BridgeBio Oncology Therapeutics Inc. (BBOT), a clinical-stage biopharmaceutical company, on Tuesday presented preclinical data evaluating BBO-10203 in blocking interactions between RAS an PI3Ka in tumors at the 2026 annual meeting of the American Association of Cancer Research (AACR).
BBO-10203 is an orally bioavailable small molecule drug, developed to inhibit RAS-driven PI3Ka-AKT signaling in tumors without the risk of hyperglycemia by blocking physical interactions between RAS and PI3Ka. The protein-protein inhibitor binds to the RAS-binding domain of PI3Ka, preventing its activation by the KRAS, HRAS, and NRAS oncogenes, thus reducing downstream signaling and tumor growth.
The company reported preclinical data that indicated that BBO-10203 can block interactions between RAS and PI3Ka without blocking the kinase activity of PI3Ka. The drug's action was consistent independent of mutations on RAS and PI3Ka, indicating a larger potential patient population.
Preclinical testing in HER2AMP breast cancer cell lines showed that PI3Ka activity was dependent on RAS. BBO-10203 induced tumor regression at 30 mg/kg QD, and no hyperglycemia was observed at 100 mg/kg QD. When tested in combination with HER2-targeted therapies tucatinib and trastuzumab, the drug showed strong activity in HER2AMP in vivo models.
BBO-10203 is currently in the Phase 1 BREAKER-101 trial for the treatment of HER2+ breast cancer, HR+/HER2 breast cancer, KRAS-mutant colorectal cancer, and KRAS-mutant non-small cell lung cancer (NSCLC).
BBOT closed Tuesday at $9.46, up 2.16%.
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