Metabolic substrate

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.

Metabolic inducer

–

Metabolic inhibitor

Ledipasvir : P-gp and BCRP (intestinal weak), OATP1B1/1B3, BSEP and UGT1A1 (hepatic only at doses higher than those obtained in the clinic)

Pharmacodynamic effects

Possible decrease of clinical efficacy.

Recommendations

–

Alternative solution(s)

–

Metabolic substrate

3A4 (mainly), 2C8, 2C9 and 2C19

Metabolic inducer

3A4 (potent), 2C9 and 2C19 (weak), P-gp

Metabolic inhibitor

–

Pharmacodynamic effects

–

Recommendations

Contraindicated. Use alternative.

Alternative solution(s)

Selective inhibitor serotonin reuptake (SSRIs)