Safety, tolerability, pharmacokinetics, and time course of pharmacologic response of the active metabolite of roxifiban, XV459, a glycoprotein IIb/IIIa antagonist, following oral administration in healthy volunteers

Journal of Clinical Pharmacology

Volumn 42, Issue 7, 2002, Pages 738-753

  Pieniaszek, Henry J ^a   Sy, Sherwin K B ^a,b   Ebling, William ^a,c   Fossler, Michael J ^a,d   Cain, Valerie A ^a   Mondick, John T ^a   Ma, Su ^a,e   Kornhauser, David M ^a  

^a BRISTOL MYERS SQUIBB   (United States)

^b Innaphase Corporation   (United States)

^c PHARSIGHT CORPORATION   (United States)

^d GLAXOSMITHKLINE   (United States)

^e MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [[[3 [4 (AMINOIMINOMETHYL)PHENYL] 4,5 DIHYDRO 5 ISOXAZOLYL]ACETYL]AMINO] N (BUTOXYCARBONYL)ALANINE; ACETYLSALICYLIC ACID; AMIDINE; AMINO ACID; ANTITHROMBOCYTIC AGENT; FIBRINOGEN RECEPTOR; ISOXAZOLE DERIVATIVE; PRODRUG; ROXIFIBAN; ADENOSINE DIPHOSPHATE; FIBRINOGEN RECEPTOR ANTAGONIST;

ADOLESCENT; ADULT; AGE; AGED; AREA UNDER THE CURVE; ARTICLE; BLEEDING TIME; BLOOD; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG ANTAGONISM; DRUG INTERACTION; FEMALE; HUMAN; HYDROLYSIS; MALE; MIDDLE AGED; ORAL DRUG ADMINISTRATION; TIME; ANOREXIA; ASTHENIA; BLOOD VESSEL OCCLUSION; DRUG BLOOD LEVEL; DRUG HYDROLYSIS; DRUG SAFETY; DRUG TOLERABILITY; FATIGUE; HEADACHE; HUMAN EXPERIMENT; NAUSEA; NORMAL HUMAN; PAIN; PRURITUS; RHINITIS; STEADY STATE; THORAX PAIN; THROMBOCYTE AGGREGATION; TREMOR;

ADMINISTRATION, ORAL; ADOLESCENT; ADULT; AGE FACTORS; AGED; AMIDINES; AMINO ACIDS; AREA UNDER CURVE; ASPIRIN; BLEEDING TIME; DOSE-RESPONSE RELATIONSHIP, DRUG; DOUBLE-BLIND METHOD; DRUG INTERACTIONS; FEMALE; HUMANS; HYDROLYSIS; ISOXAZOLES; MALE; MIDDLE AGED; PLATELET AGGREGATION INHIBITORS; PLATELET GLYCOPROTEIN GPIIB-IIIA COMPLEX; PRODRUGS; TIME FACTORS; HUMAN; MIDDLE AGE;

EID: 0035998752     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/009127002401102687     Document Type: Article

References (40)

1. Platelet activation in unstable coronary disease
2. A perspective on the potential problems with aspirin as an antithrombotic agent: A comparison of studies in an animal model with clinical trials
3. A platelet alpha granule membrane protein (GMP-140) is expressed on the plasma membrane after activation
4. Platelet membrane glycoprotein IIb/IIIa: Member of a family of Asp-Gly-Asp-specific adhesion receptors
5. Ligand binding to GP IIb-IIIa: A status report
6. Use of a monoclonal antibody directed against the platelet glycoprotein IIb/IIIa receptor in high-risk coronary angioplasty
7. Effects of platelet glycoprotein IIb/IIIa blockade with tirofiban on adverse cardiac events in patients with unstable angina or acute myocardial infarction undergoing coronary angioplasty
8. Final report on the aspirin component of the ongoing physicians' health study
9. Inhibition of platelet glycoprotein IIb/IIIa with tirofiban in unstable angina and non-Q-wave myocardial infarction
10. Inhibition of platelet glycoprotein IIb/IIIa with eptifibatide in patients with acute coronary syndromes
11. Two-year follow-up of aspirin responder and aspirin non-responder: A pilot-study including 180 post-stroke patients
12. A randomised, blinded, trial of clopidogrel versus aspirin in patients at risk of ischaemic events (CAPRIE)
13. Thrombotic thrombocytopenic purpura and clopidogrel: A need for new approaches to drug safety
14. Thrombotic thrombocytopenic purpura associated with ticlopidine in the setting of coronary artery stents and stroke prevention
15. Agranulocytosis caused by ticlopidine and its mechanism
16. Anaemia and agranulocytosis associated with ticlopidine therapy
17. Antiplatelet efficacy of XV459, a novel nonpeptide platelet GPIIb/IIIa antagonist: Comparative platelet binding profiles with c7E3
18. Mass spectrometric and NMR characterization of metabolites of roxifiban, a potent and selective antagonist of the platelet glycoprotein IIb/IIIa receptor
19. Orally active isoxazoline GP IIb/IIIa antagonists
20. Intravenous and oral antithrombotic efficacy of the novel platelet GP IIb/IIIa antagonist roxifiban (DMP754) and its free acid form, XV459
21. 3 binding sites in the guinea pig
22. Comparison of PFA-100 closure time and template bleeding time of patients with inherited disorders causing defective platelet function
23. Antiplatelet and antithrombotic efficacy of DMP 728, a novel platelet GP IIb/IIIa receptor antagonist
24. Novel nonpeptide antiplatelet glycoprotein IIb/IIIa receptor antagonist, DMP 754: Receptor binding affinity and specificity
25. Comparative in vitro efficacy of different platelet glycoprotein IIb/IIIa antagonists on platelet-mediated clot strength induced by tissue factor with use of thromboelastography: Differentiation among glycoprotein IIb/IIIa antagonists
26. Comparison of thromboelastography to bleeding time and standard coagulation tests in patients after cardiopulmonary bypass
27. Thromboelastography as an indicator of post-cardiopulmonary bypass coagulopathies
28. Ultrastructure of clots during isometric contraction
29. Increased mortality with oral platelet glycoprotein IIb/IIIa antagonists: A meta-analysis of phase III multicenter randomized trials
30. Oral glycoprotein GP IIb/IIIa inhibition with orbofiban in patients with unstable coronary syndromes (OPUS-TIMI 16) trial
31. Randomized trial of an oral glycoprotein GP IIb/IIIa antagonist, sibrafiban, in patients after an acute coronary syndrome: Results of the TIMI 12 trial
32. Long-term treatment with platelet glycoprotein-receptor antagonist after percutaneous coronary revascularization
33. Comparison of sibrafiban with aspirin for prevention of cardiovascular events after acute coronary syndromes: A randomized trial
34. Commentary: Difficulties with oral platelet glycoprotein IIb/IIIa receptor antagonists
35. Oral inhibitors of platelet membrane receptor glycoprotein IIb/IIIa in clinical cardiology: Issues and opportunities
36. Pharmacokinetics and pharmacodynamics of glycoprotein IIb-IIIa inhibitors
37. Pharmacokinetics and pharmacodynamics of sibrafiban, an orally administered GP IIb/IIIa antagonist, in patients with acute coronary syndrome
38. SmithKline Beecham halts tests of lotrafiban, an oral glycoprotein IIb/IIIa inhibitor
39. Roxifiban, a new oral IIb/IIIa glycoprotein receptor antagonist, in patients with coronary artery disease
40. Exit of platelet glycoprotein IIb/IIIa-receptor inhibitors?