bleomycin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antibiotics, produced by Streptomyces strains 4742 11056-06-7

Description:

MoleculeDescription

Synonyms:

  • bleomycin
  • bleomycins
  • bleomycin sulfate
  • bleomycin hydrochloride
  • bleomycin HCl
A complex of related glycopeptide antibiotics from Streptomyces verticillus consisting of bleomycin A2 and B2. It inhibits DNA metabolism and is used as an antineoplastic, especially for solid tumors.
  • Molecular weight: 2841.07
  • Formula: C110H168N37O42S5
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 688.97
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.35 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 0.43 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 1.26 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 3.90 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
July 31, 1973 FDA BRISTOL MYERS SQUIBB

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 216.46 27.89 135 5269 94492 46586166
Ovarian germ cell teratoma 209.99 27.89 31 5373 82 46680576
Pulmonary toxicity 204.42 27.89 56 5348 4637 46676021
Teratoma 174.57 27.89 28 5376 147 46680511
Neutropenia 170.28 27.89 137 5267 143067 46537591
Second primary malignancy 111.44 27.89 38 5366 6546 46674112
Deafness 94.07 27.89 43 5361 16025 46664633
Product use in unapproved indication 93.74 27.89 80 5324 90193 46590465
Mucosal inflammation 92.34 27.89 57 5347 38919 46641739
Teratoma benign 83.16 27.89 13 5391 56 46680602
Myelodysplastic syndrome 82.50 27.89 39 5365 15672 46664986
Acute myeloid leukaemia 82.34 27.89 39 5365 15739 46664919
Pulmonary fibrosis 70.60 27.89 38 5366 20054 46660604
Bone marrow failure 66.74 27.89 42 5362 29627 46651031
Respiratory symptom 64.36 27.89 19 5385 2051 46678607
Cutaneous calcification 64.34 27.89 11 5393 90 46680568
Interstitial lung disease 62.54 27.89 51 5353 53898 46626760
Febrile bone marrow aplasia 62.08 27.89 25 5379 6837 46673821
Pancytopenia 58.52 27.89 60 5344 84998 46595660
Premature baby 57.39 27.89 32 5372 18080 46662578
Foetal exposure during pregnancy 55.66 27.89 38 5366 30709 46649949
Exposure during pregnancy 51.53 27.89 63 5341 108149 46572509
Drug resistance 47.82 27.89 28 5376 17340 46663318
Malignant neoplasm progression 46.82 27.89 47 5357 64879 46615779
Aplasia 46.60 27.89 17 5387 3559 46677099
Acute respiratory distress syndrome 44.25 27.89 29 5375 21893 46658765
Sarcoidosis 43.93 27.89 18 5386 5141 46675517
Thrombocytopenia 43.76 27.89 63 5341 126518 46554140
Combined immunodeficiency 43.14 27.89 8 5396 108 46680550
Premature menopause 42.94 27.89 11 5393 700 46679958
Primary immunodeficiency syndrome 42.70 27.89 7 5397 43 46680615
Off label use 40.99 27.89 116 5288 379725 46300933
Leukaemia 40.48 27.89 15 5389 3280 46677378
Vulvovaginal inflammation 40.25 27.89 10 5394 562 46680096
Disease progression 39.99 27.89 51 5353 91249 46589409
Cardiotoxicity 39.35 27.89 18 5386 6704 46673954
Chloroma 38.91 27.89 8 5396 189 46680469
Anaemia 38.89 27.89 89 5315 255690 46424968
Tumour lysis syndrome 38.08 27.89 18 5386 7218 46673440
Necrotising gastritis 36.44 27.89 6 5398 38 46680620
Haemophagocytic lymphohistiocytosis 35.65 27.89 18 5386 8324 46672334
Maternal exposure during pregnancy 35.36 27.89 51 5353 102498 46578160
Flagellate dermatitis 34.31 27.89 7 5397 159 46680499
Encephalitis viral 33.92 27.89 11 5393 1619 46679039
Lymphopenia 32.75 27.89 21 5383 15272 46665386
Capillary leak syndrome 32.28 27.89 11 5393 1886 46678772
Acute promyelocytic leukaemia 31.04 27.89 9 5395 912 46679746
Lung disorder 30.56 27.89 31 5373 43273 46637385
Meningitis streptococcal 29.17 27.89 6 5398 142 46680516
Septic shock 27.99 27.89 34 5370 57859 46622799

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 369.14 24.71 275 8105 106418 29837680
Second primary malignancy 317.48 24.71 103 8277 6253 29937845
Pulmonary toxicity 224.70 24.71 73 8307 4443 29939655
Acute myeloid leukaemia 201.41 24.71 99 8281 17907 29926191
Azoospermia 147.45 24.71 32 8348 390 29943708
Pulmonary fibrosis 127.66 24.71 70 8310 15820 29928278
Pneumonitis 115.46 24.71 80 8300 27374 29916724
Myelodysplastic syndrome 109.05 24.71 67 8313 18711 29925387
Interstitial lung disease 100.81 24.71 103 8277 60094 29884004
Neutropenia 88.27 24.71 141 8239 128399 29815699
Acute respiratory distress syndrome 86.21 24.71 63 8317 23409 29920689
Cardiotoxicity 76.72 24.71 33 8347 4381 29939717
Bone marrow failure 72.95 24.71 63 8317 29722 29914376
Endocarditis noninfective 70.05 24.71 14 8366 110 29943988
Off label use 64.05 24.71 183 8197 249107 29694991
Traumatic lung injury 62.42 24.71 20 8360 1161 29942937
Papillary thyroid cancer 60.60 24.71 17 8363 623 29943475
Pyrexia 59.70 24.71 199 8181 294290 29649808
Cytomegalovirus chorioretinitis 55.37 24.71 24 8356 3244 29940854
Respiratory failure 55.20 24.71 100 8280 100542 29843556
Pneumomediastinum 54.26 24.71 20 8360 1771 29942327
Pneumocystis jirovecii pneumonia 54.06 24.71 42 8338 17078 29927020
Lung disorder 52.87 24.71 54 8326 31415 29912683
Vena cava thrombosis 52.17 24.71 17 8363 1041 29943057
Testicular disorder 52.08 24.71 15 8365 605 29943493
Product use in unapproved indication 52.05 24.71 82 8298 73611 29870487
Chronic myeloid leukaemia 50.55 24.71 21 8359 2556 29941542
Flagellate dermatitis 50.54 24.71 8 8372 11 29944087
Scleroderma 48.40 24.71 17 8363 1310 29942788
Thrombocytopenia 46.73 24.71 112 8268 136932 29807166
Pneumothorax 43.21 24.71 36 8344 16157 29927941
Chloroma 42.93 24.71 12 8368 434 29943664
Pulmonary embolism 42.00 24.71 77 8303 78058 29866040
Leukopenia 41.74 24.71 64 8316 56095 29888003
Osteonecrosis 41.25 24.71 35 8345 16100 29927998
Myositis 40.69 24.71 29 8351 10348 29933750
Malignant neoplasm progression 39.81 24.71 72 8308 72215 29871883
Deafness 38.53 24.71 28 8352 10297 29933801
High-grade B-cell lymphoma 38.45 24.71 9 8371 157 29943941
Subcutaneous emphysema 37.23 24.71 13 8367 984 29943114
Blood pressure decreased 36.89 24.71 55 8325 47020 29897078
Pancytopenia 36.21 24.71 76 8304 84976 29859122
Cardiac dysfunction 34.91 24.71 13 8367 1184 29942914
Mucosal inflammation 33.54 24.71 42 8338 30452 29913646
Autoimmune neutropenia 33.44 24.71 9 8371 282 29943816
Taeniasis 32.99 24.71 7 8373 76 29944022
Pneumonia salmonella 32.87 24.71 6 8374 27 29944071
Premature ageing 32.34 24.71 7 8373 84 29944014
Choriocarcinoma 32.03 24.71 6 8374 32 29944066
Osteosarcoma 31.92 24.71 8 8372 188 29943910
Lung infiltration 31.60 24.71 27 8353 12532 29931566
Ichthyosis 31.48 24.71 7 8373 96 29944002
Acute promyelocytic leukaemia 31.45 24.71 10 8370 566 29943532
Carotid artery thrombosis 31.20 24.71 9 8371 365 29943733
Cerebral infarction 30.09 24.71 37 8343 26336 29917762
Splenic infarction 29.60 24.71 13 8367 1812 29942286
Fatigue 29.34 24.71 28 8352 320645 29623453
Haematotoxicity 28.32 24.71 19 8361 6151 29937947
Neutropenic sepsis 27.64 24.71 24 8356 11385 29932713
Death 27.44 24.71 36 8344 357247 29586851
Septic shock 27.24 24.71 57 8323 63550 29880548
Cerebral venous thrombosis 26.91 24.71 9 8371 598 29943500
Ischaemic cerebral infarction 26.77 24.71 10 8370 919 29943179
Fall 26.40 24.71 9 8371 181863 29762235
Blindness 26.07 24.71 24 8356 12285 29931813
Paternal exposure timing unspecified 26.05 24.71 5 8375 31 29944067
Dizziness 26.04 24.71 11 8369 194898 29749200

Pharmacologic Action:

SourceCodeDescription
ATC L01DC01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
CYTOTOXIC ANTIBIOTICS AND RELATED SUBSTANCES
Other cytotoxic antibiotics
CHEBI has role CHEBI:25212 metabolites
CHEBI has role CHEBI:35610 cytostatic
MeSH PA D000903 Antibiotics, Antineoplastic
MeSH PA D000970 Antineoplastic Agents
FDA EPC N0000180854 Cytoprotective Agent

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Diffuse non-Hodgkin's lymphoma, large cell indication 109969005
Hodgkin's disease indication 118599009
Non-Hodgkin's lymphoma indication 118601006
Malignant tumor of head and/or neck indication 255056009
Follicular non-Hodgkin's lymphoma indication 308121000
Malignant tumor of cervix indication 363354003 DOID:4362
Malignant tumor of penis indication 363516004 DOID:11615
International Federation of Gynecology and Obstetrics stage finding for vulvar carcinoma indication 385370007
Squamous cell carcinoma indication 402815007 DOID:1749
Pleural Malignant Effusions indication
Testicular Germ Cell Tumor indication
Mycosis fungoides off-label use 118618005
Ovarian Germ Cell Tumor Carcinoma off-label use

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

None

External reference:

IDSource
40S1VHN69B UNII
D02177 KEGG_DRUG
4019637 VUID
N0000147730 NUI
67763-87-5 SECONDARY_CAS_RN
4018135 VANDF
4019637 VANDF
C0005740 UMLSCUI
CHEBI:3139 CHEBI
CHEMBL403664 ChEMBL_ID
CHEMBL3085504 ChEMBL_ID
DB00290 DRUGBANK_ID
D001761 MESH_DESCRIPTOR_UI
2721 INN_ID
84068 PUBCHEM_CID
1621 RXNORM
4293 MMSL
9784 MMSL
d00177 MMSL
002661 NDDF
004820 NDDF
009872 NDDF
15660006 SNOMEDCT_US
372843005 SNOMEDCT_US
703085003 SNOMEDCT_US
76591000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 0143-9240 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 23 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 0143-9241 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 23 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 0409-0323 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 21 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 0409-0332 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 21 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 0703-3154 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 19 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 0703-3155 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 19 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 16714-886 POWDER, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 23 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 16714-908 POWDER, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 23 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 61703-323 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 13 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 61703-332 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 13 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 63323-136 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 12 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 63323-137 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 12 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 69097-364 INJECTION 15 [USPU] INTRAMUSCULAR ANDA 20 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 70121-1567 INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION 15000 [iU] INTRA-ARTERIAL UNULLPPROVED DRUG FOR USE IN DRUG SHORTAGE 18 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 71288-106 POWDER, FOR SOLUTION 15 [USPU] INTRAMUSCULAR ANDA 24 sections
Bleomycin HUMAN PRESCRIPTION DRUG LABEL 1 71288-107 POWDER, FOR SOLUTION 30 [USPU] INTRAMUSCULAR ANDA 24 sections