Tenofovir Disoproxil Fumarate + Boceprevir = Unknown or no reaction

Effect on Concentration

Applies within class?
No
Boceprevir
No change
Applies within class?
No

Pharmacologic Effects

Effect
N/A
Applies within class?
No
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 10-Jul-2018

Summary

Sources

Study Design

This was a study by the manufacturer on the effect of co-administered drugs on boceprevir pharmacokinetics and the effect of boceprevir on co-administered drugs' pharmacokinetics. The dosing schedule was tenofovir disoproxil fumarate 300mg daily for 7 days and boceprevir 800mg three times a day for 7 days.

Study Results

The results were an increase in boceprevir Cmax, AUC and Cmin by 5%, 8% and 8%, respectively. Also, it was found that boceprevir increased tenofovir Cmax and AUC by 32% and 5%, respectively.

Study Conclusions

Boceprevir is partly metabolized by CYP3A4/5 and is a strong inhibitor of CYP3A4/5. Also, boceprevir is a potential inhibitor of p-glycoprotein (P-gp) and a substrate of P-gp. Tenofovir has minimal cytochrome activity, by weakly inhibiting CYP1A2. As well, tenofovir is not a P-gp substrate, inhibitor or inducer. These two drugs do not have any overlapping metabolic or transport pathways. The only notable pharmacokinetic parameter change when co-administering these two drugs, was the increase in tenofovir Cmax by 32%. No dosage adjustment is needed when co-administering these two drugs.

References

Kiser JJ, Burton JR, Anderson PL, Everson GT. Review and management of drug interactions with boceprevir and telaprevir. Hepatology. 2012; 5: 1620-1628.