Products
Remdesivir is commercially available as a powder for a concentrate for the preparation of an infusion solution (Veklury, Gilead Sciences Inc, USA). Provisional approval was granted in many countries and in the EU in July 2020. On November 25, 2020, the approval will be granted. In the U.S., the drug was registered in October.
Structure and properties
Remdesivir (C27H35N6O8P, Mr = 602.6 g/mol) is an analog of the nucleoside adenosine and is a monophosphoramidate prodrug of the active GS-441524 that is additionally triphosphorylated in target cells. Background information on the structure can also be found in the article Nucleic Acids.
Effects
Remdesivir has antiviral properties with a broad spectrum of activity against a number of RNA viruses. These include coronaviruses such as SARS-CoV-2 and MERS-CoV, as well as Ebola virus and respiratory syncytial virus (RSV). Its effects are based on integration into viral RNA, leading to premature termination of synthesis. It selectively inhibits viral RNA polymerase, viral RNA synthesis, and viral replication. The triphosphate of the active compound competes with the natural substrate adenosine triphosphate (ATP). The active metabolite GS-441524 has a half-life of 27 hours.
Indications
For the treatment of coronavirus disease Covid-19 in adults and adolescents 12 years of age and older who have SARS-CoV-2-related pneumonia and require supplemental oxygen.
Dosage
The drug is administered as an intravenous infusion.
Contraindications
- Hypersensitivity
For complete precautions, see the drug label.
Interactions
Remdesivir is a substrate of CYP2C8, CYP2D6, and CYP3A4, as well as OATP1B1 and P-glycoprotein. Combination with chloroquine or hydroxychloroquine is not recommended.
Adverse effects
The most common potential adverse effects include headache, nausea, elevated transaminases, and a rash.
