Osilodrostat

928134-65-0

C13H10FN3

DMSO : >= 83.3 mg/mL (366.57 mM)

Metabolic Enzyme/Protease

Osilodrostat (LCI699) is a potent inhibitor of human 11beta-hydroxylase and aldosterone synthase with IC₅₀ values of 2.5 and 0.7 nM, respectively. IC50 & Target: IC50: 2.5 nM (human 11beta-hydroxylase), 0.7 nM (aldosterone synthase)^[1] In Vivo: Osilodrostat and pasireotide monotherapies are associated with significant changes in the histology and mean weights of the pituitary and adrenal glands, liver, and ovary/oviduct. Osilodrostat alone is associated with adrenocortical hypertrophy and hepatocellular hypertrophy. In combination, osilodrostat/pasireotide does not exacerbate any target organ changes and ameliorated the liver and adrenal gland changes observed with monotherapy. C_max and AUC_0–24h of osilodrostat and pasireotide increase in an approximately dose-proportional manner^[1]. Osilodrostat treatment reduces urinary free cortisol in patients with Cushing's disease; 78.9% has normal urinary free cortisol at week 22. Treatment with osilodrostat is generally well tolerated^[2].