On March 17, 2026 BlossomHill Therapeutics, Inc., a privately-held, clinical-stage biopharmaceutical company focused on the design and development of next-generation medicines for cancer, reported it will introduce its next-generation KRAS pipeline at the American Association for Cancer Research (AACR) (Free AACR Whitepaper) Annual Meeting 2026. These two non-covalent pan-KRAS inhibitors leverage a differentiated chemical scaffold to address limitations of contemporary molecules – achieving sub-nanomolar potency and a prolonged off-rate, combined with oral bioavailability. In addition, the company will present new preclinical data supporting the continued advancement of its clinical programs BH-30643, a first-in-class, mutant-selective, macrocyclic OMNI-EGFRTM inhibitor, and BH-30236, an oral CLK inhibitor for hematologic malignancies. The AACR (Free AACR Whitepaper) Annual Meeting 2026 will be held April 17-22, 2026, in San Diego.

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"We are excited to share new data from across our pipeline at AACR (Free AACR Whitepaper), including new preclinical data supporting the continued advancement of our lead clinical programs BH-30643 and BH-30236, and the introduction of our novel switch II-targeting KRAS programs, one of which will be highlighted during a minisymposium," said Jean Cui, Ph.D., Founder and Chief Executive Officer of BlossomHill Therapeutics. "KRAS remains one of the most important and historically difficult targets in oncology. Our next-generation pan-KRAS inhibitors are intentionally designed using a differentiated chemical scaffold to deliver pseudo-irreversible target engagement and improved drug-like properties we believe will translate to clinical impact. We look forward to engaging with the scientific community at the upcoming AACR (Free AACR Whitepaper) meeting."

Details of the presentations are as follows:

Title: Discovery and characterization of BH-501284: A non-covalent, pan-KRAS inhibitor for treatment of diverse KRAS-mutant tumors (#6736)
Date & Time: April 21, 2026; 2:30-4:30 p.m. PT
Session Title: Targeted Therapies
Session Type: Minisymposium
Location: San Diego Convention Center
Key Findings: BH-501284 is a potent, selective, orally available non-covalent pan-KRAS inhibitor that demonstrates picomolar binding affinity, broad activity across KRAS mutations, and durable tumor regression in non-small cell lung cancer (NSCLC), colorectal cancer (CRC) and pancreatic ductal adenocarcinoma (PDAC models). By preferentially targeting inactive KRAS and maintaining activity under growth factor-driven resistance conditions, BH-501284 may overcome key limitations of existing KRAS inhibitors.

Title: Design and discovery of BH-501242, a novel pan-KRAS on/off inhibitor targeting KRAS switch II pocket (#5120)
Date & Time: April 21, 2026; 9:00 a.m.-12:00 p.m. PT
Session Title: New Ligands and Inhibitors
Location: San Diego Convention Center, Poster Section 38
Key Findings: Preclinical data demonstrate that BH-501242, a novel pan-KRAS inhibitor targeting the switch II pocket, potently inhibits a broad range of KRAS mutations, including G12D, G12V, and G12C, with sub-nanomolar cellular activity and robust tumor regression in multiple xenograft models. Its ability to bind both active and inactive KRAS and achieve strong oral exposure supports further development as a differentiated, mutation-agnostic KRAS therapy.

Title: CLK inhibitor BH-30236 synergizes with venetoclax in anti-leukemia activity via splicing modulation in preclinical AML and CLL models (#5872)
Date & Time: April 21, 2026; 2:00-5:00 p.m. PT
Session Title: Tyrosine Kinase, Phosphatase, and Other Inhibitors
Location: San Diego Convention Center, Poster Section 18
Key Findings: BH-30236, a novel oral CLK1/2/4 inhibitor, modulates alternative splicing to induce apoptosis and suppress leukemia stem cell–associated pathways, demonstrating robust anti-leukemia activity in acute myeloid leukemia (AML) and chronic lymphocytic leukemia (CLL) models. In combination with venetoclax, BH-30236 produced synergistic tumor regression, including durable, complete responses in resistant xenograft models.

Title: BH-30643, a novel macrocyclic non-covalent, mutant-selective EGFR inhibitor, addresses the resistance and potency limitations of contemporary EGFR TKIs (#5877)
Date & Time: April 21, 2026; 2:00-5:00 p.m. PT
Session Title: Tyrosine Kinase, Phosphatase, and Other Inhibitors
Location: San Diego Convention Center, Poster Section 18
Key Findings: BH-30643 is a macrocyclic, non-covalent, mutant-selective OMNI-EGFR inhibitor that uniquely overcomes T790M and C797S resistance mutations while maintaining potent activity against classical EGFR drivers and sparing wildtype EGFR. In preclinical studies, BH-30643 demonstrated prolonged suppression of tumor cell proliferation compared to osimertinib, including under growth factor-mediated resistance conditions.

(Press release, BlossomHill Therapeutics, MAR 17, 2026, View Source [SID1234663669])