Products
Doravirin was approved in the US and EU in 2018 and in many countries in 2019 in film-coated tablet form (Pifeltro). It is also combined with lamivudine and tenofovirdisoproxil fixed (Delstrigo).
Structure and properties
Doravirin (C17H11ClF3N5O3, Mr = 425.8 g/mol) is a pyridinone and triazole derivative that is practically insoluble in water. The drug has a non-nucleoside structure (NNRTI).
Effects
Doravirin (ATC J05AG06) has antiviral properties. The effects are due to inhibition of the viral enzyme reverse transcriptase, which plays an important role in viral replication. It converts single-stranded RNA into double-stranded DNA, which is inserted into the human genome by integrase. Doravirin is also effective against the major mutant variants of HIV. The half-life is approximately 15 hours.
Indications
In combination with other antiretroviral agents for the treatment of HIV-1 virus infection.
Dosage
According to the SmPC. The tablet is taken once daily, regardless of meals.
Contraindications
- Hypersensitivity
- Combination with strong CYP450 inducers such as rifampicin or carbamamzepine.
Full precautions can be found in the drug label.
Interactions
Doravirin is a substrate of CYP3A and corresponding drug-drug interactions may occur.
Adverse effects
The most common possible adverse effects include nausea, dizziness, headache, fatigue, diarrhea, abdominal pain, and unusual dreams.
