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molecules of the month

ervogastat

systemic, oral DGAT2 inhibitor

Ph. II for NASH with fibrosis

opt. of liver-targeting candidate PF-06427878

J. Med. Chem., 02 November 2022

Pfizer, Cambridge, MA and Groton, CT

ervogastat chemical structure systemic, oral DGAT2 inhibitor- Pfizer, Cambridge, MA and Groton, CT
4 mins read

Toward a first-in-class DGAT2 inhibitor for the treatment of NASH. Hepatic triglyceride (TG) accumulation is a symptom of non-alcoholic fatty liver disease (NAFLD), which can progress to non-alcoholic steatohepatitis (NASH), which is characterized by hepatocyte damage, inflammation and collagen deposits (fibrosis). NASH has been estimated to impact 3-5% of the global population, with up to 29% of these individuals developing cirrhosis within 10 years and 4−27% of these patients developing hepatocellular carcinoma. Despite significant research, there are currently no FDA-approved medications for this burgeoning global health crisis. Several targets and mechanisms to treat NASH are being evaluated, including diacylglycerol acyltransferase (DGAT) inhibition. DGAT2 as a target. DGAT enzymes catalyze the esterification of diacylglycerol (DAG) in the final step of triglycerol…


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