Nagy A Farid

Summary

Affiliation: Eli Lilly and Company
Country: USA

Publications

  1. ncbi request reprint Interactions of two major metabolites of prasugrel, a thienopyridine antiplatelet agent, with the cytochromes P450
    Jessica 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
  2. ncbi request reprint Determination of the active and inactive metabolites of prasugrel in human plasma by liquid chromatography/tandem mass spectrometry
    Nagy 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
  3. ncbi request reprint The disposition of prasugrel, a novel thienopyridine, in humans
    Nagy A Farid
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Drug Metab Dispos 35:1096-104. 2007
  4. ncbi request reprint Prasugrel, a new thienopyridine antiplatelet drug, weakly inhibits cytochrome P450 2B6 in humans
    Nagy A Farid
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    J Clin Pharmacol 48:53-9. 2008
  5. doi request reprint Effect of atorvastatin on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrel in healthy subjects
    Nagy A Farid
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 46285, USA
    Pharmacotherapy 28:1483-94. 2008
  6. ncbi request reprint Cytochrome P450 3A inhibition by ketoconazole affects prasugrel and clopidogrel pharmacokinetics and pharmacodynamics differently
    N A Farid
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, Indiana, USA
    Clin Pharmacol Ther 81:735-41. 2007
  7. doi request reprint 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
  8. doi request reprint 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 administration
    Joseph A Jakubowski
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA
    Thromb Haemost 99:409-15. 2008
  9. doi request reprint Pharmacodynamics and pharmacokinetics of single doses of prasugrel 30 mg and clopidogrel 300 mg in healthy Chinese and white volunteers: an open-label trial
    David S Small
    Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, Indiana 46285, USA
    Clin Ther 32:365-79. 2010
  10. ncbi request reprint Increased active metabolite formation explains the greater platelet inhibition with prasugrel compared to high-dose clopidogrel
    Christopher D Payne
    Lilly Research Laboratories, Eli Lilly and Company, Windlesham, Surrey, UK
    J Cardiovasc Pharmacol 50:555-62. 2007

Collaborators

Detail Information

Publications33

  1. ncbi request reprint Interactions of two major metabolites of prasugrel, a thienopyridine antiplatelet agent, with the cytochromes P450
    Jessica 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...
  2. ncbi request reprint Determination of the active and inactive metabolites of prasugrel in human plasma by liquid chromatography/tandem mass spectrometry
    Nagy 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...
  3. ncbi request reprint The disposition of prasugrel, a novel thienopyridine, in humans
    Nagy 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...
  4. ncbi request reprint Prasugrel, a new thienopyridine antiplatelet drug, weakly inhibits cytochrome P450 2B6 in humans
    Nagy 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...
  5. doi request reprint Effect of atorvastatin on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrel in healthy subjects
    Nagy 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...
  6. ncbi request reprint Cytochrome P450 3A inhibition by ketoconazole affects prasugrel and clopidogrel pharmacokinetics and pharmacodynamics differently
    N 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...
  7. doi request reprint 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...
  8. doi request reprint 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 administration
    Joseph 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...
  9. doi request reprint Pharmacodynamics and pharmacokinetics of single doses of prasugrel 30 mg and clopidogrel 300 mg in healthy Chinese and white volunteers: an open-label trial
    David 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...
  10. ncbi request reprint Increased active metabolite formation explains the greater platelet inhibition with prasugrel compared to high-dose clopidogrel
    Christopher 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...
  11. doi request reprint A comparison of the antiplatelet effects of prasugrel and high-dose clopidogrel as assessed by VASP-phosphorylation and light transmission aggregometry
    Joseph 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...
  12. doi request reprint Effects of the proton pump inhibitor lansoprazole on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrel
    David 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...
  13. ncbi request reprint 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...
  14. doi request reprint Effect of age on the pharmacokinetics and pharmacodynamics of prasugrel during multiple dosing: an open-label, single-sequence, clinical trial
    David 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...
  15. doi request reprint Switching directly to prasugrel from clopidogrel results in greater inhibition of platelet aggregation in aspirin-treated subjects
    Christopher 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...
  16. doi request reprint Inhibition of platelet aggregation with prasugrel and clopidogrel: an integrated analysis in 846 subjects
    Ying 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...
  17. doi request reprint Effect of ranitidine on the pharmacokinetics and pharmacodynamics of prasugrel and clopidogrel
    David 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...
  18. ncbi request reprint A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formation
    John 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...
  19. doi request reprint Integrated analysis of pharmacokinetic data across multiple clinical pharmacology studies of prasugrel, a new thienopyridine antiplatelet agent
    David 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...
  20. doi request reprint Metabolism and disposition of the thienopyridine antiplatelet drugs ticlopidine, clopidogrel, and prasugrel in humans
    Nagy 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...
  21. doi request reprint Effect of intrinsic and extrinsic factors on the clinical pharmacokinetics and pharmacodynamics of prasugrel
    David 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...
  22. ncbi request reprint Comparison of speed of onset of platelet inhibition after loading doses of clopidogrel versus prasugrel in healthy volunteers and correlation with responder status
    Govinda 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...
  23. ncbi request reprint The platelet inhibitory effects and pharmacokinetics of prasugrel after administration of loading and maintenance doses in healthy subjects
    Joseph 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...
  24. doi request reprint The biotransformation of prasugrel, a new thienopyridine prodrug, by the human carboxylesterases 1 and 2
    Eric 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...
  25. ncbi request reprint Stereoselective metabolism of prasugrel in humans using a novel chiral liquid chromatography-tandem mass spectrometry method
    Enaksha 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...
  26. ncbi request reprint Disposition of LY333531, a selective protein kinase C beta inhibitor, in the Fischer 344 rat and beagle dog
    J 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...
  27. ncbi request reprint 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 rats
    E J Perkins
    Lilly Research Laboratories, Indianapolis, IN, USA
    Drug Metab Dispos 31:1382-90. 2003
    ....
  28. doi request reprint 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...
  29. doi request reprint Pharmacokinetics and pharmacodynamics of prasugrel in subjects with moderate liver disease
    D 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...
  30. ncbi request reprint 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...
  31. ncbi request reprint Confidence interval criteria for assessment of dose proportionality
    B 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...
  32. ncbi request reprint Disposition and metabolic fate of prasugrel in mice, rats, and dogs
    R 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...
  33. doi request reprint Effect of rifampin on the pharmacokinetics and pharmacodynamics of prasugrel in healthy male subjects
    N A Farid
    Lilly Research Laboratories, Eli Lilly and Company, Indianapolis, IN 6285, USA
    Curr Med Res Opin 25:1821-9. 2009
    ....