Tipranavir

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


Wikimedia Foundation. 2010.

Игры ⚽ Поможем сделать НИР

Look at other dictionaries:

  • Tipranavir — Nombre (IUPAC) sistemático [R (R*,R*)] N [3 [1 [5,6 dihidro 4 hidroxi 2 oxo 6 (2 feniletil) 6 propil 2H piran 3 il]propil]fenil] 5 (trifluorometil) 2 pir …   Wikipedia Español

  • Tipranavir — Strukturformel Allgemeines Freiname Tipranavir Ander …   Deutsch Wikipedia

  • tipranavir disodium — noun The salt form of the protease inhibitor drug tipranavir used in the treatment of HIV infected patients …   Wiktionary

  • tipranavir — noun An anti retroviral drug of the protease inhibitor class that is used in to treat HIV infected patients …   Wiktionary

  • tipranavir — ti·pran·a·vir (ti pranґə vir) an HIV protease inhibitor used in treatment of human immunodeficiency virus infection and the acquired immunodeficiency syndrome; administered orally …   Medical dictionary

  • Discovery and development of HIV-protease inhibitors — Many major physiological processes depend on regulation of proteolytic enzyme activity and there can be dramatic consequences when equilibrium between an enzyme and its substrates is disturbed. In this prospective, the discovery of small molecule …   Wikipedia

  • HAART — Der Begriff Hochaktive antiretrovirale Therapie, abgekürzt HAART, englisch Highly Active Anti Retroviral Therapy, bezeichnet eine 1996 eingeführte Kombinationstherapie aus mindestens drei verschiedenen antiretroviralen Medikamenten (ARV) zur… …   Deutsch Wikipedia

  • Highly Active Antiretroviral Therapy — Der Begriff Hochaktive antiretrovirale Therapie, abgekürzt HAART, englisch Highly Active Anti Retroviral Therapy, bezeichnet eine 1996 eingeführte Kombinationstherapie aus mindestens drei verschiedenen antiretroviralen Medikamenten (ARV) zur… …   Deutsch Wikipedia

  • Kombi-Therapie — Der Begriff Hochaktive antiretrovirale Therapie, abgekürzt HAART, englisch Highly Active Anti Retroviral Therapy, bezeichnet eine 1996 eingeführte Kombinationstherapie aus mindestens drei verschiedenen antiretroviralen Medikamenten (ARV) zur… …   Deutsch Wikipedia

  • Compassionate-Use — Unter dem englischen Begriff Compassionate Use (wörtliche Übersetzung: „Anwendung aus Mitgefühl“) versteht man den Einsatz (noch) nicht zugelassener Arzneimittel an Patienten. In der deutschen Sprache gibt es kein unmittelbares Äquivalent. In der …   Deutsch Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”