Brand Name
Korlym
Generic Name
Mifepristone
View Brand Information FDA approval date: February 17, 2012
Classification: Progestin Antagonist
Form: Tablet
What is Korlym (Mifepristone)?
Mifepristone is a cortisol receptor blocker indicated to control hyperglycemia secondary to hypercortisolism in adult patients 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: Mifepristone should not be used in the treatment of patients with type 2 diabetes unless it is secondary to Cushing's syndrome. Mifepristone is a cortisol receptor blocker indicated to control hyperglycemia secondary to hypercortisolism in adult patients with endogenous Cushing's syndrome who have type 2 diabetes mellitus or glucose intolerance and have failed surgery or are not candidates for surgery . Important Limitations of Use: Do not use for the treatment of type 2 diabetes mellitus unrelated to endogenous Cushing's syndrome.
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Brand Information
Korlym (Mifepristone)
WARNING: TERMINATION OF PREGNANCY
Mifepristone is a potent antagonist of progesterone and cortisol via the progesterone and glucocorticoid (GR-II) receptors, respectively. The antiprogestational effects will result in the termination of pregnancy. Pregnancy must therefore be excluded before the initiation of treatment with KORLYM and prevented during treatment and for one month after stopping treatment by the use of a non-hormonal medically acceptable method of contraception unless the patient has had a surgical sterilization, in which case no additional contraception is needed. Pregnancy must also be excluded if treatment is interrupted for more than 14 days in females of reproductive potential.
1INDICATIONS AND USAGE
KORLYM (mifepristone) is a cortisol receptor blocker indicated to control hyperglycemia secondary to hypercortisolism in adult patients 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:
- KORLYM should not be used in the treatment of patients with type 2 diabetes unless it is secondary to Cushing's syndrome.
2DOSAGE FORMS AND STRENGTHS
Tablets: 300 mg
Oval shaped, light yellow to yellow tablets debossed with “Corcept” on one side and “300” on the other side. The tablets are not scored.
3CONTRAINDICATIONS
KORLYM is contraindicated in:
- Pregnancy
- Patients taking drugs metabolized by CYP3A such as simvastatin, lovastatin, and CYP3A substrates with narrow therapeutic ranges, such as cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus, due to an increased risk of adverse events.
- Patients receiving systemic corticosteroids for lifesaving purposes (e.g., immunosuppression after organ transplantation) because KORLYM antagonizes the effect of glucocorticoids.
- Women with a history of unexplained vaginal bleeding or with endometrial hyperplasia with atypia or endometrial carcinoma.
- Patients with known hypersensitivity to mifepristone or to any of the product components.
4DRUG INTERACTIONS
Based on the long terminal half-life of mifepristone after reaching steady state, at least 2 weeks should elapse after cessation of KORLYM before initiating or increasing the dose of any interacting concomitant medication.
4.1Drugs Metabolized by CYP3A
Because KORLYM is an inhibitor of CYP3A, concurrent use of KORLYM with a drug whose metabolism is largely or solely mediated by CYP3A is likely to result in increased plasma concentrations of the drug. Discontinuation or dose reduction of such medications may be necessary with KORLYM co-administration.
KORLYM increased the exposure to simvastatin and simvastatin acid significantly in healthy subjects. Concomitant use of simvastatin or lovastatin is contraindicated because of the increased risk of myopathy and rhabdomyolysis.
The exposure of other substrates of CYP3A with narrow therapeutic ranges, such as cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus, may be increased by concomitant administration with KORLYM. Therefore, the concomitant use of such CYP3A substrates with KORLYM is contraindicated.
Other drugs with similar high first pass metabolism in which CYP3A is the primary route of metabolism should be used with extreme caution if co-administered with KORLYM. The lowest possible dose and/or a decreased frequency of dosing must be used with therapeutic drug monitoring when possible. Use of alternative drugs without these metabolic characteristics is advised when possible with concomitant KORLYM.
If drugs that undergo low first pass metabolism by CYP3A or drugs in which CYP3A is not the major metabolic route are co-administered with KORLYM, use the lowest dose of concomitant medication necessary, with appropriate monitoring and follow-up.
4.2CYP3A Inhibitors
Medications that inhibit CYP3A could increase plasma mifepristone concentrations and dose reduction of KORLYM may be required.
Ketoconazole and other strong inhibitors of CYP3A, such as itraconazole, nefazodone, ritonavir, nelfinavir, indinavir, atazanavir, amprenavir and fosamprenavir, clarithromycin, conivaptan, lopinavir /ritonavir, posaconazole, saquinavir, telithromycin, or voriconazole may increase exposure to mifepristone. Caution should be used when strong CYP3A inhibitors are prescribed in combination with KORLYM. The benefit of concomitant use of these agents should be carefully weighed against the potential risks. The dose of KORLYM should be limited to 900 mg, and strong inhibitors of CYP3A should be used only when necessary.
4.3CYP3A Inducers
No medications that induce CYP3A have been studied when co-administered with KORLYM. Avoid co-administration of KORLYM and CYP3A inducers such as rifampin, rifabutin, rifapentin, phenobarbital, phenytoin, carbamazepine, and St. John's wort.
4.4Drugs Metabolized by CYP2C8/2C9
Because KORLYM is an inhibitor of CYP2C8/2C9, concurrent use of KORLYM with a drug whose metabolism is largely or solely mediated by CYP2C8/2C9 is likely to result in increased plasma concentrations of the drug.
KORLYM significantly increased exposure of fluvastatin, a typical CYP2C8/2C9 substrate, in healthy subjects. When given concomitantly with KORLYM, drugs that are substrates of CYP2C8/2C9 (including non-steroidal anti-inflammatory drugs, warfarin, and repaglinide) should be used at the smallest recommended doses, and patients should be closely monitored for adverse effects.
4.5Drugs Metabolized by CYP2B6
Mifepristone is an inhibitor of CYP2B6 and may cause significant increases in exposure of drugs that are metabolized by CYP2B6 such as bupropion and efavirenz. Since no study has been conducted to evaluate the effect of mifepristone on substrates of CYP2B6, the concomitant use of bupropion and efavirenz should be undertaken with caution.
4.6Use of Hormonal Contraceptives
Mifepristone is a progesterone-receptor antagonist and will interfere with the effectiveness of hormonal contraceptives. Therefore, non-hormonal contraceptive methods should be used.
5OVERDOSAGE
There is no experience with overdosage of KORLYM.
6DESCRIPTION
KORLYM (mifepristone) is a cortisol receptor blocker for oral administration. The chemical name of mifepristone is 11β-(4-dimethylaminophenyl)-17β-hydroxy-17α-(1-propynyl)-estra-4, 9-dien-3-one. The chemical formula is C
Mifepristone demonstrates a pH-related solubility profile. The greatest solubility is achieved in acidic media (~ 25 mg/mL at pH 1.5) and solubility declines rapidly as the pH is increased. At pH values above 2.5 the solubility of mifepristone is less than 1 mg/mL.
Each KORLYM tablet for oral use contains 300 mg of mifepristone. The inactive ingredients of KORLYM tablets are silicified microcrystalline cellulose, sodium starch glycolate, hydroxypropylcellulose, sodium lauryl sulfate, magnesium stearate, hypromellose, titanium dioxide, triacetin, D&C yellow 10 aluminum lake, polysorbate 80, and FD&C yellow 6 aluminum lake.
7HOW SUPPLIED/STORAGE AND HANDLING
KORLYM is supplied as a light yellow to yellow, film-coated, oval-shaped tablet debossed with “Corcept” on one side and “300” on the other. Each tablet contains 300 mg of mifepristone. KORLYM tablets are available in bottles of 28 tablets (NDC 76346-073-01) and bottles of 280 tablets (NDC 76346-073-02).
Store at controlled room temperature, 25 °C (77 °F); excursions permitted to 15 to 30 °C (59 – 86 °F).
8PATIENT COUNSELING INFORMATION
As a part of patient counseling, doctors must review the KORLYM
8.1Importance of Preventing Pregnancy
- Advise patients that KORLYM will cause termination of pregnancy. KORLYM is contraindicated in pregnant patients.
- KORLYM reduces the effectiveness of hormonal contraceptives. Counsel females of reproductive potential regarding pregnancy prevention and planning with a non-hormonal contraceptive prior to use of KORLYM and up to one month after the end of treatment.
- Instruct patients to contact their physician immediately if they suspect or confirm they are pregnant.