Drug intelligence / Profile preview

GW273629

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Intravenous, Intraperitoneal
01

Overview

**GW273629** is a potent, highly selective, time-dependent inhibitor of **human inducible nitric oxide synthase (iNOS/NOS2)**, showing over 100-fold selectivity versus endothelial NOS (eNOS) and over 80-fold selectivity versus neuronal NOS (nNOS)[1][3][7]. It acts as an arginine-competitive, NADPH-dependent inhibitor of iNOS with a steady-state dissociation constant (Kd) of less than 90 nM and demonstrates high oral bioavailability in preclinical species (>90%) with a short plasma half-life (around 3 hours in rats, 10 minutes in mice)[1][3][7]. GW273629 was evaluated for indications such as migraine but did not progress to advanced clinical phases and development was discontinued[5].

Other names
3-[[2-[(1-iminoethyl)amino]ethyl]sulphonyl]-L-alanine
02

Targets

NOS2 (Nitric Oxide Synthase 2)

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