Inhibition of fatty acid synthase with FT‐4101 safely reduces hepatic de novo lipogenesis and steatosis in obese people with non‐alcoholic fatty liver disease: Results from two early phase randomized trials
Diabetes, Obesity and Metabolism Dec 10, 2020
Beysen C, Schroeder P, Wu E, et al. - In treating non‐alcoholic fatty liver disease (NAFLD), researchers examined the treatment potential of fatty acid synthase (FASN) inhibition with FT‐4101 (a potent, selective, orally bioavailable, small‐molecule). For this purpose, they assessed the dose‐response of single FT‐4101 doses (3, 6 and 9 mg) on hepatic de novo lipogenesis (DNL) in healthy people (study 1) and focused on the safety, tolerability as well as the efficacy on hepatic steatosis following 12 weeks FT‐4101 dosing in NALFD patients (study 2). Study 1 comprised three sequential cohorts of healthy men (n = 10/cohort), randomly assigned to receive a single dose of FT‐4101 (n = 5/cohort) or placebo (n = 5/cohort) followed by crossover dosing following 7 days. Study 2 included men and women with NAFLD (n=14) who were randomized to 12 weeks of intermittent once‐daily dosing (4 cycles of 2 weeks on, followed by 1 week off treatment) of 3 mg FT‐4101 (n = 9) or placebo (n = 5). Findings demonstrated that at 3 mg, FT‐4101 safely inhibits FASN and reduces hepatic DNL and steatosis in NAFLD patients.
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