Randomized, Multicenter, Placebo-Controlled, Double-Blind, Parallel Group Study of INS50589 Intravenous Infusion in Subjects Undergoing Coronary Artery Bypass Graft Surgery Involving Cardiopulmonary Bypass

The purpose of this trial is to identify a dose or doses of INS50589 intravenous infusion that are well-tolerated and which reduce postoperative bleeding and blood product transfusion.

开始日期2006-04-01

申办/合作机构

Merck Sharp & Dohme Corp.

NCT00099450 / Completed临床1期

Single-Center, Open-Labeled Dose Escalation Followed by Randomized, Double-Blind, Placebo-Controlled Cohort Study of the Tolerability, Pharmacokinetics, and Pharmacodynamics of INS50589 Intravenous Infusion in Healthy Volunteers

The objectives of this study are to look at the safety and tolerability of the experimental drug, how people process the drug, how the drug affects people, and to identify a dose or doses to study in subsequent future studies.

开始日期2004-12-01

申办/合作机构

Merck Sharp & Dohme Corp.

100 项与 Regrelor Disodium 相关的临床结果

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100 项与 Regrelor Disodium 相关的转化医学

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100 项与 Regrelor Disodium 相关的专利（医药）

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项与 Regrelor Disodium 相关的文献（医药）

2007-01-01·Platelets3区 · 医学

Rapid and reversible modulation of platelet function in man by a novel P2Y₁₂ADP-receptor antagonist, INS50589

3区 · 医学

Article

作者: Philip T. Leese ; Anthony W. Fox ; José L. Boyer ; Christopher Crean ; Fred L. Johnson ; Todd Durham ; Ramesh Krishnamoorthy ; Donald J. Kellerman

P2Y(12) receptors participate in ADP-induced activation and aggregation of human platelets. INS50589, a selective P2Y(12) receptor antagonist, is being developed for use where controlled, reversible modulation of the platelet hemostatic function is needed. The tolerability, pharmacokinetics, and pharmacodynamics of INS50589 were tested in healthy human volunteers. Thirty-six subjects received intravenous infusions of placebo or INS50589 at 0.1-3 mg/kg/h for four hours. Platelet function, clotting parameters, bleeding time, safety assessments, and plasma concentrations of INS50589 and its major metabolite were monitored for 24 hours. Near-steady state plasma concentrations of INS50589 and effects on platelet function were achieved rapidly. The average maximal plasma concentration of INS50589 was linearly related to the dose administered. Intravenous INS50589 produced dose-dependent inhibition of platelet activation and aggregation in response to ADP in vitro until nearly full inhibition was achieved at the higher doses. Bleeding time was correspondingly increased, without any effect on activated clotting time, prothrombin time, or activated partial thromboplastin time. Platelet response to ADP had returned to at least 75% of the baseline value within 0.25-4 h after cessation of the intravenous infusion of INS50589, depending upon the dose and ADP challenge concentration. Infusions were well tolerated up to the highest dose tested. There was no evidence that the principal metabolite (INS51088) contributed to these effects. INS50589 is a well-tolerated, reversible, competitive antagonist of ADP at the P2Y(12) human platelet receptor, and its potential therapeutic utility in various cardiovascular settings is discussed.

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外链

KEGG	Wiki	ATC	Drug Bank
D08983	-	-	DB05553

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
冠状动脉疾病	临床2期	美国	Merck Sharp & Dohme Corp.	2006-04-01
血栓形成	临床2期	美国	Inspire Pharmaceuticals, Inc.	-
血栓形成	临床2期	-	Merck Sharp & Dohme Corp.	-