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药品详细

Cidofovir(西多福韦)

化学结构式图
中文名
西多福韦
英文名
Cidofovir
分子式
C8H14N3O6P
化学名
({[(2S)-1-(4-amino-2-oxo-1,2-dihydropyrimidin-1-yl)-3-hydroxypropan-2-yl]oxy}methyl)phosphonic acid
分子量
Average: 279.187
Monoisotopic: 279.062021707
CAS号
113852-37-2
ATC分类
J05A Direct acting antivirals
药物类型
small molecule
阶段
approved
商品名
HPMPC;Vistide;
同义名
CDV;Cidofovir Anhydrous;
基本介绍

Cidofovir is an injectable antiviral medication for the treatment of cytomegalovirus (CMV) retinitis in patients with AIDS. It suppresses CMV replication by selective inhibition of viral DNA synthesis. [Wikipedia]

生产厂家
  • Gilead sciences inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
规格
化合物类型
Type small molecule
Classes
  • Pyrimidines and Derivatives
Substructures
  • Hydroxy Compounds
  • Phosphonic Acids and Derivatives
  • Aliphatic and Aryl Amines
  • Ethers
  • Alcohols and Polyols
  • Pyrimidines and Derivatives
  • Heterocyclic compounds
  • Aromatic compounds
  • Phosphinic Acids and Derivatives
  • Cyanamides
适应症
ANTIVIRALS 抗病毒;
药理
Indication For the treatment of CMV retinitis in patients with acquired immunodeficiency syndrome (AIDS)
Pharmacodynamics Cidofovir is a new anti-viral drug. It is classified as a nucleotide analogue and is active against herpes cytomegalovirus (CMV) retinitis infection. Most adults are infected with CMV. Cidofovir suppresses cytomegalovirus (CMV) replication by selective inhibition of viral DNA synthesis.
Mechanism of action Cidofovir acts through the selective inhibition of viral DNA polymerase.Biochemical data support selective inhibition of CMV DNA polymerase by cidofovir diphosphate, the active intracellular metabolite of cidofovir. Cidofovir diphosphate inhibits herpesvirus polymerases at concentrations that are 8- to 600-fold lower than those needed to inhibit human cellular DNA polymerase alpha, beta, and gamma(1,2,3). Incorporation of cidofovir into the growing viral DNA chain results in reductions in the rate of viral DNA synthesis.
Absorption 100%
Volume of distribution
  • 537 ± 126 mL/kg [VISTIDE ADMINISTERED WITHOUT PROBENECID]
  • 410 ± 102 mL/kg [VISTIDE ADMINISTERED WITH PROBENECID]
Protein binding 6%
Metabolism
Not Available
Route of elimination Not Available
Half life 2.4 to 3.2 hours
Clearance
  • 179 +/- 23.1 mL/min/1.73 m2 [WITHOUT PROBENECID]
  • 148 +/- 38.8 mL/min/1.73 m2 [WITH PROBENECID]
Toxicity Kidney damage, fall in the number of white blood cells, decreased platelets
Affected organisms
  • Human Immunodeficiency Virus
Pathways Not Available
理化性质
Properties
State solid
Experimental Properties
Property Value Source
melting point 480 °C Not Available
water solubility =170 mg/mL at pH 6-8 Not Available
logP -3.9 Not Available
Predicted Properties
Property Value Source
water solubility 1.15e+01 g/l ALOGPS
logP -2.1 ALOGPS
logP -3.4 ChemAxon
logS -1.4 ALOGPS
pKa (strongest acidic) 1.19 ChemAxon
pKa (strongest basic) 2.15 ChemAxon
physiological charge -1 ChemAxon
hydrogen acceptor count 8 ChemAxon
hydrogen donor count 4 ChemAxon
polar surface area 145.68 ChemAxon
rotatable bond count 6 ChemAxon
refractivity 60.43 ChemAxon
polarizability 24.44 ChemAxon
药物相互作用
食物相互作用
Not Available

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