Tipranavir

drugbox
IUPAC_name = ["R"-("R*,R*")] -"N"- [3- [1- [5,6-dihydro-4-hydroxy-2-oxo-6-(2-phenylethyl)-6-propyl-2H-pyran-3-yl] propyl] phenyl] -5-(trifluoromethyl)-2-pyridinesulfonamide

---

CAS_number = 174484-41-4
ATC_prefix = J05
ATC_suffix = AE09
ATC_supplemental =
PubChem = 65027
DrugBank = APRD01306
C = 31 | H = 33 | N = 2 | O = 5 | F = 3 | S = 1
molecular_weight = 602.66 g/mol
bioavailability =
protein_bound = 99.9%
metabolism = Hepatic
elimination_half-life = 5–6 hours
excretion = Fecal
pregnancy_US = C
legal_UK = POM
legal_US = Rx-only
legal_status =
routes_of_administration = Oral
licence_EU =Aptivus
licence_US =Tipranavir

Tipranavir, or tipranavir disodium, is a nonpeptidic protease inhibitor (PI) manufactured by Boehringer-Ingelheim under the trade names Aptivus. It is administered with ritonavir in combination therapy to treat HIV infection and is given as two 250mg capsules together with 200mg of ritonavir twice daily.

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. [cite journal
author = Doyon L, Tremblay S, Bourgon L, Wardrop E, Cordingley M
title = Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic protease inhibitor tipranavir.
journal = Antiviral Res
volume = 68
issue = 1
pages = 27–35
year = 2005
pmid = 16122817
accessdate = 2006-01-20
doi = 10.1016/j.antiviral.2005.07.003]

Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005, and was approved for pediatric use on June 24, 2008. [cite press release
title = New Aptivus® (tipranavir) Oral Solution Approved for Treatment-Experienced Pediatric and Adolescent HIV Patients
publisher = Boehringer Ingelheim
date = 2008-06-24
url = http://us.boehringer-ingelheim.com/newsroom/2008/06-25-08_aptivus_pediatric.html
accessdate = 2008-09-02] Like lopinavir and atazanavir, it is very potent and is effective in "salvage" therapy for patients with some drug resistance. However, side effects of tipranavir can be more severe than other anti-retrovirals. Some side effects include intracranial hemorragingFact|date=February 2007, hepatitis ["Aptivus (tipranavir) Capsules, 250 mg, Prescribing Information", Boehringer Ingelheim, 2007. Revised February 5, 2007.] , and diabetes mellitusFact|date=February 2007. The drug has also been shown to cause increases in total cholesterol and triglyceridesFact|date=February 2007.

References