Omvitrastat

Omvitrastat (OP-3136) is an orally active, highly selective inhibitor of KAT6A and KAT6B. Omvitrastat inhibits the proliferation of prostate cancer, ovarian cancer and non-small cell lung cancer cells that express or overexpress KAT6A. Omvitrastat reduces the proliferative capacity of cancer cells and suppresses cell growth in ER + breast cancer cell models with KAT6 overexpression. Omvitrastat induces tumor regression and inhibits tumor growth in an ovarian cancer xenograft model in immunodeficient mice. Omvitrastat inhibits tumor growth in a non-small cell lung cancer xenograft model in immunodeficient mice. Omvitrastat can be used in research related to HR + /HER 2- breast cancer, prostate cancer, ovarian cancer and non-small cell lung cancer (NSCLC) ^{[1] [2]}.

In Vivo, Omvitrastat (OP-3136) (0.5-1 mg/kg; p.o.) monotherapy induces tumor regression in OVCAR3 ovarian cancer xenografts with TGIs of 104.5% and 105.4% at doses of 0.5 mg/kg and 1 mg/kg, respectively^[1]. Omvitrastat (1 mg/kg; p.o.) monotherapy inhibits tumor growth in LCLC-97TM1 NSCLC xenografts with a TGI of 62% at a dose of 1 mg/kg^[1].

In Vitro, Omvitrastat (OP-3136) inhibits proliferation of VCAP, OAW28, OVCAR3, and LCLC-97TM1 cell lines^[1]. Omvitrastat reduces the proliferation of breast cancer cell lines and inhibits growth in KAT6-overexpressing ER+ breast cancer cell models^[2].

References:
[1]. Gopinath S. Palanisamy, et al. Abstract LB166: OP-3136, a selective KAT6 inhibitor, demonstrates anti-tumor activity in prostate, ovarian, and non-small cell lung cancer preclinical models. Cancer Res (2025) 85 (8_Supplement_2): LB166.
[2]. Roussel-Simonin C, et al. Exploring KAT6 as a therapeutic target in breast cancer: epigenetic approaches for precision medicine. NPJ Breast Cancer. 2025 Dec 19;11(1):146.