Elvitegravir / Cobicistat

Rosuvastatin

Potential interaction.

No pharmaceutical opinion available for this interaction.

Mechanism

Elvitegravir / Cobicistat may inhibit hepatic transports OATP1B1/B3 and BCRP and increase plasma concentration of Rosuvastatin.

Elvitegravir / Cobicistat

Pharmacodynamic effects

Recommendations

Alternative solution(s)

Rosuvastatin

Pharmacodynamic effects

Probably without any clinical consequence.

Recommendations

No a priori dosage adjustment is recommended.

Monitor for adverse effects.

See comments.

Alternative solution(s)

Monitor

Tests

Pharmacokinetic parameters
Parameters
Reference number
# patients
HIV
Dose
Frequency
AUC
Cmin
Cmax
Elvitegravir / Cobicistat
3360
10
-
150/150 mg
QD
+ 2%
- 2%
- 6%
Rosuvastatin
3360
10
-
10 mg
x 1
+ 38%
+ 43%
+ 89%
Comment

Ref #3360, 2570 and 3281 : The increase in AUC ranged from 48-142% and the increase in AUC ranged from 13-67% depending on the subject under study.
Likely driven by inhibition of intestinal efflux by BCRP or hepatic uptake by OATPs by EVG/c. No serious adverse events or grade 2, 3 or 4 AEs or grade 3 or 4 laboratory abnormalities occurred.
The study used as a reference a concentration of rosuvastatin alone with the equivalence limits of 70-143% for AUC and 70-175% for Cmax.
The modest increase observed is considered clinically insignificant. Elvitegravir/cobicistat can be taken with rosuvastatin.

Reference
  • 2570
    Elvitegravir/cobicistat/emtricitabine/tenofovir (Stribild), Gilead, Ontario, Canada, 17 septembre 2018.
  • 3281
    Elvitegravir/cobicistat/emtricitabine/tenofovir alafenamide (Genvoya), Gilead, Ontario, Canada, 6 août 2021.
  • 3360
    Custodio J, Wang H, Hao J, Lepist EI, Ray AS et al. Pharmacokinetics of cobicistat boosted-elvitegravir administered in combination with rosuvastatin. Clin Pharmacol, 2014, 54(6): 649-56.
  • 1490
    Rosuvastatin (Crestor), AstraZeneca, Ontario, Canada, 21 avril 2015.