药品详细
Bleomycin(博来霉素)
化学结构式图
中文名
博来霉素
英文名
Bleomycin
分子式
C55H84N17O21S3
化学名
(3-{[2-(2-{2-[(2S,3R)-2-[(2S,3S,4R)-4-[(2S,3R)-2-({6-amino-2-[(1S)-1-{[(2S)-2-amino-2-carbamoylethyl]amino}-2-carbamoylethyl]-5-methylpyrimidin-4-yl}formamido)-3-[(3-{[4-(carbamoyloxy)-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl)oxy]-3-(1H-imidazol-5-yl)propanamido]-3-hydroxy-2-methylpentanamido]-3-hydroxybutanamido]ethyl}-1,3-thiazol-4-yl)-1,3-thiazol-4-yl]formamido}propyl)dimethylsulfanium
分子量
Average: 1415.552
Monoisotopic: 1414.518979905
Monoisotopic: 1414.518979905
CAS号
11056-06-7
ATC分类
L01D 细胞毒素抗生素及相关物质
药物类型
small molecule
阶段
approved
商品名
Blenoxane;Bleo;
同义名
Bleocin;Bleomicin;Bleomicina [INN-Spanish];Bleomycin A2;Bleomycin B2;Bleomycin sulfate;Bleomycine [INN-French];Bleomycinum [INN-Latin];BLM;
基本介绍
A complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2 (B2 CAS # 9060-10-0). It inhibits DNA metabolism and is used as an antineoplastic, especially for solid tumors. Bleomycin A2 is used as the representative structure for Bleomycin.
生产厂家
- App pharmaceuticals llc
- Bedford laboratories div ben venue laboratories inc
- Bristol myers squibb co pharmaceutical research institute
- Hospira inc
- Pharmachemie bv
- Teva parenteral medicines inc
封装厂家
参考
| Synthesis Reference | Not Available |
| General Reference |
|
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
|
| Substructures |
|
适应症
Cancer 癌症;
药理
| Indication | For palliative treatment in the management malignant neoplasm (trachea, bronchus, lung), squamous cell carcinoma, and lymphomas. |
| Pharmacodynamics | Bleomycin is an antibiotic which has been shown to have antitumor activity. Bleomycin 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. Bleomycin 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. The antibiotic antitumor drugs are cell cycle-nonspecific except for Bleomycin (which has major effects in G2 and M phases). |
| Mechanism of action | Although the exact mechanism of action of bleomycin is unknown, available evidence would seem to indicate that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis. DNA cleavage by bleomycin depends on oxygen and metal ions, at least in vitro. It is believed that bleomycin chelates metal ions (primarily iron) producing a pseudoenzyme that reacts with oxygen to produce superoxide and hydroxide free radicals that cleave DNA. |
| Absorption | Systemic absorption is approximately 45%. |
| Volume of distribution | Not Available |
| Protein binding | 1% |
| Metabolism |
Hepatic
|
| Route of elimination | It was reported that patients with moderately severe renal failure excreted less than 20% of the dose in the urine. |
| Half life | 115 minutes |
| Clearance | Not Available |
| Toxicity | Excessive exposure may cause fever, chills, nausea, vomiting, mental, confusion, and wheezing. Bleomycin may cause irritation to eyes, skin and respiratory tract. It may also cause a darkening or thickening of the skin. It may cause an allergic reaction. |
| Affected organisms |
|
| Pathways | Not Available |
理化性质
| Properties | |||||||||||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
|
||||||||||||||||||||||||||||||||||||||||||
| Predicted Properties |
|
||||||||||||||||||||||||||||||||||||||||||
药物相互作用
| Drug | Interaction |
|---|---|
| BRENTUXIMAB VEDOTIN | Pulmonary toxicity of bleomycin may be increased. Avoid combination. |
| Digoxin | The antineoplasic agent decreases the effect of digoxin |
| Fosphenytoin | The antineoplasic agent decreases the effect of hydantoin |
| Leflunomide | Immunosuppressants like bleomycin may enhance the adverse/toxic effect of Leflunomide. Specifically, the risk for hematologic toxicity such as pancytopenia, agranulocytosis, and/or thrombocytopenia may be increased. Consider eliminating the use of a leflunomide loading dose in patients who are receiving other immunosuppressants in order to reduce the risk for serious adverse events such as hematologic toxicity. |
| Natalizumab | Immunosuppressants like bleomycin may enhance the adverse/toxic effect of Natalizumab. Specifically, the risk of concurrent infection may be increased. Patients receiving natalizumab should not use concurrent immunosuppressants. |
| Phenytoin | The antineoplasic agent decreases the effect of hydantoin |
| Pimecrolimus | Pimecrolimus may enhance the adverse/toxic effect of immunosuppressants like bleomycin. This combination is contraindicated |
| Roflumilast | Roflumilast may enhance the immunosuppressive effect of Immunosuppressants.The Canadian product monograph (Daxas brand) recommends avoiding concurrent use with immunosuppressants. U.S. prescribing information (Daliresp brand) does not include such a warning. |
| Tacrolimus | Tacrolimus (Topical) may enhance the adverse/toxic effect of Immunosuppressants. Avoid use of tacrolimus ointment in patients receiving immunosuppressants. |
| 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
收藏