Tipranavir

Tipranavir (TPV), or tipranavir disodium, is a nonpeptidic protease inhibitor (PI) manufactured by Boehringer Ingelheim under the trade name Aptivus /ˈæptɪvəs/ AP-tiv-əs. It is administered with ritonavir in combination therapy to treat HIV infection.

Tipranavir
Clinical data
Pronunciation/tɪpˈrænəvɪər/ tip-RAN-ə-veer
Trade namesAptivus
AHFS/Drugs.comMonograph
MedlinePlusa606009
License data
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
    Routes of
    administration    		By mouth (soft capsules)
    ATC code
    Legal status
    Legal status
    Pharmacokinetic data
    Protein binding99.9%
    MetabolismHepatic
    Elimination half-life4.8–6 hours
    ExcretionFeces (82.3%), urine (4.4%)
    Identifiers
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    ChEMBL
    NIAID ChemDB
    PDB ligand
    CompTox Dashboard (EPA)
    ECHA InfoCard100.158.066
    Chemical and physical data
    FormulaC31H33F3N2O5S
    Molar mass602.67 g·mol−1
    3D model (JSmol)
     NY (what is this?)  (verify)

    Tipranavir has the ability to inhibit the replication of viruses that are resistant to other protease inhibitors and it recommended for patients who are resistant to other treatments. Resistance to tipranavir itself seems to require multiple mutations.[1] Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008.[2]

    Tipranavir should only be taken in combination with ritonavir and other antiretroviral drugs, and is not approved for treatment-naïve patients.[3] Like lopinavir and atazanavir, it is very potent and is effective in salvage therapy for patients with drug resistance. However, side effects of tipranavir may be more severe than those of other antiretrovirals. Some side effects include intracranial hemorrhage, hepatitis, hepatic decompensation, hyperglycemia and diabetes mellitus. The drug has also been shown to cause increases in total cholesterol and triglycerides.[3]

    Aptivus labeling has a black box warning regarding hepatotoxicity and intracranial hemorrhage.[3]

    References
    1. Doyon L, Tremblay S, Bourgon L, Wardrop E, Cordingley MG (October 2005). "Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic protease inhibitor tipranavir". Antiviral Research. 68 (1): 27–35. doi:10.1016/j.antiviral.2005.07.003. PMID 16122817.
    2. "New Aptivus (tipranavir) Oral Solution Approved for Treatment-Experienced Pediatric and Adolescent HIV Patients" (Press release). Boehringer Ingelheim. 2008-06-24. Retrieved 2008-09-02.
    3. "Aptivus (tipranavir) Capsules, Oral Solution. Full Prescribing Information" (PDF). Boehringer Ingelheim Pharmaceuticals, Inc.
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