Products
Darunavir is commercially available as film-coated tablets and as an oral suspension (Prezista). It has been approved in many countries since 2006. In 2016, a fixed-dose combination with cobicistat was approved (Rezolsta film-coated tablets). In 2018, generic versions of the tablets entered the market.
Structure and properties
Darunavir (C27H37N3O7S, Mr = 547.7 g/mol) is present in drugs as darunavir ethanolate, a white powder. Darunavir has a nonpeptidic structure.
Effects
Darunavir (ATC J05AE10) has antiviral properties against HIV-1, with effects based on inhibition of HIV protease, which plays a central role in viral maturation and replication. The half-life with ritonavir is approximately 15 hours.
Indications
For the treatment of HIV-1 infection (combination antiretroviral therapy).
Dosage
According to the SmPC. Tablets are taken once or twice daily with food. Darunavir is combined with a pharmacokinetic booster such as ritonavir or cobicistat. These are CYP inhibitors that reduce the metabolic breakdown of the drug.
Contraindications
- Hypersensitivity
- Severe renal insufficiency
- Severe liver dysfunction
- Combination with certain drugs
Full details of precautions and interactions can be found in the drug label.
Interactions
Darunavir is metabolized predominantly by CYP3A4. Drug-drug interactions are possible with CYP substrates, inhibitors, and inducers.
Adverse effects
The most common possible adverse effects include diarrhea, nausea, rash, headache, abdominal pain, and vomiting.
