Nelfinavir

Products

Nelfinavir was commercially available in the form of film-coated tablets (Viracept). It was approved in many countries in 1997 and withdrawn from the market in 2013 for commercial reasons.

Structure and properties

Nelfinavir (C32H45N3O4S, Mr = 567.8 g/mol) is present in the drug as nelfinavir mesilate, a white, amorphous powder that is sparingly soluble in water at an acidic pH.

Effects

Nelfinavir (ATC J05AE04) has antiviral properties. The effects are due to inhibition of HIV protease, which plays an important role in viral maturation and replication.

Indications

For treatment of infection with HIV (combination antiretroviral therapy).

Dosage

According to the SmPC. Tablets are taken two to three times daily with a meal containing fat.

Contraindications

Nelfinavir is contraindicated in hypersensitivity, during lactation, and in combination with rifampicin, omeprazole, and St. John’s wort. It should not be co-administered with CYP3A4 substrates, which have a narrow therapeutic range. For complete precautions and drug-drug interactions, see the Drug Information Leaflet.

Interactions

Nelfinavir is metabolized by CYP3A, CYP2C19, CYP2C9, and CYP2D6. Corresponding interactions are possible.

Adverse effects

The most common possible adverse effects include diarrhea, flatulence, nausea, vomiting, rash, weakness, and hypersensitivity reactions.