DescriptionSources: http://news.cancerconnect.com/wp-content/uploads/2010/06/bleomycin.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdfhttp://www.drugbank.ca/drugs/DB00290#targetsCurator's Comment: description was created based on several sources, including, http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdf
Sources: http://news.cancerconnect.com/wp-content/uploads/2010/06/bleomycin.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdfhttp://www.drugbank.ca/drugs/DB00290#targets
Curator's Comment: description was created based on several sources, including, http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdf
Bleomycin is a mixture of cytotoxic glycopeptide antibiotics isolated from a strain of Streptomyces verticillus. Bleomycin has 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).
Originator
Sources: https://www.ncbi.nlm.nih.gov/pubmed/5953301 | https://www.ncbi.nlm.nih.gov/pubmed/23060708http://onlinelibrary.wiley.com/doi/10.1002/1097-0142(1967)20:5%3C891::AID-CNCR2820200550%3E3.0.CO;2-V/pdf
Curator's Comment: Umezawa et al (Institute of Microbial Chemistry, Tokyo National Institute of Health, Tokyo, Japan)
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL2311221 |
20.0 µM [Kd] | ||
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | BLEOMYCIN SULFATE Approved UseBleomycin for Injection, USP should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agents:
Squamous Cell Carcinoma: Head and neck (including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingivae, epiglottis, skin, larynx), penis, cervix, and vulva. The response to Bleomycin for Injection is poorer in patients with previously irradiated head and neck cancer.
Lymphomas: Hodgkin’s disease, non-Hodgkin’s lymphoma.
Testicular Carcinoma: Embryonal cell, choriocarcinoma, and teratocarcinoma.
Bleomycin for Injection, USP has also been shown to be useful in the management of:
Malignant Pleural Effusion: Bleomycin for Injection is effective as a sclerosing agent for the treatment of malignant pleural effusion and prevention of recurrent pleural effusions. Launch Date1.12924803E11 |
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| Primary | BLEOMYCIN SULFATE Approved UseBleomycin for Injection, USP should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agents:
Squamous Cell Carcinoma: Head and neck (including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingivae, epiglottis, skin, larynx), penis, cervix, and vulva. The response to Bleomycin for Injection is poorer in patients with previously irradiated head and neck cancer.
Lymphomas: Hodgkin’s disease, non-Hodgkin’s lymphoma.
Testicular Carcinoma: Embryonal cell, choriocarcinoma, and teratocarcinoma.
Bleomycin for Injection, USP has also been shown to be useful in the management of:
Malignant Pleural Effusion: Bleomycin for Injection is effective as a sclerosing agent for the treatment of malignant pleural effusion and prevention of recurrent pleural effusions. Launch Date1.12924803E11 |
|||
| Primary | BLEOMYCIN SULFATE Approved UseBleomycin for Injection, USP should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agents:
Squamous Cell Carcinoma: Head and neck (including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingivae, epiglottis, skin, larynx), penis, cervix, and vulva. The response to Bleomycin for Injection is poorer in patients with previously irradiated head and neck cancer.
Lymphomas: Hodgkin’s disease, non-Hodgkin’s lymphoma.
Testicular Carcinoma: Embryonal cell, choriocarcinoma, and teratocarcinoma.
Bleomycin for Injection, USP has also been shown to be useful in the management of:
Malignant Pleural Effusion: Bleomycin for Injection is effective as a sclerosing agent for the treatment of malignant pleural effusion and prevention of recurrent pleural effusions. Launch Date1.12924803E11 |
|||
| Primary | BLEOMYCIN SULFATE Approved UseBleomycin for Injection, USP should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agents:
Squamous Cell Carcinoma: Head and neck (including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingivae, epiglottis, skin, larynx), penis, cervix, and vulva. The response to Bleomycin for Injection is poorer in patients with previously irradiated head and neck cancer.
Lymphomas: Hodgkin’s disease, non-Hodgkin’s lymphoma.
Testicular Carcinoma: Embryonal cell, choriocarcinoma, and teratocarcinoma.
Bleomycin for Injection, USP has also been shown to be useful in the management of:
Malignant Pleural Effusion: Bleomycin for Injection is effective as a sclerosing agent for the treatment of malignant pleural effusion and prevention of recurrent pleural effusions. Launch Date1.12924803E11 |
|||
| Primary | BLEOMYCIN SULFATE Approved UseBleomycin for Injection, USP should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agents:
Squamous Cell Carcinoma: Head and neck (including mouth, tongue, tonsil, nasopharynx, oropharynx, sinus, palate, lip, buccal mucosa, gingivae, epiglottis, skin, larynx), penis, cervix, and vulva. The response to Bleomycin for Injection is poorer in patients with previously irradiated head and neck cancer.
Lymphomas: Hodgkin’s disease, non-Hodgkin’s lymphoma.
Testicular Carcinoma: Embryonal cell, choriocarcinoma, and teratocarcinoma.
Bleomycin for Injection, USP has also been shown to be useful in the management of:
Malignant Pleural Effusion: Bleomycin for Injection is effective as a sclerosing agent for the treatment of malignant pleural effusion and prevention of recurrent pleural effusions. Launch Date1.12924803E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
|||
| Primary | BLENOXANE Approved UseBLENOXANE should be considered a palliative treatment. It has been shown to be useful in the management of the following neoplasms either as a single agent or in proven combinations with other approved chemotherapeutic agent:Squamous Cell Carcinoma, Lymphomas, Testicular Carcinoma, Malignant Pleural Effusion. Launch Date1.74355202E11 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Ultrastructural study of the effect of bleomycin A2 on the nucleolus and its possibly related cytoplasmic constituents in Novikoff hepatoma cells. | 1975 Feb |
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| Lack of metabolism as the biochemical basis of bleomycin-induced pulmonary toxicity. | 1983 May |
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| Hypomagnesemia, renal dysfunction, and Raynaud's phenomenon in patients treated with cisplatin, vinblastine, and bleomycin. | 1985 Dec 15 |
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| Hemolytic uremic syndrome following cisplatin, bleomycin, and vincristine chemotherapy: a report of a case and a review of the literature. | 1989 |
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| Vascular toxicity and the mechanism underlying Raynaud's phenomenon in patients treated with cisplatin, vinblastine and bleomycin. | 1990 Jul |
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| CC-chemokine receptor 2 required for bleomycin-induced pulmonary fibrosis. | 2003 Dec 21 |
|
| Dual roles of IL-4 in lung injury and fibrosis. | 2003 Feb 15 |
|
| The prognostic role of CD4+ and CD8+ lymphocytes during chemoimmunotherapy in metastatic melanoma. | 2004 Dec |
|
| Role of Eotaxin-1 (CCL11) and CC chemokine receptor 3 (CCR3) in bleomycin-induced lung injury and fibrosis. | 2005 Dec |
|
| [Rat alveolar type II injured by bleomycin]. | 2005 Feb |
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| Effect of Feitai on bleomycin-induced pulmonary fibrosis in rats. | 2005 Jan 15 |
|
| Pharmacological inhibition of leukotrienes in an animal model of bleomycin-induced acute lung injury. | 2006 Nov 21 |
|
| Dexrazoxane-associated risk for acute myeloid leukemia/myelodysplastic syndrome and other secondary malignancies in pediatric Hodgkin's disease. | 2007 Feb 10 |
|
| Are platinum-based chemotherapeutic drugs safe for patients with Charcot-Marie-Tooth disease? | 2007 Jun |
|
| FDG-PET in bleomycin-induced pneumonitis following ABVD chemotherapy for Hodgkin's disease--a useful tool for monitoring pulmonary toxicity and disease activity. | 2007 Nov |
|
| Simvastatin attenuates bleomycin-induced pulmonary fibrosis in mice. | 2008 Sep 20 |
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| Effects of erlotinib on lung injury induced by intratracheal administration of bleomycin (BLM) in rats. | 2010 Aug |
|
| XRCC1 deficiency sensitizes human lung epithelial cells to genotoxicity by crocidolite asbestos and Libby amphibole. | 2010 Dec |
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| Influence of p53 expression on sensitivity of cancer cells to bleomycin. | 2010 Jul-Aug |
|
| Pulmonary fibrosis inducer, bleomycin, causes redox-sensitive activation of phospholipase D and cytotoxicity through formation of bioactive lipid signal mediator, phosphatidic acid, in lung microvascular endothelial cells. | 2011 Feb |
|
| Thymoquinone blocks lung injury and fibrosis by attenuating bleomycin-induced oxidative stress and activation of nuclear factor Kappa-B in rats. | 2012 Dec 16 |
|
| The ToxTracker assay: novel GFP reporter systems that provide mechanistic insight into the genotoxic properties of chemicals. | 2012 Jan |
|
| Diallylsulfide attenuates excessive collagen production and apoptosis in a rat model of bleomycin induced pulmonary fibrosis through the involvement of protease activated receptor-2. | 2013 Sep 1 |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: Bleomycin can be given intramuscularly, or subcutaneously in Squamous cell carcinoma, non-Hodgkin’s lymphoma, testicular carcinoma, Hodgkin’s disease and as a single dose bolus intrapleural injection (60 units) in Malignant Pleural Effusion.
The main components of Bleomycin for Injection are bleomycins A2 and B2.
Squamous cell carcinoma, non-Hodgkin’s lymphoma, testicular carcinoma - 0.25 to 0.50 units/kg
(10 to 20 units/m2) given intravenously, intramuscularly, or subcutaneously weekly or twice weekly.
Route of Administration:
Other
Purified nucleolar DNA was markedly degraded at a concentration of 13 ug/ml by bleomycin A2; bleomycin concentrations 20-30 times greater were required to degrade nucleoplasmic DNA. Whole nuclear DNA was degraded to only a small extent at 13 ug/ml but was markedly degraded at higher bleomycin concentrations.
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LIVERTOX |
NBK548499
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QL01DC01
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C2311
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WHO-ESSENTIAL MEDICINES LIST |
8.2
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FDA ORPHAN DRUG |
118498
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FDA ORPHAN DRUG |
326510
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WHO-ATC |
L01DC01
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4742
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3139
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Bleomycin
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1622
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SUB00842MIG
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3208
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CHEMBL3039590
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C313
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M2589
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DB00290
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BLEOMYCIN
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ACTIVE MOIETY
