Document made available to the pharmacist to communicate a drug interaction to the doctor.DOWNLOAD
Rifampin may induce P-gp and decrease the plasma concentration of Ledipasvir / Sofosbuvir.
Ledipasvir : P-gp and BCRP; primarily excreted (>98%) unchanged in the feces, with little renal excretion, P-gp / Sofosbuvir : P-gp and BCRP; rapidly converted to the predominant circulating metabolite GS-331007 that accounts for greater than 90% of drug related material systemic exposure.
Ledipasvir : P-gp and BCRP (intestinal weak), OATP1B1/1B3, BSEP and UGT1A1 (hepatic only at doses higher than those obtained in the clinic)
Possible decrease of clinical efficacy.
1A2, 2C9, 2E1, P-gp
1A2, 2C9, 2C19, 3A4-7, UGT 1A1, P-gp
Contraindicated. Use alternative.
|90 mg *||400 mg **|
|x 1 *||x 1 **|
|- 35% *||- 77% ** †|
|- 59% *||- 72% ** †|
|600 mg||600 mg|
Ref #3073 : * Study conducted with ledipasvir administered as single agent and in the presence of two other investigational HCV direct-acting agents.
Ref #3082 : ** Study conducted with sofosbuvir administered as single agent.
† GS-331007, sofosbuvir active metabolite : AUC ±0% and Cmax +24%.