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 Bleomycin sulfate

bleomycin sulfate is a  mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus. Bleomycin sulfate forms complexes with iron that reduce molecular oxygen to superoxide and hydroxyl radicals which cause single- and double-stranded breaks in DNA; these reactive oxygen species also induce lipid peroxidation, carbohydrate oxidation, and alterations in prostaglandin synthesis and degradation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).

BLENOXANE® (bleomycin sulfate for injection, USP) is a mixture of cytotoxic glycopeptide antibiotics isolated from a strain of Streptomyces verticillus. It is freely soluble in water. Note: A unit of bleomycin is equal to the formerly used milligram activity. The term milligram activity is a misnomer and was changed to units to be more precise.

Mechanism of Action

Although the exact mechanism of action of BLENOXANE is unknown, available evidence indicates that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis. Bleomycin is known to cause single, and to a lesser extent, double-stranded breaks in DNA. In in vitro and in vivo experiments, bleomycin has been shown to cause cell cycle arrest in G2 and in mitosis. When administered into the pleural cavity in the treatment of malignant pleural effusion, BLENOXANE acts as a sclerosing agent.

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352: Yamashita T. [The drug sensitivity of human gastric cancer implanted into the subcutis and stomach wall of nude mice]. Nippon Gan Chiryo Gakkai Shi. 1989 Mar 20;24(3):611-6. Japanese. PubMed PMID: 2475559.

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461: Singh B, Gupta RS. Mutagenic responses of thirteen anticancer drugs on mutation induction at multiple genetic loci and on sister chromatid exchanges in Chinese hamster ovary cells. Cancer Res. 1983 Feb;43(2):577-84. PubMed PMID: 6848181.

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482: Moore CW. Control of in vivo (cellular) phleomycin sensitivity by nuclear genotype, growth phase, and metal ions. Cancer Res. 1982 Mar;42(3):929-33. PubMed PMID: 6174219.

483: Wu PC, Ozols RF, Hatanaka M, Boone CW. Anticancer drugs: effect on the cloning of Raji lymphoma cells in soft agar. J Natl Cancer Inst. 1982 Jan;68(1):115-21. PubMed PMID: 6948121.

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528: Abe I, Sato S. Beta-glucuronidase activity of Yoshida ascites hepatomas of different drug-sensitivity and its change after treatment of host rats with various anticancer agents. Gann. 1976 Feb;67(1):55-65. PubMed PMID: 57896.

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