Etravirine + Cabotegravir = Unknown or no reaction

Effect on Concentration

Etravirine
Unknown
Applies within class?
No
Cabotegravir
No change
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 22-Nov-2022

Summary

Concomitant use of cabotegravir with ETR had no effect on PK parameters of cabotegravir in healthy subjects. The investigators concluded that caboteravir may be coadministered with ETR without dose adjustment.

Sources

Cabotegravir vs etravirine ^

Study Design

In an open-label, 2-period, single-sequence crossover study, 12 healthy subjects received cabotegravir (formerly known as S/GSK1265744) 30 mg once daily (QD) for 10 days (Days 1-10; period 1), followed by coadministration of cabotegravir 30 mg QD and etravirine (ETR) 200 mg twice daily (BID) for 14 days (Days 1-14; period 2). Serial pharmacokinetic (PK) samples for analysis of cabotegravir were obtained predose and at 1, 2, 3, 4, 8,12, and 24 hours postdose of cabotegravir on Day10 of period 1. Serial PK samples for analysis of cabotegravir plus ETR were obtained on Day14 of period 2.

Study Results

Coadministration of cabotegravir 30 mg QD with ETR 200 mg BID resulted in similar exposures and plasma concentrations of cabotegravir compared to cabotegravir 30 mg QD without ETR; the geometric mean ratios (GMRs; cabotegravir + ETR / cabotegravir) [90% CIs] of cabotegravir were: 1.04 [0.987, 1.09] for Cmax, 1.01 [0.956, 1.06] for AUC, and 0.999 [0.942, 1.06] for Cmin. No deaths, serious adverse events, Grade 3-4 adverse events (AEs), or withdrawals due to AEs occured.

Study Conclusions

References

Susan L Ford, Elizabeth Gould, Shuguang Chen, Yu Lou, Etienne Dumont, William Spreen, Stephen Piscitelli. Effects of etravirine on the pharmacokinetics of the integrase inhibitor s/gsk1265744. Antimicrobial Agents And Chemotherapy. 2013; 1: 277-280.