RG-13965(RG-13965) - 药物靶点：GP IIb/IIIa_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

GP IIb/IIIa

作用机制

GP IIb/IIIa拮抗剂(糖蛋白 IIb/IIIa拮抗剂)

治疗领域

心血管疾病

在研适应症-

非在研适应症

血栓形成

原研机构

Aventis SA

在研机构-

非在研机构

Aventis SA

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 RG-13965 相关的临床结果

登录后查看更多信息

100 项与 RG-13965 相关的转化医学

登录后查看更多信息

100 项与 RG-13965 相关的专利（医药）

登录后查看更多信息

1

项与 RG-13965 相关的文献（医药）

1996-06-01·Thrombosis Research3区 · 医学

Anti-thrombotic activity of RG13965, a novel platelet fibrinogen receptor antagonist

3区 · 医学

Article

作者: Jeffrey S. Bostwick ; Christopher T. Dunwiddie ; Jacquelynn J. Cook ; Ralph D. Sabatino ; Charles J. Kasiewski ; Valeria Chu ; Robert J. Leadley ; Scott I. Klein ; Mark H. Perrone

RG13965, a pseudotetrapeptide analogue of Arg-Gly-Asp (RGD), inhibited collagen-induced dog, monkey, human, hamster, mouse, and pig platelet aggregation in vitro with IC50 values of 3.7, 4.6, 6.3, 126, 136 and 1600 microM, respectively. RG13965 (3, 10, and 30 mg/kg, i.v.) decreased the incidence of collagen/epinephrine-induced thrombosis in mice from 90% in untreated animals to 63, 37, and 0%, respectively. In hamsters, RG13965 (10 and 30 mg/kg, i.v.) prolonged the time required for formation of a hemostatic plug in severed mesenteric arteries by 1.6- and 3.6-fold, respectively. In a canine model of repetitive platelet thrombus formation in the coronary artery, RG13965 (0.1, 0.3, and 1 mg/kg, i.v.) reversibly inhibited cyclic flow reductions (CFRs) and inhibited ADP-induced ex vivo platelet aggregation by 29, 57, and 77%, respectively. RG13965 (1 mg/kg) completely inhibited CFRs for at least 40 min. Platelet count was not altered at any dose and template bleeding time was prolonged modestly (1.8-fold) at only the highest dose. RG13965 dose-dependently and reversibly inhibited thrombus formation at doses which did not completely inhibit ex vivo platelet aggregation and only modestly prolonged template bleeding time.

100 项与 RG-13965 相关的药物交易

登录后查看更多信息