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Table 1 Medical therapy for Cushing’s disease

From: Update on medical treatment for Cushing’s disease

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

 
  1. D2R dopamine D2 receptor, SRL somatostatin receptor ligand, SC subcutaneous, IM intramuscular, LAR long-acting repeatable, PAECs- progesterone-receptor modulator-associated endometrial changes
  2. aFDA approved