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Mobocertinib is an oral small molecule kinase inhibitor specifically designed to target epidermal growth factor receptor (EGFR) exon 20 insertion mutations in non-small cell lung cancer (NSCLC). These mutations are associated with resistance to standard EGFR inhibitors and a poorer prognosis. Mobocertinib binds irreversibly to the mutant EGFR at cysteine 797 in the active site, leading to sustained inhibition of EGFR enzymatic activity and suppression of tumor cell proliferation. It was developed for use in adults with locally advanced or metastatic NSCLC harboring EGFR exon 20 insertion mutations whose disease has progressed on or after platinum-based chemotherapy. Mobocertinib received accelerated approval from the US FDA in 2021 but was voluntarily withdrawn worldwide following results from a phase III trial that did not meet its primary endpoint.
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