Edgewood Oncology Begins Phase 2a BTX-A51 Dosing in Genetically-Defined Breast Cancer

BROOKLINE, Mass.-- Edgewood Oncology, a clinical-stage biotechnology company, recently announced that the initial patients with metastatic breast cancer have been treated with BTX-A51. This treatment, a multi-specific kinase inhibitor, targets key cancer regulators: casein kinase 1 alpha (CK1α) and cyclin-dependent kinases 7 and 9 (CDK7 and CDK9). The drug is currently undergoing a Phase 2a clinical trial specifically aimed at estrogen receptor-positive/human epidermal growth factor receptor 2-negative (ER+/HER2-) metastatic breast cancer, both with and without GATA binding protein 3 (GATA3) mutations.

GATA3 is crucial in maintaining healthy breast cells. Mutations in this protein, present in about 15% of breast cancer cases, are linked to shorter progression-free survival (PFS) and overall survival (OS). Interestingly, these mutations are usually paired with a non-mutated p53 tumor suppressor protein. Recent research indicates that targeting MDM2, a molecule responsible for p53 degradation, could be particularly effective against cancers harboring GATA3 mutations. Edgewood Oncology hypothesizes that BTX-A51, due to its ability to reduce MDM2 expression, could be advantageous for this specific breast cancer subgroup.

"This milestone is significant for Edgewood Oncology and for patients with ER+/HER2- breast cancer, particularly those with GATA3 mutations who require better-targeted treatments," remarked Zung L. Thai, M.D., Ph.D., the chief medical officer of Edgewood Oncology. "While CDK4/6 inhibitors are central to current treatment regimes, resistance to these drugs is a significant challenge. By targeting CDK7 and CDK9, which are crucial for cell cycle progression, BTX-A51 aims to overcome this resistance and potentially transform the treatment paradigm."

The ongoing Phase 2a trial of BTX-A51 involves multiple centers, is open-label, nonrandomized, and assesses multiple doses. This study aims to evaluate the safety, toxicity, pharmacokinetics, and preliminary efficacy of BTX-A51 in patients with ER+/HER2- metastatic breast cancer with and without GATA3 mutations. Enrollment is currently open at multiple sites. 

Edgewood Oncology is committed to advancing BTX-A51, an investigational small molecule that acts as a multi-selective kinase inhibitor targeting CK1α, CDK7, and CDK9. This drug synergistically co-targets master regulators of cancer, promoting programmed cell death, or apoptosis. Currently, BTX-A51 shows promise in treating acute myeloid leukemia and genetically defined solid tumors, which are the primary focus of ongoing clinical programs.

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