BBOT Announces First Patient Dosed with BBO-11818, a PanKRAS Dual Inhibitor, in the Phase 1 KONQUER-101 Trial for Advanced Solid Tumors

• The first patient has been dosed with BBO-11818 in the KONQUER-101 first-in-human clinical study
• BBO-11818 is an orally bioavailable small molecule panKRAS dual (“ON” and “OFF” states) inhibitor that directly binds to KRAS with picomolar affinity
• BBO-11818 is expected to provide significant benefit to patients with tumors driven by these oncogenes by safely achieving optimal target inhibition

Excerpt from the Press Release:

SOUTH SAN FRANCISCO, Calif.–(BUSINESS WIRE)–TheRas, Inc. d/b/a BridgeBio Oncology Therapeutics (“BBOT” or the “Company”), a clinical-stage biopharmaceutical company focused on RAS-pathway malignancies, today announced that the first patient has been dosed with BBO-11818 in the Phase 1 KONQUER-101 trial for advanced solid tumors. BBO-11818 is an orally bioavailable small molecule dual inhibitor that directly binds to both the “ON” and “OFF” states of KRAS. KONQUER-101 will enroll patients globally with certain KRAS mutations.

“The dosing of the first patient is a major milestone in assessing BBO-11818’s potential benefit for patients with tumors driven by mutant KRAS,” said Dr. Ignacio Garrido-Laguna, MD, PhD, Principal Investigator at Huntsman Cancer Institute at the University of Utah. “We are committed to bringing cutting-edge therapies to patients with advanced cancer in the Mountain Region. BBO-11818 has the potential to safely achieve optimal target inhibition and combine with other targeted therapies. We look forward to evaluating it in the KONQUER-101 trial.”

BBO-11818 was designed to non-covalently bind both the inactive GDP-bound “OFF” and active GTP-bound “ON” forms of KRAS^G12D and KRAS^G12V. In cellular assays, EC₅₀ values for pERK inhibition in selected KRAS G12D and G12V-mutant cell lines range from sub-nanomolar to single-digit nanomolar potency. BBO-11818 is similarly effective in reducing cell viability in KRAS^G12D, KRAS^G12V, and KRAS^G12C-mutant cell lines. Further, NRAS and BRAF mutant cell lines show insensitivity to BBO-11818, and the molecule exhibits more than 500-fold selectivity for KRAS over H- and NRAS.

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