Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C25H35N3O6S |
Molecular Weight | 505.627 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CC(C)CN(C[C@@H](O)[C@H](CC1=CC=CC=C1)NC(=O)O[C@H]2CCOC2)S(=O)(=O)C3=CC=C(N)C=C3
InChI
InChIKey=YMARZQAQMVYCKC-OEMFJLHTSA-N
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
Molecular Formula | C25H35N3O6S |
Molecular Weight | 505.627 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 3 / 3 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23519392 | https://www.ncbi.nlm.nih.gov/pubmed/11152018 | https://www.ncbi.nlm.nih.gov/pubmed/15341507
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23519392 | https://www.ncbi.nlm.nih.gov/pubmed/11152018 | https://www.ncbi.nlm.nih.gov/pubmed/15341507
Amprenavir is an inhibitor of HIV-1 protease. Amprenavir binds to the active site of HIV-1 protease and thereby prevents the processing of viral gag and gag-pol polyprotein precursors, resulting in the formation of immature non-infectious viral particles. Amprenavir-containing combination regimens have shown virological efficacy, and have generally been well tolerated, in patients with HIV infection (primarily treatment-naive or protease inhibitor-naive). Fosamprenavir (GW433908, Lexiva, Telzir) is an oral prodrug of amprenavir, with a reduced daily pill burden. The use of protease inhibitors has also been associated with dyslipidemia and an increased risk of cardiovascular disease. Amprenavir activates Pregnane X receptor to mediate dyslipidemia.
CNS Activity
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3401 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23519392 |
8.6 µM [EC50] | ||
Target ID: CHEMBL2364675 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10952482 |
2.5 µM [IC50] | ||
Target ID: CHEMBL243 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | AGENERASE Approved UseAGENERASE (amprenavir) is indicated in combination with other antiretroviral agents for the treatment of HIV-1 infection. Launch Date9.2404803E11 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.36 μg/mL |
1200 mg 2 times / day multiple, oral dose: 1200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
6.18 μg/mL |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT |
|
9.72 μg/mL |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
6.77 μg/mL |
20 mg/kg bw 2 times / day multiple, oral dose: 20 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
3.99 μg/mL |
15 mg/kg bw 3 times / day multiple, oral dose: 15 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
18.5 μg × h/mL |
1200 mg 2 times / day multiple, oral dose: 1200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
22.06 μg × h/mL |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT |
|
28.05 μg × h/mL |
1200 mg single, oral dose: 1200 mg route of administration: Oral experiment type: SINGLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED |
|
15.46 μg × h/mL |
20 mg/kg bw 2 times / day multiple, oral dose: 20 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
|
8.73 μg × h/mL |
15 mg/kg bw 3 times / day multiple, oral dose: 15 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: CHILD sex: UNKNOWN food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.85 h |
1200 mg 2 times / day multiple, oral dose: 1200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
10% |
1200 mg 2 times / day multiple, oral dose: 1200 mg route of administration: Oral experiment type: MULTIPLE co-administered: |
AMPRENAVIR plasma | Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Disc. AE: Nausea, Vomiting... AEs leading to discontinuation/dose reduction: Nausea (12%) Sources: Page: p.1387Vomiting (6%) Loose stools (3%) Abdominal pain (2%) Abdominal discomfort (2%) Rash (3%) |
1200 mg single, oral Recommended Dose: 1200 mg Route: oral Route: single Dose: 1200 mg Sources: Page: p.1688 |
unhealthy, 33+/-6.7 n = 12 Health Status: unhealthy Condition: HIV-1 infection Age Group: 33+/-6.7 Sex: M+F Population Size: 12 Sources: Page: p.1688 |
|
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Sources: Page: p.11 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.11 |
Disc. AE: Reaction skin, Stevens-Johnson syndrome... AEs leading to discontinuation/dose reduction: Reaction skin (grade 3-4) Sources: Page: p.11Stevens-Johnson syndrome (grade 3-4) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Nausea | 12% Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Abdominal discomfort | 2% Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Abdominal pain | 2% Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Loose stools | 3% Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Rash | 3% Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Vomiting | 6% Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Co-administed with:: lamivudine, po(150 mg, BID) Sources: Page: p.1387zidovudine, po(300 mg, BID) |
unhealthy, 21-62 n = 113 Health Status: unhealthy Condition: HIV-1 infection Age Group: 21-62 Sex: M+F Population Size: 113 Sources: Page: p.1387 |
Reaction skin | grade 3-4 Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Sources: Page: p.11 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.11 |
Stevens-Johnson syndrome | grade 3-4 Disc. AE |
1200 mg 2 times / day multiple, oral Recommended Dose: 1200 mg, 2 times / day Route: oral Route: multiple Dose: 1200 mg, 2 times / day Sources: Page: p.11 |
unhealthy Health Status: unhealthy Condition: HIV-1 infection Sources: Page: p.11 |
PubMed
Title | Date | PubMed |
---|---|---|
Four new antiretroviral medications will soon offer more options to HIV patients. | 1998 Jul-Aug |
|
Structural and kinetic analyses of the protease from an amprenavir-resistant human immunodeficiency virus type 1 mutant rendered resistant to saquinavir and resensitized to amprenavir. | 2000 Aug |
|
BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. | 2000 Aug |
|
Novel inhibitors of HIV protease: design, synthesis and biological evaluation of picomolar inhibitors containing cyclic P1/P2 scaffolds. | 2000 Jun 5 |
|
Inhibition of HIV-1 protease by a boron-modified polypeptide. | 2000 Oct 1 |
|
A phase II trial of dual protease inhibitor therapy: amprenavir in combination with indinavir, nelfinavir, or saquinavir. | 2001 Apr 15 |
|
Liquid chromatographic-tandem mass spectrometric determination of amprenavir (agenerase) in serum/plasma of human immunodeficiency virus type-1 infected patients receiving combination antiretroviral therapy. | 2001 Apr 20 |
|
Combination of protease inhibitors for the treatment of HIV-1-infected patients: a review of pharmacokinetics and clinical experience. | 2001 Dec |
|
Therapeutic drug monitoring of HIV protease inhibitors using high-performance liquid chromatography with ultraviolet or photodiode array detection. | 2001 Dec |
|
[Resistance to protease inhibitors]. | 2001 Feb |
|
New developments in anti-HIV chemotherapy. | 2001 Jan-Feb |
|
Antiretroviral activity and safety of abacavir in combination with selected HIV-1 protease inhibitors in therapy-naive HIV-1-infected adults. | 2001 Jun |
|
Simultaneous determination of the HIV-protease inhibitors indinavir, amprenavir, ritonavir, saquinavir and nelfinavir in human plasma by reversed-phase high-performance liquid chromatography. | 2001 Jun 15 |
|
Phase III trials for new PI. | 2001 Mar |
|
Resistant to everything. | 2001 May |
|
Simultaneous determination of the HIV protease inhibitors indinavir, amprenavir, saquinavir, ritonavir and nelfinavir in human plasma by high-performance liquid chromatography. | 2001 May 5 |
|
[Drug interactions with antiretroviral agents]. | 2001 May-Jun |
|
From amprenavir to GW433908. | 2001 Nov |
|
DPC 681 and DPC 684: potent, selective inhibitors of human immunodeficiency virus protease active against clinically relevant mutant variants. | 2001 Nov |
|
New developments in anti-HIV chemotherapy. | 2001 Nov |
|
Anti-human immunodeficiency virus drugs are ineffective against Pneumocystis carinii in vitro and in vivo. | 2001 Nov 15 |
|
Methadone blood concentrations are decreased by the administration of abacavir plus amprenavir. | 2001 Oct |
|
Effectors of HIV-1 protease peptidolytic activity. | 2001 Sep 18 |
|
Amping amprenavir with ritonavir. | 2001 Spring |
|
Retroviral proteases. | 2002 |
|
Simultaneous determination of the six HIV protease inhibitors (amprenavir, indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir) plus M8 nelfinavir metabolite and the nonnucleoside reverse transcription inhibitor efavirenz in human plasma by solid-phase extraction and column liquid chromatography. | 2002 Apr |
|
Amino acid substitutions in Gag protein at non-cleavage sites are indispensable for the development of a high multitude of HIV-1 resistance against protease inhibitors. | 2002 Feb 22 |
|
Clinical pharmacology and pharmacokinetics of amprenavir. | 2002 Jan |
|
Unfavourable interaction of amprenavir and lopinavir in combination with ritonavir? | 2002 Jan 25 |
|
Longitudinal use of phenotypic resistance testing to HIV-1 protease inhibitors in patients developing HAART failure. | 2002 Jul |
|
Dual vs single protease inhibitor therapy following antiretroviral treatment failure: a randomized trial. | 2002 Jul 10 |
|
The pharmacokinetics of amprenavir, zidovudine, and lamivudine in the genital tracts of men infected with human immunodeficiency virus type 1 (AIDS clinical trials group study 850). | 2002 Jul 15 |
|
Synthesis and antiviral activity of new anti-HIV amprenavir bioisosteres. | 2002 Jul 18 |
|
Efavirenz-induced skin eruption and successful desensitization. | 2002 Mar |
|
Delavirdine increases drug exposure of ritonavir-boosted protease inhibitors. | 2002 Mar 29 |
|
Salvage therapy with amprenavir and ritonavir: prospective study in 17 heavily pretreated patients. | 2002 Mar-Apr |
|
Prevalence of the HIV protease mutation N88S causing hypersensitivity to amprenavir. | 2002 May 1 |
|
Amprenavir-resistant HIV-1 exhibits lopinavir cross-resistance and reduced replication capacity. | 2002 May 3 |
|
Therapeutic vaccination in primary HIV infection, the Quest trial. | 2002 May 6 |
Sample Use Guides
Adults: The recommended oral dose of AGENERASE Capsules for adults is 1200 mg (eight 150-mg capsules) twice daily in combination with other antiretroviral agents. Concomitant Therapy: If AGENERASE and ritonavir are used in combination, the recommended dosage regimens are: AGENERASE 1200 mg with ritonavir 200 mg once daily or AGENERASE
600 mg with ritonavir 100 mg twice daily.
Pediatric Patients: For adolescents (13 to 16 years), the recommended oral dose of AGENERASE Capsules is 1200 mg (eight 150-mg capsules) twice daily in combination with other antiretroviral agents. For patients between 4 and 12 years of age or for patients 13 to 16 years of age with weight of
<50 kg, the recommended oral dose of AGENERASE Capsules is 20 mg/kg twice daily or 15 mg/kg 3 times daily (to a maximum daily dose of 2400 mg) in combination with other antiretroviral agents.
Route of Administration:
Oral
The in vitro antiviral activity of amprenavir was evaluated against HIV-1 IIIB in both acutely and chronically infected lymphoblastic cell lines (MT-4, CEM-CCRF, 43 H9) and in peripheral blood lymphocytes. The 50% inhibitory concentration (IC50) of amprenavir ranged from 0.012 to 0.08 µM in acutely infected cells and was 0.41 µM in chronically infected cells (1 µM = 0.50 mcg/mL).
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:17:12 UTC 2023
by
admin
on
Wed Jul 05 23:17:12 UTC 2023
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Record UNII |
5S0W860XNR
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Record Status |
Validated (UNII)
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Record Version |
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Classification Tree | Code System | Code | ||
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EMA ASSESSMENT REPORTS |
AGENERASE (WITHDRAWN: HIV INFECTIONS)
Created by
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WHO-ATC |
J05AE05
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NDF-RT |
N0000175889
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NCI_THESAURUS |
C97366
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NDF-RT |
N0000000246
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WHO-VATC |
QJ05AE05
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LIVERTOX |
NBK548011
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Code System | Code | Type | Description | ||
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N0000182141
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PRIMARY | Cytochrome P450 3A4 Inhibitors [MoA] | ||
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5S0W860XNR
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PRIMARY | |||
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N0000185506
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PRIMARY | Cytochrome P450 3A4 Inducers [MoA] | ||
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200
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PRIMARY | |||
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C095108
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PRIMARY | |||
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228656
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PRIMARY | RxNorm | ||
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65016
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PRIMARY | |||
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C28824
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PRIMARY | |||
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7751
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PRIMARY | |||
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DTXSID5046061
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DB00701
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40050
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JJ-94
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PRIMARY | |||
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CHEMBL116
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AMPRENAVIR
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5S0W860XNR
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PRIMARY | |||
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M1855
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PRIMARY | Merck Index | ||
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N0000191264
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PRIMARY | P-Glycoprotein Inducers [MoA] | ||
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161814-49-9
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PRIMARY | |||
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100000089388
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SUB00511MIG
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7157
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Related Record | Type | Details | ||
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BINDER->LIGAND |
The high affinity binding protein for amprenavir is alpha1-acid glycoprotein (AAG).
BINDING
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR |
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EXCRETED UNCHANGED |
URINE
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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TRANSPORTER -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLIC ENZYME -> INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> INHIBITOR | |||
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TRANSPORTER -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT |
IN VITRO
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METABOLITE -> PARENT |
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PRODRUG -> METABOLITE ACTIVE |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Tmax | PHARMACOKINETIC |
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SINGLE DOSE |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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