Drug intelligence / Profile preview

GSK2239633

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK2239633 is a small molecule antagonist of the CC chemokine receptor 4 (CCR4), developed by GSK. It exhibits a novel anti-inflammatory profile by acting mainly on a subset of Th2 cells and was investigated for the oral treatment of all severities of asthma. The drug inhibits thymus- and activation-regulated chemokine (TARC)-induced actin polymerization, achieving significant CCR4 occupancy in clinical studies. Pharmacokinetic studies showed rapid absorption after oral dosing with low bioavailability and mild to moderate adverse events. No approved indications or marketing authorizations are reported for this compound[1][2][5][9].

Other names
N-(3-((3-(5-chlorothiophene-2-sulfonamido)-4-methoxy-1H-indazol-1-yl)methyl)benzyl)-2-hydroxy-2-methylpropanamide
02

Targets

CCR4 (C-C Motif Chemokine Receptor 4)

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