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Drug Interactions between Alunbrig and etravirine

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

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Interactions between your drugs

Major

etravirine brigatinib

Applies to: etravirine and Alunbrig (brigatinib)

GENERALLY AVOID: Coadministration of brigatinib with moderate inducers of CYP450 3A4 such as etravirine may decrease the plasma concentrations of brigatinib, which is partially metabolized by the isoenzyme. When a single 180 mg dose of brigatinib was administered with the potent CYP450 3A4 inducer rifampin (600 mg once daily), brigatinib peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 60% and 80%, respectively, compared to brigatinib administered alone. Based on simulations from a physiologically-based pharmacokinetic model, moderate CYP450 3A inducers may decrease the AUC of brigatinib by approximately 50%. Additionally, brigatinib has been shown in vitro to induce CYP450 3A4 at clinically relevant plasma concentrations and therefore may induce the metabolism of etravirine, a CYP450 3A4 substrate, and increase the risk of viral resistance associated with subtherapeutic antiretroviral drug levels.

MANAGEMENT: Concomitant use of a moderate CYP450 3A4 inducer, such as etravirine should generally be avoided during brigatinib therapy due to the potential for diminished pharmacologic effects of brigatinib. According to product labeling for etravirine, caution is advised if a CYP450 3A4 inducer such as brigatinib, is coadministered with etravirine due to the risk of reduced etravirine drug levels which increases the risk of viral resistance. If coadministration cannot be avoided, close clinical and laboratory monitoring for potential diminished pharmacologic effect of both brigatinib and etravirine is recommended. If concomitant use of brigatinib and moderate CYP450 3A4 inducers cannot be avoided, the manufacturer labeling recommends increasing the dose of brigatinib in 30 mg increments as tolerated every 7 days up to a maximum of twice the brigatinib dose that was tolerated prior to initiating the moderate CYP450 3A4 inducer. After discontinuation of the moderate CYP450 3A4 inducer, the brigatinib dose tolerated prior to initiating the moderate CYP450 3A4 inducer should be resumed.

References (4)
  1. Cerner Multum, Inc. "UK Summary of Product Characteristics."
  2. (2008) "Product Information. Intelence (etravirine)." Ortho Biotech Inc
  3. Cerner Multum, Inc. "Australian Product Information."
  4. (2017) "Product Information. Alunbrig (brigatinib)." Ariad Pharmaceuticals Inc

Drug and food interactions

Moderate

etravirine food

Applies to: etravirine

ADJUST DOSING INTERVAL: Coadministration with food increases the oral bioavailability of etravirine. The mechanism is unknown. Compared to administration following a meal, the systemic exposure (AUC) to etravirine was decreased by about 50% when the drug was administered under fasting conditions. The types of meal studied (ranging from 345 kilocalories containing 17 grams fat to 1160 kilocalories containing 70 grams fat) did not appear to make a difference with respect to impact on etravirine bioavailability.

MANAGEMENT: Etravirine should always be administered following a meal.

References (1)
  1. (2008) "Product Information. Intelence (etravirine)." Ortho Biotech Inc
Moderate

brigatinib food

Applies to: Alunbrig (brigatinib)

GENERALLY AVOID: Grapefruit juice may increase the plasma concentrations of brigatinib. The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit. 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. Itraconazole, a potent CYP450 3A4 inhibitor, has been shown to double brigatinib systemic exposure (AUC) in healthy volunteers. Increased exposure to brigatinib may increase the risk of adverse effects such as nausea, vomiting, diarrhea, hypertension, bradycardia, hyperglycemia, visual disturbances, lymphopenia, anemia, and elevations in pancreatic enzymes and creatine phosphokinase.

Food does not significantly affect the oral bioavailability of brigatinib. When brigatinib was administered to healthy volunteers after a high-fat meal (920 calories; 59 g fat, 58 g carbohydrates, 40 g proteins), brigatinib peak plasma concentration (Cmax) decreased by 13% and systemic exposure (AUC) did not change compared to administration after overnight fasting.

MANAGEMENT: Brigatinib may be taken with or without food. Patients should avoid consumption of grapefruit and grapefruit juice during treatment with brigatinib.

References (1)
  1. (2017) "Product Information. Alunbrig (brigatinib)." Ariad Pharmaceuticals 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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