Identification
- Summary
-
Amprenaviris a protease inhibitor used to treat HIV infection.
- Generic Name
- Amprenavir
- DrugBank Accession Number
- DB00701
- Background
-
Amprenavir is a protease inhibitor used to treat HIV infection.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
-
Structure for Amprenavir (DB00701)
- Weight
-
Average: 505.627
Monoisotopic: 505.224656557 - Chemical Formula
- C25H35N3O6S
- Synonyms
-
- (3S)-Tetrahydro-3-furanyl ((1S,2R)-3-(((4-aminophenyl)sulfonyl)(2-methylpropyl)amino)-2-hydroxy-1-(phenylmethyl)propyl)carbamate
- Amprenavir
- Amprénavir
- Amprenavirum
- External IDs
-
- 141 W 94
- 141W94
- KVX 478
- KVX-478
- VX-478
Pharmacology
- Indication
-
For the treatment of HIV-1 infection in combination with other antiretroviral agents.
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with evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets. - Contraindications & Blackbox Warnings
-
Avoid life-threatening adverse drug eventsImprove clinical decision support with information oncontraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support. - Pharmacodynamics
-
Amprenavir is a protease inhibitor with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Protease inhibitors block the part of HIV called protease. HIV-1 protease is an enzyme required for the proteolytic cleavage of the viral polyprotein precursors into the individual functional proteins found in infectious HIV-1. Amprenavir binds to the protease active site and inhibits the activity of the enzyme. This inhibition prevents cleavage of the viral polyproteins resulting in the formation of immature non-infectious viral particles. Protease inhibitors are almost always used in combination with at least two other anti-HIV drugs.
- Mechanism of action
-
Amprenavir inhibits the HIV viral proteinase enzyme which prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles.
Target Actions Organism AHuman immunodeficiency virus type 1 protease inhibitorHuman immunodeficiency virus 1 - Absorption
-
Rapidly absorbed after oral administration in HIV-1-infected patients with a time to peak concentration (Tmax)之间的典型的1 and 2 hours after a single oral dose. The absolute oral bioavailability of amprenavir in humans has not been established.
- Volume of distribution
-
Not Available
- Protein binding
-
Very high (90%). Amprenavir has the highest affinity for alpha(1)-acid glycoprotein.
- Metabolism
-
Hepatic. Amprenavir is metabolized in the liver by the cytochrome P450 3A4 (CYP3A4) enzyme system. The 2 major metabolites result from oxidation of the tetrahydrofuran and aniline moieties. Glucuronide conjugates of oxidized metabolites have been identified as minor metabolites in urine and feces.
- Route of elimination
-
Not Available
- Half-life
-
7.1-10.6 hours
- Clearance
-
Not Available
- Adverse Effects
-
Improve decision support & research outcomesWith structured adverse effects data, including:blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data. - Toxicity
-
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRsBrowse all" title="" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug InteractionsLearn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
-
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Amprenavir. Abametapir The serum concentration of Amprenavir can be increased when it is combined with Abametapir. Abatacept The metabolism of Amprenavir can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Amprenavir. Abiraterone The metabolism of Abiraterone can be decreased when combined with Amprenavir. Abrocitinib The metabolism of Abrocitinib can be decreased when combined with Amprenavir. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Amprenavir. Acebutolol The metabolism of Amprenavir can be decreased when combined with Acebutolol. Acenocoumarol The metabolism of Acenocoumarol can be decreased when combined with Amprenavir. Acetaminophen The metabolism of Acetaminophen can be decreased when combined with Amprenavir. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
-
- Avoid alcohol. Drug impairs alcohol metabolism.
- Avoid fatty foods.
- Take with or without food.
Products
-
Drug product information from 10+ global regionsOur datasets provide approved product information including:
dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions. - International/Other Brands
- Agemerase (GlaxoSmithKline)/Prozei (Kissei Pharmaceuticals Co., Ltd.)
- Brand Name Prescription Products
-
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Agenerase 所以lution 15 mg/1mL Oral Glaxosmithkline Inc 1999-04-15 2008-10-31 US 
Agenerase Capsule 150 mg Oral Glaxo Group Limited 2016-09-07 2011-06-21 EU 
Agenerase Liquid 15 mg / mL Oral Glaxosmithkline Inc 2001-03-26 2008-05-27 Canada 
Agenerase Capsule 150 mg Oral Glaxosmithkline Inc 2001-03-16 2008-05-27 Canada Agenerase Capsule 150 mg Oral Glaxo Group Limited 2016-09-07 2011-06-21 EU Agenerase Capsule 50 mg/1 Oral Glaxosmithkline Inc 1999-04-15 2008-02-26 US Agenerase Capsule 50 mg Oral Glaxosmithkline Inc 2001-03-21 2008-05-27 Canada Agenerase 所以lution 15 mg/ml Oral Glaxo Group Limited 2016-09-07 2011-06-21 EU Agenerase Capsule 50 mg Oral Glaxo Group Limited 2016-09-07 2011-06-21 EU
Categories
- ATC Codes
- J05AE05 — Amprenavir
- Drug Categories
-
- Acids, Acyclic
- Amides
- Amprenavir and Prodrugs
- Anti-HIV Agents
- 抗感染的药物
- Anti-Retroviral Agents
- Antibiotics, Antitubercular
- Antiinfectives for Systemic Use
- Antiviral Agents
- Antivirals for Systemic Use
- 细胞色素P-450 CYP2B6 Inhibitors
- 细胞色素P-450 CYP2B6 Inhibitors (weak)
- 细胞色素P-450 CYP2C19 Inhibitors
- 细胞色素P-450 CYP2C19 inhibitors (strength unknown)
- 细胞色素P-450 CYP2C9 Substrates
- 细胞色素P-450 CYP2D6 Substrates
- 细胞色素P-450 CYP3A Inducers
- 细胞色素P-450 CYP3A Inhibitors
- 细胞色素P-450 CYP3A Substrates
- 细胞色素P-450 CYP3A4 Inducers
- 细胞色素P-450 CYP3A4 Inducers (strength unknown)
- 细胞色素P-450 CYP3A4 Inhibitors
- 细胞色素P-450 CYP3A4 Inhibitors (strength unknown)
- 细胞色素P-450 CYP3A4 Inhibitors (strong)
- 细胞色素P-450 CYP3A4 Substrates
- 细胞色素P-450 CYP3A5 Substrates
- 细胞色素P-450 Enzyme Inducers
- 细胞色素P-450 Enzyme Inhibitors
- 细胞色素P-450 Substrates
- Direct Acting Antivirals
- Drugs for Treatment of Tuberculosis
- Enzyme Inhibitors
- HIV Protease Inhibitors
- OATP1B1/SLCO1B1 Inhibitors
- P-glycoprotein inducers
- P-glycoprotein substrates
- Protease Inhibitors
- Sulfones
- Sulfur Compounds
- Viral Protease Inhibitors
- Chemical TaxonomyProvided byClassyfire
-
- Description
- This compound belongs to the class of organic compounds known as aminobenzenesulfonamides. These are organic compounds containing a benzenesulfonamide moiety with an amine group attached to the benzene ring.
- Kingdom
- Organic compounds
- Super Class
- Benzenoids
- Class
- Benzene and substituted derivatives
- Sub Class
- Benzenesulfonamides
- Direct Parent
- Aminobenzenesulfonamides
- Alternative Parents
- Phenylbutylamines/Amphetamines and derivatives/Benzenesulfonyl compounds/Aniline and substituted anilines/Organosulfonamides/Tetrahydrofurans/Aminosulfonyl compounds/Carbamate esters/二级醇/Organic carbonic acids and derivatives show 7 more
- Substituents
- Alcohol/Amine/Aminobenzenesulfonamide/Aminosulfonyl compound/Amphetamine or derivatives/Aniline or substituted anilines/Aromatic heteromonocyclic compound/Benzenesulfonyl group/Carbamic acid ester/Carbonic acid derivative show 21 more
- Molecular Framework
- Aromatic heteromonocyclic compounds
- External Descriptors
- carbamate ester, sulfonamide, tetrahydrofuryl ester (CHEBI:40050)
- Affected organisms
-
- Human Immunodeficiency Virus
Chemical Identifiers
- UNII
- 5S0W860XNR
- CAS number
- 161814-49-9
- InChI Key
- YMARZQAQMVYCKC-OEMFJLHTSA-N
- InChI
-
InChI=1S/C25H35N3O6S/c1-18(2)15-28(35(31,32)22-10-8-20(26)9-11-22)16-24(29)23(14-19-6-4-3-5-7-19)27-25(30)34-21-12-13-33-17-21/h3-11,18,21,23-24,29H,12-17,26H2,1-2H3,(H,27,30)/t21-,23-,24+/m0/s1
- IUPAC Name
-
(3S)-oxolan-3-yl N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropyl)4-aminobenzenesulfonamido]-1-phenylbutan-2-yl]carbamate
- SMILES
-
CC(C)CN(C[C@@H](O)[C@H](CC1=CC=CC=C1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)C1=CC=C(N)C=C1
References
- Synthesis Reference
- US5585397
- General References
- Not Available
- External Links
-
- Human Metabolome Database
- HMDB0014839
- KEGG Drug
- D00894
- KEGG Compound
- C08086
- PubChem Compound
- 65016
- PubChem Substance
- 46507537
- ChemSpider
- 58532
- BindingDB
- 577
- 228656
- ChEBI
- 40050
- ChEMBL
- CHEMBL116
- ZINC
- ZINC000003809192
- Therapeutic Targets Database
- DAP000170
- PharmGKB
- PA448422
- PDBe Ligand
- 478
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Amprenavir
- PDB Entries
- 1hpv/1t7j/3ekp/3ekv/3em3/3nu3/3nu4/3nu5/3nu6/3nu9… show 15 more
- FDA label
-
Download (120 KB)
Clinical Trials
- Clinical TrialsLearn More" title="" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
-
Phase Status Purpose Conditions Count 4 Completed Diagnostic Cardiovascular Disease (CVD)/HIV Lipodystrophy Syndrome 1 4 Completed Treatment Human Immunodeficiency Virus (HIV) Infections 1 4 Unknown Status Treatment Human Immunodeficiency Virus (HIV) Infections 1 3 Completed Treatment Human Immunodeficiency Virus (HIV) Infections 4 2 Completed Treatment Human Immunodeficiency Virus (HIV) Infections 17 2, 3 Completed Treatment Human Immunodeficiency Virus (HIV) Infections 2 1 Completed Treatment Acquired Immune Deficiency Syndrome (AIDS)/Human Immunodeficiency Virus (HIV) Infections 1 1 Completed Treatment Human Immunodeficiency Virus (HIV) Infections 4 1 Terminated Treatment Human Immunodeficiency Virus (HIV) Infections 1 Not Available Completed Not Available Coronavirus Disease 2019 (COVID‑19)/Human Immunodeficiency Virus (HIV) Infections 1
Pharmacoeconomics
- Manufacturers
-
- Glaxosmithkline
- Packagers
-
- Catalent Pharma Solutions
- Dosage Forms
-
Form Route Strength Capsule Oral Capsule Oral 150 mg Capsule Oral 50 mg/1 Capsule Oral 50 mg Liquid Oral 15 mg / mL 所以lution Oral 所以lution Oral 15 mg/ml 所以lution Oral 15 mg/1mL 所以lution Oral 1.5 g Capsule, liquid filled Oral 150 mg - Prices
-
Unit description 成本 Unit Agenerase 50 mg capsule 0.65USD capsule Agenerase 15 mg/ml Solution 0.21USD ml DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. - Patents
-
Patent Number Pediatric Extension Approved Expires (estimated) Region US5585397 No 1996-12-17 2013-12-17 US US6730679 No 2004-05-04 2017-11-11 US
Properties
- State
- 所以lid
- Experimental Properties
- Not Available
- Predicted Properties
-
Property Value 所以urce Water Solubility 0.0491 mg/mL ALOGPS logP 1.85 ALOGPS logP 2.43 Chemaxon logS -4 ALOGPS pKa (Strongest Acidic) 13.61 Chemaxon pKa (Strongest Basic) 2.39 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 131.19 Å2 Chemaxon Rotatable Bond Count 11 Chemaxon Refractivity 134.08 m3·mol-1 Chemaxon Polarizability 53.57 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
-
Property Value Probability Human Intestinal Absorption + 0.9132 Blood Brain Barrier - 0.5886 Caco-2 permeable + 0.8866 P-glycoprotein substrate Substrate 0.7175 P-glycoprotein inhibitor I Inhibitor 0.7973 P-glycoprotein inhibitor II Non-inhibitor 0.8383 Renal organic cation transporter Non-inhibitor 0.8815 CYP450 2C9 substrate Non-substrate 0.5 CYP450 2D6 substrate Substrate 0.8919 CYP450 3 a4衬底 Substrate 0.6176 CYP450 1A2 substrate Non-inhibitor 0.7641 CYP450 2C9 inhibitor Non-inhibitor 0.6591 CYP450 2D6 inhibitor Non-inhibitor 0.8821 CYP450 2C19 inhibitor Non-inhibitor 0.6641 CYP450 3A4 inhibitor Inhibitor 0.6185 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7229 Ames test Non AMES toxic 0.6097 Carcinogenicity Non-carcinogens 0.8218 Biodegradation Not ready biodegradable 1.0 Rat acute toxicity 2.4787 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9884 hERG inhibition (predictor II) Non-inhibitor 0.8733
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
-
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available LC-MS/MS Spectrum - LC-ESI-qTof , Positive LC-MS/MS Not Available
Targets
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- Kind
- Protein
- Organism
- Human immunodeficiency virus 1
- Pharmacological action
-
Yes
- Actions
-
Inhibitor
- General Function
- Aspartic-type endopeptidase activity
- Specific Function
- Not Available
- Gene Name
- pol
- Uniprot ID
- Q72874
- Uniprot Name
- Pol polyprotein
- 分子量
- 10778.7 Da
References
- Wittayanarakul K, Hannongbua S, Feig M: Accurate prediction of protonation state as a prerequisite for reliable MM-PB(GB)SA binding free energy calculations of HIV-1 protease inhibitors. J Comput Chem. 2008 Apr 15;29(5):673-85. [Article]
- Dandache S, Sevigny G, Yelle J, Stranix BR, Parkin N, Schapiro JM, Wainberg MA, Wu JJ: In vitro antiviral activity and cross-resistance profile of PL-100, a novel protease inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2007 Nov;51(11):4036-43. Epub 2007 Jul 16. [Article]
- Sadler BM, Hanson CD, Chittick GE, Symonds WT, Roskell NS: Safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus (HIV) type 1 protease inhibitor, following oral administration of single doses to HIV-infected adults. Antimicrob Agents Chemother. 1999 Jul;43(7):1686-92. [Article]
- Authors unspecified: Amprenavir: a new HIV protease inhibitor. Med Lett Drugs Ther. 1999 Jul 16;41(1057):64-6. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- 分子量
- 56277.81 Da
References
- Hesse LM, von Moltke LL, Shader RI, Greenblatt DJ: Ritonavir, efavirenz, and nelfinavir inhibit CYP2B6 activity in vitro: potential drug interactions with bupropion. Drug Metab Dispos. 2001 Feb;29(2):100-2. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Inhibitor
- Curator comments
- Amprenavir at high concentrations has been shown to inhibit CYP2C19 in vitro. The clinical correlation is unknown.
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- 分子量
- 55930.545 Da
References
- Veronese L, Rautaureau J, Sadler BM, Gillotin C, Petite JP, Pillegand B, Delvaux M, Masliah C, Fosse S, Lou Y, Stein DS: Single-dose pharmacokinetics of amprenavir, a human immunodeficiency virus type 1 protease inhibitor, in subjects with normal or impaired hepatic function. Antimicrob Agents Chemother. 2000 Apr;44(4):821-6. doi: 10.1128/aac.44.4.821-826.2000. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- 分子量
- 55627.365 Da
References
- Fung HB, Kirschenbaum HL, Hameed R: Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor. Clin Ther. 2000 May;22(5):549-72. doi: 10.1016/S0149-2918(00)80044-2. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- 分子量
- 55768.94 Da
References
- Fung HB, Kirschenbaum HL, Hameed R: Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor. Clin Ther. 2000 May;22(5):549-72. doi: 10.1016/S0149-2918(00)80044-2. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Substrate
- General Function
- Oxygen binding
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- 分子量
- 57108.065 Da
References
- Treluyer JM, Bowers G, Cazali N, Sonnier M, Rey E, Pons G, Cresteil T: Oxidative metabolism of amprenavir in the human liver. Effect of the CYP3A maturation. Drug Metab Dispos. 2003 Mar;31(3):275-81. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
SubstrateInhibitorInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- 分子量
- 57342.67 Da
References
- Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [Article]
- Brophy DF, Israel DS, Pastor A, Gillotin C, Chittick GE, Symonds WT, Lou Y, Sadler BM, Polk RE: Pharmacokinetic interaction between amprenavir and clarithromycin in healthy male volunteers. Antimicrob Agents Chemother. 2000 Apr;44(4):978-84. doi: 10.1128/aac.44.4.978-984.2000. [Article]
- Granfors MT, Wang JS, Kajosaari LI, Laitila J, Neuvonen PJ, Backman JT: Differential inhibition of cytochrome P450 3A4, 3A5 and 3A7 by five human immunodeficiency virus (HIV) protease inhibitors in vitro. Basic Clin Pharmacol Toxicol. 2006 Jan;98(1):79-85. doi: 10.1111/j.1742-7843.2006.pto_249.x. [Article]
- Fung HB, Kirschenbaum HL, Hameed R: Amprenavir: a new human immunodeficiency virus type 1 protease inhibitor. Clin Ther. 2000 May;22(5):549-72. doi: 10.1016/S0149-2918(00)80044-2. [Article]
- Treluyer JM, Bowers G, Cazali N, Sonnier M, Rey E, Pons G, Cresteil T: Oxidative metabolism of amprenavir in the human liver. Effect of the CYP3A maturation. Drug Metab Dispos. 2003 Mar;31(3):275-81. [Article]
- Wire MB, Shelton MJ, Studenberg S: Fosamprenavir : clinical pharmacokinetics and drug interactions of the amprenavir prodrug. Clin Pharmacokinet. 2006;45(2):137-68. doi: 10.2165/00003088-200645020-00002. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
SubstrateInducer
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- 分子量
- 141477.255 Da
References
- Perloff MD, von Moltke LL, Fahey JM, Daily JP, Greenblatt DJ: Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture. AIDS. 2000 Jun 16;14(9):1287-9. [Article]
- Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, Serabjit-Singh CS: Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther. 2001 Nov;299(2):620-8. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Inhibitor
- General Function
- Transporter activity
- Specific Function
- Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
- Gene Name
- ABCC1
- Uniprot ID
- P33527
- Uniprot Name
- Multidrug resistance-associated protein 1
- 分子量
- 171589.5 Da
References
- Olson DP, Scadden DT, D'Aquila RT, De Pasquale MP: The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein 1 (MRP-1). AIDS. 2002 Sep 6;16(13):1743-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
-
Unknown
- Actions
-
Inhibitor
- General Function
- 所以dium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
- Gene Name
- SLCO1B1
- Uniprot ID
- Q9Y6L6
- Uniprot Name
- 所以lute carrier organic anion transporter family member 1B1
- 分子量
- 76447.99哒
References
- Karlgren M, Ahlin G, Bergstrom CA, Svensson R,朋友m J, Artursson P: In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012 Feb;29(2):411-26. doi: 10.1007/s11095-011-0564-9. Epub 2011 Aug 23. [Article]
Drug created at June 13, 2005 13:24 / Updated at March 03, 2023 17:37