Claus G Roehrborn
    Department of Urology, UT Southwestern Medical Center, Dallas, Texas 75390 9110, USA
    Eur Urol 57:123-31. 2010
    ....
  8. ncbi Efficacy and safety of a dual inhibitor of 5-alpha-reductase types 1 and 2 (dutasteride) in men with benign prostatic hyperplasia
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390 9110, USA
    Urology 60:434-41. 2002
    ..To study the efficacy and safety of dutasteride, a dual inhibitor of the 5-alpha-reductase isoenzymes types I and II...
  9. ncbi Differential expression of steroid 5alpha-reductase isozymes and association with disease severity and angiogenic genes predict their biological role in prostate cancer
    Kakoli Das
    Cancer Science Institute, Department of Pathology, National University Health System, National University of Singapore, 28 Medical Drive, Singapore
    Endocr Relat Cancer 17:757-70. 2010
    ..Interestingly, some angiogenic genes remained activated after treatment, possibly due to the duration of treatment and tumor resistance to inhibitors...
  10. ncbi Dutasteride, the dual 5alpha-reductase inhibitor, inhibits androgen action and promotes cell death in the LNCaP prostate cancer cell line
    C B Lazier
    Department of Biochemistry and Molecular Biology, Dalhousie University, Halifax, NS, Canada
    Prostate 58:130-44. 2004
    ..The objective of this study was to compare and contrast the effects of a potent new 5alphaR inhibitor, dutasteride, with finasteride in the LNCaP prostate cancer cell line...
  11. pmc Projecting prostate cancer mortality in the PCPT and REDUCE chemoprevention trials
    Paul F Pinsky
    Division of Cancer Prevention, National Cancer Institute, Bethesda, MD 20892, USA
    Cancer 119:593-601. 2013
    ..The authors attempted to estimate the effect of these drugs on prostate cancer mortality to be able to better evaluate the cost-benefit tradeoff...
  12. pmc The effect of finasteride and dutasteride on the growth of WPE1-NA22 prostate cancer xenografts in nude mice
    Alexander B Opoku-Acheampong
    Department of Human Nutrition, Kansas State University, Manhattan, Kansas, United States of America
    PLoS ONE 7:e29068. 2012
    ....
  13. pmc Effects of the 5 alpha-reductase inhibitor dutasteride on gene expression in prostate cancer xenografts
    Lucy J Schmidt
    Department of Urology Research, Mayo Clinic College of Medicine, Mayo Clinic, Rochester, MN 55905, USA
    Prostate 69:1730-43. 2009
    ..In this study, we sought to determine how dutasteride is functioning at the molecular level, using a prostate cancer xenograft model...
  14. ncbi Effect of the dual 5alpha-reductase inhibitor dutasteride on markers of tumor regression in prostate cancer
    G L Andriole
    Division of Urologic Surgery, Washington University School of Medicine, 660 S Euclid, St Louis, MO 63110, USA
    J Urol 172:915-9. 2004
    ..In this short-term pilot study we examined the effect of the dual 5alphaR inhibitor dutasteride on markers of tumor regression...
  15. ncbi Effects of dutasteride on prostate growth in the large probasin-large T antigen mouse model of prostate cancer
    T C Shao
    Department of Medicine, Michael E DeBakey Veterans Affairs Medical Center, Houston, Texas 77030, USA
    J Urol 178:1521-7. 2007
    ..We evaluated the effects of dutasteride for preventing or delaying prostate growth and neoplastic changes in a transgenic model of prostate cancer...
  16. ncbi Recent advances in azasteroids chemistry
    Malika Ibrahim-Ouali
    UMR 6180 CNRS and Universite d Aix Marseille III Chirotechnologies catalyse et biocatalyse, Laboratoire de Synthese Organique associe au CNRS, Faculte des Sciences et Techniques de Saint Jerome, Marseille Cedex 20, France
    Steroids 73:375-407. 2008
    ..Moreover, the biological properties of modified steroids have proved to be of interest. The recent development in the partial and total syntheses of azasteroids is herein described.
  17. ncbi Formulation and in vivo evaluation of a self-microemulsifying drug delivery system of dutasteride
    G H Choo
    Department of Pharmaceutical Engineering, Inje University, Gimhae, Republic of Korea
    Drug Res (Stuttg) 63:203-9. 2013
    ..Therefore, preliminary results from our study suggest that the dutasteride-loaded self-microemulsifying formulation has a great potential for clinical application...
  18. ncbi Effect of dutasteride on the detection of prostate cancer in men with benign prostatic hyperplasia
    G L Andriole
    Washington University School of Medicine, St Louis, Missouri 63110, USA
    Urology 64:537-41; discussion 542-3. 2004
    ..However, its effect on the development of prostate cancer is unknown...
  19. ncbi 5alpha-Reductase inhibitor treatment of prostatic diseases: background and practical implications
    J Dörsam
    St Theresienkrankenhaus, Nurnberg, Germany
    Prostate Cancer Prostatic Dis 12:130-6. 2009
    ..Whether the different pharmacokinetic and pharmacodynamic properties of Finasteride and Dutasteride are of clinical importance cannot be judged at this time...
  20. ncbi Chemoprevention of prostate cancer in men at high risk: rationale and design of the reduction by dutasteride of prostate cancer events (REDUCE) trial
    Gerald Andriole
    Division of Urologic Surgery, Department of Surgery, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Urol 172:1314-7. 2004
    ..It represents a biologically plausible target for chemoprevention through the inhibition of 5alpha-reductase isoenzymes...
  21. ncbi Side chain azasteroids and thiasteroids as sterol methyltransferase inhibitors in ergosterol biosynthesis
    Delphine Renard
    Department Pharmazie Zentrum für Pharmaforschung, Ludwig Maximilians Universitat, Butenandtstrasse 5 13, 81377 Munich, Germany
    Bioorg Med Chem 17:8123-37. 2009
    The synthesis of some novel azasteroids and thiasteroids based on a pregnan nucleus with a Delta7 double bond in two to five steps from the key aldehyde (3S,20S)-20-formylpregn-7-en-3-yl acetate has been disclosed herein...
  22. ncbi The effects of dutasteride, tamsulosin, and the combination on storage and voiding in men with benign prostatic hyperplasia and prostatic enlargement: 2-year results from the Combination of Avodart and Tamsulosin study
    E Becher
    Division of Urology, University of Buenos Aires, Buenos Aires, Argentina
    Prostate Cancer Prostatic Dis 12:369-74. 2009
    ..Dutasteride was as effective as tamsulosin for control of storage symptoms, but provided significantly greater relief of voiding symptoms than tamsulosin...
  23. ncbi Clinical outcomes after combined therapy with dutasteride plus tamsulosin or either monotherapy in men with benign prostatic hyperplasia (BPH) by baseline characteristics: 4-year results from the randomized, double-blind Combination of Avodart and Tamsulo
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center, Dallas, TX, USA
    BJU Int 107:946-54. 2011
    ....
  24. ncbi Effect of dutasteride on the symptoms of benign prostatic hyperplasia, and patient quality of life and discomfort, in clinical practice
    Francois Desgrandchamps
    Department of Urology, Saint Louis Hospital, Paris, France
    BJU Int 98:83-8. 2006
    ..To assess the improvements in symptoms, quality of life (QoL), discomfort and satisfaction in patients with symptomatic benign prostatic hyperplasia (BPH) treated with dutasteride in clinical practice...
  25. ncbi Efficacy of neoadjuvant bicalutamide and dutasteride as a cytoreductive regimen before prostate brachytherapy
    Gregory S Merrick
    Schiffler Cancer Center and Wheeling Jesuit University, Wheeling Hospital, Wheeling, West Virginia 26003 6300, USA
    Urology 68:116-20. 2006
    ..To evaluate the cytoreductive effectiveness of combined neoadjuvant bicalutamide and dutasteride before prostate brachytherapy for clinically localized prostate cancer...
  26. ncbi Long-term sustained improvement in symptoms of benign prostatic hyperplasia with the dual 5alpha-reductase inhibitor dutasteride: results of 4-year studies
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center, Dallas, TX 75390 9110, USA
    BJU Int 96:572-7. 2005
    ....
  27. ncbi Chemoprevention using dutasteride: the REDUCE trial
    Leonard G Gomella
    Department of Urology, Thomas Jefferson University, Philadelphia, Pennsylvania 19107, USA
    Curr Opin Urol 15:29-32. 2005
    ....
  28. ncbi Long-term therapy with the dual 5alpha-reductase inhibitor dutasteride is well tolerated in men with symptomatic benign prostatic hyperplasia
    Claude Schulman
    Department of Urology, University Clinics of Brussels, Erasme Hospital, Brussels, Belgium
    BJU Int 97:73-9; discussion 79-80. 2006
    ..To examine the long-term (4-year) safety and tolerability of dutasteride in the treatment of symptomatic benign prostatic hyperplasia (BPH)...
  29. ncbi Azasteroids as antifungals
    Joachim Burbiel
    Department für Pharmazie Zentrum für Pharmaforschung, Ludwig Maximilians Universitat Munchen, Butenandtstr 5 13, 81377 Munchen, Germany
    Steroids 68:587-94. 2003
    b>Azasteroids and derivatives thereof with antifungal potential are reviewed. Special emphasis is put on steroids with nitrogen as part of the steroidal framework, natural substances, and lines of development emerging from them.
  30. ncbi Improvements in benign prostatic hyperplasia-specific quality of life with dutasteride, the novel dual 5alpha-reductase inhibitor
    M P O'Leary
    Department of Surgery, Harvard Medical School, Division of Urology, Brigham and Women s Hospital, Boston, USA
    BJU Int 92:262-6. 2003
    ....
  31. ncbi Eliciting preferences for drug treatment of lower urinary tract symptoms associated with benign prostatic hyperplasia
    V Watson
    Health Economics Research Unit, University of Aberdeen, United Kingdom
    J Urol 172:2321-5. 2004
    ..We investigated the relative importance of and trade-offs between the attributes of the 5alpha-reductase inhibitor dutasteride and alpha-blockers in community dwelling men using a validated technique...
  32. ncbi Combination therapy with dutasteride and tamsulosin in men with moderate-to-severe benign prostatic hyperplasia and prostate enlargement: the CombAT (Combination of Avodart and Tamsulosin) trial rationale and study design
    Paul Siami
    Department of Urology, Welborn Clinic, Evansville, IN 47714, USA
    Contemp Clin Trials 28:770-9. 2007
    ..5 ng/mL. A total of 4838 subjects have been enrolled. This paper describes the rationale, design and baseline data of the CombAT study...
  33. ncbi The effects of dutasteride, tamsulosin and combination therapy on lower urinary tract symptoms in men with benign prostatic hyperplasia and prostatic enlargement: 2-year results from the CombAT study
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center, Dallas, Texas, USA
    J Urol 179:616-21; discussion 621. 2008
    ..We report preplanned 2-year analyses...
  34. pmc Inhibition of the M. tuberculosis 3β-hydroxysteroid dehydrogenase by azasteroids
    Suzanne T Thomas
    Department of Chemistry, Stony Brook University, Stony Brook, NY 11794 3400, United States
    Bioorg Med Chem Lett 21:2216-9. 2011
    ..Three series of 6-azasteroids and 4-azasteroids were employed to define the substrate preferences of M. tb 3β-hydroxysteroid dehydrogenase...
  35. ncbi Dutasteride: a review of its use in the management of prostate disorders
    Susan J Keam
    Wolters Kluwer Health Adis, Auckland, New Zealand
    Drugs 68:463-85. 2008
    ....
  36. ncbi Effective treatment of female androgenic alopecia with dutasteride
    Malgorzata Olszewska
    Department of Dermatology, Warsaw Medical School, Warsaw, Poland
    J Drugs Dermatol 4:637-40. 2005
    ..No side effects were observed. In conclusion, theoretical data and our experience in this case show that dutasteride might develop into a true alternative in treatment of androgenic alopecia...
  37. ncbi [Prevention of prostate cancer]
    M P Wirth
    Klinik und Poliklinik fur Urologie, Technische Universitat Dresden, Dresden
    Dtsch Med Wochenschr 130:2002-4. 2005
    ..Pharmacological prevention seems a possibility with drugs acting on intraprostatic testosterone metabolism. Several large randomised trials are ongoing to clarify the potential for successful prostate cancer prevention...
  38. ncbi The effect of 5alpha-reductase inhibition with dutasteride and finasteride on semen parameters and serum hormones in healthy men
    John K Amory
    Department of Medicine, Veterans Affairs Puget Sound Health Care System, University of Washington, Seattle, WA 98195, USA
    J Clin Endocrinol Metab 92:1659-65. 2007
    ..Dutasteride and finasteride are 5alpha-reductase inhibitors (5ARIs) that dramatically reduce serum levels of dihydrotestosterone (DHT)...
  39. doi Preventing prostate cancer: new analyses put finasteride back on the map
    Brian Vastag
    J Natl Cancer Inst 100:1132-3. 2008
  40. ncbi Selecting therapy for maintaining sexual function in patients with benign prostatic hyperplasia
    Ajay Nehra
    Department of Urology, Mayo Clinic, Rochester, MN 55905, USA
    BJU Int 96:237-43. 2005
    ..Finally, the capacity to be creative in academic departments is extolled as a core property of academicians, and its surfacing described as having the potential to revitalize individuals and departments...
  41. ncbi [Dutasteride-induced gynecomastia]
    David Fernández Olarte
    Med Clin (Barc) 128:279. 2007
  42. pmc The rationale for inhibiting 5alpha-reductase isoenzymes in the prevention and treatment of prostate cancer
    Donald J Tindall
    Mayo Clinic, Rochester, Minnesota 55905, USA
    J Urol 179:1235-42. 2008
    ..Dihydrotestosterone, the primary prostatic androgen, is transformed from testosterone by types 1 and 2 5alpha-reductase and, thus, a potential therapeutic benefit could be achieved through the inhibition of 5alpha-reductase...
  43. ncbi Efficacy and tolerability of the dual 5alpha-reductase inhibitor, dutasteride, in the treatment of benign prostatic hyperplasia in African-American men
    C G Roehrborn
    Department of Urology, The University of Texas Southwestern Medical Center at Dallas, Dallas, TX 75390, USA
    Prostate Cancer Prostatic Dis 9:432-8. 2006
    ..Therefore, dutasteride demonstrated similar efficacy and safety profiles in African-Americans and Caucasians...
  44. ncbi Finasteride to evaluate the efficacy of dutasteride in the management of patients with lower urinary tract symptoms and enlarged prostate
    I R Ravish
    Department of Urology, KLES Kidney Foundation, Belgaum, India
    Arch Androl 53:17-20. 2007
    ..Dutasteride with its inhibitory effects on type 1 and 2 5alpha-reductase, produces significantly better results than Finasteride...
  45. ncbi The REDUCE trial: chemoprevention in prostate cancer using a dual 5alpha-reductase inhibitor, dutasteride
    Mireia Musquera
    University Clinics of Barcelona, c o Alexandre R Zlotta, Mount Sinai Hospital, Joseph and Wolf Lebovic Building, 60 Murray Street, 6th Floor, Box 19, Toronto, Ontario M5T 3L9, Canada
    Expert Rev Anticancer Ther 8:1073-9. 2008
    ..As a result, dutasteride is being investigated for prostate cancer prevention in the ongoing Reduction by Dutasteride of Prostate Cancer Events (REDUCE) trial, which is discussed here...
  46. ncbi Update on prostate cancer chemoprevention
    Jennifer Fisher Lowe
    Department of Pharmacy, Akron General Medical Center, Akron, Ohio 44307, USA
    Pharmacotherapy 26:353-9. 2006
    ..Its high rate of occurrence and long lead time to clinically significant disease make prostate cancer an ideal disease for pharmacologic or nutritional chemoprevention...
  47. ncbi Effects of dutasteride on prostate carcinoma primary cultures: a comparative study with finasteride and MK386
    Claudio Festuccia
    Department of Experimental Medicine, University of L Aquila, L Aquila, Italy
    J Urol 180:367-72. 2008
    ....
  48. ncbi Actions of 5alpha-reductase inhibitors on the epididymis
    Bernard Robaire
    Departments of Pharmacology and Therapeutics and of Obstetrics and Gynecology, McGill University, Montreal, Que, Canada
    Mol Cell Endocrinol 250:190-5. 2006
    ..Mating females to treated males resulted in fewer successful pregnancies and a higher rate of pre-implantation loss. Thus, there may be a role for dual 5alpha-reductase inhibitors as potential components of a male contraceptive...
  49. ncbi Comparative analysis of alpha-blocker utilization in combination with 5-alpha reductase inhibitors for enlarged prostate in a managed care setting among Medicare-aged men
    Muta M Issa
    Department of Urology, Emory University, 1670 Clairmont Rd, Decatur, GA 30033, USA
    Am J Manag Care 14:S160-6. 2008
    ..To evaluate the likelihood of alpha-adrenergic antagonist (alpha-blocker) discontinuation in combination with dutasteride or finasteride among patients aged > or =65 years with enlarged prostate...
  50. ncbi [Effect of dutasteride on reduction of plasma DHT following finasteride therapy in patients with benign prostatic hyperplasia]
    Henry Botto
    Service d Urologie, Hopital Foch, Suresnes, France
    Prog Urol 15:1090-5. 2005
    ....
  51. ncbi Oral testosterone in oil: pharmacokinetic effects of 5alpha reduction by finasteride or dutasteride and food intake in men
    John K Amory
    University of Washington, Box 356429, 1959 NE Pacific St, Seattle, WA 98195, USA
    J Androl 27:72-8. 2006
    ..Additional studies of the combination of oral T in oil with 5alpha-reductase inhibitors as a novel form of oral T therapy are warranted...
  52. ncbi An update on the use of 5alpha-reductase inhibitors
    Charlotte L Foley
    Institute of Urology and Nephrology, UCL, London, UK
    Drugs Today (Barc) 40:213-23. 2004
    ..Wider applications of 5alpha-reductase inhibitors are also emerging, though their perhaps most important new role as chemopreventive agents remains unclear...
  53. ncbi Pharmacogenetic analysis of human steroid 5 alpha reductase type II: comparison of finasteride and dutasteride
    Nick Makridakis
    Department of Biochemistry and Molecular Biology and Institute for Genetic Medicine, Keck School of Medicine of the University of Southern California, 2250 Alcazar Street, IGM240, Los Angeles, California 90089 9075, USA
    J Mol Endocrinol 34:617-23. 2005
    ....
  54. ncbi RE: Effect of the dual 5alpha-reductase inhibitor dutasteride on markers of tumor regression in prostate cancer
    W Reid Pitts
    J Urol 173:1433-4; author reply 1434-5. 2005
  55. ncbi 5 alpha-reductase inhibitors: what's new?
    Charlotte L Foley
    Prostate Cancer Research Unit, Institute of Urology and Nephrology, University College London, 67 Riding House Street, London W1W 7EY, UK
    Curr Opin Urol 13:31-7. 2003
    ..Medical therapy is now the first-line treatment for most men with symptomatic benign prostatic hyperplasia. This review aims to highlight the recent contributions to our understanding of 5 alpha-reductase inhibitor usage...
  56. ncbi [Benign prostatic hyperplasia: medical therapy]
    B Schlenker
    Klinik und Poliklinik fur Urologie, Klinikum Grosshadern, Ludwig Maximilians Universitat Munchen
    MMW Fortschr Med 149:29-31; quiz 32. 2007
    ..Plant extracts, alpha-blockers and 5-alpha reductase inhibitors represent the most common prescribed substances. Recent data suggest beneficial effects for the use of antimuscarinic agents and phosphodiesterase type 5 inhibitors...
  57. ncbi Dihydrotestosterone and the concept of 5alpha-reductase inhibition in human benign prostatic hyperplasia
    G Bartsch
    Department of Urology, University of Innsbruck, Austria
    World J Urol 19:413-25. 2002
    ..A clinical evaluation of potent dual 5alpha-reductase inhibitors may help to define the relative roles of human type 1 and 2 5alpha-reductase in the pathophysiology of benign prostatic hyperplasia and other androgen-dependent diseases...
  58. ncbi Efficacy and safety of dutasteride in the four-year treatment of men with benign prostatic hyperplasia
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center at Dallas, Dallas, Texas 75390 9110, USA
    Urology 63:709-15. 2004
    ..To assess the long-term safety and efficacy of dutasteride, a dual type 1 and type 2 5-alpha-reductase inhibitor, in the treatment of symptomatic benign prostatic hyperplasia and associated lower urinary tract symptoms...
  59. ncbi Pharmacokinetic parameters and mechanisms of inhibition of rat type 1 and 2 steroid 5alpha-reductases: determinants for different in vivo activities of GI198745 and finasteride in the rat
    J D Stuart
    Division of Biochemistry, Glaxo Wellcome Inc, 5 Moore Drive, Research Triangle Park, NC 27709, USA
    Biochem Pharmacol 62:933-42. 2001
    ..Therefore, we hypothesize that because of its pharmacokinetic parameters and increased potency against r5AR1, GI198745 is more effective than finasteride in preventing the growth of the rat prostate...
  60. ncbi Stable expression of the human 5alpha-reductase isoenzymes type I and type II in HEK293 cells to identify dual and selective inhibitors
    W Reichert
    Fachrichtung 12.1 Pharmazeutische und Medizinische Chemie, , , Germany
    J Enzyme Inhib 16:47-53. 2001
    ..Reaction products were quantified by a HPLC reversed phase technique. Using the new cell assays, selective as well as novel dual 5alpha-reductase inhibitors with IC50 values between 1.0 and 2.5 microM were identified...
  61. ncbi Type 1 and type 2 5alpha-reductase expression in the development and progression of prostate cancer
    Lynn N Thomas
    Department of Biochemistry and Molecular Biology, Dalhousie University, Halifax, Nova Scotia, Canada
    Eur Urol 53:244-52. 2008
    ..The objective of this study was to evaluate the role of both isoenzymes during development/progression of prostate cancer...
  62. ncbi 5-Alpha reductase inhibitors in men with an enlarged prostate: an evaluation of outcomes and therapeutic alternatives
    Michael Naslund
    University of Maryland School of Medicine, Baltimore, MD, USA
    Am J Manag Care 14:S148-53. 2008
    ....
  63. pmc Role of 5 alpha-reductase inhibitors in the management of prostate cancer
    Steven J Hudak
    Urology Service, Department of Surgery, Brooke Army Medical Center, Fort Sam Houston, TX 78234 6200, USA
    Clin Interv Aging 1:425-31. 2006
    ..Finally, 5AR inhibitors have been studied as a component of multimodal therapy for all stages of prostate cancer, with the goal of improving oncologic outcomes while avoiding the toxicity of medical and surgical castration...
  64. ncbi A review of the clinical efficacy and safety of 5alpha-reductase inhibitors for the enlarged prostate
    Michael J Naslund
    University of Maryland School of Medicine, Baltimore, Maryland 21201, USA
    Clin Ther 29:17-25. 2007
    ..Current pharmacologic treatment options include alpha-blockers (alfuzosin, doxazosin, tamsulosin, and terazosin) and 5alpha-reductase inhibitors (5ARIs) (finasteride and dutasteride)...
  65. ncbi Effects of 5 alpha reductase inhibitors on androgen-dependent human prostatic carcinoma cells
    Claudio Festuccia
    Prostate Biology Laboratory Department of Experimental Medicine, University of L Aquila Science and Technology School, Via Vetoio Coppito 2, 67100 L Aquila, Italy
    J Cancer Res Clin Oncol 131:243-54. 2005
    ....
  66. pmc Two for the price of one?
    Mike Wyllie
    Urodoc Ltd, Maryland Ridgeway Road, Herne, Kent CT6 7LN, UK
    Br J Pharmacol 144:1-2. 2005
  67. ncbi Effect of dutasteride on intraprostatic androgen levels in men with benign prostatic hyperplasia or prostate cancer
    Roger Rittmaster
    Urology Clinical Development and Medical Affairs, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA
    Urology 72:808-12. 2008
    ..The aim of this analysis was to assess the effects of the approved dose of dutasteride (0.5 mg/d), given for 2 weeks to 4 months, on the serum and intraprostatic DHT and testosterone levels in 3 randomized studies...
  68. ncbi Evaluation and medical management of benign prostatic hyperplasia
    Thomas J Beckman
    Division of General Internal Medicine, Men s Health Center for Urology, and Department of Urology, Mayo Clinic College of Medicine, Rochester, MN 55905, USA
    Mayo Clin Proc 80:1356-62. 2005
    ..We also review supporting evidence and treatment considerations for saw palmetto and the 2 major classes of prescription medications, alpha1-adrenergic antagonists and 5alpha-reductase inhibitors...
  69. ncbi Dutasteride: a potent dual inhibitor of 5-alpha-reductase for benign prostatic hyperplasia
    Xavier Rabasseda
    Medical Information Department, Prous Science, Barcelona, Spain
    Drugs Today (Barc) 40:649-61. 2004
    ....
  70. ncbi Dihydrotestosterone and the prostate: the scientific rationale for 5alpha-reductase inhibitors in the treatment of benign prostatic hyperplasia
    Gerald Andriole
    Division of Urological Surgery, Washington University in St Louis, St Louis, Missouri 63110, USA
    J Urol 172:1399-403. 2004
    ..We reviewed the physiological and pathogenic role of dihydrotestosterone (DHT), evidence for the beneficial effects of decreasing DHT through 5alpha-reductase inhibition and the effects of altering the androgen balance with these agents...
  71. ncbi Association between 5-alpha reductase inhibition and risk of hip fracture
    Steven J Jacobsen
    Department of Research and Evaluation, Kaiser Permanente Southern California, 100 S Los Robles Ave, Second Floor, Pasadena, CA 91101, USA
    JAMA 300:1660-4. 2008
    ..Short-term studies show no effects of these agents on bone metabolism,but long-term data are not available...
  72. ncbi [Hormonal therapy for benign prostatic hyperplasia]
    Hideki Sakai
    Department of Urology, Nagasaki University School of Medicine
    Nihon Rinsho 60:358-61. 2002
  73. ncbi Effects of potential inhibitors on Brugia pahangi in vitro: macrofilaricidal action and inhibition of microfilarial production
    G C Barker
    Department of Parasitology, Liverpool School of Tropical Medicine, UK
    Parasitology 99:409-16. 1989
    ..The azasteroids, 25-azacoprostane and 25-azacholestane, inhibited the production of microfilariae at 5 ppm, the former also ..
  74. ncbi Tissue distribution and kinetic characteristics of rat steroid 5 alpha-reductase isozymes. Evidence for distinct physiological functions
    K Normington
    Department of Molecular Genetics, University of Texas Southwestern Medical Center, Dallas 75235
    J Biol Chem 267:19548-54. 1992
    ..The isozymes differ in their inhibition by various 4-azasteroids with the type 2 isozyme showing exquisite sensitivity (Ki = 40 pM) to 21,21-pentamethylene-4-aza-5 alpha-pregn-..
  75. pmc Structural and biochemical properties of cloned and expressed human and rat steroid 5 alpha-reductases
    S Andersson
    Department of Molecular Genetics, University of Texas Southwestern Medical Center, Dallas 75235
    Proc Natl Acad Sci U S A 87:3640-4. 1990
    ..However, synthetic 4-azasteroids demonstrated marked differences in their abilities to inhibit the human and rat steroid 5 alpha-reductases.
  76. ncbi 3D-QSAR studies on unsaturated 4-azasteroids as human 5alpha-reductase inhibitors: a self organizing molecular field analysis approach
    Saurabh Aggarwal
    University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160 014, India
    Eur J Med Chem 45:476-81. 2010
    b>Azasteroids have been reported as inhibitors of human 5alpha-reductase enzyme. These were designed by substitution of one carbon atom of steroidal A ring by heteroatom nitrogen...
  77. ncbi Substrate interaction with 5alpha-reductase enzyme: influence of the 17beta-chain chirality in the mechanism of action of 4-azasteroid inhibitors
    P Grisenti
    Poli Industria Chimica SpA, Via Volturno 45 48, Quinto de Stampi, Rozzano, Milan, Italy
    Steroids 66:803-10. 2001
    ..For this purpose diastereomerically pure 4-azasteroids epimers at C-22 were prepared (compounds 1-11) and tested as inhibitors of 5AR in "in vitro" tests...
  78. ncbi [Specific antigen prostatic changes during treatment with finasteride or dutasteride for benign prostatic hyperplasia]
    F Arena
    Struttura Semplice di Urologia, Ospedale S Maria, Borgo Val di Taro Parma, Italy
    Minerva Urol Nefrol 65:211-6. 2013
    ....
  79. ncbi Advances in prostate cancer chemoprevention: a translational perspective
    Dhanya Nambiar
    Cancer Biology Laboratory, School of Life Sciences, Jawaharlal Nehru University, New Delhi, India
    Nutr Cancer 65:12-25. 2013
    ..Incoherency of data with these agents urges for a stringent study design and thorough interpretation to accurately judge the necessity and feasibility of the preventive measures...
  80. ncbi Activity of dutasteride plus ketoconazole in castration-refractory prostate cancer after progression on ketoconazole alone
    Oliver Sartor
    Dana Farber Cancer Institute, Boston, MA, USA
    Clin Genitourin Cancer 7:E90-2. 2009
    ..We hypothesized that SRDA5 inhibition in combination with ketoconazole would mitigate progression after treatment with ketoconazole alone...
  81. ncbi Effect of dutasteride, tamsulosin and the combination on patient-reported quality of life and treatment satisfaction in men with moderate-to-severe benign prostatic hyperplasia: 2-year data from the CombAT trial
    Jack Barkin
    Department of Urology, University of Toronto, Toronto, Canada
    BJU Int 103:919-26. 2009
    ....
  82. ncbi Comparative study of sister chromatid exchange induction and antitumor effects by homo-aza-steroidal esters of [p-[bis(2-chloroethyl)amino]phenyl]butyric acid
    C Camoutsis
    Laboratory of Pharmaceutical Chemistry, Patras, Greece
    Cancer Detect Prev 25:558-64. 2001
    ..Therefore, the order of the antitumor effectiveness of the three compounds coincided with the order of the cytogenetic effects they induced...
  83. ncbi Pharmacological approaches to reducing the risk of prostate cancer
    Roger S Rittmaster
    Oncology Clinical Development, GlaxoSmithKline, Research Triangle Park, North Carolina 27709, USA
    Eur Urol 55:1064-73. 2009
    ..It is now possible to reduce a man's risk of developing biopsy-detectable prostate cancer. This review addresses the evidence and issues surrounding prostate cancer risk reduction...
  84. ncbi [Add-on effect of dutasteride in patients with benign prostatic hyperplasia treated with alpha blocker : its effect on overactive bladder]
    Naoki Wada
    The Department of Renal and Urologic Surgery, Asahikawa Medical University, Japan
    Hinyokika Kiyo 58:475-80. 2012
    ..In conclusion, dutasteride add-on therapy is beneficial in patients with BPH who do not show enough improvement with alpha-blocker monotherapy...
  85. ncbi Aromatization mediates aggressive behavior in quail
    B A Schlinger
    Department of Psychology, University of California, Los Angeles 90024
    Gen Comp Endocrinol 79:39-53. 1990
    ....
  86. ncbi Multicomponent domino reactions for the synthesis of biologically active natural products and drugs
    L F Tietze
    Institute of Organic Chemistry of the Georg August Universität, Tammannstrasse 2, D 37075 G ottingen, Germany
    Med Res Rev 20:304-22. 2000
    ..23 and (-)-dihydroantirhine 24 as well as heterosteroids 62, D-homosteroids 65 and 68, and azasteroids 25 are prepared...
  87. ncbi Frontal fibrosing alopecia: a retrospective review of 19 patients seen at Duke University
    Barry Ladizinski
    Hair Disorders Research and Treatment Center, Duke University Medical Center, Durham, North Carolina, USA
    J Am Acad Dermatol 68:749-55. 2013
    ..The incidence is unknown, but the number of women presenting with this condition has significantly increased in recent years. No effective therapy has been established...
  88. ncbi 5-alpha reductase inhibitors in patients on active surveillance: do the benefits outweigh the risk?
    Ghazi Al Edwan
    Division of Urology, Princess Margaret Hospital, University Health Network, Toronto, Ontario, Canada
    Curr Urol Rep 14:223-6. 2013
    ....
  89. pmc Prostate cancer cells differ in testosterone accumulation, dihydrotestosterone conversion, and androgen receptor signaling response to steroid 5α-reductase inhibitors
    Yue Wu
    Department of Cancer Prevention and Control, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Prostate 73:1470-82. 2013
    ..Factors affecting intracellular androgen levels and the androgen receptor (AR) signaling axis need to be examined systematically in order to fully understand the outcome of interventions using these drugs...
  90. ncbi Inhibition of pyridine-nucleotide-dependent enzymes by pyrazoles. Synthesis and enzymology of a novel A-ring pyrazole steroid
    D A Holt
    Department of Medicinal Chemistry, Smith Kline and French Laboratories, Swedeland, PA 19479
    Steroids 48:213-22. 1986
    ..Dead end inhibition studies indicate an ordered binding of cofactor prior to substrate or pyrazole inhibitor...
  91. ncbi Novel 4-azasteroidal N-glycoside analogues bearing sugar-like D ring: synthesis and anticancer activities
    Li Hua Huang
    School of Pharmaceutical Science, Zhengzhou Univercity, Ke Xue Da Dao 100, Zhengzhou 450001, PR China
    Bioorg Med Chem Lett 21:6203-5. 2011
    ....
  92. ncbi Samarium diiodide induced ketyl-(het)arene cyclisations towards novel N-heterocycles
    Christine Beemelmanns
    Institut fur Chemie und Biochemie, Freie Universitat Berlin, Takustrasse 3, 14195 Berlin, Germany
    Chem Soc Rev 40:2199-210. 2011
    ..All these examples demonstrate the high synthetic potential of samarium ketyl-(het)arene cyclisations for the preparation of various types of important heterocyclic compounds...
  93. ncbi Discovery and clinical development of dutasteride, a potent dual 5alpha-reductase inhibitor
    Stephen V Frye
    Department of High Throughput Chemistry, Discovery Research, GlaxoSmithKline Research and Development, Research Triangle Park, North Carolina 27709, USA
    Curr Top Med Chem 6:405-21. 2006
    ..The connections between preclinical drug design and clinical outcomes during the discovery and development of dutasteride are exemplified...
  94. ncbi The effects of dutasteride or tamsulosin alone and in combination on storage and voiding symptoms in men with lower urinary tract symptoms (LUTS) and benign prostatic hyperplasia (BPH): 4-year data from the Combination of Avodart and Tamsulosin (CombAT) s
    Francesco Montorsi
    Universita Vita Salute San Raffaele, Milan, Italy
    BJU Int 107:1426-31. 2011
    ....
  95. ncbi Male androgenetic alopecia
    Deepani Rathnayake
    Department of Dermatology, St Vincent s Hospital Melbourne, Fitzroy, Melbourne, Victoria 3065, Australia
    Expert Opin Pharmacother 11:1295-304. 2010
    ..Hair loss results in reduced self esteem, loss of confidence and anxiety in affected men. An effective treatment for hair baldness would be desirable...
  96. ncbi Dutasteride improves outcomes of benign prostatic hyperplasia when evaluated for prostate cancer risk reduction: secondary analysis of the REduction by DUtasteride of prostate Cancer Events (REDUCE) trial
    Claus G Roehrborn
    Department of Urology, University of Texas Southwestern Medical Center, Dallas, Texas 75390 9110, USA
    Urology 78:641-6. 2011
    ....
  97. ncbi Effects of the dual 5 alpha-reductase inhibitor dutasteride on apoptosis in primary cultures of prostate cancer epithelial cells and cell lines
    Ann Maria McCrohan
    University College Dublin School of Medicine and Medical Sciences, Mater Misericordiae University Hospital, Dublin, Ireland
    Cancer 106:2743-52. 2006
    ..The objective of the current study was to determine whether dutasteride would induce apoptosis in a range of prostate epithelial cell lines and primary cultures...
  98. ncbi Operating characteristics of a partial-block randomized crossover bioequivalence study for dutasteride, a drug with a long half-life: investigation through simulation and comparison with final results
    Gengqian Cai
    Department of Quantitative Sciences, GlaxoSmithKline, King of Prussia, PA 19406, USA
    J Clin Pharmacol 50:1142-50. 2010
    ..The results showed that this design demonstrated acceptable consumer and producer risk. Partial-block crossover designs should be considered for studies when the half-life of the drug is long and there are more than 2 periods...
  99. pmc A potential biochemical mechanism underlying the influence of sterol deprivation stress on Caenorhabditis elegans longevity
    Mi Cheong Cheong
    Department of Biochemistry, College of Life Science and Biotechnology, Yonsei University, Seoul 120 749, Korea
    J Biol Chem 286:7248-56. 2011
    ..Moreover, expression of the stress-response transcription factor SKN-1 was decreased in amphid neurons by Aza and that of DAF-28 was increased when DAF-6 was involved, contributing to lifespan reduction...
  100. ncbi Dutasteride in localised prostate cancer management: the REDEEM randomised, double-blind, placebo-controlled trial
    Neil E Fleshner
    Princess Margaret Hospital, University of Toronto, Toronto, Ontario, Canada
    Lancet 379:1103-11. 2012
    ..We aimed to investigate the safety and efficacy of dutasteride, a 5α-reductase inhibitor, on prostate cancer progression in men with low-risk disease who chose to be followed up with active surveillance...
  101. ncbi Dutasteride, who is it more effective for? Second to fourth digit ratio and the relationship with prostate volume reduction by dutasteride treatment
    Tae Beom Kim
    Department of Urology, Gachon University Gil Hospital, Incheon, Republic of Korea
    BJU Int 110:E857-63. 2012
    ..Patients with a higher digit ratio respond well to dutasteride treatment compared to those with a lower digit ratio. These results suggest that the digit ratio might be a predictor of the response to dutasteride treatment...

Research Grants18

  1. Minimally Invasive Surgical Therapies Treatment Consort*
    Claus Roehrborn; Fiscal Year: 2005
    ..The MIST Study Group will be a blueprint for a technology assessment group applicable to other areas of urology and other medical or surgical subspecialties. ..
  2. Oral Androgen Administration and Function in Man
    JOHN AMORY; Fiscal Year: 2008
    ..Matsumoto M.D., Director, Clinical Research Unit VA-Puget Sound and Professor of Medicine, University of Washington School of Medicine will co-mentor this award. [unreadable] [unreadable]..
  3. Role of 5-alpha Reductase in Testosterone Actions
    Shalendar Bhasin; Fiscal Year: 2007
    ..abstract_text> ..
  4. TESTOSTERONE REPLACEMENT & PHYSICAL FUNCTION IN HIV+MEN
    Shalender Bhasin; Fiscal Year: 2005
    ..This study should help identify a therapeutic intervention that might improve physical function in HIV-infected men with weight loss, and enhance our understanding of the mechanisms by which testosterone stimulates muscle accretion. ..
  5. Rhesus Embryonic Stem Cell-Derived Serotonin Neurons
    CYNTHIA BETHEA; Fiscal Year: 2007
    ..The knowledge obtained from this work will lead to novel treatments for psychoneuropathologies. [unreadable] [unreadable]..
  6. US Prostate Cancer Detection with Dutasteride Pretreatment
    Ethan Halpern; Fiscal Year: 2008
    ..unreadable] [unreadable] [unreadable]..
  7. Testosterone Modulation of Response to Phosphodiesterase Inhibitors
    Shalendar Bhasin; Fiscal Year: 2009
    ....
  8. Urodynamic and Multiethnic Variability of Men Treated b*
    Steven Kaplan; Fiscal Year: 2005
    ..Baseline urodynamic parameters which may predict improved outcome after MIST 3. The success of various types of MIST in treating BPH in African - American, Hispanic and Caucasian men. ..
  9. Mechanisms of Testosterone Effects on Body Composition
    Shalendar Bhasin; Fiscal Year: 2007
    ..abstract_text> ..
  10. Testosterone:Physical Function in Men on Hemodialysis
    Shalender Bhasin; Fiscal Year: 2004
    ..Therefore, if successful, this study should help identify a therapeutic intervention that might improve physical function and reduce disability in men with end stage renal disease. ..
  11. SARCOPENIA--TESTOSTERONE DOSE RESPONSE IN OLDER MEN
    Shalender Bhasin; Fiscal Year: 2002
    ....
  12. Population-Based Reference Ranges for Testosterone
    VASAN S RAMACHANDRAN; Fiscal Year: 2010
    ..These steps will facilitate the development of rational criteria for classifying men into androgen-deficient and androgen-replete categories. ..
  13. OVARIAN STEROID REGULATION OF SEROTONIN IN PRIMATES
    CYNTHIA LOUISE BETHEA; Fiscal Year: 2010
    ..Altogether, we will show that ovarian steroids support serotonin neuron survival and we will provide pivotal underlying genomic mechanisms. ..
  14. Interstitial Cystitis Clinical Research Network (ICCRN)
    J Nickel; Fiscal Year: 2007
    ..site with Dr. Nickel as PI has the experience, expertise and the proven ability to design, implement and enroll patients with IC in clinical strudies and will be a valuable partner in the proposed ICCRN and UCPPSCG. ..
  15. Chronic Prostatitis Collaborative Research Network CPCRN
    J Nickel; Fiscal Year: 2007
    ..Nickel as PI has the experience, expertise and the proven ability to design, implement and enroll patients with CPPS in clinical studies and will be a valuable partner in the proposed CPCRN and UCPPSCG. ..
  16. Primary Care Colorectal Ca Screening Surveillance System
    Richard Hoffman; Fiscal Year: 2005
    ..abstract_text> ..
  17. CHARACTERIZATION & TREATMENT OF CATEGORY III PROSTATITIS
    J Nickel; Fiscal Year: 2003
    ..Results from this 3 part study will be analyzed and correlated between groups and within groups, both concurrently and sequentially. ..
  18. Trainee-Focusted Training for Research Integrity
    Steven Jacobsen; Fiscal Year: 2003
    ..6. Identify high frequency perceptions or frames of reference, which are substantially at odds with accepted research norms and begin designing better interventions to alter them. ..