Tipranavir
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Tipranavir
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| Systematic (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 |
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| Identifiers | |
| CAS number | |
| ATC code | J05 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C31H33F3N2O5S |
| Mol. mass | 584.726 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Protein binding | 99.9% |
| Metabolism | Hepatic |
| Half life | 5-6 hours |
| Excretion | Fecal |
| Therapeutic considerations | |
| Licence data |
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| Pregnancy cat. |
C(US) |
| Legal status | |
| Routes | Oral |
Tipranavir, or tipranavir disodium, is a nonpeptidic protease inhibitor (PI) manufactured by Boehringer Ingelheim Pharmaceuticals Inc 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.[1] Tipranavir is given in combination with ritonavir 200 mg twice daily.
Tipranavir was approved by the Food and Drug Administration (FDA) on June 22, 2005. 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 hemorraging[citation needed], hepatitis[citation needed], and diabetes mellitus[citation needed]. The drug has also been shown to cause increases in total cholesterol and triglycerides[citation needed].
[edit] References
- ^ Doyon L, Tremblay S, Bourgon L, Wardrop E, Cordingley M (2005). "Selection and characterization of HIV-1 showing reduced susceptibility to the non-peptidic protease inhibitor tipranavir.". Antiviral Res 68 (1): 27-35. PMID 16122817. Retrieved on 2006-01-20.
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| Anti-herpesvirus | Aciclovir, Cidofovir, Docosanol, Famciclovir, Fomivirsen, Foscarnet, Ganciclovir, Idoxuridine, Penciclovir, Trifluridine, Tromantadine, Valaciclovir, Valganciclovir, Vidarabine |
| Anti-influenza agents | Amantadine, Arbidol, Oseltamivir, Peramivir, Rimantadine, Zanamivir |
| Antiretrovirals: NRTIs | Abacavir, Didanosine, Emtricitabine, Lamivudine, Stavudine, Zalcitabine, Zidovudine |
| Antiretrovirals: NtRTIs | Tenofovir |
| Antiretrovirals: NNRTIs | Efavirenz, Delavirdine, Nevirapine, Loviride |
| Antiretrovirals: PIs | Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir |
| Antiretrovirals: Fusion inhibitors | Enfuvirtide |
| Other antiviral agents | Adefovir, Fomivirsen, Imiquimod, Inosine, Interferon, Podophyllotoxin, Ribavirin, Viramidine |
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