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 |
|---|---|---|
| Biochemical effects of bleomycin A2 on Novikoff hepatoma ascites cells. | 1975 |
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| 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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| The effect of bleomycin A2(-Cu) on the proliferation of brain tumor cells and strained epithelial cells in vitro. | 1976 Mar 20 |
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| Lack of metabolism as the biochemical basis of bleomycin-induced pulmonary toxicity. | 1983 May |
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| Renovascular hypertension after combination chemotherapy for testicular cancer. | 1988 Jan |
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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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| Raynaud's phenomenon in patients treated with cisplatin, vinblastine, and bleomycin for germ cell cancer: measurement of vasoconstrictor response to cold. | 1989 Jul |
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| Long-term neurotoxicity in patients treated with cisplatin, vinblastine, and bleomycin for metastatic germ cell cancer. | 1989 Oct |
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| Autonomic neuropathy after treatment with cisplatin, vinblastine, and bleomycin for germ cell cancer. | 1990 Feb 24 |
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| Hemolytic-uremic syndrome associated with neoadjuvant chemotherapy in the treatment of advanced cervical cancer. | 1990 Nov |
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| Selective loss of optic nerve beta-tubulin in vincristine-induced blindness. | 1992 Aug |
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| Lethal ischemic stroke after cisplatin-based chemotherapy for testicular carcinoma and cannabis inhalation. | 2002 |
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| A case of treatment-related myelodysplastic syndrome and acute myelogenous leukemia following high-dose chemotherapy with autologous stem cell transplantation for non-Hodgkin's lymphoma. | 2002 Aug |
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| An antisense oligonucleotide targeted to human Ku86 messenger RNA sensitizes M059K malignant glioma cells to ionizing radiation, bleomycin, and etoposide but not DNA cross-linking agents. | 2002 Oct 15 |
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| Codon 64 of K-ras gene mutation pattern in hepatocellular carcinomas induced by bleomycin and 1-nitropyrene in A/J mice. | 2003 |
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| Dual roles of IL-4 in lung injury and fibrosis. | 2003 Feb 15 |
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| The prognostic role of CD4+ and CD8+ lymphocytes during chemoimmunotherapy in metastatic melanoma. | 2004 Dec |
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| Inhibition of key cytokines by tetrathiomolybdate in the bleomycin model of pulmonary fibrosis. | 2004 Dec |
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| The influence of dexamethasone on the proliferation and apoptosis of pulmonary inflammatory cells in bleomycin-induced pulmonary fibrosis in rats. | 2004 Mar |
|
| Regulation of found in inflammatory zone 1 expression in bleomycin-induced lung fibrosis: role of IL-4/IL-13 and mediation via STAT-6. | 2004 Sep 1 |
|
| Feitai, a Chinese herbal medicine, reduces transforming growth factor-beta1 and monocyte chemoattractant protein-1 expression in bleomycin-induced lung fibrosis in mice. | 2005 Dec |
|
| ROLE OF ENDOGENOUS AND EXOGENOUS LIGANDS FOR THE PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR alpha IN THE DEVELOPMENT OF BLEOMYCIN-INDUCED LUNG INJURY. | 2005 Dec |
|
| Role of Eotaxin-1 (CCL11) and CC chemokine receptor 3 (CCR3) in bleomycin-induced lung injury and fibrosis. | 2005 Dec |
|
| [Effects of valsartan on bleomycin-induced pulmonary fibrosis in rats and the expression of hepatocyte growth factor in lung tissue]. | 2005 Jul |
|
| Resveratrol alleviates bleomycin-induced lung injury in rats. | 2007 |
|
| 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 |
|
| PPAR-gamma agonists inhibit profibrotic phenotypes in human lung fibroblasts and bleomycin-induced pulmonary fibrosis. | 2008 May |
|
| Simvastatin attenuates bleomycin-induced pulmonary fibrosis in mice. | 2008 Sep 20 |
|
| Rosiglitazone abrogates bleomycin-induced scleroderma and blocks profibrotic responses through peroxisome proliferator-activated receptor-gamma. | 2009 Feb |
|
| Epigallocatechin-3-gallate exhibits anti-fibrotic effect by attenuating bleomycin-induced glycoconjugates, lysosomal hydrolases and ultrastructural changes in rat model pulmonary fibrosis. | 2009 Jul 15 |
|
| Bleomycin-induced nuclear factor-kappaB activation in human bronchial epithelial cells involves the phosphorylation of glycogen synthase kinase 3beta. | 2009 Jun 22 |
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| Effects of erlotinib on lung injury induced by intratracheal administration of bleomycin (BLM) in rats. | 2010 Aug |
|
| Influence of p53 expression on sensitivity of cancer cells to bleomycin. | 2010 Jul-Aug |
|
| C/EBPβ-Thr217 phosphorylation signaling contributes to the development of lung injury and fibrosis in mice. | 2011 |
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| Anti-inflammatory and antifibrotic effects of methyl palmitate. | 2011 Aug 1 |
|
| Links between DNA polymerase beta expression and sensitivity to bleomycin. | 2011 Mar 15 |
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| Removal of reactive oxygen species-induced 3'-blocked ends by XPF-ERCC1. | 2011 Nov 21 |
|
| Testing chemical agents with the cytokinesis-block micronucleus cytome assay. | 2012 |
|
| Preventing cleavage of Mer promotes efferocytosis and suppresses acute lung injury in bleomycin treated mice. | 2012 Aug 15 |
|
| 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 |
|
| Assessment of Brd4 inhibition in idiopathic pulmonary fibrosis lung fibroblasts and in vivo models of lung fibrosis. | 2013 Aug |
|
| Comparison of bleomycin-induced pulmonary apoptosis between NMRI mice and C57BL/6 mice. | 2013 Jan |
|
| Suppression of nuclear factor erythroid 2-related factor 2 via extracellular signal-regulated kinase contributes to bleomycin-induced oxidative stress and fibrogenesis. | 2013 Jun 20 |
|
| Matrix metalloproteinase Mmp-1a is dispensable for normal growth and fertility in mice and promotes lung cancer progression by modulating inflammatory responses. | 2013 May 17 |
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| Berberine attenuates bleomycin induced pulmonary toxicity and fibrosis via suppressing NF-κB dependant TGF-β activation: a biphasic experimental study. | 2013 May 23 |
|
| 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 |
|
| Direct activation of ATM by resveratrol under oxidizing conditions. | 2014 |
|
| Distinct mechanisms of cell-kill by triapine and its terminally dimethylated derivative Dp44mT due to a loss or gain of activity of their copper(II) complexes. | 2014 Oct 1 |
|
| Protocatechuic aldehyde ameliorates experimental pulmonary fibrosis by modulating HMGB1/RAGE pathway. | 2015 Feb 15 |
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 |
116
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WHO-VATC |
QL01DC01
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NCI_THESAURUS |
C2311
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NDF-RT |
N0000180854
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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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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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D001761
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11056-06-7
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11056-06-7
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C313
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40S1VHN69B
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M2589
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DB00290
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BLEOMYCIN
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2721
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ACTIVE MOIETY
