Building on recent preclinical findings, this study introduces BBO-10203, a first-in-class, orally bioavailable small-molecule inhibitor targeting the RAS-PI3Kα interaction.

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Combined inhibition of R/RRAS2 plus RMC-6236 leads to pAKT suppression equivalent to BBO-10203, suggesting important contribution from canonical and non-canonical RAS signaling

BBO-10203, a first-in-class breaker of the PI3Kα:RAS interaction, demonstrates in vitro and in vivo efficacy alone or in combination with standard-of-care therapies in solid tumor models

First in human study to evaluate the safety, tolerability, and pharmacokinetics (PK) of BBO-10203, a PI3Kα:RAS breaker, alone and in combination with other anti-cancer agents in patients with advanced solid tumors.

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.

The compound gained momentum in 2026 when Merck acquired Terns, adding the FDA Orphan Drug- and Breakthrough Therapy-designated asset to its hematology pipeline.

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This presentation is the intellectual property of Pedro J. Beltran. Contact them at Pedro.Beltran@bridgebio.com for permission to reprint and/or distribute.

BBO-10203, an orally bioavailable small molecule that disrupts the RAS:PI3Kα interaction leading to pAKT and tumor growth inhibition in models of breast, lung and colorectal cancer