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药品详细

Amsacrine(安吖啶)

化学结构式图
中文名
安吖啶
英文名
Amsacrine
分子式
C21H19N3O3S
化学名
N-{4-[(acridin-9-yl)amino]-3-methoxyphenyl}methanesulfonamide
分子量
Average: 393.459
Monoisotopic: 393.114712179
CAS号
51264-14-3
ATC分类
L01X 其它抗肿瘤药
药物类型
small molecule
阶段
approved
商品名
AMSA P-D;Amsidine;Amsidyl;Amsine;
同义名
Acridinyl Anisidide;M-AMSA;MAMSA;
基本介绍

Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. [PubChem]

生产厂家
    封装厂家
    参考
    Synthesis Reference Not Available
    General Reference
    1. Link
    剂型
    规格
    化合物类型
    Type small molecule
    Classes
    • Acridines
    Substructures
    • Acridines
    • Aliphatic and Aryl Amines
    • Phenols and Derivatives
    • Pyridines and Derivatives
    • Sulfonyls
    • Ethers
    • Benzene and Derivatives
    • Aminoquinolines and Derivatives
    • Aminopyridines and Derivatives
    • Heterocyclic compounds
    • Aromatic compounds
    • Anisoles
    • (Iso)quinolines and Derivatives
    • Sulfonamides
    • Phenyl Esters
    • Anilines
    适应症
    Cancer 癌症;
    药理
    Indication For treatment of acute myeloid leukaemia.
    Pharmacodynamics Amsacrine is an aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects.
    Mechanism of action Amsacrine binds to DNA through intercalation and external binding. It has a base specificity for A-T pairs. Rapidly dividing cells are two to four times more sensitive to amsacrine than are resting cells. Amsacrine appears to cleave DNA by inducing double stranded breaks. Amsacrine also targets and inhibits topoisomerase II. Cytotoxicity is greatest during the S phase of the cell cycle when topoisomerase levels are at a maximum.
    Absorption Poorly absorbed
    Volume of distribution Not Available
    Protein binding 96-98%
    Metabolism
    Extensive, primarily hepatic, converted to glutathione conjugate.
    Route of elimination Not Available
    Half life 8-9 hours
    Clearance Not Available
    Toxicity Symptoms of overdose include nausea and vomiting, diarrhea, some cardiotoxicity (rarely).
    Affected organisms
    • Humans and other mammals
    Pathways Not Available
    理化性质
    Properties
    State solid
    Experimental Properties
    Property Value Source
    melting point 235 °C PhysProp
    water solubility <1 mg/mL Not Available
    logP 3.8 Not Available
    Predicted Properties
    Property Value Source
    water solubility 3.17e-03 g/l ALOGPS
    logP 4.66 ALOGPS
    logP 3.16 ChemAxon
    logS -5.1 ALOGPS
    pKa (strongest acidic) 10.82 ChemAxon
    pKa (strongest basic) 8.44 ChemAxon
    physiological charge 1 ChemAxon
    hydrogen acceptor count 5 ChemAxon
    hydrogen donor count 2 ChemAxon
    polar surface area 80.32 ChemAxon
    rotatable bond count 4 ChemAxon
    refractivity 107.69 ChemAxon
    polarizability 41.65 ChemAxon
    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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