Interaction Checker
No Interaction Expected
Lopinavir/ritonavir (LPV/r)
Etravirine (ETR)
Quality of Evidence: Low
Summary:
Coadministration of lopinavir/ritonavir tablets and etravirine decreased etravirine AUC (35%), Cmax (30%) and Cmin (45%) and decreased lopinavir AUC (13%), Cmax (11%) and Cmin (20%). Etravirine and lopinavir/ritonavir can be co-administered without dose adjustments because the reduction in the mean systemic exposures of etravirine in the presence of lopinavir/ritonavir is similar to the reduction in mean systemic exposures of etravirine in the presence of darunavir/ritonavir. Coadministration of etravirine, saquinavir, lopinavir and ritonavir to HIV+ subjects decreased AUC, Cmax and Cmin of the PIs (saquinavir decreased by 13%, 15%, and 13%, respectively; lopinavir decreased by 18%, 16% and 8%, respectively; ritonavir decreased by 13%, 11% and 12% respectively). Etravirine pharmacokinetics were comparable to those obtained when coadministered with a single boosted PI. These changes were not considered likely to be clinically significant.
Description:
Coadministration with Kaletra tablets (400/100 mg twice daily) decreased etravirine AUC, Cmin and Cmax by 35%, 45% and 30%, respectively. No dose adjustment necessary.
Kaletra Summary of Product Characteristics, AbbVie Ltd, January 2021.
Drug interaction studies reveal no clinically significant interaction between Kaletra and etravirine. Coadministration of etravirine (200 mg twice daily) and lopinavir/ritonavir (400/100 mg twice daily) was studied in 16 subjects. Lopinavir Cmax, AUC and Cmin decreased by 11%, 13% and 20%, respectively. Etravirine Cmax, AUC and Cmin decreased by 30%, 35% and 45%, respectively.
Kaletra Prescribing Information, AbbVie Inc, October 2020.
Coadministration with lopinavir/ritonavir (400/100 mg tablets twice daily) decreased lopinavir AUC (13%), Cmax (11%) and Cmin (20%). Etravirine AUC, Cmax and Cmin decreased by 35%, 30% and 45%, respectively. Etravirine and lopinavir/ritonavir can be used without dose adjustments.
Intelence Summary of Product Characteristics, Janssen-Cilag Ltd, March 2019.
The mean systemic exposure (AUC) of etravirine was reduced after co-administration of etravirine with lopinavir/ritonavir (tablet). Because the reduction in the mean systemic exposures of etravirine in the presence of lopinavir/ritonavir is similar to the reduction in mean systemic exposures of etravirine in the presence of darunavir/ritonavir, etravirine and lopinavir/ritonavir can be co-administered without dose adjustments. Coadministration of lopinavir/ritonavir (400/100 mg tablets twice daily) and etravirine was studied in 16 subjects. Etravirine Cmax, AUC and Cmin decreased by 30%, 35%, and 45%, respectively. Lopinavir Cmax, AUC and Cmin decreased by 11%, 13% and 20%, respectively.
Intelence US Prescribing Information, Janssen Therapeutics, July 2019.
The interaction between etravirine (200 mg twice daily) and the tablet formulation of lopinavir/ritonavir (400/100 mg twice daily) was studied in 16 HIV- subjects. Coadministration decreased etravirine AUC, Cmax and Cmin by 35%, 30% and 45%, respectively; lopinavir AUC, Cmax and Cmin decreased by 13%, 11% and 20%, respectively. There was no change in the pharmacokinetics of ritonavir.
Pharmacokinetic interaction between etravirine and lopinavir/ritonavir. Scholler-Gyure M, Kakuda TN, Akuma SH, et al. 49th Interscience Conference on Antimicrobial Agents and Chemotherapy, San Francisco, September 2009, abstract A1-1298.
Coadministration of etravirine (1600 mg twice daily, phase II formulation) and lopinavir/ritonavir (400/100 mg twice daily) was studied in HIV- subjects. Coadministration increase etravirine AUC (17%), Cmax (15%) and Cmin (23%). Lopinavir AUC, Cmax and Cmin decreased by 19%, 15% and 8% respectively; there was no effect on ritonavir pharmacokinetics. These data suggest that no dosage adjustment is required when etravirine and lopinavir/ritonavir are coadministered.
TMC125 does not alter lopinavir/ritonavir pharmacokinetics in healthy volunteers. Piscitelli SC, Baede P, Van’t Klooster G, Graham. 42nd Interscience Conference on Antimicrobial Agents and Chemotherapy, San Diego, September 2002, abstract A-1824.
Lopinavir/Saquinavir/Ritonavir
The effect of adding etravirine (800 mg twice daily, phase II formulation) to a regimen of lopinavir/ritonavir (400/100 mg twice daily) plus saquinavir (800 or 1000 mg twice daily) was studied in 11 HIV+ subjects. Coadministration had no statistically significant effect on saquinavir AUC (13% decrease), Cmax (15% decrease) or Cmin (13% decrease). Similarly, ritonavir pharmacokinetics were not significantly altered (13% decrease in AUC, 11% decrease in Cmax, 12% decrease in Cmin). However, there was a statistically significant decrease in lopinavir AUC (18%) and Cmax (16%), but the decrease in Cmin (24%) was not significant. The authors conclude that the changes in plasma PI concentrations are unlikely to be clinically significant.
Pharmacokinetics and safety of adding TMC125 to stable regimens of saquinavir, lopinavir, ritonavir, and NRTI in HIV+ adults. Harris M, Zala C, Ramierez S, et al. 13th Conference on Retroviruses and Opportunistic Infections, Denver, February, 2006, abstract 575b.
View all available interactions with Lopinavir/ritonavir (LPV/r) by clicking here.
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