BDTX-1535 Goes after Osimertinib Resistance

    Cancer Discovery
    |October 27, 2021
    PubMed

    Insights

    The investigational drug BDTX-1535 shows promise in overcoming resistance to osimertinib for EGFR-mutant non-small cell lung cancer. This tyrosine kinase inhibitor also demonstrated preclinical effectiveness in treating brain tumors like glioblastoma.

    Area of Science:

    • Oncology
    • Pharmacology
    • Neuro-oncology

    Background:

    • Osimertinib is a standard treatment for EGFR-mutant non-small cell lung cancer (NSCLC).
    • Resistance to osimertinib remains a significant clinical challenge in NSCLC treatment.
    • Glioblastoma (GBM) is an aggressive primary brain tumor with limited treatment options.

    Purpose of the Study:

    • To evaluate the potential of BDTX-1535, an investigational tyrosine kinase inhibitor, in overcoming osimertinib resistance in EGFR-mutant NSCLC.
    • To assess the preclinical efficacy of BDTX-1535 in treating central nervous system (CNS) metastases, specifically in glioblastoma models.

    Main Methods:

    • Preclinical studies were conducted to assess the activity of BDTX-1535.
    • The in vitro and in vivo models included EGFR-mutant NSCLC cell lines with acquired resistance to osimertinib.
    • Glioblastoma models were utilized to evaluate CNS efficacy.

    Main Results:

    • BDTX-1535 demonstrated the potential to mitigate or overcome resistance to osimertinib in preclinical models of EGFR-mutant NSCLC.
    • The investigational agent showed preclinical efficacy in glioblastoma models, suggesting potential for treating CNS metastases.

    Conclusions:

    • BDTX-1535 represents a potential therapeutic strategy for patients with EGFR-mutant NSCLC who develop resistance to osimertinib.
    • The drug's efficacy in preclinical brain tumor models warrants further investigation for CNS-targeted therapy in lung cancer patients with brain metastases.