药品详细
Tenofovir(替诺福韦)
化学结构式图
中文名
替诺福韦
英文名
Tenofovir
分子式
C9H14N5O4P
化学名
({[(2R)-1-(6-amino-9H-purin-9-yl)propan-2-yl]oxy}methyl)phosphonic acid
分子量
Average: 287.2123
Monoisotopic: 287.078340473
Monoisotopic: 287.078340473
CAS号
147127-20-6
ATC分类
J05A Direct acting antivirals
药物类型
small molecule
阶段
approved
商品名
Apropovir;Viread;
同义名
D,L-Tenofovir;PMPA;TDF;Tenofovir disoproxil;Tenofovir disoproxil fumarate;
基本介绍
Tenofovir, marketed by Gilead Sciences under the trade name Viread®, belongs to a class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (nRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people. [Wikipedia]
生产厂家
- Gilead sciences inc
- Gilead Sciences, Inc.
封装厂家
- A-S Medication Solutions LLC
- Bristol-Myers Squibb Co.
- Cardinal Health
- Dept Health Central Pharmacy
- Gilead Sciences Inc.
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Nycomed Inc.
- Patheon Inc.
- PCA LLC
- Physicians Total Care Inc.
- Quality Care
- Remedy Repack
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
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| Substructures |
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适应症
ANTIVIRALS 抗病毒;
药理
| Indication | For use, in combination with other antiretroviral agents, for the treatment of HIV-1 infection. | ||||||
| Pharmacodynamics | Tenofovir belongs to a class of antiretroviral drugs known as nucleotide analogue reverse transcriptase inhibitors (NtRTIs), which block reverse transcriptase, an enzyme crucial to viral production in HIV-infected people. Tenofovir is currently in late-stage clinical trials for the treatment of hepatitis B. Tenofovir disoproxil fumarate is an acyclic nucleoside phosphonate diester analog of adenosine monophosphate. Tenofovir requires initial diester hydrolysis for conversion to tenofovir and subsequent phosphorylations by cellular enzymes to form tenofovir diphosphate. Tenofovir diphosphate is a weak inhibitor of mammalian DNA polymerases α, β, and mitochondrial DNA polymerase γ. | ||||||
| Mechanism of action | Tenofovir inhibits the activity of HIV reverse transcriptase by competing with the natural substrate deoxyadenosine 5’-triphosphate and, after incorporation into DNA, by DNA chain termination. Specifically, the drugs are analogues of the naturally occurring deoxynucleotides needed to synthesize the viral DNA and they compete with the natural deoxynucleotides for incorporation into the growing viral DNA chain. However, unlike the natural deoxynucleotides substrates, NRTIs and NtRTIs (nucleoside/tide reverse transcriptase inhibitors) lack a 3'-hydroxyl group on the deoxyribose moiety. As a result, following incorporation of an NRTI or an NtRTI, the next incoming deoxynucleotide cannot form the next 5'-3' phosphodiester bond needed to extend the DNA chain. Thus, when an NRTI or NtRTI is incorporated, viral DNA synthesis is halted, a process known as chain termination. All NRTIs and NtRTIs are classified as competitive substrate inhibitors. | ||||||
| Absorption | The oral bioavailability in fasted patients is approximately 25%. Administration of food (high fat meal containing 40 to 50% fat) increases the oral bioavailability, with an increase in the AUC of approximately 40%. | ||||||
| Volume of distribution |
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| Protein binding | Very low: < 0.7% to human plasma proteins and < 7.2% to serum proteins | ||||||
| Metabolism |
Neither tenofovir disoproxil nor tenofovir are substrates of CYP450 enzymes.
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| Route of elimination | Not Available | ||||||
| Half life | Approximately 17 hours. | ||||||
| Clearance | Not Available | ||||||
| Toxicity | Limited clinical experience at doses higher than the therapeutic dose of tenofovir 300 mg is available. In Study 901 tenofovir disoproxil fumarate 600 mg was administered to 8 patients orally for 28 days. No severe adverse reactions were reported. The effects of higher doses are not known. | ||||||
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理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Atazanavir | Concomitant therapy may result in decreased serum levels of Atazanavir and increased levels of Tenofovir. Concomitant therapy should only be used with the inclusion of Ritonavir. |
| Didanosine | Tenofovir may decrease the therapeutic effects and increase the adverse effects of Didanosine. Monitor for changes in virologic response and Didanosine toxicity during concomitant therapy. |
| Valganciclovir | The excretion rates of Valganciclovir and/or Tenofovir may decrease as both drugs are eliminated by active tubular secretion. Monitor for increased serum concentrations and toxicity of both agents. |
食物相互作用
Not Available
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