Inhibition of fatty acid synthase with FT‐4101 safely reduces hepatic de novo lipogenesis and steatosis in obese subjects with non‐alcoholic fatty liver disease: Results from two early‐phase randomized trials

• Published in: Diabetes, obesity & metabolism Vol. 23; no. 3; pp. 700 - 710
• Main Authors: Beysen, Carine, Schroeder, Patricia, Wu, Eric, Brevard, Julie, Ribadeneira, Maria, Lu, Wei, Dole, Kiran, O'Reilly, Terry, Morrow, Linda, Hompesch, Marcus, Hellerstein, Marc K., Li, Kelvin, Johansson, Lars, Kelly, Patrick F.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.03.2021; Wiley Subscription Services, Inc
• Subjects: Acetic acid; Biomarkers; Clinical trials; Dosage; drug development; drug mechanism; Fatty Acid Synthases - metabolism; Fatty acids; Fatty liver; fatty liver disease; Fatty-acid synthase; Female; Glucose metabolism; Humans; Labeling; Lipid metabolism; Lipogenesis; Liver - metabolism; Liver diseases; Magnetic resonance imaging; Male; Non-alcoholic Fatty Liver Disease - complications; Non-alcoholic Fatty Liver Disease - drug therapy; Non-alcoholic Fatty Liver Disease - metabolism; Obesity; Obesity - complications; Obesity - drug therapy; Obesity - metabolism; Original; Pharmacodynamics; phase I−II study; Placebos; Randomized Controlled Trials as Topic; randomized trial; Steatosis; drug development; drug mechanism; pharmacodynamics; randomized trial; fatty liver disease; phase I−II study

Aims To assess the therapeutic potential of fatty acid synthase (FASN) inhibition with FT‐4101, a potent, selective, orally bioavailable, small‐molecule by (a) evaluating the dose−response of single FT‐4101 doses (3, 6 and 9 mg) on hepatic de novo lipogenesis (DNL) in healthy participants (Study 1)...