Bedaquiline + Rifampin = Prohibited

Effect on Concentration

Bedaquiline
Decrease
Applies within class?
No
Rifampin
Unknown
Applies within class?
No

Pharmacologic Effects

Bedaquiline
Effect
N/A
Applies within class?
No
Rifampin
Effect
N/A
Applies within class?
No

Interaction History

N/A

Last Updated 22-Nov-2022

Summary

The authors recommend avoiding rifampin when constructing bedaquiline-containing anti-tuberculosis regimens.

Sources

Bedaquiline vs rifampicine or rifapentine ^

Study Design

Healthy volunteers (n=29) were administered a single dose of 400 mg of bedaquiline (TMC207). Cmax and AUC were determined for bedaquiline and its less active metabolite (M2).Then, subjects were administered either 600 mg of rifampin or 600 mg of rifapentine for 22 days. On day 10, a single dose of 400 mg of bedaquiline was administered, and the Cmax and AUC of bedaquiline and M2 were again determined.

Study Results

Rifampin had a greater effect on bedaquiline than its metabolite, M2.On average, rifampin decreased the bedaquiline Cmax by 39.8% and its AUC by 58.6%.

Study Conclusions

References

MOAB0304 Everitt D, H Winter, E Egizi. Pharmacokinetic interaction between the investigational anti-tuberculosis agent tmc207 and rifampicin and rifapentin. Xix International Aids Conference. Washington, D.C., USA. ; 2012.