Glecaprevir/Pibrentasvir + Efavirenz = Prohibited

Effect on Concentration

Glecaprevir/Pibrentasvir
Decrease
Applies within class?
No
Efavirenz
No change
Applies within class?
No

Pharmacologic Effects

Glecaprevir/Pibrentasvir
Effect
N/A
Applies within class?
No
Efavirenz
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 01-Mar-2022

Summary

The use of efavirenz with GLE/PIB is not recommended.

Sources

Drug-Drug Interactions of Glecaprevir and Pibrentasvir Coadministered With Human Immunodeficiency Virus Antiretrovirals. ^

Study Design

In a parallel 2-periods, open-label, single-center, phase I study, the pharmacokinetic (PK) drug interaction potential was assessed betweeen GLE/PIB and ATV/r. Healthy adults age between 18 and 55 recevied GLE 300mg/PIB 120mg (n7) once daily in period 1(Days 1-7). In period 2 (days 1-14), subjects recevied GLE/PIB with ATV 300mg/r 100mg once daily (n13). For assessment of the GLE/PIB plasma concentration, samples were collected on period 1 day 7 and period 2 days 1 and 14 prior dosing. For ATV/r, samples were collected on period 2 days 1 and 14.

Study Results

When coadministered with GLE/PIB, EFV, and FTC exposures were similar (&8804;13 difference), and tenofovir exposures were slightly higher (&8804;38 increase) compared to EFV/FTC/TDF alone. The geometric mean exposures of GLE (AUC24, 1270ng&8729;h/mL) and PIB (AUC24, 636 ng&8729;h/mL) were &8805;47 lower than observed for GLE/PIB alone in the other antiretroviral drug drug interaction studies (GLE AUC24, 23801270 ng&8729;h/mL; PIB AUC24, 14702790 ng&8729;h/mL).

Study Conclusions

The use of efavirenz with GLE/PIB is not recommended.

References

Koloski MP, et al.. Drug-drug interactions of glecaprevir and pibrentasvir coadministered with human immunodeficiency virus antiretrovirals. Journal Of Infectious Diseases. 2020; 2: 223-31.