Generic
Sofosbuvir
13 brands available in the market
At a glance
Sofosbuvir is an HCV NS5B polymerase inhibitor used in combination with other antiviral agents for the treatment of chronic hepatitis C infection. It works by inhibiting viral replication.
Description
Sofosbuvir is a nucleotide analog inhibitor that specifically inhibits HCV NS5B RNA-dependent RNA polymerase. Following intracellular metabolism, the pharmacologically active uridine analog triphosphate (GS-461203) is formed, which is incorporated into HCV RNA by NS5B polymerase and acts as a chain terminator, stopping viral replication.
Indications
- Chronic hepatitis C (HCV) infection (genotypes 1, 2, 3, 4)
Therapeutic class
Hepatic Viral Infections (Hepatitis C)
Pharmacological class
HCV NS5B Polymerase Inhibitor
Pharmacology
Sofosbuvir is a nucleotide prodrug that is converted intracellularly to the active metabolite GS-461203. This active metabolite binds to the GDD active site of HCV NS5B RNA-dependent RNA polymerase, terminates viral RNA chain elongation, and prevents HCV replication.
Mechanism of action
Inhibits HCV NS5B polymerase to stop viral replication.
Dosage
Adult Dose (Oral):
- 400 mg tablet once daily (with or without food)
- Genotype 1 or 4: Sofosbuvir + Peginterferon alfa + Ribavirin (12 weeks)
- Genotype 2: Sofosbuvir + Ribavirin (12 weeks)
- Genotype 3: Sofosbuvir + Ribavirin (24 weeks)
- Hepatocellular carcinoma (awaiting liver transplant): Up to 48 weeks
Administration
- Take orally with or without food
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
- Do not stop without your doctor's advice
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects (≥20%):
- Fatigue
- Headache
- Nausea
- Insomnia
- Anemia
- Pruritus, asthenia, rash
- Decreased appetite, chills, pyrexia
- Diarrhea, neutropenia, myalgia
Precautions & warnings
- No dose recommendation for severe renal impairment or ESRD
- Serious bradycardia with amiodarone co-administration (caution)
- Caution in pregnancy and lactation (contraindicated with ribavirin combination)
Contraindications
- When used with ribavirin or peginterferon, their contraindications apply
- Combination with ribavirin is contraindicated in pregnant women
Drug interactions
- Strong P-gp inducers (rifampicin, St. John's wort, carbamazepine, phenytoin): Reduced therapeutic effect
- P-gp/BCRP inhibitors
- Amiodarone (with another DAA): Serious bradycardia
Food interactions
It is not known whether alcohol is safe with Sofosbuvir; consult your doctor.
Use in pregnancy
Use in Pregnancy: Generally safe; animal studies show low or no adverse effects; limited human data; combination with ribavirin is contraindicated; consult your doctor.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited data suggests no significant risk; consult your doctor.
Pediatric use
Safety and efficacy not established in children <18 years
Geriatric use
Response rates similar to younger patients; no dose adjustment needed
Renal / hepatic impairment
Renal Impairment: Mild-moderate: no dose adjustment; severe or ESRD: no dose recommendation; consult your doctor.
Hepatic Impairment: Safe in liver disease; no dose adjustment needed; consult your doctor.
Overdose effects
Highest dose: 1200 mg single dose; no specific antidote; monitor vital signs and provide supportive care.
Storage conditions
Store in a cool and dry place, protected from light; keep out of reach of children.
Chemical structure
Sofosbuvir