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Drug Interactions between lenacapavir and telotristat

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

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Interactions between your drugs

Major

telotristat ethyl lenacapavir

Applies to: telotristat and lenacapavir

GENERALLY AVOID: Coadministration with drugs that are combined P-glycoprotein (P-gp) and moderate inducers of CYP450 3A4 or sole moderate inducers of CYP450 3A4 may decrease the plasma concentrations of lenacapavir and result in a potential loss of virologic response. The proposed mechanism is increased clearance due to induction of the isoenzyme CYP450 3A4, which is partly responsible for the metabolism of lenacapavir and induction of the P-gp transporter of which lenacapavir is a substrate. In pharmacokinetic studies conducted in fasted subjects without HIV, coadministration of a single oral dose of lenacapavir 300 mg with the combined P-gp and moderate inducer of CYP450 3A4 efavirenz 600 mg once daily decreased the systemic exposure (AUC) and peak plasma concentration (Cmax) of lenacapavir by approximately 56% and 36%, respectively.

MANAGEMENT: Given the risk of reduced viral susceptibility and resistance development associated with subtherapeutic antiviral drug levels, concomitant use of lenacapavir with drugs that are combined P-gp and moderate inducers of CYP450 3A4 or sole moderate inducers of CYP450 3A4 should generally be avoided.

References

  1. (2022) "Product Information. Sunlenca (lenacapavir)." Gilead Sciences
  2. (2023) "Product Information. Sunlenca (lenacapavir)." Gilead Sciences Pty Ltd, SUNLENCA Product Inf

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Drug and food interactions

Moderate

telotristat ethyl food

Applies to: telotristat

ADJUST DOSING INTERVAL: Food increases the systemic exposure to both telotristat ethyl and its active metabolite, telotristat. Following administration of a single 500 mg dose of telotristat ethyl (twice the recommended dose) with a high-fat meal, telotristat ethyl peak plasma concentration (Cmax) and systemic exposure (AUC) were 112% and 264% higher, respectively, compared to administration under fasted conditions. The Cmax and AUC values for telotristat were also increased by 47% and 33%, respectively. The in vitro inhibitory potency of telotristat towards tryptophan hydroxylase has been shown to be approximately 29 times higher than that of the parent drug.

MANAGEMENT: Telotristat ethyl should be administered with food.

References

  1. (2017) "Product Information. Xermelo (telotristat ethyl)." Lexicon Pharmaceuticals, 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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