Asunaprevir + Ketoconazole = Prohibited

Effect on Concentration

Asunaprevir
Increase
Applies within class?
No
Ketoconazole
Unknown
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 22-Nov-2022

Summary

The study population consisted of Asian and Indian men. No serious adverse events occurred despite having a roughly 10-fold higher exposure to asunaprevir when administered with ketoconazole.

Sources

Ketoconazole vs asunaprevir ^

Study Design

Nineteen healthy subjects aged 18-49 years were administered asunaprevir 200mg twice daily with food for 14 days. Ketoconazole 200mg twice daily was co-administered on days 8-14; serial pharmacokinetic parameters were measured on days 7 and 14.

Study Results

The geometric mean ratio (GMR) of the AUC of asunaprevir with ketoconazole vs. without was 960% (90% confidence interval [CI] 860% to 1080%). Similarly, the GMR of the Cminwas 940% (90% CI 830% to 1050%) and the Cmax 690% (90% CI 590% to 810%).

Study Conclusions

References

T Eley, B He, S-P Huang, et al. Effect of multiple-dose ketoconazole and the effect of multiple-dose rifampin on pharmacokinetics (pk) of the hcv ns3 protease inhibitor asunaprevir. 8th International Workshop On Clinical Pharmacology Of Hepatitis Therapy. . ; 2013.