Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies[2].IC50 & Target:Progesterone receptor.In Vitro:Nomegestrol acetate (0.3, 1, 3, 10, 30, 100 μM; 24, 48, 72 h) shows anti-proliferative activity against RL95-2 cells in a dose-dependent manner.
Nomegestrol acetate (4, 20, 100 μM; 6, 24, 48 h) upregulates protein levels of SUFU and Wnt7a in RL95-2 cells.In Vivo:Nomegestrol acetate (50, 100, 200 mg/kg; p.o.; single daily for 28 days) inhibits growth of RL95-2 xenograft tumors in vivo.
Nomegestrol acetate (100, 200 mg/kg; p.o.; single daily for 28 days) surpresses the expression of SUFU and Wnt7a in tumor tissues.
Nomegestrol acetate (1, 2.5 mg/rat; p.o.; single daily for 4 days) inhibits ovulation in rats[2].