Liverpool HIV Interactions

Potential Weak Interaction

Rilpivirine (RPV)

Lopinavir/ritonavir (LPV/r)

Quality of Evidence: Low

Summary:

No dose adjustment is required when rilpivirine is co-administered with lopinavir/ritonavir. Coadministration of rilpivirine (150 mg once daily) and lopinavir/ritonavir (400/100 mg twice daily) increased rilpivirine Cmax, AUC and Cmin by 29%, 52% and 74%, respectively. Lopinavir Cmax, AUC and Cmin decreased by 4%, 1% and 11%, respectively. [Note: this interaction study has been performed with a dose higher than the licensed dose for rilpivirine assessing the maximal effect on the co-administered drug. The dosing recommendation is applicable to the licensed dose of rilpivirine 25 mg once daily.] Both lopinavir and rilpivirine have risks of QT prolongation and/or TdP on the CredibleMeds.org website (possible risk for lopinavir; possible risk for rilpivirine). Although the product label for lopinavir advises caution when prescribing lopinavir with medicinal products which have the potential to increase the QT interval, there is no anticipated increased risk of QT prolongation when combining these drugs. Rilpivirine has been associated with prolongation of the QTc interval at supra-therapeutic doses but equivalent rilpivirine concentrations are unlikely to occur during coadministration with lopinavir/ritonavir.

Description:

Concomitant use of Kaletra with rilpivirine causes an increase in the plasma concentrations of rilpivirine, but no dose adjustment is required. Coadministration with Kaletra capsules (400/100 mg twice daily) increased rilpivirine AUC, Cmin and Cmax by 52%, 74% and 29%, respectively. There was no change in lopinavir AUC or Cmax, but Cmin decreased by 11%.

Kaletra Summary of Product Characteristics, AbbVie Ltd, January 2021.

Drug interaction studies reveal no clinically significant interaction between Kaletra and rilpivirine. Coadministration of rilpivirine (150 mg once daily) and lopinavir/ritonavir (400/100 mg twice daily) was studied in 15 subjects. Lopinavir Cmax, AUC and Cmin decreased by 4%, 1% and 11%, respectively. Rilpivirine Cmax, AUC and Cmin increased by 29%, 52% and 74%, respectively.

Kaletra Prescribing Information, AbbVie Inc, October 2020.

Concomitant use of rilpivirine with ritonavir-boosted PIs causes an increase in the plasma concentrations of rilpivirine, but no dose adjustment is required. Coadministration of lopinavir/ritonavir (400/100 mg twice daily, soft gel capsule) and a higher than the recommended dose of rilpivirine had no effect on lopinavir AUC or Cmax, but decreased Cmin by 11%. Rilpivirine AUC, Cmin and Cmax increased by 52%, 74% and 29%, respectively, due to inhibition of CYP3A enzymes.

Edurant Summary of Product Characteristics, Janssen-Cilag Ltd, January 2019.

Concomitant use of rilpivirine with lopinavir/ritonavir may cause an increase in the plasma concentrations of rilpivirine (inhibition of CYP3A enzymes). No dose adjustment is required when rilpivirine is co-administered with lopinavir/ritonavir. Coadministration of rilpivirine (150 mg once daily) and lopinavir/ritonavir (400/100 mg twice daily) was studied in 15 subjects. Rilpivirine Cmax, AUC and Cmin increased by 29%, 52% and 74%, respectively. Lopinavir Cmax, AUC and Cmin decreased by 4%, 1% and 11%, respectively.

Edurant US Prescribing Information, Janssen Therapeutics, May 2019.

Coadministration of rilpivirine (150 mg once daily) and lopinavir/ritonavir (400/100 mg twice daily) was studied in 15 HIV-negative subjects. Rilpivirine Cmax, AUC and Cmin increased by 29%, 52% and 74%, respectively. Lopinavir Cmax, AUC and Cmin decreased by 4%, 1% and 11%, respectively.
Hoetelmans R, et al. Pharmacokinetic interaction between TMC278, an investigational non-nucleoside reverse transcriptase inhibitor, and lopinavir/ritonavir in healthy volunteers. 10th European AIDS Conference, Dublin, October 2005, abstract P4.3/1.

View all available interactions with Rilpivirine (RPV) by clicking here.