Boceprevir + Cyclosporine = Precautionary

Effect on Concentration

Boceprevir
No change
Applies within class?
No
Cyclosporine
Increase
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 10-Jul-2018

Summary

Sources

Pharmacokinetic interaction between the hepatitis C virus protease inhibitor boceprevir and cyclosporine and tacrolimus in healthy volunteers. ^

Study Design

In this drug-drug interaction trial in healthy adults the effect of boceprevir on cyclosporine was evaluated and vice versa. Subjects received different combinations of boceprevir and cyclosporine over 12 days, always at 800mg of boceprevir and 100mg of cyclosporine. From single doses of each separately, to single doses combined, to boceprevir given TID for six days and a single dose of cyclosporine on day 5.

Study Results

At the 100mg dose of cyclosporine the AUC and Cmax of boceprevir was minimally changed. However, boceprevir did cause a substantial change in cyclosporine AUC and Cmax. The geometric means of cyclosporine Cmax and AUC(0-inf) increased by 2.01-fold and 2.68-fold, respectively, with boceprevir co-administration.

Study Conclusions

The manufacturer states that clinicians should anticipate the need for dose adjustment of cyclosporine if it is co-administered with boceprevir, with close monitoring of cyclosporine blood levels, renal function and cyclosporine adverse events.

References

Huskotte E, Gupta E, Xuan F, van Zutven M, Omara E, Feng HP, Butterton J. Pharmacokinetic interaction between the hepatitis c virus protease inhibitor boceprevir and cyclosporine and tacrolimus in healthy volunteers. Hepatology. 2012; 5: 1622-1630.