Generic Name and Formulations:
Mifepristone 300mg; tabs.
Indications for KORLYM:
To control hyperglycemia secondary to hypercortisolism in adults with endogenous Cushing’s syndrome who have type 2 diabetes mellitus or glucose intolerance and have failed surgery or are not candidates for surgery.
Limitations Of use:
Not for treatment of type 2 diabetes unless secondary to Cushing’s syndrome.
Swallow whole. Take with food. Initially 300mg once daily. May increase in 300mg increments (once every 2–4 weeks) to a max of 1200mg once daily, based on response and tolerability. Max: 20mg/kg per day. Renal or mild-to-moderate hepatic impairment: max 600mg once daily. Severe hepatic impairment: not recommended. Concomitant strong CYP3A4 inhibitors (if necessary): max 600mg once daily; see full labeling.
Pregnancy (Cat.X). Currently taking simvastatin, lovastatin, or CYP3A substrates with narrow therapeutic range (eg, cyclosporine, ergots, fentanyl, pimozide, quinidine, sirolimus, tacrolimus). Concomitant long-term corticosteroids for serious conditions/illnesses. Women with endometrial hyperplasia with atypia, endometrial carcinoma, or history of unexplained vaginal bleeding.
Exclude pregnancy before the initiation or treatment interruption for >14 days. Females of reproductive potential should use non-hormonal contraceptives during and for 1 month after discontinuing treatment. Monitor for adrenal insufficiency; discontinue and treat if suspected; resume therapy at lower dose after resolution. Correct hypokalemia prior to treatment. Measure serum potassium 1–2 weeks after initiation, during dose increases, and periodically thereafter. Risk of QT interval prolongation or opportunistic infections (eg, Pneumocystis jiroveci pneumonia). Avoid in patients with potassium channel variants resulting in a long QT interval. Underlying heart conditions (including heart failure, coronary vascular disease). Women who have hemorrhagic disorders or receiving concurrent anticoagulant therapy. Renal or hepatic impairment. Nursing mothers: not recommended.
See Contraindications. Avoid initiating or increasing the dose of any interacting concomitant drugs after discontinuing Korlym for at least 2 weeks. Avoid concomitant CYP3A inducers (eg, rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, St. John’s wort) or QT interval-prolonging drugs. Potentiated by strong CYP3A inhibitors (eg, ketoconazole, itraconazole, nefazodone, ritonavir, nelfinavir, indinavir, atazanavir, amprenavir and fosamprenavir, clarithromycin, conivaptan, lopinavir/ritonavir, posaconazole, saquinavir, telithromycin, voriconazole); caution, if co-admin necessary; limit dose to 600mg (see Adult). Potentiates CYP2C8/2C9 substrates (eg, fluvastatin, NSAIDs, warfarin, repaglinide); use lower dose of these and monitor closely. Caution with drugs that are metabolized by CYP2B6 (eg, bupropion, efavirenz). Antagonizes hormonal contraceptives.
Cortisol receptor blocker.
Nausea, fatigue, headache, decreased blood potassium, arthralgia, vomiting, peripheral edema, hypertension, dizziness, decreased appetite, endometrial hypertrophy.