Ledipasvir (GS5885)

Description: Ledipasvir (formerly GS5885; GS-5885; trade name Harvoni) is a novel and potent HCV NS5A polymerase inhibitor that is used for the treatment of HCV-hepatitis C virus infection. As an inhibitor of the hepatitis C virus NS5A, it has EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively. The combination product of ledipasvir 90 mg/sofosbuvir 400 mg (trade name Harvoni) was approved by FDA in October 2014. The ledipasvir/sofosbuvir combination is a direct-acting antiviral agent that interferes with HCV replication and can be used to treat patients with genotypes 1a or 1b without PEG-interferon or ribavirin. Ledipasvir has an extended plasma half-life of 37-45 h in healthy volunteers and produces a rapid > 3 log viral load reduction in monotherapy at oral doses of 3 mg or greater with once-daily dosing in genotype 1a HCV-infected patients. It has been shown to be safe and efficacious, with SVR12 rates up to 100% when used in combination with direct-acting antivirals having complementary mechanisms.

References: J Med Chem. 2014 Mar 13; 57(5):2033-46.

Related CAS: 1441674-54-9 (Ledipasvir acetone); 1502655-48-2 (Ledipasvir diacetone); 1502654-87-6 (Ledipasvir D-tartrate)