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Asengeprast (FT011) is a first-in-class, oral small molecule antagonist of G protein-coupled receptor 68 (GPR68), also known as OGR1 (Ovarian Cancer G-Protein-Coupled Receptor 1). Developed by Certa Therapeutics, it is primarily being investigated for the treatment of diffuse systemic sclerosis (SSc) and other chronic fibrotic conditions affecting the kidneys, lungs, and heart. GPR68 is a proton-sensing receptor that remains silent under normal physiological conditions but becomes activated in response to tissue injury and acidic microenvironments, triggering pro-fibrotic and inflammatory pathways. By inhibiting GPR68, asengeprast aims to reduce scarring and inflammation. In Phase 2 clinical trials, the drug demonstrated significant improvements in skin thickness and lung function in patients with diffuse systemic sclerosis. It has received FDA Fast Track and Orphan Drug designations in both the U.S. and Europe.
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