BridgeBio Oncology Therapeutics Inc. has announced new preclinical data for BBO-10203, a first-in-class, orally bioavailable selective inhibitor that blocks the interaction between RAS and PI3Kα. The data, presented at the 2025 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics, demonstrate that BBO-10203 inhibits RAS-driven PI3Kα-AKT signaling in tumor cells without affecting glucose metabolism. The compound showed robust tumor growth inhibition as a monotherapy and in combination with BBOT's KRASG12C ON/OFF inhibitor, BBO-8520, and the panKRAS inhibitor, BBO-11818, in KRAS-mutant models at well-tolerated dose levels. BBO-10203 is currently being evaluated in the Phase 1 BREAKER-101 trial for patients with HER2+ amplified or HR+/HER2- breast cancer, as well as KRAS mutant colorectal or non-small cell lung cancer, with initial Phase 1 clinical data expected in the first half of 2026.