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Amprenavir

产品号 DB00701 公司名称 DrugBank
CAS号 161814-49-9 公司网站 http://www.ualberta.ca/
分子式 C25H35N3O6S 电 话 (780) 492-3111
分子量 505.6269 传 真
纯 度 电子邮件 david.wishart@ualberta.ca
保 存 Chembase数据库ID: 583

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产品别名

标题
Amprenavir
IUPAC标准名
(3S)-oxolan-3-yl N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropyl)4-aminobenzenesulfonamido]-1-phenylbutan-2-yl]carbamate
IUPAC传统名
(3S)-oxolan-3-yl N-[(2S,3R)-3-hydroxy-4-[N-(2-methylpropyl)4-aminobenzenesulfonamido]-1-phenylbutan-2-yl]carbamate
商标名
Vertex
Agenerase
Prozei
别名
AMP
APV
VX-478
AMV

产品登记号

PubChem SID 46507537
CAS号 161814-49-9
PubChem CID 65016

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产品详细信息

详细说明 (English)
Item Information
Drug Groups approved
Description Amprenavir is a protease inhibitor used to treat HIV infection.
Indication For the treatment of HIV-1 infection in combination with other antiretroviral agents.
Pharmacology 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.
Affected Organisms
Human Immunodeficiency Virus
Biotransformation 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.
Absorption Rapidly absorbed after oral administration in HIV-1-infected patients with a time to peak concentration (Tmax) typically between 1 and 2 hours after a single oral dose. The absolute oral bioavailability of amprenavir in humans has not been established.
Half Life 7.1-10.6 hours
Protein Binding Very high (90%). Amprenavir has the highest affinity for alpha(1)-acid glycoprotein.
External Links
Wikipedia
RxList
PDRhealth
Drugs.com

参考文献