Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of a Liver‐Targeting Acetyl‐CoA Carboxylase Inhibitor (PF‐05221304): A Three‐Part Randomized Phase 1 Study

PF‐05221304 is a liver‐targeted inhibitor of acetyl‐CoA carboxylase, an enzyme that catalyzes the first committed step in de novo lipogenesis (DNL). This first‐in‐human study investigated safety/tolerability and pharmacokinetics of single and multiple ascending oral PF‐05221304 doses, and fructose‐stimulated DNL inhibition with repeated oral doses. Healthy subjects (n = 96) received single (1‐240 mg) or repeated (2‐200 mg daily) doses for 14...