Cabotegravir + Levonorgestrel = Precautionary

Effect on Concentration

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

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 22-Nov-2022

Summary

Co-administration of CAB 30 mg once daily with an oral contraceptive containing EE and LNG did not affect the PK of LNG to a clinically meaningful extent.

Sources

Study Design

In an open-label, fixed-sequence crossover study, 20 healthy adult female subjects (18-39 years) received ethinyl estradiol/levonorgestrel (EE/LNG; 0.03 mg/0.15 mg tablet; MicrogynonŽ) once daily for 10 days (Days 1-10), followed by coadministration of EE 0.03 mg/LNG 0.15 mg once daily plus cabotegravir (CAB) 30 mg once daily for 10 days (Day 11-21). Blood samples were collected for the pharmacokinetic (PK) assessment on Day 10 for EE and LNG and Day 21 for CAB.

Study Results

When subjects were given CAB 30 mg once daily together with EE/LNG, CAB had no significant effect on the pharmacokinetics (PK) of LNG. The geometric mean ratios (GMRs; CAB + EE/LNG / EE/LNG) [90% CIs] for LNG were: 1.05 [0.96, 1.15] for Cmax and 1.11 [1.06, 1.16] for AUC.

Study Conclusions

References

C Trezza, Ford SL, E Gould, et al. Lack of effect of oral cabotegravir on the pharmacokinetics of a levonorgestrel/ethinyl estradiol containing oral contraceptive in healthy adult females. abstract 82. 16th International Workshop On Clinical Pharmacology Of Hiv And Heptatitis Therapy. Washington, DC. ; 2015.