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. 2016 Sep 6;19(6):643–653. doi: 10.1007/s11102-016-0742-1

Table 1.

Mechanisms of action of steroidogenesis inhibitors [21]

Mechanism of action Efficacy (%) Common side effects
Ketoconazole Inhibitor of CYP17A1, CYP11A1, and CYP11B1 53–88 Liver enzyme increase
Gastrointestinal AEs
Interactions with multiple drugs
Not approved for use during pregnancy
Metyrapone Inhibitor of CYP11B1, CYP11B2, and CYP17A1 75 Hypokalemia
Hypertension
Gastrointestinal AEs
Hirsutism
Not approved for use during pregnancy
Etomidate Inhibitor of CYP11B1, CYP17A1, and CYP11A1 NR Hypnosis
Not approved for use during pregnancy
Mitotane Inhibitor of CYP11A1, CYP11B1, and CYP11B2 ~70 Gastrointestinal AEs
Neurological side effects
Teratogen (not approved for use during pregnancy)
Osilodrostat (LCI699) Inhibitor of CYP11B2 and CYP11B1 at higher doses 78–92 Nausea
Hirsutism
Fatigue
Headache
Hypokalemia
Not approved for use during pregnancy
Levoketoconazole (COR-003) Inhibitor of CYP17A1, CYP11A1, CYP11B1, and CYP21A2 NR Headachea
Nauseaa
Mild liver enzyme increasea
Not approved for use during pregnancy

CYP, cytochrome P450; AE, adverse event; NR, not reported. All of these drugs can induce adrenal insufficiency

aIn patients with diabetes mellitus