Raltegravir + Sofosbuvir = Unknown or no reaction

Effect on Concentration

Raltegravir
No change
Applies within class?
No
Sofosbuvir
No change
Applies within class?
No

Pharmacologic Effects

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

Interaction History

N/A

Last Updated 16-Jul-2018

Summary

Sources

Drug interactions between direct acting anti-HCV antivirals sofosbuvir and ledipasvir and HIV antiretrovirals. ^

Study Design

In a phase 1, fixed sequence, cohort study, healthy volunteers received a single dose of sofosbuvir (SOF) 400 mg before and after 10 days of raltegravir (RAL, 400 mg BID, n=19, fasted). SOF was administered on Day 1, followed by a 3-day washout period. RAL was then administered on days 5-14, followed by RAL + single dose SOF on day 15. Geometric means ratio (GMR) (90% CI) of PK parameters AUCinf and Cmax for SOF and GS-331007 (circulating nucleoside metabolite of SOF), as well as AUCtau, Cmax, and Ctau for RAL were evaluated against a predetermined 70-143% equivalence boundary.

Study Results

Co-administration of SOF with RAL did not result in any clinically relevant changes in PK parameters of SOF or GS-331007 (major circulating metabolite); AUCinf and Cmax were 0.95 (0.82-1.09) and 0.87 (0.71-1.08), respectively, for SOF and 1.03 (0.97-1.08) and 1.09 (0.99-1.20), respectively, for GS-331007. Exposure of RAL was decreased; AUCtau, Cmax and Ctau were 0.73 (0.59-0.91), 0.57 (0.44-0.75) and 0.95 (0.81-1.12), respectively, when co-administered with SOF. Lower exposure of RAL was comparable to that observed when RAL was co-administered with tipranavir/ritonavir and efavirenz, which did not necessitate RAL dose adjustment. The manufacturer states that this interaction is not clinically significant and that no dose adjustment is necessary for either agent when RAL and SOF are administered together.

Study Conclusions

The manufacturer states that this interaction is not clinically significant and that no dose adjustment is necessary for either agent when RAL and SOF are administered together.

References

German P, Pang P, West S, Han L, Sajwani K, Mathias A. Drug interactions between direct acting anti-hcv antivirals sofosbuvir and ledipasvir and hiv antiretrovirals. International Workshop On Clinical Pharmacology Of Hiv And Hepatitis T Herapy . Washingston DC, USA. 15; May 2014.