- Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes
Dallas Diabetes and Endocrine Center at Medical City, Dallas, Texas, USA
Diabetes Care 35:1232-8. 2012
..To evaluate the effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, in type 2 diabetes mellitus inadequately controlled with metformin monotherapy...
- Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise
Clinical Trial Center, Sahlgrenska University Hospital, Gothenburg, Sweden
Diabetes Obes Metab 15:372-82. 2013
..Canagliflozin is a sodium glucose co-transporter 2 inhibitor in development for type 2 diabetes mellitus (T2DM). The efficacy and safety of canagliflozin were evaluated in subjects with T2DM inadequately controlled with diet and exercise...
- Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin
Janssen Research and Development, LLC, Raritan, NJ 08869, USA
Diabetes Obes Metab 14:539-45. 2012
..Canagliflozin is a sodium-glucose co-transporter 2 (SGLT2) inhibitor that is being investigated for the treatment of type 2 diabetes mellitus (T2DM)...
- Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects
Johnson and Johnson Pharmaceutical Research and Development, LLC, Raritan, NJ 08869, USA
Diabetes Obes Metab 13:669-72. 2011
..Canagliflozin was generally well tolerated; most adverse events were mild and no hypoglycaemia was reported. These results support further study of canagliflozin...
- Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models
Johnson and Johnson Pharmaceutical Research and Development, LLC, Spring House, Pennsylvania, United States of America
PLoS ONE 7:e30555. 2012
..Canagliflozin is a sodium glucose co-transporter (SGLT) 2 inhibitor in clinical development for the treatment of type 2 diabetes mellitus (T2DM)...
- Rivaroxaban versus enoxaparin for thromboprophylaxis after hip arthroplasty
Bengt I Eriksson
Sahlgrenska University Hospital Ostra, Gothenburg, Sweden
N Engl J Med 358:2765-75. 2008
..This phase 3 trial compared the efficacy and safety of rivaroxaban, an oral direct inhibitor of factor Xa, with those of enoxaparin for extended thromboprophylaxis in patients undergoing total hip arthroplasty...
- Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty
Michael R Lassen
Nordsjaellands Hospital, Hørsholm, Denmark
N Engl J Med 358:2776-86. 2008
..We investigated the efficacy of rivaroxaban, an orally active direct factor Xa inhibitor, in preventing venous thrombosis after total knee arthroplasty...
- Rivaroxaban versus enoxaparin for thromboprophylaxis after total knee arthroplasty (RECORD4): a randomised trial
Alexander G G Turpie
McMaster University, Hamilton, Ontario L8L 2X2, Canada
Lancet 373:1673-80. 2009
..We aimed to test the efficacy and safety of oral rivaroxaban for the prevention of venous thromboembolism after total knee arthroplasty...
- Dual effect of strontium ranelate: stimulation of osteoblast differentiation and inhibition of osteoclast formation and resorption in vitro
Laboratoire de Génomique Fonctionelle de Lyon, Université de Lyon UMR5242, CNRS INRA ENS Université Lyon1 IFR 128 Biosciences Lyon Gerland, 46, Allee d Italie, 69007 Lyon, France
Bone 42:129-38. 2008
..It stimulates bone formation through its positive action on osteoblast differentiation and function, and decreases osteoclast differentiation as well as function by disrupting actin cytoskeleton organization...
- Prasugrel versus clopidogrel in patients with acute coronary syndromes
Stephen D Wiviott
Brigham and Women s Hospital and Harvard Medical School, Boston, MA 02115, USA
N Engl J Med 357:2001-15. 2007
..Dual-antiplatelet therapy with aspirin and a thienopyridine is a cornerstone of treatment to prevent thrombotic complications of acute coronary syndromes and percutaneous coronary intervention...
- Extended duration rivaroxaban versus short-term enoxaparin for the prevention of venous thromboembolism after total hip arthroplasty: a double-blind, randomised controlled trial
Ajay K Kakkar
Barts and the London School of Medicine and Dentistry, London, UK
Lancet 372:31-9. 2008
..Our aim was to compare the use of rivaroxaban for extended thromboprophylaxis with short-term thromboprophylaxis with enoxaparin...
- AZD7762, a novel checkpoint kinase inhibitor, drives checkpoint abrogation and potentiates DNA-targeted therapies
Sonya D Zabludoff
AstraZeneca R and D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA
Mol Cancer Ther 7:2955-66. 2008
- Safety, pharmacodynamics, and pharmacokinetics of single doses of BAY 59-7939, an oral, direct factor Xa inhibitor
Bayer HealthCare AG, Institute of Clinical Pharmocology, D 42096 Wuppertal, Germany
Clin Pharmacol Ther 78:412-21. 2005
..The aim of this study was to investigate the safety, pharmacodynamics, and pharmacokinetics of BAY 59--7939, an oral, direct factor Xa inhibitor...
- Safety, pharmacodynamics, and pharmacokinetics of BAY 59-7939--an oral, direct Factor Xa inhibitor--after multiple dosing in healthy male subjects
Institute of Clinical Pharmacology, Bayer HealthCare AG, 42096 Wuppertal, Germany
Eur J Clin Pharmacol 61:873-80. 2005
- Rotigotine effects on early morning motor function and sleep in Parkinson's disease: a double-blind, randomized, placebo-controlled study (RECOVER)
Department of Clinical Neurophysiology, University of Goettingen and Paracelsus Elena Klinik, Kassel, Germany
Mov Disord 26:90-9. 2011
..Twenty-four-hour transdermal delivery of rotigotine to PD patients with early-morning motor dysfunction resulted in significant benefits in control of both motor function and nocturnal sleep disturbances...
- Dose-escalation study of the pharmacokinetics and pharmacodynamics of rivaroxaban in healthy elderly subjects
Clinical Pharmacology, Bayer HealthCare AG, D 42096 Wuppertal, Germany
Curr Med Res Opin 24:2757-65. 2008
..The aim of this study was to investigate the pharmacokinetics and pharmacodynamics of rivaroxaban--a novel, oral, direct Factor Xa (FXa) inhibitor--in healthy elderly subjects...
- Assessment of laboratory assays to measure rivaroxaban--an oral, direct factor Xa inhibitor
Meyer Michel Samama
Hotel Dieu University Hospital, Paris, France 2Biomnis Laboratory, Ivry sur Seine, France
Thromb Haemost 103:815-25. 2010
..Finally, all clotting and chromogenic assays showed a concentration-dependent effect induced by rivaroxaban...
- Discovery of canagliflozin, a novel C-glucoside with thiophene ring, as sodium-dependent glucose cotransporter 2 inhibitor for the treatment of type 2 diabetes mellitus
Medicinal Chemistry Research Laboratories, Mitsubishi Tanabe Pharma Corporation, 2 2 50 Kawagishi, Toda, Saitama, Japan
J Med Chem 53:6355-60. 2010
..A novel thiophene derivative 4b-3 (canagliflozin) was a highly potent and selective SGLT2 inhibitor and showed pronounced anti-hyperglycemic effects in high-fat diet fed KK (HF-KK) mice...
- P2Y(12) inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use
Uppsala Clinical Research Centre, University Hospital, Uppsala SE 75185, Sweden
Eur Heart J 30:1964-77. 2009
..The objectives of this systematic review are to summarize the pharmacokinetics, pharmacodynamics, and pharmacogenetics of the different P2Y(12) inhibitors and to discuss the clinical implications for treatment of patients...
- Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and
Patricia L Podolin
Respiratory and Inflammation Center of Excellence for Drug Discovery, GlaxoSmithKline, King of Prussia, PA 19406, USA
J Pharmacol Exp Ther 312:373-81. 2005
..5 mg/kg, i.p., every other day. These results suggest that reduction of proinflammatory mediators and inhibition of antigen-induced T cell proliferation are mechanisms underlying the attenuation of CIA by the IKK-2 inhibitor, TPCA-1...
- Population pharmacokinetics and pharmacodynamics of rivaroxaban--an oral, direct factor Xa inhibitor--in patients undergoing major orthopaedic surgery
Clinical Pharmacology, Bayer HealthCare AG, Aprather Weg 18a, Wuppertal, Germany
Clin Pharmacokinet 47:203-16. 2008
- Identification and characterization of a selective peroxisome proliferator-activated receptor beta/delta (NR1C2) antagonist
Barry G Shearer
Research and Development, GlaxoSmithKline, Research Triangle Park, NC 27709, USA
Mol Endocrinol 22:523-9. 2008
..Here we describe the first report of a PPARbeta/delta small molecule antagonist ligand. This antagonist ligand will be a useful tool for elucidating the biological roles of PPARbeta/delta...
- The clinical efficacy of a topical dorzolamide in the management of cystoid macular edema in patients with retinitis pigmentosa
Department of Ophthalmology, Graduate School of Medical Sciences, Kyushu University, 3 1 1 Maidashi, Higashi ku, Fukuoka 812 8582, Japan
Graefes Arch Clin Exp Ophthalmol 250:809-14. 2012
..The objective of this work was to evaluate the clinical efficacy of a topical dorzolamide (a carbonic anhydrase inhibitor) in CME associated with RP...
- Strontium ranelate inhibits key factors affecting bone remodeling in human osteoarthritic subchondral bone osteoblasts
Steeve Kwan Tat
Osteoarthritis Research Unit, University of Montreal Hospital Research Centre, Montreal, Quebec, Canada
Bone 49:559-67. 2011
..In this study, we investigated in human OA subchondral bone osteoblasts the modulatory effect of strontium ranelate on the above key factors...
- Effects of the oral, direct factor xa inhibitor rivaroxaban on platelet-induced thrombin generation and prothrombinase activity
Pharmazentrum frankfurt ZAFES, Institute of Clinical Pharmacology, University Hospital, Frankfurt Main, Theodor Stern Kai 7, D 60590 Frankfurt am Main, Germany
J Clin Pharmacol 47:1398-407. 2007
..Rivaroxaban strongly inhibits platelet-induced thrombin generation, after activation of either platelets or the coagulation pathway, even in the presence of minimal factor Xa inhibition in plasma...
- Rate of nuisance bleedings and impact on compliance to prasugrel in acute coronary syndromes
Departement de Cardiologie, Hopital Universitaire Nord, Faculte de Medecine, Universite de la Mediterranee, Marseille, France
Am J Cardiol 108:1710-3. 2011
..In conclusion, in the present study, minor bleedings were common during the first month after percutaneous coronary intervention and were significantly associated with prasugrel withdrawal...
- Rotigotine transdermal patch in early Parkinson's disease: a randomized, double-blind, controlled study versus placebo and ropinirole
Movement Disorders Unit, Department of Neurology, Tel Aviv Sourasky Medical Center, Sackler School of Medicine, Tel Aviv University, Tel Aviv, Israel
Mov Disord 22:2398-404. 2007
..Application-site reactions were predominantly mild or moderate in intensity. In conclusion, the rotigotine transdermal patch represents an effective and safe option for the treatment of patients with early Parkinson's disease...
- Rebalancing bone turnover in favour of formation with strontium ranelate: implications for bone strength
J E Fonseca
Rheumatology Research Unit, Instituto de Medicina Molecular, Edificio Egas Moniz, Faculdade de Medicina da Universidade de Lisboa, Av Professor Egas Moniz, 1649 028 Lisboa, Portugal
Rheumatology (Oxford) 47:iv17-19. 2008
..The overall effect is a rebalanced bone turnover in favour of improved bone geometry, cortical thickness, trabecular bone morphology and intrinsic bone tissue quality, which translates into enhanced bone strength...
- Efficacy of pramipexole and transdermal rotigotine in advanced Parkinson's disease: a double-blind, double-dummy, randomised controlled trial
Werner H Poewe
Department of Neurology, Innsbruck Medical University, Innsbruck, Austria
Lancet Neurol 6:513-20. 2007
- Prasugrel overcomes high on-clopidogrel platelet reactivity post-stenting more effectively than high-dose (150-mg) clopidogrel: the importance of CYP2C19*2 genotyping
Department of Cardiology, Patras University Hospital, Patras, Greece
JACC Cardiovasc Interv 4:403-10. 2011
- High-affinity peroxisome proliferator-activated receptor β/δ-specific ligands with pure antagonistic or inverse agonistic properties
Institute of Molecular Biology and Tumor Research IMT, Philipps University, Marburg, Germany
Mol Pharmacol 80:828-38. 2011
..The possibility to differentially modulate specific functions of PPARβ/δ makes these novel compounds invaluable tools to advance our understanding of PPARβ/δ biology...
- Evaluation of vulvovaginal symptoms and Candida colonization in women with type 2 diabetes mellitus treated with canagliflozin, a sodium glucose co-transporter 2 inhibitor
Department of Obstetrics and Gynecology, Drexel University College of Medicine, Philadelphia, PA 19102, USA
Curr Med Res Opin 28:1173-8. 2012
..Vaginal Candida colonization and symptomatic vulvovaginal adverse events (VVAE) were assessed in females with T2DM treated with canagliflozin, a SGLT2 inhibitor...
- Effect of canagliflozin, a sodium glucose co-transporter 2 (SGLT2) inhibitor, on bacteriuria and urinary tract infection in subjects with type 2 diabetes enrolled in a 12-week, phase 2 study
Lindsay E Nicolle
University of Manitoba, Winnipeg, Canada
Curr Med Res Opin 28:1167-71. 2012
..To examine the effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor that lowers blood glucose by increasing urinary glucose excretion (UGE), on asymptomatic bacteriuria and urinary tract infections (UTIs)...
- Small organic probes as amyloid specific ligands--past and recent molecular scaffolds
K Peter R Nilsson
Department of Chemistry, IFM, Linkoping University, Linkoping, Sweden
FEBS Lett 583:2593-9. 2009
..In this review, past and recent molecular scaffolds that have been utilized for the development of small organic amyloid imaging agents are discussed...
- Identification of SR8278, a synthetic antagonist of the nuclear heme receptor REV-ERB
ACS Chem Biol 6:131-4. 2011
..Thus, SR8278 represents a unique chemical tool for probing REV-ERB function and may serve as a point for initiation of further optimization to develop REV-ERB antagonists with the ability to explore circadian and metabolic functions...
- Morbidity and Mortality After Stroke, Eprosartan Compared with Nitrendipine for Secondary Prevention: principal results of a prospective randomized controlled study (MOSES)
Department of Internal Medicine, St Josefs Hospital, Cloppenburg, Germany
Stroke 36:1218-26. 2005
..In hypertensive stroke patients, for the same level of blood pressure control, eprosartan will be more effective than nitrendipine in reducing cerebrovascular and cardiovascular morbidity and mortality...
- Strontium ranelate promotes osteoblastic cell replication through at least two different mechanisms
Service of Bone Diseases, Department of Rehabilitation and Geriatrics, University Hospital of Geneva, CH 1211 Geneva 14, Switzerland
Bone 42:1131-6. 2008
- Strontium ranelate does not stimulate bone formation in ovariectomized rats
R K Fuchs
Department of Anatomy and Cell Biology, Indiana University School of Medicine, Indianapolis, IN, USA
Osteoporos Int 19:1331-41. 2008
..We evaluated the effects of SrR on the skeleton in ovariectomized (OVX) rats and evaluated the influence of dietary calcium...
- Identification and characterization of a small molecule AMPK activator that treats key components of type 2 diabetes and the metabolic syndrome
Department of Metabolic Disease Research, Abbott Laboratories, 100 Abbott Park Road, Abbott Park, Illinois 60064, USA
Cell Metab 3:403-16. 2006
..These results demonstrate that small molecule-mediated activation of AMPK in vivo is feasible and represents a promising approach for the treatment of type 2 diabetes and the metabolic syndrome...
- Duloxetine: clinical pharmacokinetics and drug interactions
Mary Pat Knadler
Eli Lilly and Company, Indianapolis, Indiana 46285, USA
Clin Pharmacokinet 50:281-94. 2011
..While duloxetine is generally well tolerated, it is important to be knowledgeable about the potential for pharmacokinetic interactions between duloxetine and drugs that inhibit CYP1A2 or drugs that are metabolized by CYP2D6 enzymes...
- Strontium ranelate: a review of its use in the treatment of postmenopausal osteoporosis
Emma D Deeks
Adis, Auckland, New Zealand
Drugs 70:733-59. 2010
..Overall, the clinical data available suggest that strontium ranelate is an effective and generally well tolerated option for the first-line treatment of postmenopausal osteoporosis...
- Synthesis and antitumor properties of 2,5-bis(3'-indolyl)thiophenes: analogues of marine alkaloid nortopsentin
Dipartimento Farmacochimico Tossicologico e Biologico, Universita degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Italy
Bioorg Med Chem Lett 17:2342-6. 2007
- Dabigatran and rivaroxaban for prevention of venous thromboembolism--systematic review and adjusted indirect comparison
Y K Loke
School of Medicine, Health Policy and Practice, University of East Anglia, Norwich, UK
J Clin Pharm Ther 36:111-24. 2011
..Dabigatran and rivaroxaban are new oral anticoagulants for thromboprophylaxis after elective orthopaedic surgery. We aimed to systematically compare their relative benefits and harms through meta-analysis, and adjusted indirect comparison...
- Bone material quality in transiliac bone biopsies of postmenopausal osteoporotic women after 3 years of strontium ranelate treatment
Ludwig Boltzmann Institute of Osteology at the Hanusch Hospital of WGKK and AUVA Trauma Centre Meidling, 4th Medical Department, Hanusch Hospital, 1140 Vienna, Austria
J Bone Miner Res 25:891-900. 2010
..Taken together, these data provide evidence that the investigated bone quality determinants at tissue level were preserved in postmenopausal osteoporotic women after 3-year treatment with 2 g SrR per day plus calcium and vitamin D...
- Potent induction of total cellular GSH and NQO1 as well as mitochondrial GSH by 3H-1,2-dithiole-3-thione in SH-SY5Y neuroblastoma cells and primary human neurons: protection against neurocytotoxicity elicited by dopamine, 6-hydroxydopamine, 4-hydroxy-2-no
Division of Biomedical Sciences, Edward Via Virginia College of Osteopathic Medicine, Virginia Tech Corporate Research Center, 2265 Kraft Drive, Blacksburg, VA 24060, USA
Brain Res 1197:159-69. 2008
- Cost-effectiveness of rivaroxaban compared to warfarin for stroke prevention in atrial fibrillation
University of Connecticut School of Pharmacy, Storrs, CT, USA
Am J Cardiol 110:845-51. 2012
..In conclusion, this Markov model suggests that rivaroxaban therapy may be a cost-effective alternative to adjusted-dose warfarin for stroke prevention in AF...
- Rivaroxaban compared with warfarin in patients with atrial fibrillation and previous stroke or transient ischaemic attack: a subgroup analysis of ROCKET AF
Graeme J Hankey
Stroke Unit, Department of Neurology, Royal Perth Hospital, Perth, Australia
Lancet Neurol 11:315-22. 2012
..We aimed to investigate whether the efficacy and safety of rivaroxaban compared with warfarin is consistent among the subgroups of patients with and without previous stroke or transient ischaemic attack (TIA)...
- Advanced Parkinson disease treated with rotigotine transdermal system: PREFER Study
Peter A LeWitt
Clinical Neuroscience Center, Southfield, MI 48034, USA
Neurology 68:1262-7. 2007
..In patients experiencing motor fluctuations, a major treatment challenge is the reduction of "off" time, particularly upon awakening. Rotigotine (Neupro) is a novel dopaminergic agonist with 24-hour transdermal delivery...
- Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer
Department of Pharmacology, Dartmouth Medical School, Hanover, New Hampshire 03755, USA
Cancer Res 61:8412-5. 2001
..Arzoxifene is devoid of the uterotrophic effects of tamoxifen, suggesting that, in contrast to tamoxifen, it is unlikely that the clinical use of arzoxifene will increase the risk of developing endometrial carcinoma...
- Evaluation of prasugrel compared with clopidogrel in patients with acute coronary syndromes: design and rationale for the TRial to assess Improvement in Therapeutic Outcomes by optimizing platelet InhibitioN with prasugrel Thrombolysis In Myocardial Infar
Stephen D Wiviott
TIMI Study Group, Cardiovascular Division, Department of Medicine, Brigham and Women s Hospital, Boston, MA 02115, USA
Am Heart J 152:627-35. 2006
..TRITON-TIMI 38 is designed to compare prasugrel with clopidogrel in moderate to high-risk patients with acute coronary syndrome (ACS)...
- Strontium ranelate treatment improves trabecular and cortical intrinsic bone tissue quality, a determinant of bone strength
Division of Bone Diseases, WHO Collaborting Centre for Osteoporosis Prevention, Department of Rehabilitation and Geriatrics, University Hospitals, Geneva, Switzerland
J Bone Miner Res 22:1419-25. 2007
- The effects of strontium ranelate on the risk of vertebral fracture in women with postmenopausal osteoporosis
Pierre J Meunier
Department of Rheumatology and Bone Diseases, Edouard Herriot Hospital, Lyons, France
N Engl J Med 350:459-68. 2004
- Study design and rationale of a comparison of prasugrel and clopidogrel in medically managed patients with unstable angina/non-ST-segment elevation myocardial infarction: the TaRgeted platelet Inhibition to cLarify the Optimal strateGy to medicallY manage
Chee Tang Chin
Duke Clinical Research Institute, Durham, NC, USA
Am Heart J 160:16-22.e1. 2010
- Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships
Department of Medicinal Chemistry, BMC, Uppsala University, P O Box 574, SE 751 23 Uppsala, Sweden
J Med Chem 49:7160-8. 2006
..The butyloxyphenyl (56) and the propylthienyl (50) derivatives were found to exert a high agonistic effect as deduced from their capacity to induce neurite elongation in neuronal cells, as does angiotensin II...
- Novel pentameric thiophene derivatives for in vitro and in vivo optical imaging of a plethora of protein aggregates in cerebral amyloidoses
Department of Chemistry, IFM, Linkoping University, Sweden
ACS Chem Biol 4:673-84. 2009
- Clinical laboratory measurement of direct factor Xa inhibitors: anti-Xa assay is preferable to prothrombin time assay
Yu Chen Barrett
Bristol Myers Squibb, Princeton, New Jersey, USA
Thromb Haemost 104:1263-71. 2010
..88-0.89) compared with PT/INR (r2 = 0.36) in patients undergoing VTE treatment suggested that anti-Xa activity was the better indicator of apixaban plasma concentrations...
- In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939--an oral, direct Factor Xa inhibitor
Cardiovascular Research, Bayer HealthCare AG, Wuppertal, Germany
J Thromb Haemost 3:514-21. 2005
..Bleeding times in rats and rabbits were not significantly affected at antithrombotic doses (3 mg kg(-1) p.o., AV shunt). Based on these results, BAY 59-7939 was selected for clinical development...
- Population pharmacokinetics and pharmacodynamics of once- and twice-daily rivaroxaban for the prevention of venous thromboembolism in patients undergoing total hip replacement
Bayer HealthCare AG, Aprather Weg 18a, Wuppertal, Germany
Thromb Haemost 100:453-61. 2008
- Body weight has limited influence on the safety, tolerability, pharmacokinetics, or pharmacodynamics of rivaroxaban (BAY 59-7939) in healthy subjects
Clinical Pharmacology, Bayer HealthCare AG, Building 429, Aprather Weg 18a, Wuppertal, D 42096, Germany
J Clin Pharmacol 47:218-26. 2007
..The area under the curve was unaffected by body weight or gender. No other clinically relevant differences were observed, suggesting that rivaroxaban is unlikely to require dose adjustment for body weight or gender...
- Effect of the dual peroxisome proliferator-activated receptor-alpha/gamma agonist aleglitazar on risk of cardiovascular disease in patients with type 2 diabetes (SYNCHRONY): a phase II, randomised, dose-ranging study
Robert R Henry
Department of Medicine, University of California at San Diego and VA San Diego Healthcare System, San Diego, CA 92161, USA
Lancet 374:126-35. 2009
..The SYNCHRONY study aimed to establish the glucose-lowering and lipid-modifying effects, and safety profile, of the dual PPAR-alpha and PPAR-gamma agonist aleglitazar...
- Population model of the pharmacokinetics and pharmacodynamics of rivaroxaban--an oral, direct factor xa inhibitor--in healthy subjects
Clinical Pharmacology, Pharmacometry, Bayer HealthCare AG, Wuppertal, Germany
Int J Clin Pharmacol Ther 45:335-44. 2007
..This analysis aimed to define population models for the pharmacokinetics (PK) and pharmacodynamics (PD) ofrivaroxaban in healthy males...
- Meta-analysis of duloxetine vs. pregabalin and gabapentin in the treatment of diabetic peripheral neuropathic pain
Health Economics and Outcomes Research, Uxbridge, UK
BMC Neurol 9:6. 2009
..We conducted an indirect meta-analysis to compare the efficacy and tolerability of DLX with PGB and GBP in DPNP, using placebo as a common comparator...
- Effect of food, an antacid, and the H2 antagonist ranitidine on the absorption of BAY 59-7939 (rivaroxaban), an oral, direct factor Xa inhibitor, in healthy subjects
Institute of Clinical Pharmacology, Bayer HealthCare AG, Wuppertal, Germany
J Clin Pharmacol 46:549-58. 2006
..Time to maximum PT prolongation was delayed by 0.5 to 1.5 hours after food, with no relevant influence of food type. No significant difference in C(max) and AUC was observed with coadministration of BAY 59-7939 and ranitidine or antacid...
- Common polymorphisms of CYP2C19 and CYP2C9 affect the pharmacokinetic and pharmacodynamic response to clopidogrel but not prasugrel
J T Brandt
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
J Thromb Haemost 5:2429-36. 2007
..The pharmacodynamic response to clopidogrel is more variable than the response to prasugrel, but the reasons for variation in response to clopidogrel are not well characterized...
- Oral, direct Factor Xa inhibition with BAY 59-7939 for the prevention of venous thromboembolism after total hip replacement
B I Eriksson
Sahlgrenska University HospitalOstra, Gothenburg, Sweden
J Thromb Haemost 4:121-8. 2006
..Joint replacement surgery is an appropriate model for dose-ranging studies investigating new anticoagulants...
- Effects of long-term strontium ranelate treatment on the risk of nonvertebral and vertebral fractures in postmenopausal osteoporosis: Results of a five-year, randomized, placebo-controlled trial
Jean Yves Reginster
University of Liege, Liege, Belgium
Arthritis Rheum 58:1687-95. 2008
..This study was undertaken to assess the effect of strontium ranelate on nonvertebral and vertebral fractures in postmenopausal women with osteoporosis in a 5-year, double-blind, placebo-controlled trial...
- Interaction of the active metabolite of prasugrel, R-138727, with cysteine 97 and cysteine 175 of the human P2Y12 receptor
Department of Pharmacology and Toxicology, University of Bonn, Bonn, Germany
J Thromb Haemost 6:1908-14. 2008
..The P2Y(12) receptor plays a crucial role in platelet aggregation and is the target of platelet aggregation inhibitors, including the thienopyridine compound prasugrel...
- A pharmacodynamic comparison of prasugrel vs. high-dose clopidogrel in patients with type 2 diabetes mellitus and coronary artery disease: results of the Optimizing anti-Platelet Therapy In diabetes MellitUS (OPTIMUS)-3 Trial
Dominick J Angiolillo
University of Florida College of Medicine Jacksonville, 655 W Eighth Street, Jacksonville, FL 32209, USA
Eur Heart J 32:838-46. 2011
..The aim of this study was to perform serial pharmacodynamic assessments of prasugrel with high-dose clopidogrel in patients with DM...
- Cost-utility of long-term strontium ranelate treatment for postmenopausal osteoporotic women
Department of Public Health, Epidemiology and Health Economics, University of Liege, Liege, Belgium
Osteoporos Int 21:157-65. 2010
..The results of this study suggested that long-term treatment with strontium ranelate over 5 years is cost-effective compared to no treatment for postmenopausal osteoporotic women...
- Strontium ranelate reduces the risk of nonvertebral fractures in postmenopausal women with osteoporosis: Treatment of Peripheral Osteoporosis (TROPOS) study
J Y Reginster
Department of Epidemiology, Public Health and Health Economics, University of Liege, CHU Centre Ville, 45 Quai Godefroid Kurth, 4020 Liege, Belgium
J Clin Endocrinol Metab 90:2816-22. 2005
- Solution-processed metallic conducting polymer films as transparent electrode of optoelectronic devices
Department of Materials and Engineering, National University of Singapore, Singapore
Adv Mater 24:2436-40. 2012
..These PEDOT:PSS films with conductivity and transparency comparable to ITO can replace ITO as the transparent electrode of optoelectronic devices...
- Inhibitors of the cellular trafficking of ricin
Laboratory of Molecular Toxinology and Biotechnology, Molecular engineering of proteins SIMOPRO, Life Sciences Division DSV, Institute of Biology and Technology Saclay, French Alternative Energies and Atomic Energy Commission CEA, F 91191 Gif sur Yvette, France
Toxins (Basel) 4:15-27. 2012
- Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase
Mark D Rackham
Department of Chemistry, Imperial College London, South Kensington Campus, London, SW7 2AZ, U K
J Med Chem 56:371-5. 2013
..The binding mode of this series was determined by crystallography and shows a novel binding mode for the benzothiophene ring...
- Duloxetine added to oral nonsteroidal anti-inflammatory drugs for treatment of knee pain due to osteoarthritis: results of a randomized, double-blind, placebo-controlled trial
ELIJAH P FRAKES
Eli Lilly and Company, Indianapolis, IN, USA
Curr Med Res Opin 27:2361-72. 2011
..To determine the efficacy, tolerability, and safety of duloxetine when added to oral nonsteroidal anti-inflammatory drugs (NSAIDs) in patients with osteoarthritis (OA) of the knee with pain of moderate or greater severity...
- Prasugrel overcomes high on-clopidogrel platelet reactivity in chronic coronary artery disease patients more effectively than high dose (150 mg) clopidogrel
Department of Cardiology, Patras University Hospital Rio, Greece
Am Heart J 162:733-9. 2011
..Strategies to optimize platelet inhibition in such patients are not clear...
- Chemical structure of Retro-2, a compound that protects cells against ribosome-inactivating proteins
Jewn Giew Park
Computer Aided Molecular Design Laboratory, Mayo Clinic, Rochester, MN 55905, USA
Sci Rep 2:631. 2012
..This calls for attention to (±)-2-(5-methylthiophen-2-yl)-3-phenyl-2,3-dihydroquinazolin-4(1H)-one as a promising RIP inhibitor and for chemical characterization of drug leads obtained from high-throughput screens...
- Treatment of patients with early and advanced Parkinson's disease with rotigotine transdermal system: age-relationship to safety and tolerability
Department of Neurology, Philipps Universitat, Baldingerstrasse, D 35043 Marburg, Germany
Parkinsonism Relat Disord 19:37-42. 2013
..Data from more representative PD populations are required to fully assess potential risks of DA therapy in elderly patients...
- High compliance with rotigotine transdermal patch in the treatment of idiopathic Parkinson's disease
Institute of Clinical Neuroscience and Medical Psychology, Heinrich Heine University, Universitatsstr 1, Dusseldorf, Germany
Parkinsonism Relat Disord 16:513-6. 2010
..This open, prospective, non-interventional study investigated compliance with the patch under clinical practice conditions...
- A spinal mechanism of action for duloxetine in a rat model of painful diabetic neuropathy
Department of Pathology, University of California, San Diego, La Jolla, CA 92093 0612, USA
Br J Pharmacol 164:159-69. 2011
..This study was designed to clarify mechanisms responsible for the anti-allodynic effects of duloxetine in diabetes...
- Rivaroxaban vs dabigatran for thromboprophylaxis after joint-replacement surgery: exploratory indirect comparison based on meta-analysis of pivotal clinical trials
Department of Pharmacology, Zagreb University School of Medicine, Salata 11, 10000 Zagreb, Croatia
Croat Med J 51:113-23. 2010
..To indirectly compare rivaroxaban and dabigatran for prevention of venous thromboembolism (VTE) after total hip or knee arthroplasty (THA, TKA) based on their pivotal efficacy/safety trials embracing a total of 20618 patients...
- Pharmacokinetics and pharmacodynamics of prasugrel, a thienopyridine P2Y12 inhibitor
Paul P Dobesh
College of Pharmacy, University of Nebraska Medical Center, Omaha, Nebraska 68198 6045, USA
Pharmacotherapy 29:1089-102. 2009
..Thus, prasugrel has a pharmacokinetic and pharmacodynamic profile that compares favorably with those of existing antiplatelet agents...
- Prasugrel pharmacokinetics and pharmacodynamics in subjects with moderate renal impairment and end-stage renal disease
D S Small
Eli Lilly and Company, Indianapolis, IN, USA
J Clin Pharm Ther 34:585-94. 2009
..The pharmacokinetic (PK) and pharmacodynamic (PD) responses to prasugrel were compared in three studies of healthy subjects vs. those with moderate or end-stage renal impairment...
- Ritonavir inhibits the two main prasugrel bioactivation pathways in vitro: a potential drug-drug interaction in HIV patients
Division of Clinical Pharmacology and Toxicology, Geneva University Hospitals, Geneva, Switzerland
Metabolism 60:1584-9. 2011
..This finding suggests a potential significant drug-drug interaction between these two drugs...
- The pharmacokinetics and pharmacodynamics of prasugrel in healthy Chinese, Japanese, and Korean subjects compared with healthy Caucasian subjects
David S Small
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Eur J Clin Pharmacol 66:127-35. 2010
..We compared prasugrel pharmacokinetics, pharmacodynamics, and tolerability in healthy Chinese, Japanese, Korean and Caucasian subjects...
- Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency
David R Anderson
Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA
Bioorg Med Chem Lett 19:4878-81. 2009
..Crystallographic data provide a rationale for the observed MK2 potency as well as selectivity over CDK2 for this class of inhibitors...
- Rotigotine transdermal patch for the treatment of Parkinson's disease and restless legs syndrome
Schwarz BioSciences GmbH, UCB Pharma Group, Monheim, Germany
Drugs Today (Barc) 46:483-505. 2010
..Overall, rotigotine transdermal patch has demonstrated favorable clinical efficacy and tolerability in the treatment of PD and RLS...
- Dose-dependent inhibition of human platelet aggregation by prasugrel and its interaction with aspirin in healthy subjects
Joseph A Jakubowski
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
J Cardiovasc Pharmacol 49:167-73. 2007
..Within the limitations of the study, prasugrel was found to be well tolerated when dosed as LD followed by MD in the presence of ASA and provided greater platelet inhibition than ASA alone...
- Sensitivity of cancer cells to Plk1 inhibitor GSK461364A is associated with loss of p53 function and chromosome instability
Cancer Research, GlaxoSmithKline, Collegeville, Pennsylvania 19426, USA
Mol Cancer Ther 9:2079-89. 2010
- Synthesis of a library of oligothiophenes and their utilization as fluorescent ligands for spectral assignment of protein aggregates
Department of Chemistry, Linkoping University, SE 581 83 Linkoping, Sweden
Org Biomol Chem 9:8356-70. 2011
..Such LCOs will be highly useful for studying the underlying molecular events of protein aggregation diseases and could also be utilized for the development of novel diagnostic tools for these diseases...
- Competitive enzymatic interactions determine the relative amounts of prostaglandins E2 and D2
Department of Medicinal Chemistry and Pharmacognosy, University of Illinois College of Pharmacy, 833 S Wood Street, Chicago, IL 60612 7231, USA
J Pharmacol Exp Ther 339:716-25. 2011
- Benzothiophene inhibitors of MK2. Part 2: improvements in kinase selectivity and cell potency
David R Anderson
Pfizer Global Research and Development, St Louis Laboratories, Chesterfield, MO 63017, USA
Bioorg Med Chem Lett 19:4882-4. 2009
..The selectivity of the inhibitors can be rationalized by examination of X-ray crystal structures of inhibitors bound to MK2...
- A novel approach to control hyperglycemia in type 2 diabetes: sodium glucose co-transport (SGLT) inhibitors: systematic review and meta-analysis of randomized trials
Gradenigo Hospital, Turin, Italy
Ann Med 44:375-93. 2012
..Current treatment of hyperglycemia in type 2 diabetes (T2DM) is often ineffective and has unwanted effects. Therefore, novel antidiabetic drugs are under development...
- Return to theatre following total hip and knee replacement, before and after the introduction of rivaroxaban: a retrospective cohort study
C D Jensen
Wansbeck General Hospital, Woodhorn Lane, Ashington, Northumberland NE63 9JJ, UK
J Bone Joint Surg Br 93:91-5. 2011
- Cost-effectiveness of prasugrel versus clopidogrel in patients with acute coronary syndromes and planned percutaneous coronary intervention: results from the trial to assess improvement in therapeutic outcomes by optimizing platelet inhibition with Prasug
Elizabeth M Mahoney
Saint Luke s Mid America Heart Institute, 4401 Wornall Rd, Kansas City, MO 64111, USA
Circulation 121:71-9. 2010
..We evaluated the cost-effectiveness of prasugrel versus clopidogrel from the perspective of the US healthcare system by using data from TRITON-TIMI 38...
- How strontium ranelate, via opposite effects on bone resorption and formation, prevents osteoporosis
P J Marie
Laboratory of Osteoblast Biology and Pathology, INSERM, U606, Paris 75475, France
Osteoporos Int 22:1659-67. 2011
- Intraocular pressure lowering, change of antiapoptotic molecule expression, and neuroretinal changes by dorzolamide 2%/timolol 0.5% combination in a chronic ocular hypertension rat model
Hae Y Park
Department of Ophthalmology and Visual Science, College of Medicine, St Mary s Hospital, The Catholic University of Korea, Seoul, Korea
J Ocul Pharmacol Ther 24:563-71. 2008
..5% may have neuroprotective potential in the animal model, which is not mediated by Bcl-2 or Bcl-xL. The mechanism of neuroprotection by dorzolamide 2%/timolol 0.5% in chronic glaucoma models requires further investigation...
- Is there adequate provision of venous thromboembolism prophylaxis following hip arthroplasty? An audit and international survey
B A Rogers
Adult Lower Extremity Reconstruction, Mount Sinai Hospital, Toronto, Canada
Ann R Coll Surg Engl 92:668-72. 2010
- Prasugrel compared with high-dose clopidogrel in acute coronary syndrome. The randomised, double-blind ACAPULCO study
Institut de Cardiologie AP HP, INSERM U856 and Universite Paris 6, Hopital Pitie Salpetriere, Paris, France
Thromb Haemost 103:213-23. 2010
..Thus, in ACS patients a prasugrel 10-mg MD regimen resulted in significantly greater platelet inhibition than clopidogrel at twice its approved MD or a 900-mg LD...
- Strontium ranelate effect in postmenopausal women with different clinical levels of osteoarthritis
Center for Clinical and Basic Research, Vejle, Denmark
Climacteric 14:236-43. 2011
..Women were stratified according to reported symptoms of osteoarthritis and to the baseline levels of a cartilage degradation marker...
- Incidence of venous thromboembolism in users of strontium ranelate: an analysis of data from a prescription-event monitoring study in England
Drug Safety Research Unit, Bursledon Hall, Southampton, UK
Drug Saf 33:579-91. 2010
..Strontium ranelate is indicated for the treatment of postmenopausal osteoporosis. An association between strontium ranelate and venous thromboembolism (VTE) was identified in an analysis of phase III clinical trials...
- Population pharmacokinetic analyses to evaluate the influence of intrinsic and extrinsic factors on exposure of prasugrel active metabolite in TRITON-TIMI 38
Rebecca E Wrishko
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
J Clin Pharmacol 49:984-98. 2009
..1%) was 30% (90% confidence interval [CI] 1.16-1.45) higher than exposure in patients > or =60 kg. Mean Pras-AM exposures for patients > or =75 years (10.5%) were 19% (90% CI: 1.11-1.28) higher compared with patients <75 years...