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Drug Interactions between bexarotene and gemfibrozil

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

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Interactions between your drugs

Major

gemfibrozil bexarotene

Applies to: gemfibrozil and bexarotene

GENERALLY AVOID: Coadministration with gemfibrozil may significantly increase the plasma concentrations of bexarotene. The exact mechanism of interaction is unknown. In an analysis of the pharmacokinetic data acquired during two clinical studies of bexarotene treatment in patients with cutaneous T-cell lymphoma, investigators found that mean plasma bexarotene concentrations (dose-normalized) were more than 5 times higher with concomitant gemfibrozil therapy than without. Plasma metabolite chromatography profiles were consistent with an inhibition of the oxidative metabolism of bexarotene by gemfibrozil, although the exact CYP450 isoenzyme involved has not been elucidated. The combination has also been reported to increase serum triglyceride levels in some patients. By contrast, concomitant fenofibrate did not appear to affect bexarotene pharmacokinetics; however, data were insufficient to provide an adequate assessment.

MANAGEMENT: The use of bexarotene in combination with gemfibrozil should generally be avoided.

References (3)
  1. (2001) "Product Information. Targretin (bexarotene)." Ligand Pharmaceuticals
  2. Talpur R, Ward S, Apisarnthanarax N, Breuer-Mcham J, Duvic M (2002) "Optimizing bexarotene therapy for cutaneous T-cell lymphoma." J Am Acad Dermatol, 47, p. 672-84
  3. Cato III AE, Ulm EH, Crowley CC, Loewen GR, Timony G, Yocum RC (2013) Concomitant gemfibrozil, but not atorvastatin, is associated with increased plasma bexarotene concentrations. http://www.aapsj.org/abstracts/AM_2000/3256.htm

Drug and food interactions

Moderate

bexarotene food

Applies to: bexarotene

ADJUST DOSING INTERVAL: Food may enhance the oral bioavailability of bexarotene. In one clinical study, bexarotene peak plasma concentration (Cmax) and systemic exposure (AUC) resulting from a 75 to 300 mg dose were 35% and 48% higher, respectively, when administered after a fat-containing meal relative to a glucose solution. In all clinical trials, patients were instructed to take bexarotene with or immediately following a meal.

Coadministration with inhibitors of CYP450 3A4 such as grapefruit juice may theoretically increase the plasma concentrations of bexarotene. In vitro studies suggest that bexarotene is metabolized by CYP450 3A4. However, concomitant administration with multiple doses of ketoconazole, a potent CYP450 3A4 inhibitor, did not alter bexarotene plasma concentrations, which would imply that bexarotene elimination is not substantially dependent on CYP450 3A4 metabolism in vivo.

MANAGEMENT: Because safety and efficacy data are based upon administration with food, bexarotene should be administered once daily with a meal. Patients may want to avoid consuming large amounts of grapefruit or grapefruit juice.

References (2)
  1. (2001) "Product Information. Targretin (bexarotene)." Ligand Pharmaceuticals
  2. Cerner Multum, Inc. "UK Summary of Product Characteristics."

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

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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