Tenofovir Disoproxil Fumarate + Myrcludex B = Unknown or no reaction

Effect on Concentration

Tenofovir Disoproxil Fumarate
No change
Applies within class?
No
Myrcludex B
No change
Applies within class?
No

Pharmacologic Effects

Tenofovir Disoproxil Fumarate
Effect
N/A
Applies within class?
No
Myrcludex B
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 20-Jul-2018

Summary

Sources

Tenofovir Disoproxil Fumarate versus Myrcludex B ^

Study Design

This was a phase 1, open label, prospective trial to evaluate a potential drug interaction between tenofovir disoproxil fumarate (TDF) and myrcludex B. A total of (n=12) healthy subjects received 245mg of TDF for 5 days followed by 6 days of daily subcutaneous co-administration of 10mg myrcludex B with TDF. The effects of myrcludex B on tenofovir bile acid pharmacokinetics was quantified using LC-MS/MS methods.

Study Results

Before and during myrcludex B administration the area under the TDF concentration-time curve (AUC) was 0.94 (90% confidence interval: 0.85-1.05) and the ratio of TDF peak plasma concentration was 0.85 with a 90% CI (0.71-1.03) extending below bioequivalence boundaries. A single asymptomatic grade three level increase in lipase levels occurred; other than this only mild-transient adverse events were noted.

Study Conclusions

Per the authors, co-administration of TDF and myrcludex B was well tolerated and did not alter tenofovir pharmacokinetics.

References

Blank A, Eidam A, Haag M, Hohmann N, Burhenne J, Witt L. Myrcludex b and tenofovir: assessment of the effect on plasma bile acid profiles and tenofovir pharmacokinetics. Ilc: International Liver Congress. Barcelona, Spain. 2016; April 2016.