An orally available inhibitor of specific mutant forms of both human epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2; ERBB2), with potential antineoplastic activity. Upon oral administration, EGFR/HER2 inhibitor AP32788 specifically and irreversibly binds to and inhibits certain mutant forms of EGFR and HER2. This prevents EGFR- and HER2-mediated signaling and leads to cell death in EGFR mutant- and HER2 mutant-expressing tumor cells. EGFR and HER2, receptor tyrosine kinases mutated in many tumor cell types, play key roles in tumor cell proliferation and tumor vascularization. Check for active clinical trials using this agent.
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