Real-world data demonstrate non-classical mutations are present in 20-30% of all patients with EGFRm NSCLC
Emerging data show non-classical EGFR mutations can be co-expressed with the classical L858R mutation, a setting characterized by shorter duration of response to osimertinib
BDTX-1535 profile differentiated as the most advanced fourth-generation oral TKI in clinical development addressing the full spectrum of classical, non-classical, and C797S resistance EGFR mutations
The oral presentation, titled “BDTX-1535 – A MasterKey EGFR Inhibitor Targeting Classical, Non-Classical and the C797S Resistance Mutation to Address the Evolved Landscape of EGFR Mutant NSCLC,” evaluated more than 235,000 sequenced cases of NSCLC sourced from Guardant Health (GuardantINFORM™) and Foundation Medicine (FoundationInsights™). The analyses reveal a broad spectrum of non-classical mutations, as well as an increased prevalence of the acquired resistance mutation, C797S. Over 100 unique non-classical EGFR oncogenic driver mutations were identified in newly diagnosed patients with NSCLC, and these non-classical EGFR mutations were present in 20-30% of patients across all lines of treatment.
“The landscape of EGFR mutations in NSCLC continues to evolve, revealing classical and non-classical driver mutations,” said
“Novel targeted therapies are still needed to continue to improve clinical outcomes for patients with EGFR-mutant lung cancers,” added Xiuning Le, M.D., Ph.D., Associate Professor, Thoracic/Head and Neck Medical Oncology at
Preclinical data demonstrated that BDTX-1535 potently inhibits more than 50 clinically relevant, non-classical EGFR mutations (as well as the classical L858R and exon19-del mutations) while sparing wild-type EGFR. The compound also potently inhibits the drug resistance C797S mutation, which emerges following treatment with third-generation EGFR inhibitors, including osimertinib. Real-world data indicate non-classical EGFR mutations can be co-expressed with classical mutation L858R, a setting that has been characterized by shorter duration of response to osimertinib first-line therapy. Preclinical data show that BDTX-1535 potently inhibits these co-expressed non-classical mutations.
“BDTX-1535 was designed to address a broad spectrum of more than 50 non-classical oncogenic EGFR mutations, as well as the C797S resistance mutation,” said
Phase 1 proof-of-concept data demonstrating durable responses in recurrent NSCLC patients with both non-classical and acquired resistance C797S mutations were presented in
About BDTX-1535
BDTX-1535 is an oral, brain-penetrant MasterKey inhibitor of oncogenic epidermal growth factor receptor (EGFR) mutations in non-small cell lung cancer (NSCLC), including classical driver mutations, non-classical driver mutations, and the acquired resistance C797S mutation. BDTX-1535 is a fourth-generation tyrosine kinase inhibitor (TKI) that potently inhibits, based on preclinical data, more than 50 oncogenic EGFR mutations expressed across a diverse group of patients with NSCLC in multiple lines of therapy. Based on preclinical data, BDTX-1535 also inhibits EGFR extracellular domain mutations and alterations commonly expressed in glioblastoma (GBM) and avoids paradoxical activation observed with earlier generation reversible TKIs. A “window of opportunity” trial of BDTX-1535 in patients with GBM is ongoing (NCT06072586) and a Phase 2 trial is ongoing in patients with NSCLC (NCT05256290).
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Forward-Looking Statements
Statements contained in this press release regarding matters that are not historical facts are “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995. Because such statements are subject to risks and uncertainties, actual results may differ materially from those expressed or implied by such forward-looking statements. Such statements include, but are not limited to, statements regarding: the potential of BDTX-1535 to address a broader range of mutations compared to existing therapies, the position of BDTX-1535 as compared to other fourth-generation EGFR inhibitors, the timing of clinical updates for BDTX-1535 in patients with NSCLC and in patients with recurrent GBM, and the potential of BDTX-1535 to benefit patients with NSCLC. Any forward-looking statements in this statement are based on management’s current expectations of future events and are subject to a number of risks and uncertainties that could cause actual results to differ materially and adversely from those set forth in or implied by such forward-looking statements. Risks that contribute to the uncertain nature of the forward-looking statements include those risks and uncertainties set forth in its Annual Report on Form 10-K for the year ended
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