Mobocertinib is a targeted therapy for EGFR exon 20 insertion mutation-positive non-small cell lung cancer (NSCLC) and is indicated for patients who have failed prior platinum-based chemotherapy. It selectively inhibits the activity of the EGFR exon 20 mutant protein, blocking tumor cell proliferation signals and thereby delaying disease progression.
Mechanism of Action and Indications
Mobocertinib is a tyrosine kinase inhibitor (TKI) that specifically targets EGFR exon 20 insertion mutations. These mutations account for approximately 4%-10% of EGFR-mutant NSCLC, and traditional EGFR-TKIs (such as gefitinib and osimertinib) have limited efficacy against them. Mobocertinib binds to the ATP-binding domain of the mutant protein, inhibiting downstream signaling and achieving precise targeted therapy.
The indicated population is patients with locally advanced or metastatic NSCLC who have been confirmed to have an EGFR exon 20 insertion mutation and have progressed after or are intolerant to platinum-based chemotherapy.
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