药品详细
Idarubicin (去甲氧柔红霉素 )
化学结构式图
中文名
去甲氧柔红霉素
英文名
Idarubicin
分子式
Not Available
化学名
(7S,9S)-9-acetyl-7-{[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy}-6,9,11-trihydroxy-5,7,8,9,10,12-hexahydrotetracene-5,12-dione
分子量
Average: 497.4939
Monoisotopic: 497.168581467
Monoisotopic: 497.168581467
CAS号
58957-92-9
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
Idamycin;Idamycin PFS;Idarubicin Aglycone;Idarubicin HCl PFS;
同义名
Idarubicin Hcl;Idarubicin Hydrochloride;Idarubicina [INN-Spanish];Idarubicine [INN-French];Idarubicinum [INN-Latin];
基本介绍
An orally administered anthracycline antineoplastic. The compound has shown activity against breast cancer, lymphomas and leukemias, together with the potential for reduced cardiac toxicity. [PubChem]
生产厂家
- App pharmaceuticals llc
- Bedford laboratories
- Pharmacia and upjohn co
- Teva parenteral medicines inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
| Form | Route | Strength |
|---|---|---|
| Powder, for solution | Intravenous |
规格
| Unit description | Cost | Unit |
|---|---|---|
| Idamycin pfs 1 mg/ml vial | 60.0 USD | ml |
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
Cancer 癌症;
药理
| Indication | For the treatment of acute myeloid leukemia (AML) in adults. This includes French-American-British (FAB) classifications M1 through M7. |
| Pharmacodynamics | Idarubicin is an antineoplastic in the anthracycline class. General properties of drugs in this class include: interaction with DNA in a variety of different ways including intercalation (squeezing between the base pairs), DNA strand breakage and inhibition with the enzyme topoisomerase II. Most of these compounds have been isolated from natural sources and antibiotics. However, they lack the specificity of the antimicrobial antibiotics and thus produce significant toxicity. The anthracyclines are among the most important antitumor drugs available. Doxorubicin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Idarubicin may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Idarubicin possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific. |
| Mechanism of action | Idarubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Idarubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes. |
| Absorption | Not Available |
| Volume of distribution | Not Available |
| Protein binding | 97% |
| Metabolism | |
| Route of elimination | The drug is eliminated predominately by biliary and to a lesser extent by renal excretion, mostly in the form of idarubicinol. |
| Half life | 22 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||
| Melting point | Not Available | ||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| Trastuzumab | Trastuzumab may increase the cardiotoxicity of Idarubicin. Signs and symptoms of cardiac dysfunction should be monitored for frequently. Increased risk of heart failure. 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
收藏