ONT-993 is an aliphatic droxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM).
References:
[1]. Sun H, et al. Elimination of tucatinib, a small molecule kinase inhibitor of HER2, is primarily governed by CYP2C8 enantioselective oxidation of gem-dimetl. Cancer Chemother Pharmacol. 2022 Jun;89(6):737-750.
















