CAMBRIDGE, Mass. And NEW YORK, October 8, 2021 (GLOBE NEWSWIRE) – Black Diamond Therapeutics, Inc. (Nasdaq: BDTX), a precision oncology medicine company pioneering the discovery and development of MasterKey therapies, announced today hui presenting preclinical data for three early stage pipeline programs in oral and poster sessions at the AACR-NCI-EORTC International Virtual Conference on Molecular Targets and Cancer Therapeutics.
“Despite clinical advances in precision medicines for patients with non-small cell lung cancer (NSCLC) carrying an epidermal growth factor receptor (EGFR) mutation, several areas of unmet need persist. , especially patients whose tumors have developed resistance to current generation therapies. , express non-canonical (or rare) mutations and have metastasized into the brain, ”said Elizabeth Buck, Ph.D., Scientific Director of Black Diamond Therapeutics. “BDTX-1535 has demonstrated broad coverage of oncogenic EGFR mutations expressed in NSCLC, which, together with a pharmacokinetic (PK) profile of brain penetration, supports the potential of BDTX-1535 as an optimal therapeutic candidate for these NSCLC patient populations. “
Dr. Buck continued, “In addition, B-Raf (BRAF) and fibroblast growth factor receptor (FGFR) are validated therapeutic targets, but current standards of care are associated with significant limitations, which results in persistent unmet needs for these cancer patients. Compounds in our BRAF program are designed to selectively target a full spectrum of BRAF class II / III oncogenic mutations without inducing paradoxical activation, which can lead to secondary malignancies. Our FGFR compounds are designed to target a full spectrum of oncogenic FGFR2 and FGFR3 mutations, including known resistance mutations, while sparing FGFR1, whose inhibition is associated with toxicities including hyperphosphatemia.
The presentations describe the following data:
BDTX-1535 Program: The presentation describes the preclinical data of BDTX-1535, which is designed as a potent, selective and brain-penetrating inhibitor of a spectrum of EGFR mutations expressed in glioblastoma multiforme (GBM) and NSCLC.
In cellular tests, BDTX-1535 demonstrated potent and selective inhibition of EGFR mutations expressed in NSCLC, including the EGFR-C797S mutation that can occur after treatment with osimertinib. BDTX-1535 demonstrated a favorable brain penetration PK profile in mice, rats, and canine models. In an EGFR Exon19 + C797S mouse allograft efficacy model, BDTX-1535 showed dose-dependent tumor growth inhibition and achieved complete regression without noticeable impact on body weight. Black Diamond plans to file an Investigational New Drug (IND) application for BDTX-1535 in the first half of 2022.
BRAF Program: The presentation describes preclinical data for a flagship compound in Black Diamond’s BRAF Program, which is designed for potency and selectivity against a spectrum of non-canonical Class II / III (non-V600) mutations, as well as for avoid the induction of paradoxical activation.
In cellular assays, the lead compound demonstrated potent inhibition of a spectrum of BRAF class II / III mutations. with the Black Diamond compound did not result in an increase in endoplasmic reticulum RNA-like kinase protein kinase (pERK), a paradoxical activation signal. pERK and anti-tumor efficacy. Black Diamond anticipates an IND filing in 2022.
FGFR Program: The presentation illustrates the Black Diamond approach, which focuses on a four-pronged optimization strategy designed to provide an inhibitor with broad coverage of the FGFR2 and FGFR3 oncogenes, while sparing the inhibition of FGFR1 and retaining activity against resistance mutations.
In cellular assays, compounds of the FGFR program demonstrated potent and selective inhibition of a spectrum of oncogenic FGFR2 / 3 mutations, while sparing FGFR1. Additionally, in cellular assays, compounds from the FGFR program have demonstrated enhanced potency against resistance mutations. study conducted in a UM-UC-14 mouse model (FGFR3-S249C), the compounds of the FGFR program demonstrated anti-tumor activity. In addition, in mouse and rat models, compounds of the FGFR program did not promote hyperphosphatemia. Black Diamond expects an IND filing in 2022.
“Our BDTX-1535, BRAF and FGFR programs exemplify Black Diamond’s MasterKey approach to drug discovery where we are able to harness the power of our proprietary MAP drug discovery engine to design spectrum candidates. selectively designed to overcome the limitations of current therapies in each target area, ”said David M. Epstein, Ph.D., President and CEO of Black Diamond Therapeutics. “These programs underscore the productivity of our MAP engine, and we look forward to providing updates across our entire pipeline as we move towards our goal of providing product candidates that can expand the reach of medicine from. precision and, in turn, address areas of genuine unmet need. . “
Presentations from the AACR-NCI-EORTC meeting are available in the “Scientific Presentations and Publications” section of the Black Diamond Therapeutics website.
About Black Diamond Therapeutics, Inc. Black Diamond Therapeutics is a precision cancer medicine company pioneering the discovery of MasterKey therapies. Black Diamond targets non-drug mutations in patients with genetically defined cancers. Black Diamond is built on a deep understanding of cancer genetics, protein structure and function, and medicinal chemistry. The Company’s proprietary technology platform and drug discovery engine, the Mutation-Allostery-Pharmacology (MAP) platform, is designed to enable Black Diamond to analyze population-level genetic sequencing data to identify oncogenic mutations that promote cancer across tumor types, group these mutations into families, and develop a single small molecule therapy that targets a specific family of mutations, called MasterKey therapy. Black Diamond was founded by David M. Epstein, Ph.D., and Elizabeth Buck, Ph.D. For more information, please visit www.blackdiamondtherapeutics.com.
Forward-Looking Statements Statements 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. Since such statements are subject to risks and uncertainties , actual results may differ materially from those expressed or implied by these forward-looking statements. These statements include, without limitation, statements regarding the continued development and advancement of BDTX-1535 in studies enabling IND, including expectations for filing an IND, and the development of BRAF programs. and FRGR, including the schedule for filing INDs in each program. All forward-looking statements contained in this statement are based on management’s current expectations regarding future events and are subject to a number of risks and uncertainties that could cause actual results to differ materially and adversely from those stated. or implied by these forward-looking statements. . Risks that contribute to the uncertain nature of forward-looking statements include: the success, cost and timing of the Company’s product candidate development activities and planned studies and clinical trials enabling the IND, the Company’s ability to execute its strategy, regulatory developments in the United States, the Company’s ability to finance its operations and the impact that the current COVID-19 pandemic will have on the Company’s clinical trials and preclinical studies, the supply chain and the transactions, as well as the risks and uncertainties set out in its Annual Report on Form 10-K for the year ended December 31, 2020, filed with the United States Securities and Exchange Commission and in its other documents filed with the the United States Securities and Exchange Commission. All forward-looking statements contained in this press release speak only as of the date on which they were made. The Company assumes no obligation to update these statements to reflect events that occur or circumstances that exist after the date on which they were made.
Contacts: For investors: Natalie Wildenradt [email protected]
For the media: Kathy Vincent (310) 403-8951 [email protected]