Classification | Drug name | Dose | Possible adverse events; Close monitoring is necessary for all drugs |
---|---|---|---|
Steroidogenesis inhibitors | Ketoconazole | Oral 200–1200 mg/day 2–3 times a day | Hepatitis, gastrointestinal disturbances, gynecomastia, skin rash, adrenal insufficiency. |
Fluconazole | Oral 100–200 mg/day 2 times a day | AEs similar to ketoconazole, not well studied | |
Metyrapone | Oral 0.5–6 g/day 4 times a day | Hirsutism, acne, hypertension, hypokalemia, edema, gastritis, nausea, adrenal insufficiency. | |
Etomidate | IV bolus of 0.03 mg/kg followed by 0.02–0.08 mg/kg/h | Somnolence, myoclonus, nausea, vomiting, dystonic reactions, adrenal insufficiency. | |
Mitotane | Oral 2–5 g/day 3 times a day | Gastrointestinal disturbances, hepatitis, neurologic manifestations, gynecomastia, neutropenia, lipid disorders, adrenal insufficiency; teratogenic | |
Osilodrostat | Oral 10–60 mg/day; phase III clinical trial: NCT 02180217 | Nausea, asthenia, diarrhea, adrenal insufficiency. Testosterone increase in women. | |
Levoketoconazole | Oral 400 mg /day; phase III clinical trial: NCT 01838551 | N/A. | |
Dopamine D2R agonists | Cabergoline | Oral 0.5–7 mg/week | Headache, nausea, dizziness, nasal congestion, hypotension, depression |
SRLs | Pasireotidea | SC 300–1800 µg/day 2 times a day | Hyperglycemia, diabetes, diarrhea, nausea, abdominal pain, cholelithiasis, QT prolongation |
Pasireotide LAR | IM 30–60 mg/month; phase III clinical trial | ||
GR antagonist | Mifepristonea | Oral 300–1200 mg/day Once daily | Nausea, fatigue, headache, hypokalemia, arthralgia, vomiting, peripheral edema, hypertension, dizziness, adrenal insufficiency, PAECs, endometrial thickening, vaginal bleeding; termination of pregnancy. |
CDK2/Cyclin E inhibitor | R-Roscovitine | Oral Phase II clinical trial; clinicaltrials.gov identifier: NCT02160730 | |
Nuclear receptor ligand | Retinoic acid | Oral Phase II clinical trial; clinicaltrialsregister.eu number: 2008-006379-65 |