Telbivudine
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Telbivudine 속성
- 녹는점
- 185-186?C
- 저장 조건
- -20°C Freezer
- 용해도
- DMSO(약간 용해됨), 물(약간 용해됨)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 색상
- 흰색에서 황백색까지
안전
Telbivudine C화학적 특성, 용도, 생산
개요
There are approximately 400 million people worldwide with chronic hepatitis B virus (HBV) infection, about onethird of whom have potentially progressive and life-threatening liver disease associated with the infection. Chronic hepatitis B infection can lead to cirrhosis, liver failure and hepatocellular carcinoma. Globally, HBV infection accounts for over one million deaths annually. At present, lamivudine and adefovir dipivoxil are the only approved nucleoside/ nucleotide analogs for the treatment of HBV infection. However, resistance to lamivudine is now recognized in 16 to 32% of HBV-infected patients after the first year of monotherapy and about 50% of patients after two years. With adefovir treatment, the resistance rate is much lower, at about 2.5% after two years of therapy. Experience in treating chronic HIV infections has proven the advantage of therapy with a combination of antiviral compounds. Similarly for HBV, there is a clear need for additional antiviral compounds. Several promising candidates are currently in clinical development. Idenix (then known as Novirio) discovered that the known beta-L-nucleosides, L-dA, L-dC (torcitabine) and L-dT (telbivudine), have highly specific activity against HBV. These L-nucleosides are essentially without activity against any of the other viruses tested and are similarly without effect in cell culture and in vivo toxicological tests. However, they are phosphorylated within human cells to their triphosphates which inhibit the HBV DNA polymerase,but not human polymerases. Of these three compounds, telbivudine was the only one to combine reasonable oral bioavailability with good anti-HBV activity and so was progressed to development jointly with Novartis with the highest priority.용도
Antiviral (treatment of hepatitis B infection).원료
After 1 year resistance occurred in 7–20% of patients on telbivudine depending upon past exposure to other drugs used in the treatment of hepatitis B and the type of infection. Development of resistance was less frequent in those receiving telbivudine than in those receiving lamivudine.Pharmaceutical Applications
A synthetic thymidine nucleoside analog formulated for oral use in the treatment of chronic hepatitis B infection.Pharmacokinetics
Oral absorption: 100%Cmax 600 mg/kg oral: 3.7 μg/mL
Volume of distribution: In excess of body water
Plasma protein binding:3.3%
It is eliminated renally, necessitating dose adjustment in patients with renal insufficiency. It should not be administered with pegylated interferon because of an increased risk of neuropathy.
Clinical Use
Treatment of chronic hepatitis B in patients >16 years of age부작용
Adverse effects are similar to those of lamivudine and include upper respiratory tract infection, headache, fatigue and gastrointestinal upset. Myopathy and peripheral neuropathy are rare but have been observed in some patients several weeks into the course with associated rise in serum creatine kinase levels. Acute exacerbations of hepatitis have been observed on discontinuation of therapy. Lactic acidosis may occur, necessitating drug discontinuation.Telbivudine 준비 용품 및 원자재
원자재
준비 용품
Telbivudine 공급 업체
글로벌( 14)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
SynZeal Research Pvt Ltd | -- |
standards@synzeal.com | India | 6522 | 58 |
United States Biological | -- |
chemicals@usbio.net | United States | 6256 | 80 |
Wuhan Kehaojia Biotechnology Co., Ltd. | -- |
2248475041@qq.com | CHINA | 2650 | 58 |
Beijing Luyuan Bird Biotechnology Co., Ltd. | -- |
15810802415@139.com | CHINA | 6757 | 58 |
Shanghai Weiwei Biological Technology Co., Ltd. | -- |
sales@wheybio.com | CHINA | 4398 | 58 |
Shanghai Yubo Biotechnology Co., Ltd. | -- |
344843571@qq.com | CHINA | 6322 | 58 |
Absin Bioscience Inc. | -- |
chenjw@absin.cn | CHINA | 6661 | 58 |
Shanghai Yuqi Biological Technology Co., Ltd. | -- |
847627550@qq.com | CHINA | 6087 | 58 |
Shanghai Hao Biological Technology Co., Ltd. | -- |
market@xlswkj.com | CHINA | 6805 | 58 |
Shanghai Ziqi Biological Technology Co., Ltd. | -- |
2453006496@qq.com | CHINA | 6192 | 58 |