Products
Simeprevir was approved in capsule form in the United States in 2013, in the EU in 2014, and in many countries in 2015 (Olysio).
Structure and properties
Simeprevir (C38H47N5O7S2, Mr = 749.9 g/mol) is present in the drug product as simeprevir sodium. The macrocyclic molecule contains a sulfonamide moiety, which may cause adverse effects (skin reactions).
Effects
Simeprevir (ATC J05AE14) has antiviral properties against HCV. The effects are due to noncovalent inhibition of the viral enzyme NS3/4A protease. This enzyme plays an essential role in viral replication.
Indications
For the treatment of chronic hepatitis C as part of combination therapy (peginterferon alfa, ribavirin).
Dosage
According to the SmPC. Capsules are taken once daily for 12 weeks with a meal.
Contraindications
Simeprevir is contraindicated in the presence of hypersensitivity, in combination with moderate to strong CYP3A inducers, and due to its fertility-damaging properties during pregnancy. For complete precautions, see the drug label.
Interactions
Simeprevir is metabolized primarily by CYP3A. Corresponding drug-drug interactions with CYP inhibitors and inducers are possible. Simeprevir is a substrate of P-glycoprotein, OATP1B1/3, BCRP, and MRP2.
Adverse effects
The most common potential adverse effects include rash, pruritus, and nausea. Simeprevir may make the skin sensitive to UV and sunlight (photosensitization).
