BH-30643 / BlossomHill Therap - LARVOL DELTA

Anti-tumor activity of BH-30643, a novel macrocyclic kinase inhibitor, in EGFR-mutant lung cancer models. (ASCO 2025) - P1/2 | "BH-30643 was administered twice daily via oral gavage; osimertinib when used as a comparator was dosed daily. These preclinical studies demonstrate broad activity of BH-30643 against classical and atypical EGFR activating mutations, EGFR ex20ins, as well as acquired resistance EGFR mutations. Such an "OMNI-EGFR" inhibitor may be able to overcome some of the limitations of earlier agents. Supported by favorable ADME and preclinical safety profiles, BH-30643 is now being assessed in a first-in-human study in locally advanced or metastatic NSCLC harboring EGFR and/or HER2 mutations (NCT06706076, SOLARA)."

Preclinical • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • EGFR • HER-2 • ROS1

A phase 1/2 open-label, multicenter, first-in-human study of the safety, tolerability, pharmacokinetics, and antitumor activity of BH-30643 in adult subjects with locally advanced or metastatic NSCLC harboring EGFR and/or HER2 mutations (SOLARA). (ASCO 2025) - P1/2 | "Plasma is collected for circulating tumor DNA (ctDNA) analysis at baseline and on treatment. Enrollment is underway, with planned enrollment across ~35 sites in multiple continents."

Clinical • Metastases • P1/2 data • PK/PD data • Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • EGFR • HER-2 • ROS1

Design and discovery of BH-30643: A novel, reversible, mutant-selective macrocyclic EGFR inhibitor invulnerable to common resistance mutations (AACR 2025) - "First-generation (1G) (e.g. gefitinib) and second-generation (2G) (e.g. afatinib) EGFR TKIs share an anilinoquinazoline scaffold which is vulnerable to T790M gatekeeper resistance. Third-generation (3G) (e.g. osimertinib) EGFR TKIs employ a less potent pyrimidine scaffold and obtain good potency including T790M through introduction of an irreversible binding at C797...The unique profile of BH-30643 offers a promising strategy to target a range of classical and non-classical EGFR activating mutations without vulnerability to common on-target resistance mutations. Such an "OMNI-EGFRTM" inhibitor may represent a new generation of EGFR TKIs with potential to overcome some of the limitations of earlier agents."

Lung Cancer • Non Small Cell Lung Cancer • Oncology • Solid Tumor • ALK • HER-2 • ROS1

BlossomHill Therapeutics to Present the Design and Discovery of BH-30643, the Company’s OMNI-EGFR Inhibitor, at the 2025 AACR Annual Meeting (Businesswire) - "BlossomHill Therapeutics, Inc...announced that an abstract describing the design and discovery of the company’s novel, macrocyclic, reversible, mutant-selective OMNI-EGFR inhibitor, BH-30643, was accepted for a poster presentation at the upcoming American Association for Cancer Research (AACR) Annual Meeting in Chicago, IL on April 29, 2025."

Clinical • Non Small Cell Lung Cancer

BlossomHill Therapeutics Doses Patients in the First Cohort of the Phase 1/2 SOLARA Clinical Trial of BH-30643 for EGFR- and HER2-Mutated Non-Small Cell Lung Cancer (Businesswire) - "BlossomHill Therapeutics...announced the first cohort of patients has been dosed in the SOLARA study (NCT06706076). SOLARA is a global, open label, dose escalation and expansion Phase 1/2 clinical trial assessing the safety, efficacy and tolerability of BH-30643 for locally advanced or metastatic non-small cell lung cancer (NSCLC) bearing EGFR or HER2 mutations."

Trial status • Non Small Cell Lung Cancer