DescriptionSources: http://www.drugbank.ca/drugs/DB00290#targetshttp://news.cancerconnect.com/wp-content/uploads/2010/06/bleomycin.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdfCurator's Comment: description was created based on several sources, including, http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdf
Sources: http://www.drugbank.ca/drugs/DB00290#targetshttp://news.cancerconnect.com/wp-content/uploads/2010/06/bleomycin.pdf | https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdf
Curator's Comment: description was created based on several sources, including, http://www.accessdata.fda.gov/drugsatfda_docs/label/2010/050443s036lbl.pdf
Bleomycin sulfate is an antineoplastic antibiotic isolated
from Streptomyces verticillus. It is a mixture of
glycopeptide antibiotics containing primarily Bleomycin
A2 (~70%) and B2 (~30%). Bleomycin binds to DNA, inhibits DNA
synthesis, and causes single strand scission of DNA in
vivo and in vitro at specific base sequences.
Originator
Sources: http://onlinelibrary.wiley.com/doi/10.1002/1097-0142(1967)20:5%3C891::AID-CNCR2820200550%3E3.0.CO;2-V/pdfhttps://www.ncbi.nlm.nih.gov/pubmed/5953301 | https://www.ncbi.nlm.nih.gov/pubmed/23060708
Curator's Comment: Bleomycin was discovered by Umezawa et al. (1966)
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 Date1973 |
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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 Date1973 |
|||
| 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 Date1973 |
|||
| 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 Date1973 |
|||
| 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 Date1973 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
|||
| 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 Date1975 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Hypomagnesemia, renal dysfunction, and Raynaud's phenomenon in patients treated with cisplatin, vinblastine, and bleomycin. | 1985 Dec 15 |
|
| [Raynaud's disease after treatment with bleomycin and vinblastine]. | 1986 Feb 17 |
|
| Acute vascular toxicity after combination chemotherapy with cisplatin, vinblastine, and bleomycin for testicular cancer. | 1988 May |
|
| Drug-induced encephalopathy after previous ifosfamide treatment. | 1988 Nov 5 |
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| Pulmonary emboli in patients receiving chemotherapy for non-Hodgkin's lymphoma. | 1988 Sep |
|
| Hemolytic uremic syndrome following cisplatin, bleomycin, and vincristine chemotherapy: a report of a case and a review of the literature. | 1989 |
|
| 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 |
|
| Two cycles of doxorubicin, bleomycin, vinblastine, and dacarbazine plus extended-field radiotherapy is superior to radiotherapy alone in early favorable Hodgkin's lymphoma: final results of the GHSG HD7 trial. | 2007 Aug 10 |
|
| Telomerase activity is required for bleomycin-induced pulmonary fibrosis in mice. | 2007 Dec |
|
| 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 |
|
| Characterization of DNA reactive and non-DNA reactive anticancer drugs by gene expression profiling. | 2007 Jun 1 |
|
| Effects of curcumin in treatment of experimental pulmonary fibrosis: a comparison with hydrocortisone. | 2007 Jun 13 |
|
| 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 |
|
| BMP-7 does not protect against bleomycin-induced lung or skin fibrosis. | 2008 |
|
| Hodgkin lymphoma presenting with various immunologic abnormalities, including autoimmune hepatitis, Hashimoto's thyroiditis, autoimmune hemolytic anemia, and immune thrombocytopenia. | 2008 Feb |
|
| DNA methylation inhibitor 5-Aza-2'-deoxycytidine induces reversible genome-wide DNA damage that is distinctly influenced by DNA methyltransferases 1 and 3B. | 2008 Jan |
|
| Cerebellar dysfunction caused by procarbazine and consumption of excessive amount of bananas. | 2008 Jun |
|
| PPAR-gamma agonists inhibit profibrotic phenotypes in human lung fibroblasts and bleomycin-induced pulmonary fibrosis. | 2008 May |
|
| Agents associated with lung inflammation induce similar responses in NCI-H292 lung epithelial cells. | 2008 Oct |
|
| Simvastatin attenuates bleomycin-induced pulmonary fibrosis in mice. | 2008 Sep 20 |
|
| Radiation-induced cathepsin S is involved in radioresistance. | 2009 Apr 15 |
|
| Rosiglitazone abrogates bleomycin-induced scleroderma and blocks profibrotic responses through peroxisome proliferator-activated receptor-gamma. | 2009 Feb |
|
| Protection of bleomycin-induced fibrosis and inflammation by taurine. | 2009 Jul |
|
| 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 |
|
| 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 |
|
| Influence of p53 expression on sensitivity of cancer cells to bleomycin. | 2010 Jul-Aug |
|
| The D prostanoid receptor agonist BW245C [(4S)-(3-[(3R,S)-3-cyclohexyl-3-hydroxypropyl]-2,5-dioxo)-4-imidazolidineheptanoic acid] inhibits fibroblast proliferation and bleomycin-induced lung fibrosis in mice. | 2010 Nov |
|
| C/EBPβ-Thr217 phosphorylation signaling contributes to the development of lung injury and fibrosis in mice. | 2011 |
|
| Essential role of MeCP2 in the regulation of myofibroblast differentiation during pulmonary fibrosis. | 2011 Apr |
|
| Anti-inflammatory and antifibrotic effects of methyl palmitate. | 2011 Aug 1 |
|
| 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 |
|
| Links between DNA polymerase beta expression and sensitivity to bleomycin. | 2011 Mar 15 |
|
| 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 |
|
| 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.
0.25 to 0.50 units/kg weekly or twice weekly (Squamous cell carcinoma, non-Hodgkin’s lymphoma, testicular carcinoma, Hodgkin’s disease)
Route of Administration:
Intravenous
| Substance Class |
Mixture
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BLEOMYCIN HYDROCHLORIDE
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PRIMARY | Description: A white to yellowish white powder. Solubility: Freely soluble in water and in methanol R; slightly soluble in ethanol (~750 g/l) TS; practically insoluble in acetone R and ether R. Category: Cytotoxic drug. Storage: Bleomycin hydrochloride should be kept in a tightly closed container. Labelling: The designation sterile Bleomycin hydrochloride indicates that the substance complies with the additional requirementsfor sterile Bleomycin hydrochloride and may be used for parenteral administration or for other sterile applications. CAUTION:Bleomycin hydrochloride must be handled with care, avoiding contact with the skin and inhalation of airborne particles. | ||
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SUB00843MIG
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All of the following components must be present:
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ACTIVE MOIETY |
