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Entecavir

Entecavir 구조식 이미지
카스 번호:
142217-69-4
상품명:
Entecavir
동의어(영문):
Etv;Baraclude;entikawei;2-amino-9-((1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl)-1H-purin-6(9H)-one;CS-863;CS-1236;Entecavi;SQ 34676;Enticavir;ENTECAVIR
CBNumber:
CB0506719
분자식:
C12H15N5O3
포뮬러 무게:
277.28
MOL 파일:
142217-69-4.mol

Entecavir 속성

녹는점
249-252°C
끓는 점
661.4±65.0 °C(Predicted)
밀도
1.81±0.1 g/cm3(Predicted)
저장 조건
-20°C
용해도
DMSO (Slightly), Methanol (Sparingly)
산도 계수 (pKa)
14.22±0.60(Predicted)
물리적 상태
powder
색상
white to beige
optical activity
[α]/D +25 to +40°, c = 0.2 in H2O
안정성
Hygroscopic
CAS 데이터베이스
142217-69-4(CAS DataBase Reference)

안전

안전지침서 24/25
WGK 독일 3
HS 번호 29339900
유해 물질 데이터 142217-69-4(Hazardous Substances Data)

Entecavir C화학적 특성, 용도, 생산

개요

Entecavir is a cyclopentyl guanosine analog launched for the once-daily oral treatment of chronic hepatitis B virus (HBV) infection, and it is the third nucleoside or nucleotide analog to be marketed for this indication. Lamivudine, a deoxythiacytosine analog, and adefovir dipivoxil, a nucleotide analog, have been marketed since 1998 and 2002, respectively. Entecavir and adefovir are specifically indicated for HBV, whereas lamivudine is indicated for both HBV and HIV infections. In mammalian cells, entecavir is efficiently phosphorylated to the active triphosphate form, which competes with the natural substrate deoxyguanosine triphosphate and functionally inhibits all three activities of the HBV polymerase: (1) base priming, (2) reverse transcription of the negative strand from the pregenomic messenger RNA, and (3) synthesis of the positive strand of HBV DNA.The most common adverse events associated with the use of entecavir are similar to those typically seen with HBV therapy and include headache, abdominal pain, diarrhea, fatigue, and dizziness.

화학적 성질

White to Off-White/Yellow Crystalline Powder

용도

An oral antiviral drug used in the treatment of hepatitis B infection. A guanine analogue that inhhibits all three steps in the viral replication process

정의

ChEBI: Guanine substituted at the 9 position by a 4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl group. A synthetic analogue of 2'-deoxyguanosine, it is a nucleoside reverse transcriptase inhibitor with selective antiviral activity against hepatitis B virus Entecavir is phosphorylated intracellularly to the active triphosphate form, which competes with deoxyguanosine triphosphate, the natural substrate of hepatitis B virus reverse transcriptase, inhibiting every stage of the enzyme's activity, although it ha no activity against HIV. It is used for the treatment of chronic hepatitis B.

Pharmaceutical Applications

An analog of guanosine formulated as tablets and suspension for oral use.

Pharmacokinetics

Oral absorption: 100%
Cmax 0.5 mg/kg oral: 4.2 ng/mL
Intracellular half-life: c. 16 h
Volume of distribution: In excess of body water
Plasma protein binding: 13%
Entecavir is rapidly absorbed after administration on an empty stomach, achieving peak plasma concentrations in 1–1.5 h. Plasma steady state is achieved in 6–10 days.
It is renally eliminated. Dosage adjustment is required with impaired creatinine clearance. The drug is not metabolized by cytochrome P450. No drug interactions have been identified.

Clinical Use

Treatment of chronic hepatitis B virus infection in patients >16 years of age

부작용

Severity of adverse reactions was comparable to that of lamivudine, with headache, fatigue, upper respiratory infections and abdominal pain being most common. Lactic acidosis and hepatic steatosis were rarely observed.

Entecavir 준비 용품 및 원자재

원자재

준비 용품


Entecavir 공급 업체

글로벌( 443)공급 업체
공급자 전화 이메일 국가 제품 수 이점
Lianyungang happen teng technology co., LTD
15950718863
wang666xt@163.com CHINA 296 58
Beijing Yibai Biotechnology Co., Ltd
0086-182-6772-3597
sales04@yibaibiotech.com CHINA 420 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 19231 58
Hebei Minshang Biotechnology Co.,Ltd
+8613582176207
cathy@hbminshang.cn China 302 58
Baoji Guokang Bio-Technology Co., Ltd.
0917-3909592 13892490616
gksales1@gk-bio.com CHINA 9416 58
Sinoway Industrial co., ltd.
+8613806035118
xie@china-sinoway.com China 311 58
Wuhan Golt Biotech Co., Ltd.
+8615389281203
maria@goltbiotech.com China 987 58
Nanjing Gold Pharmaceutical Technology Co. Ltd.
025-84209270 15906146951
CHINA 115 55
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
sales01@cooperate-pharm.com CHINA 1815 55
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 22021 55

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