Products
Sofosbuvir is commercially available in the form of film-coated tablets (Sovaldi). It was approved in the United States and EU in 2013 and in many countries in 2014. The very high price of the drug has been a source of debate. Sofosbuvir is also combined fixed with ledipasvir (Harvoni). Cheaper generics are available in India (e.g., MyHep, MyHep LVIR). Another fixed combination is Epclusa with velpatasvir and Vosevi with velpatasvir and voxilaprevir.
Structure and properties
Sofosbuvir (C22H29FN3O9P, Mr = 529.5 g/mol) is a prodrug that is intracellularly phosphorylated to the active uridine triphosphate analog GS-461203. Uridine is a component of ribonucleic acid (RNA). Sofosbuvir exists as a white crystalline powder and is sparingly soluble in water.
Effects
Sofosbuvir (ATC J05AX15) has antiviral properties. The effects are due to inhibition of the viral enzyme RNA-dependent RNA polymerase NS5B. The active ingredient is integrated into the RNA and leads to chain termination. This stops the virus from replicating. With the treatment, a permanent cure from the disease can be achieved. Ribavarin- and interferon-free combination therapies exist.
Indications
For the treatment of chronic hepatitis C (combination therapy).
Dosage
According to the SmPC. Tablets are taken once daily with a meal.
Contraindications
- Hypersensitivity
- Pregnancy
Full precautions can be found in the drug label.
Interactions
Sofosbuvir is a substrate of P-glycoprotein and of BCRP (breast cancer resistance protein). Corresponding drug-drug interactions are possible.
Adverse effects
The most common potential adverse effects of combination therapy include fatigue, headache, nausea, sleep disturbances, and anemia.