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Drug Interactions between selexipag and tazemetostat

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

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Interactions between your drugs

Moderate

selexipag tazemetostat

Applies to: selexipag and tazemetostat

MONITOR: Coadministration with inhibitors of CYP450 2C8 may increase exposure to the active metabolite of selexipag. According to the prescribing information, selexipag is hydrolyzed to its active metabolite in the liver and intestine by carboxylesterases, and the active metabolite subsequently undergoes oxidative metabolism catalyzed primarily by CYP450 2C8 and to a lesser extent by CYP450 3A4. Coadministration of selexipag with the moderate to potent CYP450 2C8 inhibitor clopidogrel, given at 300 mg loading dose or 75 mg once daily maintenance dose, had no relevant effect on exposure to selexipag but increased exposure to the active metabolite by approximately 2.2- and 2.7-fold following the loading and maintenance doses, respectively. The interaction has not been studied with other, less potent CYP450 2C8 inhibitors.

MANAGEMENT: Caution is advised when selexipag is prescribed with CYP450 2C8 inhibitors. Dosage adjustments as well as clinical and laboratory monitoring of selexipag may be appropriate whenever a CYP450 2C8 inhibitor is added to or withdrawn from therapy. Patients should be monitored for potentially increased side effects such as diarrhea, nausea, vomiting, flushing, anemia, and decreased appetite.

References

  1. (2001) "Product Information. Plavix (clopidogrel)." Bristol-Myers Squibb
  2. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  3. Cerner Multum, Inc. "Australian Product Information."
  4. (2016) "Product Information. Uptravi (selexipag)." Actelion Pharmaceuticals US Inc
View all 4 references

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Drug and food interactions

Major

tazemetostat food

Applies to: tazemetostat

GENERALLY AVOID: Consumption of grapefruit or grapefruit juice during tazemetostat therapy may significantly increase the plasma concentrations of tazemetostat. The proposed mechanism is inhibition of the CYP450 3A4-mediated metabolism of tazemetostat by certain compounds in grapefruit. Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability). According to the product labeling, coadministration of tazemetostat (400 mg twice daily) with the moderate CYP450 3A4 inhibitor fluconazole increased the tazemetostat steady state exposure (AUC 0 to 8 hours) by 3.1-fold and peak plasma concentration by 2.3-fold. In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands. Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition. Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict. Clinically, this interaction may result in an increased risk of the frequency or severity of adverse reactions due to tazemetostat such as hemorrhage, pleural effusion, skin infection, dyspnea, pain, and respiratory distress.

MANAGEMENT: The manufacturer advises that patients treated with tazemetostat should avoid consumption of grapefruit or grapefruit juice.

References

  1. (2020) "Product Information. Tazverik (tazemetostat)." Epizyme, Inc

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Minor

selexipag food

Applies to: selexipag

Food prolongs the gastrointestinal absorption of selexipag. When taken with food, the time to peak concentration (Tmax) was delayed and peak plasma concentration (Cmax) was approximately 30% lower. Selexipag systemic exposure (AUC) and that of its active metabolite did not significantly change, however. Selexipag may be taken with or without food. Tolerability may be improved when taken with food.

References

  1. (2016) "Product Information. Uptravi (selexipag)." Actelion Pharmaceuticals US Inc

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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.

See also

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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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