Drug intelligence / Profile preview

GS-6201

Development stage
Preclinical
Lead developer
Gilead Sciences
Modality
Small Molecules
Administration
Intraperitoneal, Oral
01

Overview

**GS-6201** is a selective, high-affinity antagonist of the **A2B adenosine receptor** (A2B AdoR), developed by Gilead Sciences. It potently and selectively blocks the A2B receptor, with more than 500-fold selectivity over the A1, A2A, and A3 adenosine receptor subtypes[1][2]. Mechanistically, GS-6201 inhibits adenosine-mediated proinflammatory signaling and is shown to blunt inflammation, reduce caspase-1 activation, inflammatory cytokines (such as IL-6 and TNF-α), and limit tissue fibrosis and remodeling, particularly after acute myocardial infarction and in models of pulmonary hypertension and lung fibrosis[1][2].

Other names
3-ethyl-1-propyl-8-(1-(3-trifluoromethylbenzyl)-1H-pyrazol-4-yl)-3,7-dihydropurine-2,6-dione
02

Targets

ADORA2B (Adenosine A2B receptor)

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