928134-65-0 | Osilodrostat

Chemical type

• Steroidogenesis inhibitor (small-molecule drug)

^[1]

• Steroidogenesis inhibitor

^[2]

Key properties

• Inhibits 11β-hydroxylase
• Reduces cortisol and aldosterone synthesis
• Orally active

^[1]

• Selectively inhibits CYP11B1 and CYP11B2 (enzymes in cortisol and aldosterone synthesis)
• Rapid onset and offset of action
• Reversible inhibition of steroidogenesis
• Longer half-life compared to metyrapone and ketoconazole
• Higher potency in lowering cortisol levels
• Rapid absorption with sustained efficacy up to 6.7 years
• Potential for adrenal insufficiency as a side effect, but generally reversible
• Less potent inhibition of CYP3A4
• Can increase deoxycorticosterone levels (risks of hypokalemia, hypertension, edema)
• Lesser increase in 11-deoxycortisol levels compared to metyrapone
• Less hyperandrogenic effects compared to metyrapone
• Well tolerated with minimal mineralocorticoid side effects in the reported case
• Twice-daily dosing

^[2]

• Pharmacologic treatment of refractory Cushing’s disease after pituitary surgery

^[1]

• Treatment of native cyclic Cushing syndrome
• Control of hypercortisolism in Cushing disease
• Bridge therapy when surgery is not possible
• Management of ACTH-dependent Cushing syndrome
• Treatment of exogenous cyclic Cushing syndrome (e.g., from pembrolizumab)

^[2]

Classification by use

• Chemicals used as endocrine therapeutics
• Chemicals used to inhibit steroid biosynthesis
• Chemicals used in Cushing’s disease management

^[1]

• Medications for Cushing syndrome
• Steroidogenesis inhibitors
• Pituitary/adrenal-targeted therapies

^[2]

A trustworthy factory and manufacturer

1. [Cite:1] Insulin Resistance Unveiled: Cushing's Disease in a Patient with Type 1 Diabetes Mellitus and Worsening Glycemic Control, AACE Endocrinology and Diabetes, 5 January 2026
2. [Cite:2] Osilodrostat for Cyclic Cushing Disease, AACE Endocrinology and Diabetes, Volume 13, Issue 1, January–February 2026, Pages 17-21