Delving into the Latest Updates on SPI-501 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

thrombin

Mechanism

thrombin inhibitors(Factor IIa inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication-

Inactive Indication

Thrombosis

Originator Organization

Daiichi Fine Chemical Co., Ltd.

Active Organization-

Inactive Organization

Daiichi Fine Chemical Co., Ltd.

Drug Highest PhaseDiscontinuedPreclinical

First Approval Date-

Regulation-

1-Butyl-3-(6,7-dimethoxy-2-naphthylsulfonyl)amino-3-(3-guanidin opropyl)-2-pyrrolidinone hydrochloride (CAS 173440-64-7, SPI-501), which has highly selective thrombin-inhibitory activity, caused a concentration-dependent increase in the time taken for coagulation induced by thrombin in rabbit plasma. The IC50 of SPI-501 was 1.7 mumol/l. Argipidine also prolonged coagulation time and its activity was one order of magnitude greater than that of SPI-501. SPI-501 and argipidine caused dose-dependent increases in the activated partial prothrombin time (APTT) and prothrombin time (PT) of rat plasma. When APTT and PT were measured, IC50 values of SPI-501 were 38.0 and 18.5 mumol/l and those of argipidine, 1.4 and 1.9 mumol/l, respectively. Intravenous administration of SPI-501 (10 and 30 mumol/kg) and argipidine (1 and 3 mumol/kg) prolonged both APTT and PT in rats. While SPI-501 was less potent than argipidine, the durations of the effects of both were the same.

100 Deals associated with SPI-501

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