Drug intelligence / Profile preview

GSK376501 + flurbiprofen

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK376501 + flurbiprofen is a combination of two small molecule drugs: GSK376501, a selective peroxisome proliferator-activated receptor gamma (PPARγ) partial agonist developed by GSK for metabolic diseases such as type 2 diabetes mellitus and obesity, and flurbiprofen, a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class that acts as a non-selective cyclooxygenase (COX) inhibitor to decrease inflammation, pain, and fever[1][2][4]. GSK376501 has completed phase 1 studies for type 2 diabetes mellitus and obesity[2][4]. Flurbiprofen is approved for symptomatic treatment of various inflammatory conditions including osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis, and is also used to manage mild-to-moderate pain[1][5].

02

Targets

ABCC4 (Multidrug resistance-associated protein 4)PTGES (Microsomal prostaglandin E synthase-1)PGHS-1 (Prostaglandin G/H Synthase 1)

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