Description
ORIC-101 is a highly potent and selective glucocorticoid receptor antagonist, with an EC 50 of 5.6 nM. Anti-cancer activity.In VitroORIC-101 shows markedly reduced androgen receptor agonism (EC 50, 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC 50, >10 µM). ORIC-101 (1-1000 nM) dose-dependently reduces the expression of n GR-mediated target gene (FKBP5 and GILZ), with IC 50 s of 17.2 and 21.2 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoORIC-101 (75 mg/kg, P.O. twice a day for 16-22 days) enhances the anti-tumor activity in combination with gemcitabine and carboplatin in OVCAR5 xenograft tumor in cortisol-treated mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: OVCAR5 xenograft tumor in cortisol-treated mice Dosage: 75 mg/kg with 100 mg/kg gemcitabine and 60 mg/kg carboplatin Administration: P.O. twice a day for 16-22 days Result: Significantly reduced tumor volume in combination with chemotherapeutic agents.Form:SolidIC50& Target:EC50: 5.6 nM (Glucocorticoid receptor)