BBOT Presents Preclinical Data Showing RAS:PI3Kα Breaker BBO-10203 Inhibits PI3Kα/AKT Signaling in HER2AMP Models at the AACR Annual Meeting 2026

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BBO-10203 physically and allosterically disrupts the interaction between RAS and PI3Kα, leading to signaling inhibition without inhibiting the kinase activity of PI3Kα and with no observed hyperglycemia BBO-10203 displays strong in vivo combination effects with HER2 inhibitors tucatinib or trastuzumab in HER2AMP models Updated clinical data are expected in the second half of 2026 SOUTH SAN FRANCISCO, Calif., April 21, 2026 (GLOBE NEWSWIRE) -- BridgeBio Oncology Therapeutics, Inc. (“BBOT”) (Nasdaq: BBOT), a clinical-stage biopharmaceutical company focused on RAS-pathway malignancies, today presented new preclinical data in an oral presentation for BBO-10203, a first-in-class covalent small molecule RAS:PI3Kα breaker that selectively blocks the physical interaction between RAS and PI3Kα resulting in the inhibition of RAS-driven PI3Kα-AKT signaling in tumors with no observed hyperglycemia. The data were presented at the American Association for Cancer Research (AACR) Annual Meeting 2026. "The interaction between RAS and PI3Kα plays a critical role in malignant cells,” said Pedro J. Beltran, PhD, Chief Scientific Officer of BBOT. “BBO-10203 physically disrupts the interaction between RAS and PI3Kα, leading to signaling inhibition and tumor regressions. Importantly, unlike competing approaches, no hyperglycemia has been observed to date. In addition, BBO-10203’s ability to block RAS-mediated activation of PI3Kα is independent of the mutational status of either RAS or PI3Kα, which may enable treatment of a broader patient population. These data suggest that non-canonical RAS proteins play a key role in PI3Kα activation in HER2AMP cell lines. Furthermore, BBO-10203 demonstrates strong in vivo combination activity with HER2-targeted therapies, including tucatinib and trastuzumab, in HER2 AMP models.” Highlights from the oral presentation include: The oral presentation is titled “The RAS:PI3Kα breaker BBO-10203 inhibits PI3Kα/AKT activity in HER2AMP models through non-canonical RAS signaling blockade.” A copy of the presentation will be available on the “Publications” page of the BBOT website following the conference. About BBO-10203BBO-10203 is an orally bioavailable small molecule with a novel mechanism of action designed to inhibit the physical interaction between RAS and PI3Kα, inhibiting RAS-driven PI3Kα-AKT signaling in tum...

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