PF-05221304 is an orally bioavailable, liver-targeted inhibitor of acetyl-CoA carboxylase (ACC), an enzyme that catalyzes the first committed step in de novo lipogenesis (DNL).
PF-05221304 inhibits DNL, stimulates fatty acid oxidation, and reduces triglyceride accumulation in primary human hepatocytes.[2]
PF-05221304 reduces DNL and steatosis in Western diet-fed rats in vivo, showing the potential to reduce hepatic lipid accumulation and potentially lipotoxicity.[2]
[1] Arthur Bergman, et al. Clin Pharmacol Drug Dev. 2020 May;9(4):514-526. [2] Ross TT, et al. Cell Mol Gastroenterol Hepatol. 2020;10(4):829-851.