- 同
- Aptivus, TPV
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2016/01/18 15:16:54」(JST)
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Tipranavir
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Systematic (IUPAC) name |
N-{3-[(1R)-1-[(2R)-6-hydroxy-4-oxo-2-(2-phenylethyl)-2-propyl-3,4-dihydro-2H-pyran-5-yl]propyl]phenyl}-5-(trifluoromethyl)pyridine-2-sulfonamide
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Clinical data |
Trade names |
Aptivus |
AHFS/Drugs.com |
monograph |
MedlinePlus |
a606009 |
Licence data |
EMA:Link, US FDA:link |
Pregnancy
category |
- AU: B3
- US: C (Risk not ruled out)
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Legal status |
- UK: POM (Prescription only)
- US: ℞-only
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Routes of
administration |
Oral |
Pharmacokinetic data |
Bioavailability |
N/D |
Protein binding |
99.9% |
Metabolism |
Hepatic |
Biological half-life |
4.8–6 hours |
Excretion |
Feces (82.3%), urine (4.4%) |
Identifiers |
CAS Number |
174484-41-4 Y |
ATC code |
J05AE09 |
PubChem |
CID: 65027 |
DrugBank |
DB00932 Y |
ChemSpider |
10482313 Y |
UNII |
ZZT404XD09 Y |
ChEMBL |
CHEMBL183041 N |
NIAID ChemDB |
032941 |
PDB ligand ID |
TPV (PDBe, RCSB PDB) |
Chemical data |
Formula |
C31H33F3N2O5S |
Molecular mass |
602.66 g/mol |
SMILES
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CCC[C@]1(CC(/O)=C(\C(=O)O1)[C@H](CC)c3cccc(NS(=O)(=O)c2ccc(cn2)C(F)(F)F)c3)CCc4ccccc4
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InChI
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InChI=1S/C31H33F3N2O5S/c1-3-16-30(17-15-21-9-6-5-7-10-21)19-26(37)28(29(38)41-30)25(4-2)22-11-8-12-24(18-22)36-42(39,40)27-14-13-23(20-35-27)31(32,33)34/h5-14,18,20,25,36-37H,3-4,15-17,19H2,1-2H3/t25-,30-/m1/s1 Y
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Key:SUJUHGSWHZTSEU-FYBSXPHGSA-N Y
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NY (what is this?) (verify) |
Tipranavir, or tipranavir disodium, is a nonpeptidic protease inhibitor (PI) manufactured by Boehringer-Ingelheim under the trade name Aptivus. It is administered with ritonavir in combination therapy to treat HIV infection.
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] 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 may be more severe than those of other anti-retrovirals. Some side effects include intracranial hemorrhage, hepatitis, hyperglycemia and diabetes mellitus. The drug has also been shown to cause increases in total cholesterol and triglycerides.[3]
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. doi:10.1016/j.antiviral.2005.07.003. PMID 16122817.
- ^ "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.
- ^ "Aptivus® (tipranavir) capsules 250 mg, oral solution 100 mg/mL, Prescribing Information", Boehringer Inhelheim, 2012. Revised April 2012. [1]
Antiviral drugs: antiretroviral drugs used against HIV (primarily J05)
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Entry/fusion inhibitors
(Discovery and development) |
- gp41 (Enfuvirtide (ENF, T-20))
- CCR5 (Maraviroc (MVC)
- Vicriviroc†, Cenicriviroc†, PRO 140†)
- CD4 (Ibalizumab†)
- gp120 (Fostemsavir†)
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Reverse-transcriptase
inhibitors (RTIs) |
Nucleoside and
nucleotide (NRTI) |
- Nucleoside analogues/NRTIs: Abacavir (ABC)°#
- Didanosine (ddI)
- Emtricitabine (FTC)°
- Lamivudine (3TC)°#
- Stavudine (d4T)#
- Zidovudine (AZT, ZDV)#
- Amdoxovir†
- Apricitabine†
- Censavudine†
- Elvucitabine†
- Racivir†
- Stampidine†
- Zalcitabine (ddC)◊
- Nucleotide analogues/NtRTIs: Tenofovir disoproxil (TDF)°#
- Tenofovir alafenamide (TAF)
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Non-nucleoside (NNRTI)
(Discovery and development) |
- (1st generation) Efavirenz (EFV)°#
- Nevirapine (NVP)#
- Delavirdine (DLV)◊
(2nd generation) diarylpyrimidines (Etravirine (ETR)
- Rilpivirine (RPV)°)
- Doravirine
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Integrase inhibitors
(Integrase strand transfer inhibitors (INSTI)) |
- Dolutegravir (DTG)°
- Elvitegravir (EVG)°
- Raltegravir (RAL)°
- BI 224436†
- Globoidnan A (experimental)
- Cabotegravir†
- Bictegravir†
- MK-2048†
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Maturation inhibitors |
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Protease Inhibitors (PI)
(Discovery and development) |
1st generation |
- Amprenavir (APV)◊
- Fosamprenavir (FPV)
- Indinavir (IDV)◊
- Lopinavir (LPV)
- Nelfinavir (NFV)
- Ritonavir (RTV)#
- Saquinavir (SQV)#
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2nd generation |
- Atazanavir (ATV)°#
- Darunavir (DRV)°#
- Tipranavir (TPV)
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Combined formulations |
- Abacavir/lamivudine°#
- Abacavir/dolutegravir/lamivudine°
- Abacavir/lamivudine/zidovudine
- Atazanavir/cobicistat
- Darunavir/cobicistat
- Efavirenz/emtricitabine/tenofovir°#
- Elvitegravir/cobicistat/emtricitabine/tenofovir°
- Emtricitabine/rilpivirine/tenofovir°
- Lamivudine/raltegravir
- Lamivudine/zidovudine#
- Lopinavir/ritonavir°#
- Tenofovir/emtricitabine°#
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Pharmacokinetic boosters |
- Cobicistat (c)
- Ritonavir (r)#
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Experimental agents |
Uncoating inhibitors |
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Transcription inhibitors |
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Translation inhibitors |
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Other |
- Abzyme
- BIT225†
- Calanolide A
- Ceragenin
- Cyanovirin-N
- Diarylpyrimidines
- Epigallocatechin gallate (EGCG)
- KP-1461†
- Foscarnet
- Fosdevirine†
- Griffithsin
- Hydroxycarbamide
- Miltefosine
- Portmanteau inhibitors
- Scytovirin
- Seliciclib†
- Synergistic enhancers
- Tre recombinase
- Zinc finger protein transcription factor
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Failed agents |
- Aplaviroc
- Atevirdine
- Brecanavir
- Capravirine
- Dexelvucitabine
- Droxinavir
- Lasinavir
- Emivirine
- Lersivirine
- Lodenosine
- Loviride
- Mozenavir
- Palinavir
- Telinavir
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
°DHHS recommended initial regimen options. ◊Formerly or rarely used agent.
Index of viral disease
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Description |
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Disease |
- Systemic
- Cutaneous
- Zoster
- Human papillomavirus
- Zoonotic
- Symptoms and signs
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Treatment |
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UpToDate Contents
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English Journal
- Simplification to dual antiretroviral therapy including a ritonavir-boosted protease inhibitor in treatment-experienced HIV-1-infected patients.
- Burgos J, Crespo M, Falcó V, Curran A, Navarro J, Imaz A, Domingo P, Podzamczer D, Mateo MG, Villar S, Van den Eynde E, Ribera E, Pahissa A.SourceDepartment of Infectious Diseases, Hospital Universitari Vall d'Hebron, Universitat Autònoma de Barcelona, Barcelona, Spain.
- The Journal of antimicrobial chemotherapy.J Antimicrob Chemother.2012 Oct;67(10):2479-86. Epub 2012 Jun 22.
- OBJECTIVES: To assess the effectiveness of simplification to a dual antiretroviral regimen containing a ritonavir-boosted protease inhibitor (PI/r) in treatment-experienced HIV-1-infected patients.METHODS: Retrospective analysis of 131 HIV-1-infected patients on suppressive antiretroviral treatment
- PMID 22729925
- The Loss of Protease Dimerization Inhibition Activity of Tipranavir (TPV) and Its Association with HIV-1 Acquisition of Resistance to TPV.
- Aoki M, Danish ML, Aoki-Ogata H, Amano M, Ide K, Koh Y, Mitsuya H.SourceDepartments of Infectious Diseases and Hematology, Kumamoto University Graduate School of Medical Sciences, Kumamoto 860-8556, Japan.
- Journal of virology.J Virol.2012 Sep 26. [Epub ahead of print]
- Tipranavir (TPV), a protease inhibitor (PI) inhibiting the enzymatic activity and dimerization of HIV-1 protease, exerts potent activity against multi-PI-resistant HIV-1 isolates. When a mixture of eleven multi-PI-resistant (but TPV-sensitive) clinical isolates (HIV(11MIX)), which included HIV(B) an
- PMID 23015723
Japanese Journal
- A liquid chromatography-tandem mass spectrometry assay for quantification of nevirapine, indinavir, atazanavir, amprenavir, saquinavir, ritonavir, lopinavir, efavirenz, tipranavir, darunavir and maraviroc in the plasma of patients infected with HIV
- Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 877(27), 3072-3082, 2009-10-01
- NAID 10028025117
- A simple and sensitive assay for determining plasma tipranavir concentration in the clinical setting by new HPLC method
- Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 848(2), 374-378, 2007-04-01
- NAID 10025794196
- A simple high performance liquid chromatography assay for monitoring plasma concentrations of tipranavir in HIV infected patients
- Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 832(2), 317-320, 2006-03-07
- NAID 10025781021
Related Links
- Drug information on Tipranavir for patients and consumers ... What is tipranavir? Tipranavir is a prescription medicine approved by the U.S. Food and Drug Administration (FDA) for the treatment of HIV infection in adults ...
- Before taking tipranavir, tell your doctor and pharmacist if you are allergic to tipranavir, ritonavir (Norvir, in Kaletra), sulfa medications, any other medications, or any of the ingredients in tipranavir capsules or solution. Ask ...
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★リンクテーブル★
[★]
- 英
- tipranavir、tipranavir disodium
- 関
- チプラナビル二ナトリウム
[★]
- 関
- tipranavir