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Drug Interactions between alpelisib and ivacaftor / lumacaftor

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

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Interactions between your drugs

Major

lumacaftor alpelisib

Applies to: ivacaftor / lumacaftor and alpelisib

GENERALLY AVOID: Coadministration of alpelisib with potent inducers of CYP450 3A4 may significantly reduce the plasma concentrations of alpelisib. The proposed mechanism, based on in vitro data, is increased clearance due to induction of CYP450 3A4, which is one of the routes of metabolism of alpelisib. The therapeutic efficacy of alpelisib may be reduced; however, clinical data are lacking.

MANAGEMENT: According to the manufacturer, concomitant use of alpelisib with potent CYP450 3A4 inducers should generally be avoided. Alternative therapeutic agents with less enzyme induction potential should be considered.

References

  1. (2019) "Product Information. Piqray (alpelisib)." Novartis Pharmaceuticals

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Moderate

ivacaftor alpelisib

Applies to: ivacaftor / lumacaftor and alpelisib

GENERALLY AVOID: Coadministration of inhibitors of the breast cancer resistance protein (BCRP) transporter with alpelisib may increase the plasma concentrations and risk of adverse effects of alpelisib, which is a substrate of this efflux transporter. Alpelisib has been identified as a substrate of BCRP in in vitro studies. However, clinical data are not available.

MANAGEMENT: If coadministration with BCRP inhibitors is required, patients should be closely monitored for alpelisib-related adverse reactions, including hyperglycemia, diarrhea, rash, acute kidney injury, abdominal pain, and anemia. Some authorities recommend coadministration of alpelisib with BCRP inhibitors be avoided whenever possible (US).

References

  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. (2019) "Product Information. Piqray (alpelisib)." Novartis Pharmaceuticals

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Drug and food interactions

Moderate

ivacaftor food

Applies to: ivacaftor / lumacaftor

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of ivacaftor. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. Elexacaftor and tezacaftor are also CYP450 3A4 substrates in vitro and may interact similarly with grapefruit juice, whereas lumacaftor is not expected to interact.

ADJUST DOSING INTERVAL: According to prescribing information, systemic exposure to ivacaftor increased approximately 2.5- to 4-fold, systemic exposure to elexacaftor increased approximately 1.9- to 2.5-fold, and systemic exposure to lumacaftor increased approximately 2-fold following administration with fat-containing foods relative to administration in a fasting state. Tezacaftor exposure is not significantly affected by administration of fat-containing foods.

MANAGEMENT: Patients treated with ivacaftor-containing medications should avoid consumption of grapefruit juice and any food that contains grapefruit or Seville oranges. All ivacaftor-containing medications should be administered with fat-containing foods such as eggs, avocados, nuts, meat, butter, peanut butter, cheese pizza, and whole-milk dairy products. A typical cystic fibrosis diet will satisfy this requirement.

References

  1. (2012) "Product Information. Kalydeco (ivacaftor)." Vertex Pharmaceuticals
  2. (2015) "Product Information. Orkambi (ivacaftor-lumacaftor)." Vertex Pharmaceuticals
  3. (2022) "Product Information. Symdeko (ivacaftor-tezacaftor)." Vertex Pharmaceuticals
  4. (2019) "Product Information. Trikafta (elexacaftor/ivacaftor/tezacaftor)." Vertex Pharmaceuticals
View all 4 references

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Moderate

alpelisib food

Applies to: alpelisib

ADJUST DOSING INTERVAL: Food significantly enhances the oral absorption and bioavailability of alpelisib. When administered with a high-fat high-calorie meal (985 calories with 58.1 g of fat) or a low-fat low-calorie meal (334 calories with 8.7 g of fat) the AUC and Cmax of a single dose of alpelisib was increased by 73% and 84% and 77% and 145%, respectively. There were no clinically significant differences in alpelisib AUC between the two types of meals. In addition, food appears to have a more pronounced effect on the solubility of alpelisib than gastric pH. When coadministered with a single 300 mg dose of alpelisib, ranitidine decreased the absorption and overall exposure of alpelisib. Following administration of ranitidine with a low-fat low-calorie meal, the mean AUC and Cmax of alpelisib was decreased by 21% and 36%, respectively. Administration of ranitidine under fasting conditions reduced the mean AUC and Cmax of alpelisib by 30% and 51%, respectively.

MANAGEMENT: To ensure maximal oral absorption, alpelisib should be administered with a meal.

References

  1. (2019) "Product Information. Piqray (alpelisib)." Novartis Pharmaceuticals

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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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