Grazoprevir (Single Agent) + Montelukast = Unknown or no reaction

Effect on Concentration

Grazoprevir (Single Agent)
No change
Applies within class?
No
Montelukast
Increase
Applies within class?
No

Pharmacologic Effects

Grazoprevir (Single Agent)
Effect
N/A
Applies within class?
No
Montelukast
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 18-Jul-2018

Summary

Sources

Grazoprevir versus Montelukast ^

Study Design

This open-label, two-period, fixed sequence study described the effect of grazoprevir on montelukast in 23 healthy subjects. Subjects were given a dose of montelukast 10 mg on day 1. After a four day washout period, the same subjects were given once daily doses of grazoprevir 200 mg for 10 days, with a single dose of montelukast 10 mg on day nine.

Study Results

Coadministration of grazoprevir with montelukast increased the exposure to montelukast with an AUC GMR of 1.11 (1.02, 1.2). Plasma Cmax of montelukast was similar when given with or without grazoprevir with GMR [90% CI] of 0.92 (0.81, 1.06). Tmax was prolonged when given with grazoprevir (3.5 h) versus when given alone (2.02 h). And terminal half-live was comparable when montelukast was given with grazoprevir compared to when it was given alone, at 6.84 h and 6.36 h, respectively.

Study Conclusions

The authors stated that coadministration of montelukast and grazoprevir resulted in minimal increased exposure to montelukast, which demonstrated that grazoprevir was not a clinically meaningful inhibitor of CYP2C8.

References

Wolford DG, Caro L, Guo Z, Jumes P, Gartner M, Bethel Brown C. No clinically meaningful pharmacokinetic interactions between hcv protease inhibitor grazoprevir and montelukast (a cyp2c8 substrate) in healthy subjects. abstract 66. Hep Dart: Frontiers In Drug Development For Viral Hepatitis 2015. Maui, Hawaii, USA. ; December 2015.