Research Topics
Genomes and GenesSpecies | Nagy A FaridSummaryAffiliation: Eli Lilly and Company Country: USA Publications
| Collaborators
|
Detail Information
Publications
Interactions of two major metabolites of prasugrel, a thienopyridine antiplatelet agent, with the cytochromes P450Jessica L Fayer Rehmel
Department of Drug Disposition, Eli Lilly and Company, Lilly Corporate Center DC0714, Indianapolis, IN 46285, USA
Drug Metab Dispos 34:600-7. 2006..These K(i) values exceed circulating concentrations in humans by 3.8- to 43-fold. Therefore, neither R-95913 nor R-138727 is expected to substantially inhibit the P450-mediated metabolism of coadministered drugs...- Determination of the active and inactive metabolites of prasugrel in human plasma by liquid chromatography/tandem mass spectrometryNagy A Farid
Lilly Research Laboratories, Lilly Corporate Center, DC 0714, Eli Lilly and Company, Indianapolis, IN 46285, USA
Rapid Commun Mass Spectrom 21:169-79. 2007..These methods have been applied to determine the concentrations of the active and inactive metabolites of prasugrel in human plasma... - The disposition of prasugrel, a novel thienopyridine, in humansNagy A Farid
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Drug Metab Dispos 35:1096-104. 2007..Total radioactivity was higher in plasma than in blood, suggesting limited penetration of prasugrel metabolites into red blood cells. Approximately 70% of the dose was excreted in the urine and 25% in the feces... - Prasugrel, a new thienopyridine antiplatelet drug, weakly inhibits cytochrome P450 2B6 in humansNagy A Farid
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
J Clin Pharmacol 48:53-9. 2008..These results are consistent with patients receiving prasugrel not requiring dose adjustments when treated with drugs primarily metabolized by CYP2B6... 
Effect of atorvastatin on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrel in healthy subjectsNagy A Farid
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
Pharmacotherapy 28:1483-94. 2008..To investigate the potential effect of atorvastatin 80 mg/day on the pharmacokinetics and pharmacodynamics of the thienopyridines prasugrel and clopidogrel...- Cytochrome P450 3A inhibition by ketoconazole affects prasugrel and clopidogrel pharmacokinetics and pharmacodynamics differentlyN A Farid
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
Clin Pharmacol Ther 81:735-41. 2007..We conclude that CYP3A4 and CYP3A5 inhibition by ketoconazole affects formation of clopidogrel's but not prasugrel's active metabolite. The decreased formation of clopidogrel's active metabolite is associated with reduced IPA... - The pharmacokinetics and pharmacodynamics of prasugrel in healthy Chinese, Japanese, and Korean subjects compared with healthy Caucasian subjectsDavid 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... - The use of the VerifyNow P2Y12 point-of-care device to monitor platelet function across a range of P2Y12 inhibition levels following prasugrel and clopidogrel administrationJoseph A Jakubowski
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Thromb Haemost 99:409-15. 2008..The determination of the clinical utility of such POC devices will require their use in clinical outcome studies... - Pharmacodynamics and pharmacokinetics of single doses of prasugrel 30 mg and clopidogrel 300 mg in healthy Chinese and white volunteers: an open-label trialDavid S Small
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
Clin Ther 32:365-79. 2010..Although the approved loading dose is 60 mg, earlier studies of prasugrel suggested that active-metabolite exposure and pharmacodynamic response may be higher in Asian subjects than in white subjects... - Increased active metabolite formation explains the greater platelet inhibition with prasugrel compared to high-dose clopidogrelChristopher D Payne
Lilly Research Laboratories, Eli Lilly and Company, Windlesham, Surrey, UK
J Cardiovasc Pharmacol 50:555-62. 2007..In conclusion, greater exposure to prasugrel's active metabolite results in faster onset, higher levels, and less variability of platelet inhibition compared with high-dose clopidogrel in healthy subjects... - A comparison of the antiplatelet effects of prasugrel and high-dose clopidogrel as assessed by VASP-phosphorylation and light transmission aggregometryJoseph A Jakubowski
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Thromb Haemost 99:215-22. 2008..86, p < 0.0001). VASP and LTA demonstrated concordance across the response range of P2Y(12) receptor blockade following thienopyridine LDs... - Effects of the proton pump inhibitor lansoprazole on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrelDavid S Small
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center DC 0724, Indianapolis, IN 46285, USA
J Clin Pharmacol 48:475-84. 2008..The overall data suggest that a prasugrel dose adjustment is not likely warranted in an individual taking prasugrel with a proton pump inhibitor such as lansoprazole... - Dose-dependent inhibition of human platelet aggregation by prasugrel and its interaction with aspirin in healthy subjectsJoseph 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... - Effect of age on the pharmacokinetics and pharmacodynamics of prasugrel during multiple dosing: an open-label, single-sequence, clinical trialDavid S Small
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
Drugs Aging 26:781-90. 2009..Prasugrel is a novel antiplatelet agent approved for the treatment of ACS patients undergoing percutaneous coronary intervention, and will be used in this population... - Switching directly to prasugrel from clopidogrel results in greater inhibition of platelet aggregation in aspirin-treated subjectsChristopher D Payne
Lilly Research Laboratories, Eli Lilly and Company, Windlesham, Surrey, UK
Platelets 19:275-81. 2008..Switching directly from clopidogrel MD to either prasugrel LD or MD was well tolerated and resulted in significantly greater levels of platelet inhibition than a clopidogrel 75 mg MD... - Inhibition of platelet aggregation with prasugrel and clopidogrel: an integrated analysis in 846 subjectsYing G Li
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Platelets 20:316-27. 2009..Gender, race, body weight, and age were identified as statistically significant covariates impacting platelet inhibition... - Effect of ranitidine on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrelDavid S Small
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
Curr Med Res Opin 24:2251-7. 2008..This study evaluated the influence of ranitidine coadministration on the pharmacokinetics and pharmacodynamics of the respective active metabolite of prasugrel and clopidogrel... - A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formationJohn T Brandt
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
Am Heart J 153:66.e9-16. 2007..Thienopyridines are prodrugs, metabolized in vivo to active metabolites that inhibit the platelet P2Y12 adenosine diphosphate (ADP) receptor... - Integrated analysis of pharmacokinetic data across multiple clinical pharmacology studies of prasugrel, a new thienopyridine antiplatelet agentDavid S Small
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
J Clin Pharmacol 51:321-32. 2011..These results characterize prasugrel's PK across a range of studies and highlight body weight as the most influential covariate on prasugrel AM exposure, with implications for prasugrel maintenance dosing in clinical practice... - Metabolism and disposition of the thienopyridine antiplatelet drugs ticlopidine, clopidogrel, and prasugrel in humansNagy A Farid
Eli Lilly and Company, Indianapolis, Indiana 46285, USA
J Clin Pharmacol 50:126-42. 2010..Current literature shows that greater ADP-mediated IPA is associated with significantly better clinical outcomes for patients with acute coronary syndrome... - Effect of intrinsic and extrinsic factors on the clinical pharmacokinetics and pharmacodynamics of prasugrelDavid S Small
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana 46285, USA
Clin Pharmacokinet 49:777-98. 2010..Although prasugrel did not alter warfarin pharmacokinetics, prasugrel and warfarin should not be used together, because of an increased bleeding risk associated with their concomitant use... - Comparison of speed of onset of platelet inhibition after loading doses of clopidogrel versus prasugrel in healthy volunteers and correlation with responder statusGovinda J Weerakkody
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
Am J Cardiol 100:331-6. 2007..After a thienopyridine LD, the initial rate of platelet inhibition was predictive of pharmacodynamic responder status... - The platelet inhibitory effects and pharmacokinetics of prasugrel after administration of loading and maintenance doses in healthy subjectsJoseph A Jakubowski
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
J Cardiovasc Pharmacol 47:377-84. 2006..Prasugrel LDs and MDs provide rapid and sustained inhibition of ADP-mediated platelet aggregation... - The biotransformation of prasugrel, a new thienopyridine prodrug, by the human carboxylesterases 1 and 2Eric T Williams
Department of Drug Disposition, Eli Lilly and Company, Lilly Research Laboratories, Indianapolis, IN 46285, USA
Drug Metab Dispos 36:1227-32. 2008..These data help explain the rapid appearance of R-138727 in human plasma, where maximum concentrations are observed 0.5 h after a prasugrel p.o. dose, and the rapid onset of action of prasugrel... - Stereoselective metabolism of prasugrel in humans using a novel chiral liquid chromatography-tandem mass spectrometry methodEnaksha R Wickremsinhe
Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
Drug Metab Dispos 35:917-21. 2007..The ratios of the R-138727 stereoisomers were consistent among subjects, regardless of the dose or time of sample collection or whether the blood was sampled after the first dose or after 4 weeks of therapy... - Disposition of LY333531, a selective protein kinase C beta inhibitor, in the Fischer 344 rat and beagle dogJ L Burkey
Lilly Research Laboratories, Division of Eli Lilly and Co, Lilly Corporate Center, Indianapolis, IN 46285, USA
Xenobiotica 32:1045-52. 2002..7 h. 6. The data indicate that the disposition of LY333531 is similar in rat and dog... - Preclinical characterization of 2-[3-[3-[(5-ethyl-4'-fluoro-2-hydroxy[1,1'-biphenyl]-4-yl)oxy]propoxy]-2-propylphenoxy]benzoic acid metabolism: in vitro species comparison and in vivo disposition in ratsE J Perkins
Lilly Research Laboratories, Indianapolis, IN, USA
Drug Metab Dispos 31:1382-90. 2003.... - Prasugrel pharmacokinetics and pharmacodynamics in subjects with moderate renal impairment and end-stage renal diseaseD 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... - Pharmacokinetics and pharmacodynamics of prasugrel in subjects with moderate liver diseaseD S Small
Eli Lilly and Company, Indianapolis, IN 46285, USA
J Clin Pharm Ther 34:575-83. 2009..As hepatic enzymes play a key role in formation of prasugrel's active metabolite, hepatic impairment could affect the safety and/or efficacy of prasugrel in such patients... - Common polymorphisms of CYP2C19 and CYP2C9 affect the pharmacokinetic and pharmacodynamic response to clopidogrel but not prasugrelJ 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... - Confidence interval criteria for assessment of dose proportionalityB P Smith
Lilly Laboratory for Clinical Research, Indianapolis, Indiana 46202 5250, USA
Pharm Res 17:1278-83. 2000..The aim of this work was a pragmatic, statistically sound and clinically relevant approach to dose-proportionality analyses that is compatible with common study designs... - Disposition and metabolic fate of prasugrel in mice, rats, and dogsR L Smith
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
Xenobiotica 37:884-901. 2007..The main circulating thiol-containing metabolite in the three animal species is the pharmacologically active metabolite, R-138727. The thiol-containing metabolites are further metabolized by S-methylation and conjugation with cysteine... - Effect of rifampin on the pharmacokinetics and pharmacodynamics of prasugrel in healthy male subjectsN A Farid
Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 6285, USA
Curr Med Res Opin 25:1821-9. 2009....