Tipranavir

Products

Tipranavir is commercially available in capsule form (Aptivus). It has been approved in many countries since 2005.

Structure and properties

Tipranavir (C31H33F3N2O5S, Mr = 602.7 g/mol) exists as a white to slightly yellowish substance that is insoluble in an aqueous buffer at pH 7.5. Tipranavir has a nonpeptidic structure.

Effects

Tipranavir (ATC J05AE09) has antiviral properties against HIV-1, with effects based on inhibition of HIV protease, which plays a central role in viral maturation and replication.

Indications

For treatment of patients with HIV infection (in combination with low-dose ritonavir, combination antiretroviral therapy).

Dosage

According to the SmPC. The drug is taken in combination with low-dose ritonavir twice daily with food.

Contraindications

  • Hypersensitivity
  • Moderate to severe hepatic insufficiency
  • Combination with certain drugs

Full precautions can be found in the drug label. Both physician and patient must be alert for incipient signs or symptoms of hepatitis.

Interactions

Tipranavir is metabolized primarily by CYP3A4 and appropriate drug interactions with CYP inhibitors, inducers, and inhibitors are possible.

Adverse effects

The most common possible adverse effects include diarrhea, nausea, headache, fever, vomiting, fatigue, and abdominal pain. Tipranavir has liver toxic properties and may cause hepatitis and severe liver disease. Patients must be informed and monitored accordingly.