molecules of the month

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).