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Other antitumour antibioticsIn useNatural product

Bleomycin

Also known as Blenoxane

A mixture of glycopeptide antibiotics from Streptomyces verticillus, given by injection. The US label lists squamous cell carcinomas, lymphomas and testicular carcinoma, and use as a sclerosing agent for malignant pleural effusion.

From discovery to approval

  1. 1966 · First described

    A 2009 review says bleomycin, made by the bacterium Streptomyces verticillus, was first reported by Umezawa and colleagues in 1966. The 1966 paper is cited by title only. A 2015 textbook chapter dates the discovery of its anticancer activity to 1962 screening in Japan.[2][3][4][5][6]

  2. 1973-07-31 · FDA regular · 7 years after first description

    Bleomycin sulfate for injection (Blenoxane), NDA 050443, original approval, classed as a new molecular entity (Type 1) in the Drugs@FDA history. The original label and letter are not available there, so the indication at approval is not stated here; the current generic label lists squamous cell carcinomas, lymphomas, testicular carcinoma and malignant pleural effusion. The type regular is an inference: no accelerated-approval wording was found.[7]

How it works

Causes single-stranded and, to a lesser extent, double-stranded DNA breaks. The label calls inhibition of DNA synthesis the main mode of action, says the exact mechanism is unknown, and reports cell cycle arrest in G2 and in mitosis.[1]

Where it came from and why

The reviews cited do not state why the screening was begun. Umezawa's 1978 paper describes bleomycin as an analogue of phleomycin chosen for lower kidney toxicity, and his 1976 review says a lower content of an inactivating enzyme was shown to be at least one reason for its activity against squamous cell carcinoma.

Cancers

  • Squamous cell carcinomas

    A 1970 European clinical screening study of 237 patients judged bleomycin more effective than earlier drugs for squamous cell carcinoma of the skin and of the penis, vulva, oesophagus and uterine cervix. The US label lists head and neck, penis, cervix and vulva.[8]

  • Lymphomas

    The US label lists Hodgkin's disease and non-Hodgkin's lymphoma, as a single agent or in combinations with other approved chemotherapy.[1]

  • Testicular cancer

    Used with cisplatin and vinblastine in a 1977 series of 50 patients with disseminated testicular cancer; the US label lists embryonal cell carcinoma, choriocarcinoma and teratocarcinoma.[9]

  • Malignant pleural effusion

    The US label says bleomycin is effective as a sclerosing agent for treating malignant pleural effusion and preventing its recurrence.[1]

Family and partners

Drugs derived from it: Peplomycin

Worth knowing

  • Umezawa's 1978 paper describes bleomycin as an analogue of phleomycin that was chosen because of its lower renal toxicity.[5]
  • In the 1970 European study of 237 patients, bleomycin showed no haemopoietic toxicity or immunosuppressive action, but caused toxic effects on skin, mucosae and lungs.[8]
  • A 2005 review says the therapeutic efficacy of the bleomycins is limited by the development of lung fibrosis.[10]
  • Umezawa's 1976 review identifies a bleomycin-inactivating enzyme as a new aminopeptidase B and says that a lower content of this enzyme was shown to be at least one reason for the drug's activity against squamous cell carcinoma.[6]

On this site

References

  1. DailyMed. Bleomycin for injection, Meitheal Pharmaceuticals Inc. (ANDA205030), SPL set id 640602f9-a7df-46f0-a9b1-19c471008bee, version 3, effective 17 April 2026 (text read through the openFDA drug label API). Source
  2. Umezawa H, Maeda K, Takeuchi T, Okami Y. New antibiotics, bleomycin A and B. J Antibiot (Tokyo). 1966;19(5):200-9. PubMed
  3. Demain AL, Sanchez S. Microbial drug discovery: 80 years of progress. J Antibiot (Tokyo). 2009;62(1):5-16. PubMedDOI
  4. Weber GF. Drugs that Suppress Proliferation (section: DNA Damaging Drugs). In: Molecular Therapies of Cancer. Cham: Springer International Publishing; 2015. p. 113-162. doi:10.1007/978-3-319-13278-5_3. DOISource
  5. Umezawa H. New microbial secondary metabolites under preclinical development for cancer treatment. Recent Results Cancer Res. 1978;63:120-34. PubMedDOI
  6. Umezawa H. Structure and action of bleomycin. Prog Biochem Pharmacol. 1976;11:18-27. PubMed
  7. U.S. Food and Drug Administration. Drugs@FDA: Approval date(s) and history, letters, labels, reviews for NDA 050443 (Blenoxane, bleomycin sulfate). Page read 2026-10-29. Source
  8. Clinical Screening Co-operative Group of the European Organization for Research on the Treatment of Cancer. Study of the clinical efficiency of bleomycin in human cancer. Br Med J. 1970;2(5710):643-5. PubMed
  9. Einhorn LH, Donohue J. Cis-diamminedichloroplatinum, vinblastine, and bleomycin combination chemotherapy in disseminated testicular cancer. Ann Intern Med. 1977;87(3):293-8. PubMedDOI
  10. Chen J, Stubbe J. Bleomycins: towards better therapeutics. Nat Rev Cancer. 2005;5(2):102-12. PubMedDOI