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Drug Interactions between ensifentrine and ivacaftor / lumacaftor

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

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Interactions between your drugs

Minor

ivacaftor ensifentrine

Applies to: ivacaftor / lumacaftor and ensifentrine

Coadministration with inhibitors of CYP450 2C9 may increase the plasma concentrations of ensifentrine. According to the prescribing information, ensifentrine's primary routes of metabolism are oxidative (hydroxylation and O-demethylation) followed by conjugation. Additionally, in vitro data indicates ensifentrine is predominantly metabolized by CYP450 2C9, and to a lesser extent by CYP450 2D6. When ensifentrine (3 mg single dose) was coadministered with the CYP450 2C9 inhibitor fluconazole (200 mg twice daily) to 28 healthy volunteers, ensifentrine systemic exposure (AUC) increased by 1.6-fold and peak plasma concentration (Cmax) increased by 1.4-fold. The increase in ensifentrine exposure by fluconazole was not considered clinically relevant.

References (2)
  1. (2024) "Product Information. Ohtuvayre (ensifentrine)." Verona Pharma
  2. Rheault T, Kankam M, ayrton j, bengtsson t, rickard k (2024) The effect of fluconazole on the pharmacokinetics of ensifentrine in healthy individuals https://erj.ersjournals.com/content/58/suppl_65/PA2137
Minor

lumacaftor ensifentrine

Applies to: ivacaftor / lumacaftor and ensifentrine

Coadministration with inhibitors of CYP450 2C9 may increase the plasma concentrations of ensifentrine. According to the prescribing information, ensifentrine's primary routes of metabolism are oxidative (hydroxylation and O-demethylation) followed by conjugation. Additionally, in vitro data indicates ensifentrine is predominantly metabolized by CYP450 2C9, and to a lesser extent by CYP450 2D6. When ensifentrine (3 mg single dose) was coadministered with the CYP450 2C9 inhibitor fluconazole (200 mg twice daily) to 28 healthy volunteers, ensifentrine systemic exposure (AUC) increased by 1.6-fold and peak plasma concentration (Cmax) increased by 1.4-fold. The increase in ensifentrine exposure by fluconazole was not considered clinically relevant.

References (2)
  1. (2024) "Product Information. Ohtuvayre (ensifentrine)." Verona Pharma
  2. Rheault T, Kankam M, ayrton j, bengtsson t, rickard k (2024) The effect of fluconazole on the pharmacokinetics of ensifentrine in healthy individuals https://erj.ersjournals.com/content/58/suppl_65/PA2137

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 (4)
  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

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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