molecules of the month


GPR84 GPCR negative allosteric modulator

oral Ph. II candidate for IPF

from 200k cmpd biochem. HTS and opt.

J. Med. Chem. Sep. 29, 2020

Galapagos, Romainville, FR / Mechelen, BE

Structure of GLPG1205
1 min read

GLPG1205 is a potent, selective, and orally bioavailable negative allosteric modulator of the GPCR GPR84, a receptor associated with inflammation. Despite possessing both a dioxane ring and an relatively unhindered alkyne, the molecule has low clearance and is highly bioavailable in preclinical species (>100% F). The molecule was taken into a Ph. IIa trial initially for IBD, but failed to meet its primary efficacy endpoint. Currently, it is being evaluated in a Ph. II study in idiopathic pulmonary fibrosis (IPF).

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