Cetilistat is an inhibitor of pancreatic lipase (IC50s = 5.95 and 54.8 nM for the human and rat enzymes, respectively).1 It reduces increases in plasma triglyceride levels in an oral fat tolerance test, indicating decreased intestinal fat absorption, in rats when administered at a doses ranging from 3 to 100 mg/kg. Dietary administration of cetilistat (4.9-50.7 mg/kg per day) decreases body weight gain without affecting food intake, as well as reduces increases in plasma triglyceride and leptin levels in a rat model of high-fat diet-induced obesity. It also reduces viral load in the culture supernatant of Vero E6 cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2; EC90 = 2.9 ?M) and inhibits SARS-CoV-2 replication in a plaque reduction assay (EC50 = 1.13 ?M).2
1.Yamada, Y., Kato, T., Ogino, H., et al.Cetilistat (ATL-962), a novel pancreatic lipase inhibitor, ameliorates body weight gain and improves lipid profiles in ratsHorm. Metab. Res.40(8)539-543(2008) 2.Yuan, S., Chan, J.F.W., Chik, K.K.H., et al.Discovery of the FDA-approved drugs bexarotene, cetilistat, diiodohydroxyquinoline, and abiraterone as potential COVID-19 treatments with a robust two-tier screening systemPharmacol. Res.159104960(2020)