Mobocertinib’s mechanism of action

Mobocertinib (Mobocertinib) is an epidermal growth factor receptor (EGFR) kinase inhibitor that irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild-type (WT) EGFR. After oral administration of moboxetinib, two pharmacologically active metabolites (AP32960 and AP32914) with inhibitory properties similar to those of moboxetinib can be found in the plasma. In vitro, mobosetinib also inhibits the activity of other EGFR family members (HER2 and HER4) and an additional kinase (BLK) at clinically relevant concentrations (IC values u200bu200b<2 nM). In animal tumor transplant models, mobosertinib demonstrated antitumor activity against xenografts harboring EGFR exon 20 insertions of NPH or ASV.