On January 11, 2022 Black Diamond Therapeutics, Inc. (Nasdaq: BDTX), a precision oncology medicine company pioneering the discovery and development of MasterKey therapies, reported that the U.S. Food and Drug Administration (FDA) has cleared an investigational new drug (IND) application for its MasterKey inhibitor BDTX-1535, an irreversible, mutant selective, brain-penetrant inhibitor of oncogenic mutations of epidermal growth factor receptor (EGFR) expressed in glioblastoma multiforme (GBM) and intrinsic and acquired resistance EGFR mutations in non-small cell lung cancer (NSCLC) (Press release, Black Diamond Therapeutics, JAN 11, 2022, View Source [SID1234598586]). The Company expects to initiate the Phase 1 study of BDTX-1535 in the first quarter of 2022 and expects to provide a clinical update in the second half of 2023.

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"We are incredibly pleased to announce the FDA allowance of our IND, representing a significant milestone for Black Diamond as we continue to mature our pipeline of MasterKey therapies," said David Epstein, Ph.D., President and Chief Executive Officer of Black Diamond Therapeutics. "Based on the unique approach of our MAP discovery engine platform, we believe that BDTX-1535 is well positioned to address the unmet needs of EGFR mutant GBM and NSCLC with robust brain penetration to ensure adequate CNS exposure and potent and selective inhibition of EGFR mutations that drive intrinsic and acquired resistance to current generation tyrosine kinase inhibitors, coupled with favorable drug-like properties seen in preclinical models. We look forward to the upcoming initiation of the Phase 1 Study in the first quarter of 2022."

In pre-clinical studies, Black Diamond has demonstrated that oncogenic alterations of EGFR, particularly those associated with GBM, result in distinct conformations which impart unique pharmacology and drug resistance. In cell-based assays, BDTX-1535 achieved potent and selective inhibition of a range of EGFR mutations expressed in GBM and NSCLC, including canonical, non-canonical, and drug-resistance mutations, such as EGFR-C797S that can arise following treatment with third generation EGFR inhibitor. BDTX-1535 demonstrated a favorable brain-penetrant pharmacokinetic (PK) profile in animal models. In a range of tumor models, including intracranial GBM models and lung cancer drug resistance models expressing the targeted EGFR mutations, BDTX-1535 showed dose-dependent tumor growth inhibition and achieved complete regression without impact on body weight.

About BDTX-1535

BDTX-1535 is designed as an irreversible, mutant selective, brain-penetrant MasterKey inhibitor of oncogenic mutations of epidermal growth factor receptor (EGFR) expressed in glioblastoma multiforme (GBM) and intrinsic and acquired resistance EGFR mutations in non-small cell lung cancer (NSCLC). In pre-clinical studies, Black Diamond has demonstrated that oncogenic alterations of EGFR, particularly those associated with GBM, result in distinct conformations which impart unique pharmacology and drug resistance. It is estimated that approximately 50% of GBM patients harbor an oncogenic EGFR alteration that has the potential to be addressed by BDTX-1535, representing a potential patient population of greater than 60,000 patients annually across the US, EU, Japan and China. It is estimated that across the US, EU, Japan and China there are approximately 20,000 patients who are diagnosed annually with non-small cell lung cancer (NSCLC) harboring an EGFR intrinsic or acquired resistance mutation.