EGFR Mutant-selective Inhibitor BBT-207

**Semantic type:** Pharmacologic Substance

**Definition:** A fourth-generation, orally bioavailable, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGFR mutant-selective inhibitor BBT-207 targets, reversibly binds to, and inhibits the activity of various sensitizing and treatment-emergent EGFR mutations, including ones involving C797S and T790M mutations, and activating mutations, involving exon 19 deletion and L858R mutations. This prevents EGFR-mediated signaling, induces cell death and inhibits growth in susceptible tumor cells harboring these mutations. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. BBT-207 may overcome resistance to third-generation EGFR inhibitors and may be active against drug-naive mutants.

**Synonyms:** - BBT 207 - BBT-207 - BBT207 - Epidermal Growth Factor Receptor Mutant-selective Inhibitor BBT-207 - Mutant-selective EGFR Inhibitor BBT-207