Liverpool HIV Interactions

Potential Interaction

Lopinavir/ritonavir (LPV/r)

Emtricitabine/Tenofovir alafenamide for PrEP (FTC/TAF, PrEP)

Quality of Evidence: Low

Summary:

Emtricitabine and tenofovir alafenamide used as PrEP are not expected to be coadministered with antiretrovirals. Coadministration of lopinavir/ritonavir (800/200 mg once daily) with emtricitabine/tenofovir alafenamide (200/10 mg, once daily) increased tenofovir AUC and Cmax by 322% and 275% (n-10). No significant effects were observed on lopinavir pharmacokinetics relative to historical controls. Coadministration of lopinavir/ritonavir (800/200 mg once daily) and tenofovir alafenamide (10 mg once daily) increased tenofovir alafenamide AUC and Cmax by 47% and 119% but had no effect on lopinavir AUC or Cmax. When administered with lopinavir/ritonavir for the treatment of HIV, the recommended dose of Descovy is 200/10 mg once daily (where available).

Description:

When given with lopinavir/ritonavir, the dose of Descovy for HIV-1 treatment is 200/10 mg once daily. Co-administration of Descovy with medicinal products that inhibit P-gp and BCRP activity (e.g., ritonavir) are expected to increase the absorption and plasma concentration of tenofovir alafenamide. Coadministration of lopinavir/ritonavir (800/200 mg once daily) and tenofovir alafenamide (10 mg once daily) increased tenofovir alafenamide AUC and Cmax by 47% and 119%, with no change in lopinavir AUC, Cmax and Cmin.

Descovy Summary of Product Characteristics, Gilead Sciences Ltd, April 2022.

Based on drug interaction studies conducted with the components of Descovy, no clinically significant drug interactions have been either observed or are expected when Descovy is combined with lopinavir/ritonavir. Coadministration of lopinavir/ritonavir (800/200 mg once daily) and tenofovir alafenamide (10 mg once daily) was studied in 10 subjects. Tenofovir alafenamide Cmax and AUC increased by 119% and 47%; there was no change in lopinavir Cmax and AUC, but Cmin decreased by 2%.

Descovy US Prescribing Information, Gilead Sciences Inc, January 2022.

Coadministration of lopinavir/ritonavir (800/200 mg, once daily) with emtricitabine/tenofovir alafenamide (200/10 mg, once daily) was studied in 10 healthy volunteers in a crossover study. Tenofovir alafenamide AUC and Cmax increased by 47% and 119%, respectively. Tenofovir AUC and Cmax increased by 322% and 275%, respectively. Lopinavir pharmacokinetic parameters were similar to historical controls. The authors hypothesise that the increase in tenofovir alafenamide and tenofovir exposures are due to intestinal inhibition of P-gp and/or BCRP by ritonavir. Coadministration of lopinavir/ritonavir with tenofovir alafenamide is supported by tenofovir alafenamide safety data.

Pharmacokinetics of tenofovir alafenamide when coadministered with other HIV antiretrovirals. Begley R, Das M, Zhong L, et al. J Acquir Immune Defic Syndr, 2018, 78(4): 465-472.

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