Drug Interactions between fostemsavir and telotristat
This report displays the potential drug interactions for the following 2 drugs:
- fostemsavir
- telotristat
Interactions between your drugs
telotristat ethyl fostemsavir
Applies to: telotristat and fostemsavir
Coadministration of fostemsavir with moderate or weak CYP450 3A4 inducers may decrease the plasma concentrations of temsavir, the active moiety of fostemsavir. According to the prescribing information, temsavir is a substrate of CYP450 3A4, esterases, P-glycoprotein (P-gp), and breast cancer resistance protein (BCRP). When fostemsavir (600 mg twice daily) was coadministered with the moderate CYP450 3A4 inducer etravirine (200 mg twice daily) in 14 study subjects, mean temsavir peak plasma concentration (Cmax), systemic exposure (AUC) and trough plasma concentration (Ctau) decreased by 48%, 50% and 52%, respectively, compared to fostemsavir administered alone. When the same dosage of fostemsavir was given to 22 study subjects with another moderate CYP450 3A4 inducer, rifabutin (300 mg once daily), mean temsavir Cmax, AUC and Ctau decreased by 27%, 30% and 41%, respectively. These changes are not considered clinically relevant, and no dosage adjustment of fostemsavir is recommended when coadministered with moderate or weak CYP450 3A4 inducers.
References (3)
- Cerner Multum, Inc. "UK Summary of Product Characteristics."
- Cerner Multum, Inc. "Australian Product Information."
- (2020) "Product Information. Rukobia (fostemsavir)." ViiV Healthcare
Drug and food interactions
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.
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
Drug Interaction Classification
Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit. | |
Moderately clinically significant. Usually avoid combinations; use it only under special circumstances. | |
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. | |
No interaction information available. |
Further information
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