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药品详细

Mitoxantrone (米托蒽醌 )

化学结构式图
中文名
米托蒽醌
英文名
Mitoxantrone
分子式
Not Available
化学名
1,4-dihydroxy-5,8-bis({2-[(2-hydroxyethyl)amino]ethyl}amino)-9,10-dihydroanthracene-9,10-dione
分子量
Average: 444.4809
Monoisotopic: 444.200884648
CAS号
65271-80-9
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
Mitox;Novantron;Novantrone;
同义名
DHAD;DHAQ;DHAQ HCl;Dihydroxyanthraquinone;Mitoxanthrone;Mitoxantron;Mitoxantrona [INN-Spanish];mitoxantrone;Mitoxantrone 2HCl;Mitoxantrone dihydrochloride;Mitoxantrone HCl;Mitoxantrone hydrochloride;Mitoxantronum [INN-Latin];Mitozantrone;Mitozantrone hydrochloride;
基本介绍

An anthracenedione-derived antineoplastic agent. [PubChem]

生产厂家
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Bioniche pharma usa llc
  • Emd serono inc
  • Fresenius kabi oncology plc
  • Hospira inc
  • Teva parenteral medicines inc
封装厂家
参考
Synthesis Reference Not Available
General Reference
  1. Fox EJ: Management of worsening multiple sclerosis with mitoxantrone: a review. Clin Ther. 2006 Apr;28(4):461-74. Pubmed
剂型
Form Route Strength
Solution Intravenous
规格
Unit description Cost Unit
Novantrone 2 mg/ml Concentrate 10ml Vial 1649.32 USD vial
Novantrone 2 mg/ml vial 158.59 USD ml
Mitoxantrone 20 mg/10 ml vial 42.0 USD ml
Mitoxantrone 25 mg/12.5 ml vial 37.5 USD ml
化合物类型
Type small molecule
Classes
  • Anthraquinones
  • Anthracenes
Substructures
  • Hydroxy Compounds
  • Aliphatic and Aryl Amines
  • Phenols and Derivatives
  • Benzoquinones
  • Benzene and Derivatives
  • Naphthoquinones
  • Anthraquinones
  • Anthracenes
  • Hydroquinones
  • Alcohols and Polyols
  • Amino Alcohols
  • Aromatic compounds
  • Benzoyl Derivatives
  • Phenyl Esters
  • Anilines
  • Ketones
适应症
Cancer 癌症;
药理
Indication For the treatment of secondary (chronic) progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis
Pharmacodynamics Mitoxantrone 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 Mitoxantrone, a DNA-reactive agent that intercalates into deoxyribonucleic acid (DNA) through hydrogen bonding, causes crosslinks and strand breaks. Mitoxantrone also interferes with ribonucleic acid (RNA) and is a potent inhibitor of topoisomerase II, an enzyme responsible for uncoiling and repairing damaged DNA. It has a cytocidal effect on both proliferating and nonproliferating cultured human cells, suggesting lack of cell cycle phase specificity.
Absorption Poorly absorbed following oral administration
Volume of distribution
  • 1000 L/m2
Protein binding 78%
Metabolism

Hepatic
Route of elimination Not Available
Half life 75 hours
Clearance
  • 21.3 L/hr/m2 [Elderly patients with breast cancer receiving IV administration of 15-90 mg/m2]
  • 28.3 L/hr/m2 [Non-elderly patients with nasopharyngeal carcinoma receiving IV administration of 15-90 mg/m2]
  • 16.2 L/hr/m2 [Non-elderly patients with malignant lymphoma receiving IV administration of 15-90 mg/m2]
Toxicity Severe leukopenia with infection.
Affected organisms
  • Humans and other mammals
Pathways Not Available
理化性质
Properties
State liquid
Melting point Not Available
Experimental Properties
Property Value Source
logP -3.1 PhysProp
Predicted Properties
Property Value Source
water solubility 7.34e-01 g/l ALOGPS
logP 0.91 ALOGPS
logP 1.17 ChemAxon Molconvert
logS -2.78 ALOGPS
pKa 11.44 ChemAxon Molconvert
hydrogen acceptor count 10 ChemAxon Molconvert
hydrogen donor count 8 ChemAxon Molconvert
polar surface area 163.18 ChemAxon Molconvert
rotatable bond count 12 ChemAxon Molconvert
refractivity 123.53 ChemAxon Molconvert
polarizability 48.49 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.
食物相互作用
Not Available

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