EXKIVITY (mobocertinib) is an orally administered kinase inhibitor designed to target specific mutations in the epidermal growth factor receptor (EGFR). Its chemical name is propan-2-yl 2-[5-(acryloylamino)-4-{2-(dimethylamino)ethylamino}-2-methoxyanilino]-4-(1-https://www.google.com/search?q=methyl-1H-indol-3-yl)pyrimidine-5-carboxylate succinate. The drug is supplied as 40 mg capsules for oral use. Mobocertinib functions by irreversibly binding to and inhibiting EGFR exon 20 insertion mutations at concentrations lower than those required to inhibit wild-type (WT) EGFR. This selective inhibition is crucial for its therapeutic effect in the indicated patient population.

The mechanism involves targeting the kinase activity of EGFR, thereby disrupting downstream signaling pathways that promote cell proliferation and survival in cancer cells harboring these specific mutations. In addition to mobocertinib itself, two pharmacologically active metabolites, AP32960 and AP32914, which have similar inhibitory profiles to the parent drug, have been identified in plasma following oral administration. In vitro studies have also shown that mobocertinib can inhibit other EGFR family members (HER2 and HER4) and one additional kinase (BLK) at clinically relevant concentrations. This targeted approach aims to provide a therapeutic benefit for patients with EGFR exon 20 insertion mutation-positive NSCLC.