How is sofosbuvir metabolized?

How is sofosbuvir metabolized?

After entering hepatocytes, sofosbuvir is metabolized by carboxylesterase 1 (CES1) cleavage to form metabolite X (10). Efficient metabolism by CES1 results in high first-pass hepatic extraction of sofosbuvir (likely >70%). Subsequent phosphoramidase cleavage releases the monophosphate metabolite.

How is Epclusa metabolized?

Velpatasvir is a substrate of and metabolized by CYP2B6, CYP2C8, and CYP3A4. Velpatasvir is not an inducer or inhibitor of any of these aforementioned CYP enzymes. Elimination: Kidney: 80% of the sofosbuvir dose is excreted in the urine.

What is Sofosbuvir Velpatasvir used for?

Sofosbuvir and velpatasvir combination is used with or without ribavirin to treat chronic hepatitis C genotype 1, 2, 3, 4, 5, or 6 infection (including with or without cirrhosis). This medicine is available only with your doctor’s prescription. This product is available in the following dosage forms: Packet.

Is velpatasvir a protease inhibitor?

Velpatasvir | ≥99%(HPLC) | Selleck | HCV Protease inhibitor.

Why is sofosbuvir a prodrug?

Mechanism of action. Sofosbuvir inhibits the hepatitis C NS5B protein. Sofosbuvir appears to have a high barrier to the development of resistance. Sofosbuvir is a prodrug of the Protide type, whereby the active phosphorylated nucleotide is granted cell permeability and oral bioavailability.

What is the mechanism of action of sofosbuvir?

Sovaldi’s mechanism of action The drug is a direct-acting antiviral agent and interferes with the HCV lifecycle, restraining viral replication. It can be incorporated into HCV RNA by the NS5B polymerase and acts as a chain terminator. The drug is available for oral use in the form of 400mg tablets.

How does Epclusa work on the liver?

Epclusa contains two antiviral ingredients, sofosbuvir and velpatasvir, and may be used to treat hepatitis C. Sofosbuvir interferes with the reproduction of genetic material of the hepatitis C virus, by inhibiting an RNA-dependent polymerase called HCV NS5B, which is also needed by the virus to replicate itself.

What are the side effects of sofosbuvir and velpatasvir?


  • Chest pain or discomfort.
  • large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs.
  • lightheadedness, dizziness or fainting.
  • skin rash, sometimes with blisters or hive-like swelling.
  • slow or irregular heartbeat.
  • unconsciousness.
  • unusual tiredness.

When do we use Vosevi?

VOSEVI is a prescription medicine used to treat adults with chronic (lasting a long time) hepatitis C (Hep C) genotype 1, 2, 3, 4, 5, or 6 infection with or without cirrhosis (compensated) who have previously been treated with a Hep C regimen containing an NS5A inhibitor.

What is NS5A inhibitor?

Non-structural protein 5A (NS5A) inhibitors are a direct-acting antiviral agent used to treat hepatitis C virus (HCV). The NS5A protein has a substantial role in viral replication, packaging, assembly and complex interactions with cellular functions.