Bleomycin
- CAS No.
- 11056-06-7
- Chemical Name:
- Bleomycin
- Synonyms
- BLM;BLEO;BLEXANE;Bleocin;Bleomycin;BLENOXANE;bleomicin;Bleocinbase;DNA helicase;Bleo Bleocin
- CBNumber:
- CB5412174
- Molecular Formula:
- C110H168N34O46S7
- Molecular Weight:
- 2927.17
- MOL File:
- 11056-06-7.mol
- MSDS File:
- SDS
- Modify Date:
- 2023/6/26 13:30:34
| storage temp. | 2-8°C |
|---|---|
| solubility | H2O: 20 mg/mL |
| form | powder |
| color | white |
| IARC | 2B (Vol. 26, Sup 7) 1987, 1 (Vol. 76, 100A) 2012 |
| EPA Substance Registry System | Bleomycin (11056-06-7) |
SAFETY
Risk and Safety Statements
| Hazard Codes | T |
|---|---|
| Risk Statements | 46-40 |
| Safety Statements | 53-36/37-45 |
| WGK Germany | 3 |
| RTECS | EC5991990 |
| F | 10 |
| Toxicity | dog,LD,oral,> 100mg/kg (100mg/kg),Japanese Journal of Antibiotics. Vol. 28, Pg. 1, 1975. |
Bleomycin Chemical Properties,Uses,Production
Description
Bleomycin is a complex of no less than 16 glycopeptide antibiotics made from the family Streptomyces verticilus, which have different R groups. Bleomycines exhibit antitumor, antiviral, and antibacterial activity. When bound to DNA, they disturb the spiraling of both single and double strands of DNA. To a lesser degree, they inhibit RNA and protein synthesis. It is administered both intravenously and intramuscularly.
Uses
Bleomycin sulfate USP (Blenoxane)is used to traet squamous cell carcinoma of head, neck, esophagus, skin, GU tract; testicular tumor; Hodgkin’s lymphomas.
Indications
The bleomycins are a group of glycopeptides that are isolated from Streptomyces verticillus. The clinical preparation, bleomycin sulfate (Blenoxane), is a mixture of several components. Bleomycin binds to DNA, in part through an intercalation mechanism, without markedly altering the secondary structure of the nucleic acid. The drug produces both single- and double-strand scission and fragmentation of DNA. It is thought that the bleomycins, which are avid metal-chelating agents, form a bleomycin–Fe ++ complex that can donate electrons to molecular oxygen, thus forming the superoxide and hydroxyl free radicals. It is these highly reactive intermediates that attack DNA and produce DNA strand breakage and maximum cytotoxicity in the late G2 and early M-phases of the cell cycle.
Definition
A species of bleomycin noted for its adverse pulmonary effects in humans. It is a complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2.
General Description
Bleomycin is a glycopeptide antibiotic complex isolatedfrom Streptomyces verticillus initially by Umezawa.Atleast 13 different fractions of bleomycin have been isolatedwith the clinically used product (Blenoxane) being a mixtureof predominantly A22 (55%–70%) and B2 (25%–32%)fractions.Of these fractions, A2 appears to possessthe greatest antineoplastic activity. Copper is found inthe naturally occurring material, and its removal is importantfor the material used clinically because it significantlyreduces activity.
Bleomycin is notable for its lack of myelotoxicity, andthis allows it to be combined with other myelosuppressantswithout a resulting additive effect. The acute toxicities seenwith bleomycin are erythema (reddening of the skin), hyperpigmentation(skin darkening) found predominately on theextremities, and pulmonary toxicity. The pulmonary toxicitymay first occur as pneumonitis (inflammation of lung tissue),which normally responds to glucocorticosteroid therapy.Chronic pulmonary toxicity is expressed as pulmonaryfibrosis, which is irreversible and limits utility of the agent.
Air & Water Reactions
Water soluble
Hazard
Possible carcinogen.
Fire Hazard
Flash point data for Bleomycin are not available. Bleomycin is probably nonflammable.
Mechanism of action
Bleomycin is poorly absorbed orally, but it can be given by various parenteral routes. Its plasma half-life is not affected by renal dysfunction as long as creatinine clearance is greater than 35 mL/minute. Bleomycin hydrolase, which inactivates bleomycin, is an enzyme that is abundant in liver and kidney but virtually absent in lungs and skin; the latter two organs are the major targets of bleomycin toxicity. It is thought that bleomycin-induced dermal and pulmonary toxicities are related to the persistence of relatively high local concentrations of active drug.
Clinical Use
Bleomycin, in combination with cisplatin or etoposide, is important as part of the potentially curative combination chemotherapy of advanced testicular carcinomas. Bleomycin is used in some standard regimens for the treatment of Hodgkin’s and non-Hodgkin’s lymphomas, and it is useful against squamous cell carcinomas of the head and neck, cervix, and skin.
Side effects
A potentially fatal lung toxicity occurs in 10 to 20% of patients receiving bleomycin. Patients particularly at risk are those who are over 70 years of age and have had radiation therapy to the chest. Rarely, bleomycin also may cause allergic pneumonitis. Bleomycin skin toxicity is manifested by hyperpigmentation, erythematosus rashes, and thickening of the skin over the dorsum of the hands and at dermal pressure points, such as the elbows. Many patients develop a low-grade transient fever within 24 hours of receiving bleomycin. Less common adverse effects include mucositis, alopecia, headache, nausea, and arteritis of the distal extremities.
Bleomycin Preparation Products And Raw materials
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Aspen Biopharma Labs Pvt Ltd | +91-9248058660 +91-9248058662 | Telangana, India | 234 | 58 | Inquiry |
| Euroasia Trans Continental | +91 22 56349035-36 | New Delhi, India | 519 | 47 | Inquiry |
| Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| Hangzhou ICH Biofarm Co., Ltd | +86-0571-28186870; +undefined8613073685410 | China | 985 | 58 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29901 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | China | 49391 | 58 | Inquiry |
| Hefei TNJ Chemical Industry Co.,Ltd. | 0551-65418671 | China | 34571 | 58 | Inquiry |
| Wuhan Fortuna Chemical Co., Ltd | +86-027-59207850 | China | 5999 | 58 | Inquiry |
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