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Drug Interactions between Korlym and ospemifene

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Moderate

miFEPRIStone ospemifene

Applies to: Korlym (mifepristone) and ospemifene

MONITOR: Coadministration with drugs that are known to inhibit both CYP450 3A4 and 2C9 may increase the plasma concentrations of ospemifene, which is primarily metabolized by these isoenzymes, with additional contribution from CYP450 2C19 and other pathways. The interaction has been studied with fluconazole, a moderate CYP450 3A4/potent CYP450 2C9/moderate CYP450 2C19 inhibitor. In 14 postmenopausal women given fluconazole 400 mg once followed by 200 mg daily for a total duration of 8 days, administration of ospemifene 60 mg after breakfast on day 5 of fluconazole treatment resulted in 1.7- and 2.7-fold increases in ospemifene peak plasma concentration (Cmax) and systemic exposure (AUC), respectively, compared to administration of ospemifene alone. The potential for increased risk of adverse events such as hot flush, thromboembolism, and endometrial or breast cancer should be considered.

MANAGEMENT: Caution is advised if ospemifene is used in combination with drugs that are inhibitors of both CYP450 3A4 and 2C9. Patients should be advised to seek medical attention if they develop potential signs and symptoms of thromboembolism such as chest pain, shortness of breath, and pain or swelling in the arms or legs.

References (1)
  1. (2013) "Product Information. Osphena (ospemifene)." Shionogi USA Inc

Drug and food interactions

Moderate

miFEPRIStone food

Applies to: Korlym (mifepristone)

ADJUST DOSING INTERVAL: Food may significantly increase the plasma concentrations of mifepristone.

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of mifepristone. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Because pharmacokinetic interactions involving grapefruit juice are often subject to a high degree of interpatient variability, the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: When mifepristone is used daily to control hyperglycemia secondary to hypercortisolism in patients with endogenous Cushing's syndrome, it should be taken with food to achieve consistent plasma drug levels. Patients should be advised to avoid consuming grapefruit or grapefruit juice during treatment with mifepristone, as it may cause increased adverse effects such as headache, dizziness, fatigue, nausea, vomiting, cramping, diarrhea, hypokalemia, adrenal insufficiency, vaginal bleeding, arthralgia, peripheral edema, and hypertension. Because mifepristone is eliminated slowly from the body, the interaction with grapefruit juice may be observed for a prolonged period.

References (2)
  1. (2001) "Product Information. Mifeprex (mifepristone)." Danco Laboratories
  2. (2012) "Product Information. Korlym (mifepristone)." Corcept Therapeutics Incorporated
Moderate

ospemifene food

Applies to: ospemifene

ADJUST DOSING INTERVAL: Food significantly enhances the oral bioavailability of ospemifene. In a cross-study comparison, administration of a single 60 mg dose of ospemifene with a high-fat/high-calorie meal (860 kcal) in postmenopausal women increased ospemifene peak plasma concentration (Cmax) and systemic exposure (AUC) by 2.3- and 1.7-fold, respectively, compared to administration under fasted condition. Elimination half-life and time to maximum concentration (Tmax) were not altered. In two separate food effect studies where different ospemifene tablet formulations were given to healthy male volunteers, ospemifene Cmax and AUC increased by 2.3- and 1.8-fold, respectively, with a low-fat/low-calorie meal (300 kcal) and 3.6- and 2.7-fold, respectively, with a high-fat/high-calorie meal (860 kcal) relative to fasting.

MANAGEMENT: Ospemifene should be taken once daily with food.

References (1)
  1. (2013) "Product Information. Osphena (ospemifene)." Shionogi USA Inc

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

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