AP32960

AP32960 is an *active metabolite* of mobocertinib, a small molecule tyrosine kinase inhibitor developed for the treatment of non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations. Mobocertinib is primarily metabolized by CYP3A to form AP32960 and AP32914; both metabolites are equipotent to mobocertinib in inhibiting EGFR activity. AP32960 accounts for roughly 36% of the combined molar exposure of mobocertinib and its active metabolites, is highly protein-bound in plasma, and has a mean elimination half-life of 24 hours at steady state. AP32960’s antitumor effect is mediated via inhibition of EGFR signaling, resulting in reduced proliferation of cancer cells with activating EGFR mutations[1][3][5][7].