Comparison of antiplatelet effects of prasugrel and ticagrelor in cynomolgus monkeys by an ELISA-based VASP phosphorylation assay and platelet aggregation

Thrombosis and Haemostasis

Volumn 110, Issue 4, 2013, Pages 769-776

  Tomizawa, Atsuyuki ^a   Ohno, Kousaku ^a   Jakubowski, Joseph A ^b   Mizuno, Makoto ^a   Sugidachi, Atsuhiro ^a  

^a DAIICHI SANKYO CO   (Japan)

^b ELI LILLY AND COMPANY   (United States)

Author keywords

P2Y12 antagonist; Platelet aggregation; Prasugrel; Ticagrelor; VASP

Indexed keywords

DRUG METABOLITE; PRASUGREL; TICAGRELOR; VASODILATOR STIMULATED PHOSPHOPROTEIN;

ADULT; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; COMPARATIVE STUDY; CONTROLLED STUDY; ENZYME LINKED IMMUNOSORBENT ASSAY; EX VIVO STUDY; HUMAN; IC 50; IN VITRO STUDY; LOADING DRUG DOSE; MACACA FASCICULARIS; MALE; NONHUMAN; NORMAL HUMAN; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SINGLE DRUG DOSE; THROMBOCYTE AGGREGATION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOCYTE POOR PLASMA; THROMBOCYTE RICH PLASMA;

P2Y12 ANTAGONIST; PLATELET AGGREGATION; PRASUGREL; TICAGRELOR; VASP;

ADENOSINE; ADENOSINE DIPHOSPHATE; ADMINISTRATION, ORAL; ADULT; ANIMALS; CELL ADHESION MOLECULES; CLINICAL PROTOCOLS; ENZYME-LINKED IMMUNOSORBENT ASSAY; HUMANS; MACACA FASCICULARIS; MALE; MICROFILAMENT PROTEINS; PHOSPHOPROTEINS; PHOSPHORYLATION; PIPERAZINES; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; PURINERGIC P2 RECEPTOR ANTAGONISTS; THIOPHENES; YOUNG ADULT;

EID: 84884867786     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1160/TH13-03-0260     Document Type: Article

References (38)

1. Niitsu Y, et al. Pharmacology of CS-747 (prasugrel, LY640315), a novel, potent antiplatelet agent with in vivo P2Y12 receptor antagonist activity. Semin Thomb Hemost 2005; 31: 184-194.
2. Jakubowski JA, et al. Prasugrel: a novel thienopyridine antiplatelet agent. A review of preclinical and clinical studies and the mechanistic basis for its distinct antiplatelet profile. Cardiovasc Drug Rev 2007; 25: 357-374.
3. Sugidachi A, et al. Antiplatelet action of R-99224, an active metabolite of a novel thienopyridine-type G(i)-linked P2T antagonist, CS-747. Br J Pharmacol 2001; 132: 47-54.
4. Sugidachi A, et al. The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel's active metabolite. J Thomb Haemost 2007; 5: 1545-1551.
5. Dobesh PP. Pharmacokinetics and pharmacodynamics of prasugrel, a thienopyridine P2Y12 inhibitor. Pharmacotherapy 2009; 29: 1089-1102.
6. Wiviott SD, et al. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Engl J Med 2007; 357: 2001-2015.
7. Li YG, et al. Inhibition of platelet aggregation with prasugrel and clopidogrel: an integrated analysis in 846 subjects. Platelets 2009; 20: 316-327.
8. van Giezen JJ, et al. Ticagrelor binds to human P2Y12 independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation. J Thomb Haemost 2009; 7: 1556-1565.
9. Wijeyeratne YD, et al. Ticagrelor: a P2Y12 antagonist for use in acute coronary syndromes. Expert Rev Clin Pharmacol 2012; 5: 257-269.
10. Wallentin L, et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes. N Engl J Med 2009; 361: 1045-1057.
11. Teng R, Butler K. Pharmacokinetics, pharmacodynamics, tolerability and safety of single ascending doses of ticagrelor, a reversibly binding oral P2Y12 receptor antagonist, in healthy subjects. Eur J Clin Pharmacol 2010; 66: 487-496.
12. Sugidachi A, et al. A comparison of the pharmacological profiles of prasugrel and ticagrelor assessed by platelet aggregation, thombus formation and haemostasis in rats. Br J Pharmacol 2013; 169: 82-89.
13. Alber HF, et al. Prasugrel vs. ticagrelor in acute coronary syndromes: which one to choose? Wien Klin Wochensch 2011; 123: 468-476.
14. Alexopoulos D, et al. Ticagrelor versus prasugrel in acute coronary syndrome patients with high on-clopidogrel platelet reactivity following percutaneous coronary intervention: a pharmacodynamic study. J Am Coll Cardiol 2012; 60: 193-199.
15. Biondi-Zoccai G, et al. Adjusted indirect comparison meta-analysis of prasugrel versus ticagrelor for patients with acute coronary syndromes. Int J Cardiol 2011; 150: 325-331.
16. Jakubowski JA, et al. A comparison of the antiplatelet effects of prasugrel and high-dose clopidogrel as assessed by VASP-phosphorylation and light transmission aggregometry. Thomb Haemost 2008; 99: 215-222.
17. Michelson AD. Methods for the measurement of platelet function. Am J Cardiol 2009; 103 (Suppl 3):20A-6A.
18. Michelson AD, et al. Current options in platelet function testing. Am J Cardiol 2006; 98: 4N-10N.
19. Jakubowski JA, et al. 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. Thomb Haemost 2008; 99: 409-415.
20. Barragan P, et al. Resistance to thienopyridines: clinical detection of coronary stent thombosis by monitoring of vasodilator-stimulated phosphoprotein phosphorylation. Catheter Cardiovasc Interv 2003; 59: 295-302.
21. Barragan P, et al. Validation of a novel ELISA-based VASP whole blood assay to measure P2Y12-ADP receptor activity. Thomb Haemost 2010; 104: 410-411.
22. Angiolillo DJ, et al. Differential effects of omeprazole and pantoprazole on the pharmacodynamics and pharmacokinetics of clopidogrel in healthy subjects: randomized, placebo-controlled, crossover comparison studies. Clin Pharmacol Ther 2011; 89: 65-74.
23. Jakubowski JA, et al. Comparison of a new ELISA assay with the flow cytometric assay for platelet vasodilator-associated stimulated phosphoprotein (VASP) phosphorylation in whole blood to assess P2Y(12) inhibition. Thomb Haemost 2012; 107: 388-395.
24. Alexander SP, et al. Guide to Receptors and Channels (GRAC), 5th edition. Br J Pharmacol 2011; 164 (Suppl 1): S1-S324.
25. Sugidachi A, et al. The in vivo pharmacological profile of CS-747, a novel antiplatelet agent with platelet ADP receptor antagonist properties. Br J Pharmacol 2000; 129: 1439-1446.
26. Savi P, et al. Identification and biological activity of the active metabolite of clopidogrel. Thomb Haemost 2000; 84: 891-896.
27. Springthorpe B, et al. From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thombosis. Bioorg Med Chem Lett 2007; 17: 6013-6018.
28. Sillén H, et al. Determination of ticagrelor and two metabolites in plasma samples by liquid chomatography and mass spectrometry. J Chomatogr B Analyt Technol Biomed Life Sci 2010; 878: 2299-2306.
29. van Giezen JJ, Humphies RG. Preclinical and clinical studies with selective reversible direct P2Y12 antagonists. Semin Thomb Hemost 2005; 31: 195-204.
30. Husted SE, et al. Pharmacokinetics and pharmacodynamics of ticagrelor in patients with stable coronary artery disease: results from the ONSET-OFFSET and RESPOND studies. Clin Pharmacokinet 2012; 51: 397-409.
31. Gurbel PA, et al. Response to ticagrelor in clopidogrel nonresponders and responders and effect of switching therapies: the RESPOND study. Circulation 2010; 121: 1188-1199.
32. Jernberg T, et al. Prasugrel achieves greater inhibition of platelet aggregation and a lower rate of non-responders compared with clopidogrel in aspirintreated patients with stable coronary artery disease. Eur Heart J 2006; 27: 1166-1173.
33. Parodi G, et al. Comparison of prasugrel and ticagrelor loading doses in ST-segment elevation myocardial infarction patients. J Am Coll Cardiol 2013; 61: 1601-1606.
34. Niitsu Y, et al. Repeat oral dosing of prasugrel, a novel P2Y12 receptor inhibitor, results in cumulative and potent antiplatelet and antithombotic activity in several animal species. Eur J Pharmacol 2008; 579: 276-282.
35. National Center for Biotechnology Information. Blast analysis of human VASP revealed close matches with hypothetical protein EGM_09874, partial of Macaca fascicularis (ACCESSION No. EHH59696). Available at: http://www.ncbi.nlm.nih.gov/protein/355755949?report=genbank&log$=prot-top&blast_rank=1&RID=C0DUXR3D014. Accessed February 26, 2013.
36. Pampuch A, et al. Comparison of VASP-phosphorylation assay to light-transmission aggregometry in assessing inhibition of the platelet ADP P2Y12 receptor. Thomb Haemost 2006; 96: 767-773.
37. Aleil B, et al. Flow cytometric analysis of intraplatelet VASP phosphorylation for the detection of clopidogrel resistance in patients with ischemic cardiovascular diseases. J Thomb Haemost 2005; 3: 85-92.
38. Bourguet N, et al. Evaluation of ELISA-based VASP assay with whole blood samples from several animal species, and compatibility with various platelet antagonists. J Thomb Haemost 2011; 9: 971-1027.