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药品详细

Mitomycin (丝裂霉素 )

化学结构式图
中文名
丝裂霉素
英文名
Mitomycin
分子式
Not Available
化学名
[(4S,6S,7R,8S)-11-amino-7-methoxy-12-methyl-10,13-dioxo-2,5-diazatetracyclo[7.4.0.0^{2,7}.0^{4,6}]trideca-1(9),11-dien-8-yl]methyl carbamate
分子量
Average: 334.3272
Monoisotopic: 334.127719706
CAS号
50-07-7
ATC分类
L01D 细胞毒素抗生素及相关物质
药物类型
small molecule
阶段
商品名
Ametycin;Ametycine;Mit-C;Mito-C;Mitocin-C;Mitomycin (TN);Mitomycin C;Mitomycin-C;Mitomycinum;Mitomycinum C;Mitomycyna C [Polish];Mitozytrex;Muamycin;Mutamycin;Mytomycin;Mytozytrex;
同义名
7-Amino-9α-methoxymitosane;Mitamycin;MMC;
基本介绍

An antineoplastic antibiotic produced by Streptomyces caespitosus. It is one of the bi- or tri-functional alkylating agents causing cross-linking of DNA and inhibition of DNA synthesis. [PubChem]

生产厂家
  • Accord healthcare inc
  • Baxter healthcare corp anesthesia and critical care
  • Bedford laboratories div ben venue laboratories inc
  • Bristol laboratories inc div bristol myers co
  • Bristol myers co
  • Hospira inc
  • Supergen inc
封装厂家
参考
Synthesis Reference Not Available
General Reference Not Available
剂型
Form Route Strength
Powder, for solution Intravesical
规格
Unit description Cost Unit
Mutamycin 40 mg vial 878.48 USD vial
Mutamycin 20 mg vial 434.8 USD vial
Mitomycin 40 mg vial 300.0 USD vial
Mitomycin 20 mg vial 142.55 USD vial
Mutamycin 5 mg vial 128.75 USD vial
Mitomycin 5 mg vial 52.43 USD vial
化合物类型
Type small molecule
Classes
  • Mitomycins
Substructures
  • Indolequinones
  • Carbamates and Derivatives
  • Aliphatic and Aryl Amines
  • Amino Ketones
  • Azirines
  • Benzoquinones
  • Piperazines
  • Pyrrolidines
  • Ethers
  • Aminals and Derivatives
  • Enamines
  • Heterocyclic compounds
  • Mitomycins
  • Pyrrolines
  • Ketones
适应症
Cancer 癌症;
药理
Indication For treatment of malignant neoplasm of lip, oral cavity, pharynx, digestive organs, peritoneum, female breast, and urinary bladder.
Pharmacodynamics Mitomycin is one of the older chemotherapy drugs, which has been around and in use for decades. It is an antibiotic which has been shown to have antitumor activity. Mitomycin selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of mitomycin-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed. Mitomycin has been shown in vitro to inhibit B cell, T cell, and macrophage proliferation and impair antigen presentation, as well as the secretion of interferon gamma, TNFa, and IL-2.
Mechanism of action Mitomycin is activated in vivo to a bifunctional and trifunctional alkylating agent. Binding to DNA leads to cross-linking and inhibition of DNA synthesis and function. Mitomycin is cell cycle phase-nonspecific.
Absorption Erratic.
Volume of distribution Not Available
Protein binding Not Available
Metabolism

Primarily hepatic, some in various other tissues.

Route of elimination Approximately 10% of a dose of mitomycin is excreted unchanged in the urine.
Half life 8-48 min
Clearance Not Available
Toxicity Oral, mouse: LD50 = 23 mg/kg; Oral, rat: LD50 = 30 mg/kg. Symptoms of overdose include nausea and vomiting.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State solid
Melting point > 360 oC
Experimental Properties
Property Value Source
water solubility Soluble (8430 mg/L) PhysProp
logP -1.6 PhysProp
pKa 10.9 Various sources
Predicted Properties
Property Value Source
water solubility 1.01e+01 g/l ALOGPS
logP -0.55 ALOGPS
logP -1.05 ChemAxon Molconvert
logS -1.52 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 7 ChemAxon Molconvert
hydrogen donor count 3 ChemAxon Molconvert
polar surface area 146.89 ChemAxon Molconvert
rotatable bond count 4 ChemAxon Molconvert
refractivity 83.27 ChemAxon Molconvert
polarizability 32.77 ChemAxon Molconvert
药物相互作用
Drug Interaction
Trastuzumab Trastuzumab may increase the risk of neutropenia and anemia. Monitor closely for signs and symptoms of adverse events.
Vinblastine Potentially severe lung toxicity
Vincristine Potentially severe lung toxicity
Vindesine Potentially severe lung toxicity
食物相互作用
Not Available

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