Bleomycin

  • C55H84N17O21S3 ( bleomycin A2)
  • C55H84N20O21S2 ( bleomycin B2)

L01DC01

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Bleomycin is an antibiotic from the group of glycopeptides, which is used as a drug in the form of its water-soluble salts ( sulfate, hydrochloride) as a cytostatic agent in the treatment of cancer (chemotherapy).

Origin and composition

Bleomycins are naturally produced by Streptomyces verticillus. Streptomycetes form a genus of Actinobacteria. Bleomycin was discovered in 1962 by Japanese scientist Hamao Umezawa.

The drug bleomycin is obtained by fermentation and consists essentially of two individual compounds of the group of substances bleomycins together: to 55 - 70 % from the Dimethylsulfoniumaminopropyl derivative ( = bleomycin A2) and 25 - 32 % from the agmatine derivative ( = bleomycin B2 ) the Bleomycinsäure; the total content of bleomycin A2 B2 is at least 85%.

Pharmacology

In oncology, bleomycin is used as a cytostatic agent, among other things, in combination with cisplatin and etoposide. Bleomycin complexed divalent metal cation, mainly Fe (II). This complex is oxidized and activated by reactive oxygen species (ROS). The activated complex caused a radical abstraction of the 4'- H atom of a nucleotide in the minor groove of DNA, resulting in DNA strand breaks result. It is so to fragment the DNA. Further inhibits Bleomycin DNA-dependent polymerase.

In dermatology, bleomycin is usually used in combination with salicylic acid wart remover.

Side effects

A significant side effect that occurs in up to 18% of patients treated with bleomycin patients, the pulmonary fibrosis. Risk factors for the development of bleomycin - induced lung fibrosis are high age, high drug dose, increased oxygen concentration in the inhaled air, irradiation of the thorax ( simultaneously or subsequently ), and renal insufficiency. Most of this side effect occurs after 1-6 months, but it can rarely, acute or even much later than 6 months occur.

Trade names

Bleo -cell (D), Bleomedac (D ), various generics (D, A, CH)

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Active ingredient
132184
de