Mobocertinib (Exkivity)

Mechanism of action

From the NCI Drug Dictionary: An orally available inhibitor of human epidermal growth factor receptor (EGFR) exon 20 insertion mutations, with antineoplastic activity. Upon oral administration, mobocertinib, and its active metabolites, specifically and irreversibly binds to and inhibits exon 20 insertion mutations of EGFR. This prevents EGFR-mediated signaling and leads to cell death in tumor cells expressing exon 20 insertion mutations. In addition, mobocertinib may inhibit the activity of other EGFR family members, such as human epidermal growth factor receptor 2 (HER2; ERBB2) and HER4.

Diseases for which it was used

• EGFRm NSCLC

History of changes in FDA indication

• 2021-09-15: Granted accelerated approval for adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 20 insertion mutations, as detected by an FDA-approved test, whose disease has progressed on or after platinum-based chemotherapy. (Based on AP32788-15-101)
  • 2024-07-09: Drug withdrawn due to failure of confirmatory trial.

Also known as

• Code names: AP-32788, TAK-788
• Brand name: Exkivity