Pharmacokinetics, pharmacodynamics, safety and tolerability of multiple ascending doses of ticagrelor in healthy volunteers.

British Journal of Clinical Pharmacology
Kathleen Butler, Renli Teng

Abstract

The antiplatelet agent clopidogrel is currently the recommended treatment for acute coronary syndrome (ACS). Inhibition of platelet aggregation (IPA) with clopidogrel is insufficient, which increases the risk for recurrent ischaemic events. Therefore, there is a need for antiplatelet agents with improved IPA. Ticagrelor (AZD6140) is a new antiplatelet agent in clinical development for reduction of thrombotic events in patients with ACS. This study assesses the optimal dosing schedule for ticagrelor in healthy volunteers and compares the degree of IPA with clopidogrel. Our findings illustrate that the pharmacokinetics of ticagrelor are predictable and are associated with consistent inhibition of platelet activity. IPA with ticagrelor was greater and better sustained at high levels with twice daily ticagrelor than once daily regimens. To determine the pharmacokinetics, pharmacodynamics, safety and tolerability of multiple oral doses of ticagrelor, a P2Y(12) receptor antagonist, in healthy volunteers. This was a randomized, single-blind, placebo-controlled, ascending dose study. Thirty-two subjects received ticagrelor 50-600 mg once daily or 50-300 mg twice daily or placebo for 5 days at three dose levels in two parallel groups. A...Continue Reading

References

Apr 26, 2003·The American Journal of Cardiology·Paul A Gurbel, Kevin P Bliden
Jun 3, 2004·Best Practice & Research. Clinical Haematology·Alan K Jacobson
Jan 18, 2005·Journal of the American College of Cardiology·Victor L SerebruanyEric J Topol
Apr 27, 2005·Seminars in Thrombosis and Hemostasis·J J J van Giezen, Robert G Humphries
Oct 4, 2005·Expert Opinion on Pharmacotherapy·Udaya S TantryPaul A Gurbel
Jan 13, 2006·Journal of Thrombosis and Haemostasis : JTH·S Heptinstall
Jul 1, 2006·Nature Clinical Practice. Cardiovascular Medicine·Paul A Gurbel, Udaya S Tantry
Jan 25, 2007·Expert Opinion on Investigational Drugs·Udaya S TantryPaul A Gurbel
Apr 10, 2007·Journal of the American College of Cardiology·Dominick J AngiolilloMarco A Costa
Jun 16, 2007·European Heart Journal·Jean-Pierre BassandWilliam Wijns
Jun 19, 2007·Journal of the American College of Cardiology·Piergiovanni BuonamiciDavid Antoniucci
Sep 11, 2007·Bioorganic & Medicinal Chemistry Letters·Brian SpringthorpePaul A Willis
Nov 6, 2007·The New England Journal of Medicine·Stephen D WiviottUNKNOWN TRITON-TIMI 38 Investigators
Jun 4, 2008·The Journal of Continuing Education in the Health Professions·Kiera KeownEmma Irvin
Sep 1, 2009·The New England Journal of Medicine·Lars WallentinMona Thorsén

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Citations

Mar 1, 2012·European Journal of Clinical Pharmacology·Renli TengKathleen Butler
Aug 28, 2012·European Journal of Clinical Pharmacology·Renli TengKathleen A Butler
Oct 25, 2012·European Journal of Clinical Pharmacology·Renli TengKathleen Butler
Jun 12, 2013·European Journal of Clinical Pharmacology·Renli Teng, Kathleen Butler
Oct 5, 2011·British Journal of Anaesthesia·H T BenzonJ A Katz
May 6, 2011·Thrombosis and Haemostasis·H FernandoJ A Shaw
Apr 12, 2011·Thrombosis and Haemostasis·Robert F Storey
Jun 18, 2014·Cardiovascular Intervention and Therapeutics·Y HiasaH Emanuelsson
Aug 29, 2012·Expert Opinion on Drug Metabolism & Toxicology·Sonya BurgessCraig P Juergens
Nov 7, 2014·Expert Opinion on Investigational Drugs·Aun-Yeong Chong, Derek Y So
Jan 25, 2011·Expert Opinion on Pharmacotherapy·Mariano A GiorgiGuillermo Di Girolamo
Apr 18, 2015·Expert Opinion on Drug Metabolism & Toxicology·Francesco MonitilloNadia Aspromonte
Jun 23, 2011·Current Medical Research and Opinion·Kathleen Butler, Renli Teng
Apr 7, 2015·The Journal of Emergency Medicine·Lim Beng Leong, Teng Kuan Peng David
Mar 21, 2012·Journal of Thrombosis and Haemostasis : JTH·T ThieleA Greinacher
Oct 5, 2011·Journal of Clinical Pharmacy and Therapeutics·R TengK Butler
Jan 24, 2014·Clinical Cardiology·Shinya Goto, Aiko Tomita
Aug 29, 2014·Pharmacotherapy·Paul P Dobesh, Julie H Oestreich
Dec 28, 2012·Expert Opinion on Pharmacotherapy·Wah Wah Htun, Steven R Steinhubl
Jun 12, 2013·Journal of the American College of Cardiology·Dimitrios AlexopoulosGeorge Hahalis
Jul 23, 2013·Clinical Therapeutics·Renli Teng, Kathleen Butler
Jul 1, 2016·Cardiovascular Drugs and Therapy·Nathan E K ProcterJohn D Horowitz
Jul 15, 2016·Fundamental & Clinical Pharmacology·Niloufar MarsousiYoussef Daali
Oct 8, 2016·Expert Opinion on Drug Metabolism & Toxicology·Gian Marco RosaClaudio Brunelli
Nov 4, 2016·Expert Review of Cardiovascular Therapy·Aung MyatPaul A Gurbel
Jan 17, 2017·Journal of Thrombosis and Haemostasis : JTH·A J GerritsA L Frelinger
Jan 31, 2014·Journal of Cardiovascular Pharmacology·Henry E SpeichLisa K Jennings

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