molecules of the month


liver-targeted acetyl-CoA carboxylase inhibitor

oral hepatoselective activity obeserved in HV

from opt. of prior candidate for liver uptake

J. Med. Chem., Sep. 18, 2020

Pfizer, Cambridge, MA / Groton, CT

Structure of PF-05221304, a liver targeted inhibitor of acetyl-CoA carboxylase (ACC)
1 min read

PF-05221304 is a liver targeted inhibitor of acetyl-CoA carboxylase (ACC). ACC is a key regulator of lipid metabolism, and there has been significant interest in ACC inhibitors for the treatment of multiple indications including NASH and diabetes. Pfizer previously took a systemic ACC inhibitor into the clinic (PF-05175157), which was found to exert the desired reduction on liver-based lipogenesis but was also found to have a side effect of reducing platelet counts due to activity in the bone marrow. To identify a potentially safer liver targeting molecule, the Pfizer team looked for molecules that were likely to be recognized by the liver uptake transporters, OATP1B1 and OATP1B3, and used a non-human primate model to confirm evaluate the therapeutic index. PF-05221304 was…

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