BAY 1001931

BAY 1001931 is a highly selective and potent allosteric inhibitor of AKT1 and AKT2, developed by Bayer. It targets the PI3K/AKT/mTOR pathway, a central regulator of tumor growth, proliferation, and survival that is frequently deregulated in various cancers. Mechanistically, BAY 1001931 prevents the activation of AKT by inhibiting its phosphorylation at both Thr308 and Ser473. Preclinical studies have demonstrated significant anti-proliferative activity in tumor models characterized by PIK3CA mutations or PTEN deletions, including luminal and HER2-positive breast cancer and androgen-sensitive prostate cancer. Furthermore, BAY 1001931 has shown synergistic anti-tumor efficacy when combined with anti-hormonal therapeutics such as tamoxifen, bicalutamide, or abiraterone acetate.