Drug intelligence / Profile preview

GW-559090

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral, Ophthalmic, Inhalation, Intranasal
01

Overview

GW‑559090 is a small molecule investigational drug that acts as a high-affinity, competitive antagonist of the integrin alpha4beta1 (α4β1), also known as very late antigen‑4 (VLA‑4). It was initially developed by GSK for the treatment of inflammatory disorders such as asthma and allergic rhinitis. The drug inhibits leukocyte trafficking and activation by blocking α4β1 integrin interactions with vascular cell adhesion molecule 1 (VCAM‑1) and fibronectin, thereby reducing inflammation. Preclinical studies have also explored its use in ocular inflammatory conditions like dry eye disease and uveitis. Development for asthma and allergic rhinitis was discontinued after phase II clinical trials[3][5][6][8].

Other names
Gw-559090(free acid)L-Tyrosine, N-((2-methylphenoxy)acetyl)-L-leucyl-, 4-(aminocarbonyl)-1-piperidinecarboxylate (ester)(2S)-3-(4-(4-Carbamoylpiperidine-1-carbonyl)oxyphenyl)-2-[[(2S)-4-methyl-2-[[(2-(2-methylphenoxy)acetyl]amino]pentanoyl]amino]propanoic acid
02

Targets

α4β1 (Integrin α4β1)

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