On September 26, 2019 Black Diamond Therapeutics, Inc., a precision oncology medicine company pioneering the discovery and development of small molecule, tumor-agnostic therapies, reported that preclinical data defining the molecular mechanism for oncogenic activation of families of epidermal growth factor receptor (EGFR) allosteric mutations and showing activity of the Company’s lead product candidate BDTX-189 will be presented at the European Society for Medical Oncology Congress 2019, taking place from September 27 to October 1, 2019 in Barcelona, Spain (Press release, Black Diamond Therapeutics, SEP 26, 2019, View Source [SID1234539814]).
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Black Diamond’s presentation, entitled "Oncogenic Mutations at the Dimer Interface of EGFR Lead to Formation of Covalent Homo-dimers and Allosteric Activation of the Kinase Domain: A Mechanism Which Alters the Selectivity Profile of Oncogenic EGFR," will be presented Saturday, September 28, 2019 at 12:00 CEST, as part of the Developmental Therapeutics data session (Presentation 501P).
Elizabeth Buck, Ph.D., Co-Founder and Executive Vice President, Discovery and Translational Sciences said, "Despite clinical success with targeting EGFR ATP-site mutants, there are currently no drugs approved by the FDA to target allosteric EGFR mutations with a single therapy, including for patients with glioblastoma or lung cancer that express these mutations. Utilizing our Mutation-Allostery-Pharmacology, or MAP, platform, we defined the molecular mechanism for oncogenic activation of families of EGFR allosteric mutations and revealed how this mechanism decreases the efficacy of current generation of small molecule ATP-site inhibitors ineffective against these mutations."
"These preclinical data illustrate how BDTX-189, a novel ATP-site small molecule, selectively inhibits the activity of a broad range of allosteric EGFR and HER2 mutants, producing growth regression of allosteric EGFR mutant patient-derived tumors in vivo," added Dr. Buck.
MAP platform
Black Diamond’s Mutation-Allostery-Pharmacology (MAP) platform is built on three central pillars – discover, reveal, and target. The Company uses population-level cancer genetic data obtained from all tumor types to identify potential families of mutations that occur within individual oncogenes and rank the mutations for potential oncogenicity. Black Diamond then uses its MAP platform to understand the mechanism for oncogenic activation and its team of experienced medicinal chemists then develops mutation spectrum-selective drugs for the identified targets. Black Diamond’s MAP platform has generated a pipeline of orally available, potent and selective small molecule kinase inhibitors that target a range of driver mutations in cancer.
About BDTX-189
BDTX-189 is designed to be an orally available, irreversible small molecule inhibitor that targets undrugged oncogenic driver mutations of the ErbB kinases in epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). These include extracellular domain allosteric mutations of HER2, as well as EGFR and HER2 domain exon 20 insertions, and additional activating oncogenic drivers of ErbB. The ErbB receptors are a group of receptor tyrosine kinases involved in key cellular functions, including cell growth and survival. Currently, there are no medicines approved by the U.S. Food and Drug Administration to target all of these oncogenic mutations with a single therapy. Black Diamond Therapeutics is completing investigational new drug (IND)-enabling activities for BDTX-189 and plans to start a combined Phase 1/2 clinical trial in the first half of 2020.