LY4045004 / Eli Lilly - LARVOL DELTA

Preclinical characterization of LY4045004, a next-generation, mutant-selective PI3Kα inhibitor (SABCS 2024) - "In vivo, orally administered LY4045004 demonstrated dose-dependent tumor regressions in PI3Kα H1047R-driven and E545K-driven breast cancer models both as monotherapy and in combination with fulvestrant without inducing hyperglycemia (no significant increase in insulin or C-peptide) or body weight change. The favorable potency, selectivity, and PK properties of LY4045004 are predicted to result in efficacy with improved tolerability in patients with prevalent PI3Kα helical- and kinase-domain mutant HR+ breast cancers. Global regulatory submissions are planned in the first half of 2025."

Preclinical • Breast Cancer • Hormone Receptor Breast Cancer • PIK3CA

Lilly to Present…Additional Results from Its Breast Cancer Portfolio at the San Antonio Breast Cancer Symposium (PRNewswire) - "Additional presentations from investigational mutant selective PI3Ka inhibitor assets include preclinical characterization data for LY4045004, which is expected to enter the clinic in the first half of 2025, and Phase 1a/b clinical data for a predecessor molecule, LOXO-783, which informed the development of LY4045004."

New trial • P1 data • Preclinical • Breast Cancer