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AMPRENAVIR

AMPRENAVIR 구조식 이미지
카스 번호:
161814-49-9
상품명:
AMPRENAVIR
동의어(영문):
PROZEI;141W94;VX 478;KVX-478;AGENERASE;AMPRENAVIR;Angenerase;Amprenavir(KVX-478);AMprenavir(agenerase);141W94, KVX-478, Agenerase, Prozei,
CBNumber:
CB4186139
분자식:
C25H35N3O6S
포뮬러 무게:
505.63
MOL 파일:
161814-49-9.mol

AMPRENAVIR 속성

녹는점
72-74°C
저장 조건
-20°C Freezer
용해도
DMSO: soluble20mg/mL, clear
물리적 상태
powder
색상
white to beige
optical activity
[α]/D +8 to +12°, c = 0.5 in methanol
InChIKey
YMARZQAQMVYCKC-OEMFJLHTSA-N

안전

유엔번호(UN No.) 3077
WGK 독일 3
HS 번호 29350090

AMPRENAVIR C화학적 특성, 용도, 생산

개요

Amprenavir was launched as Agenerase in the US for the treatment of AIDS patients in combination with approved agent antiretroviral nucleoside analogs. It is the fifth non-peptidic inhibitor of HIV-1 protease to be marketed in this indication after the last approved Neflinavir. Amprenavir, designed via a structure-based process, is the smallest molecule in the 《navir》 class and exhibits a reduced peptidic character. An improved process for preparation comprising four steps from a (1S, 2R)-2-hydroxy-3-aminopropylcarbamate has been developed. Amprenavir is a potent inhibitor of HIV-1 aspartyl protease (Ki = 0.6nM), an enzyme required by the virus to cleave pro-form polyproteins to structural proteins during the last stage in the replication process. The compound displays good oral bioavailability in humans and penetrates the CNS, which is an important advantage in long-term treatment. Its plasma half-life is approximately 10h. Treatment with Amprenavir in combination with nucleoside analog reverse transcriptase inhibitors considerably decreases viral load and restores CD4+ T-cell counts in patients with HIV infection.

화학적 성질

Off-White to Pale Yellow

Originator

Vertex Pharm (US)

용도

A selective HIV protease inhibitor. An analogue of Ritonavir

용도

Protease inhibitor, anti-HIV agent

상표명

Agenerase (GlaxoSmithKline).

원료

Mutations at position 50, 76 and 84 of the protease enzyme gene are associated with significantly reduced susceptibility.

Pharmaceutical Applications

A synthetic compound formulated as the calcium salt of the oral prodrug fosamprenavir.

Pharmacokinetics

Oral absorption: Not known/available
Cmax 700 mg + ritonavir 100 mg:c. 6.08 mg/L
twice daily
Cmin 700 mg + ritonavir 100 mg:c. 2.12 mg/L
twice daily
Plasma half-life: c. 7.7 h
Volume of distribution: c. 430 L
Plasma protein binding: c. 90%
Absorption
Fosamprenavir is rapidly and almost completely hydrolyzed to amprenavir and inorganic phosphate by cellular phosphatases in the gut epithelium as it is absorbed. Absolute bioavailability has not been established. It can be taken without regard to food.
Distribution
It penetrates moderately well into the CNS. The semen:plasma ratio is negligible. It is not known if it is distributed into breast milk.
Metabolism and excretion
It is extensively metabolized by the cytochrome P450 (CYP) 3A4 enzyme system. Two major metabolites have been identified that appear to result from the oxidation of the tetrahydrofuran and aniline moieties. Around 14% of a dose is eliminated in the urine and 75% in feces, <3% as unchanged drug. Metabolites account for >90% of administered drug found in fecal samples. It should be used with caution and at reduced doses in adults with mild or moderate hepatic impairment; it is contraindicated in patients with severe hepatic impairment.

Clinical Use

Treatment of HIV infection (in combination with other antiretroviral drugs)

부작용

The most common adverse events in patients receiving boosted fosamprenavir were diarrhea, nausea, headache, fatigue, vomiting and rash. Ritonavir-boosted fosamprenavir is associated with a dyslipidemia profile characteristic of those treated with other protease inhibitors boosted with 200 mg of ritonavir.

AMPRENAVIR 준비 용품 및 원자재

원자재

준비 용품


AMPRENAVIR 공급 업체

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Alpha Biopharmaceuticals Co., Ltd
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0086-411-39042693 sales@alphabiopharm.com China 1954 58
Capot Chemical Co.,Ltd.
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+86 (0)571-858 647 95 sales@capotchem.com China 19947 60
Biochempartner
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Hubei Jusheng Technology Co.,Ltd.
86-188-71490254
peter@hubeijusheng.com CHINA 20201 58
Shanghai Hanxiang Biotechnology Co. Ltd. 15971444841
amber@biochempartner.net China 4996 58
Shanghai Boyle Chemical Co., Ltd.
86-21-57758967 sales@boylechem.com China 2927 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
+86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76
3B Pharmachem (Wuhan) International Co.,Ltd. 86-21-50328103 * 801、802、803、804 Mobile:18930552037
86-21-50328109 3bsc@sina.com China 15921 69
Alabiochem Tech.Co., Ltd. 0086-512-58900862; 400-0707-518; 0086-512-56727736
0086-512-56765862 sales@alabiochem.com China 944 59

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