Velpatasvir

Velpatasvir is an NS5A inhibitor (by Gilead) which is used together with sofosbuvir in the treatment of hepatitis C infection of all six major genotypes.

Pharmacology

Mechanism of action

Further information: Discovery and development of NS5A inhibitors § Mechanism of action

The substance blocks NS5A, a protein necessary for hepatitis C virus replication and assembly.

Pharmacokinetics

Velpatasvir reaches highest blood plasma levels three hours after oral intake together with sofosbuvir. Plasma protein binding is over 99.5%. It is slowly metabolised by the liver enzymes CYP2B6, CYP2C8 and CYP3A4. While monohydroxylated and demethylated metabolites have been identified in human blood plasma and faeces, over 98% of the circulating substance is velpatasvir itself.[3] 94% are excreted via the faeces, and only 0.4% via the urine. Biological half-life is about 15 hours