FT-6876 / Novo Nordisk - LARVOL DELTA

Targeting resistance mechanisms to AR-targeted therapy in prostate cancer through inhibition of CREBBP/EP300 (AACR 2024) - "Differential changes in protein abundance and protein acetylation between enzalutamide sensitive and resistant cell lines identified changes in fatty acid metabolism as a common, downstream event in response to treatment with FT-6876, suggesting an additional mechanism for response to FT-6876.Together, our integrated theoretical and experimental analyses support the hypothesis that targeting CREBBP/EP300 may provide therapeutic benefits to prostate cancer patients. Further, the subnetworks identified may serve as mechanistically-informed biomarkers for identifying patients who may benefit from inhibition of CREBBP/EP300."

Genito-urinary Cancer • Oncology • Prostate Cancer • Solid Tumor • CREBBP • EP300

FT-6876, a Potent and Selective Inhibitor of CBP/p300, is Active in Preclinical Models of Androgen Receptor-Positive Breast Cancer. (PubMed, Target Oncol) - "Our findings demonstrate FT-6876 as a promising new CBP/p300 bromodomain inhibitor, with efficacy in preclinical models of AR+ breast cancer."

Journal • Preclinical • Breast Cancer • Genito-urinary Cancer • Hormone Receptor Breast Cancer • Oncology • Prostate Cancer • Solid Tumor • Triple Negative Breast Cancer • AR • ER

[VIRTUAL] FT-6876, a potent and selective inhibitor of CBP/p300 with antitumor activity in AR-positive breast cancer (AACR-II 2020) - "This was associated with a reduction in H3K27Ac, AR and ER target gene modulation, and reduction in Ki67. FT-6876 is a promising new CBP/p300 bromodomain inhibitor demonstrating efficacy in preclinical models of AR+ breast cancer."

IO Biomarker • Breast Cancer • Hormone Receptor Breast Cancer • Hormone Receptor Positive Breast Cancer • Oncology • Solid Tumor • Triple Negative Breast Cancer • AR • ER