vinblastine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
vinca alkaloids 2823 865-21-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vinblastine
  • vincaleukoblastine
  • vincaleucoblastin
  • vincaleucoblastine
  • vinblastin
  • vinblastine sulfate
  • vinblastine sulphate
Antitumor alkaloid isolated from Vinca rosea. (Merck, 11th ed.)
  • Molecular weight: 810.99
  • Formula: C46H58N4O9
  • CLOGP: 4.30
  • LIPINSKI: 3
  • HAC: 13
  • HDO: 3
  • TPSA: 154.10
  • ALOGS: -4.68
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 10 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 0.50 % Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability) 0 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 28 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 3.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.14 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 67 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Nov. 5, 1965 FDA

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
Neutropenia 201.27 28.05 146 5360 174859 63308657
Febrile neutropenia 188.82 28.05 121 5385 118328 63365188
Pulmonary toxicity 104.89 28.05 37 5469 9418 63474098
Pancytopenia 87.12 28.05 70 5436 96863 63386653
Second primary malignancy 80.19 28.05 29 5477 7924 63475592
Malignant neoplasm progression 71 28.05 58 5448 82063 63401453
Disease progression 70.91 28.05 69 5437 122689 63360827
Tissue infiltration 69.33 28.05 15 5491 614 63482902
Basal ganglion degeneration 68.48 28.05 14 5492 434 63483082
Product use in unapproved indication 62.15 28.05 77 5429 179003 63304513
Myelodysplastic syndrome 59.34 28.05 29 5477 16725 63466791
Uterine enlargement 58.87 28.05 15 5491 1253 63482263
Inguinal hernia 52.04 28.05 15 5491 1992 63481524
Anaesthesia 51.48 28.05 11 5495 424 63483092
Dysaesthesia 51.47 28.05 18 5488 4460 63479056
Refractory anaemia with an excess of blasts 51.18 28.05 11 5495 436 63483080
Pneumocystis jirovecii pneumonia 50.27 28.05 26 5480 16888 63466628
Psychogenic seizure 49.98 28.05 14 5492 1678 63481838
Febrile bone marrow aplasia 49.66 28.05 20 5486 7305 63476211
Interstitial lung disease 47.84 28.05 41 5465 61867 63421649
Toxic neuropathy 46.01 28.05 10 5496 418 63483098
Neurological decompensation 43.84 28.05 14 5492 2624 63480892
Hypochromic anaemia 43.69 28.05 13 5493 1929 63481587
Off label use 43.08 28.05 142 5364 674320 62809196
Ileus 41.94 28.05 22 5484 14703 63468813
Monoplegia 41.18 28.05 14 5492 3187 63480329
Premature baby 40.03 28.05 24 5482 20711 63462805
Hyperpyrexia 39.45 28.05 14 5492 3618 63479898
Congestive cardiomyopathy 38.89 28.05 16 5490 6166 63477350
Pleuroparenchymal fibroelastosis 38.83 28.05 7 5499 109 63483407
Premature menopause 38.77 28.05 10 5496 876 63482640
Pyrexia 38.35 28.05 108 5398 470370 63013146
Neuropathy peripheral 37.97 28.05 48 5458 113619 63369897
Acute myeloid leukaemia 36.12 28.05 21 5485 17126 63466390
Mucosal inflammation 34.06 28.05 30 5476 46898 63436618
Lymphadenopathy 32.85 28.05 27 5479 38431 63445085
Foetal exposure during pregnancy 32.80 28.05 25 5481 31937 63451579
Intervertebral disc disorder 32.06 28.05 13 5493 4830 63478686
Pericarditis constrictive 30.87 28.05 7 5499 356 63483160
Klebsiella infection 30.84 28.05 15 5491 8551 63474965
Pseudohyponatraemia 30.57 28.05 5 5501 42 63483474
Meningitis streptococcal 30.55 28.05 6 5500 151 63483365
Splenomegaly 29.88 28.05 16 5490 11141 63472375
Abdominal tenderness 28.50 28.05 14 5492 8152 63475364
Renal cyst 28.22 28.05 15 5491 10287 63473229
Cardiotoxicity 28.07 28.05 14 5492 8424 63475092

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 229.81 25.93 188 5776 136661 34814306
Second primary malignancy 200.47 25.93 68 5896 7818 34943149
Neutropenia 141.93 25.93 153 5811 156625 34794342
Acute myeloid leukaemia 132.84 25.93 64 5900 18206 34932761
Azoospermia 97.38 25.93 21 5943 420 34950547
Cardiotoxicity 91.80 25.93 35 5929 5613 34945354
Product use in unapproved indication 81.30 25.93 100 5864 117399 34833568
Endocarditis noninfective 75.27 25.93 14 5950 126 34950841
Neutrophil count decreased 68.58 25.93 62 5902 51042 34899925
Pulmonary toxicity 68.39 25.93 29 5935 6118 34944849
Off label use 65.30 25.93 187 5777 419337 34531630
Chronic myeloid leukaemia 63.70 25.93 21 5943 2203 34948764
Malignant neoplasm progression 60.93 25.93 75 5889 87971 34862996
Pneumocystis jirovecii pneumonia 57.61 25.93 38 5926 19672 34931295
Myositis 55.19 25.93 31 5933 12039 34938928
Cytomegalovirus chorioretinitis 53.88 25.93 21 5943 3568 34947399
Testicular disorder 50.79 25.93 14 5950 797 34950170
Autoimmune neutropenia 48.85 25.93 11 5953 270 34950697
Disease progression 47.53 25.93 74 5890 108003 34842964
Myelodysplastic syndrome 46.57 25.93 33 5931 19175 34931792
Interstitial lung disease 44.13 25.93 55 5909 65227 34885740
Bone marrow failure 42.20 25.93 37 5927 29216 34921751
Cytopenia 38.31 25.93 25 5939 12698 34938269
Cardiac dysfunction 36.23 25.93 14 5950 2324 34948643
Optic glioma 36.02 25.93 6 5958 26 34950941
Neuropathy peripheral 35.17 25.93 56 5908 83207 34867760
Pneumonia salmonella 32.78 25.93 6 5958 49 34950918
Polyneuropathy 32.47 25.93 24 5940 14872 34936095
Asthenospermia 31.33 25.93 6 5958 64 34950903
Pyrexia 30.77 25.93 125 5839 332888 34618079
Pulmonary fibrosis 30.06 25.93 25 5939 18371 34932596
Myelosuppression 29.05 25.93 25 5939 19240 34931727
Cryptococcal fungaemia 28.90 25.93 6 5958 99 34950868
Guillain-Barre syndrome 28.81 25.93 16 5948 6071 34944896
Ichthyosis 28.57 25.93 6 5958 105 34950862
Spindle cell sarcoma 27.40 25.93 6 5958 129 34950838
Pancytopenia 27.25 25.93 54 5910 95103 34855864
Treatment failure 26.33 25.93 36 5928 46661 34904306

FDA Adverse Event Reporting System (Geriatric)

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 361.61 22.06 273 10131 230726 79503258
Neutropenia 304.90 22.06 271 10133 287439 79446545
Second primary malignancy 280.33 22.06 95 10309 14255 79719729
Acute myeloid leukaemia 172.42 22.06 83 10321 30802 79703182
Pulmonary toxicity 163.40 22.06 62 10342 12852 79721132
Product use in unapproved indication 140.69 22.06 168 10236 250191 79483793
Malignant neoplasm progression 139.31 22.06 126 10278 135864 79598120
Disease progression 129.53 22.06 139 10265 184223 79549761
Myelodysplastic syndrome 107.29 22.06 60 10344 30241 79703743
Pneumocystis jirovecii pneumonia 103.36 22.06 60 10344 32448 79701536
Pancytopenia 90.94 22.06 110 10294 165635 79568349
Off label use 86.96 22.06 287 10117 906928 78827056
Chronic myeloid leukaemia 86.48 22.06 28 10376 3636 79730348
Interstitial lung disease 84.48 22.06 88 10316 112512 79621472
Neutrophil count decreased 84.43 22.06 81 10323 93878 79640106
Cardiotoxicity 84.11 22.06 38 10366 12201 79721783
Endocarditis noninfective 72.01 22.06 14 10390 217 79733767
Neuropathy peripheral 63.56 22.06 85 10319 141220 79592764
Myelitis 63.54 22.06 20 10384 2371 79731613
Cytopenia 60.51 22.06 36 10368 20347 79713637
Pleuroparenchymal fibroelastosis 58.31 22.06 11 10393 144 79733840
Pyrexia 57.15 22.06 206 10198 678503 79055481
Myelosuppression 54.81 22.06 44 10360 40252 79693732
Basal ganglion degeneration 51.96 22.06 12 10392 436 79733548
Tissue infiltration 51.72 22.06 13 10391 678 79733306
Myositis 49.58 22.06 31 10373 19137 79714847
Uterine enlargement 48.20 22.06 13 10391 895 79733089
Mucosal inflammation 46.08 22.06 53 10351 75527 79658457
Tooth malformation 45.74 22.06 9 10395 149 79733835
Lung disorder 44.98 22.06 54 10350 80503 79653481
Cytomegalovirus chorioretinitis 44.02 22.06 19 10385 5471 79728513
Congestive cardiomyopathy 40.79 22.06 23 10381 11757 79722227
Anaesthesia 39.87 22.06 10 10394 517 79733467
Dysaesthesia 39.67 22.06 18 10386 5830 79728154
Refractory anaemia with an excess of blasts 38.99 22.06 11 10393 895 79733089
Autoimmune neutropenia 38.57 22.06 10 10394 591 79733393
Polyneuropathy 38.55 22.06 29 10375 24122 79709862
Psychogenic seizure 38.53 22.06 13 10391 1918 79732066
Bone marrow failure 36.60 22.06 39 10365 51068 79682916
Asthenospermia 35.07 22.06 6 10398 43 79733941
Haematotoxicity 34.94 22.06 23 10381 15496 79718488
Ileus 34.32 22.06 28 10376 26183 79707801
Toxic neuropathy 33.73 22.06 10 10394 970 79733014
Pneumonia salmonella 33.38 22.06 6 10398 59 79733925
Guillain-Barre syndrome 32.39 22.06 18 10386 8947 79725037
Ileus paralytic 31.21 22.06 18 10386 9602 79724382
Neoplasm progression 31.09 22.06 36 10368 51646 79682338
Febrile bone marrow aplasia 31.03 22.06 20 10384 13000 79720984
Thrombocytopenia 30.77 22.06 90 10314 265169 79468815
Bronchopulmonary aspergillosis 29.58 22.06 24 10380 22270 79711714
Pneumonitis 29.48 22.06 38 10366 60822 79673162
Monoplegia 29.42 22.06 13 10391 3958 79730026
Hypothyroidism 29.04 22.06 35 10369 52357 79681627
Therapy partial responder 28.01 22.06 21 10383 17376 79716608
Ichthyosis 27.88 22.06 6 10398 157 79733827
Optic glioma 27.56 22.06 5 10399 52 79733932
Cryptococcal fungaemia 27.32 22.06 6 10398 173 79733811
Hypochromic anaemia 27.01 22.06 11 10393 2740 79731244
Infusion site joint movement impairment 26.24 22.06 4 10400 12 79733972
Peripheral sensory neuropathy 26.19 22.06 18 10386 13015 79720969
Neurological decompensation 25.95 22.06 13 10391 5240 79728744
Haemophagocytic lymphohistiocytosis 25.84 22.06 22 10382 21815 79712169
Spindle cell sarcoma 25.72 22.06 6 10398 228 79733756
Lymphadenopathy 25.40 22.06 33 10371 53214 79680770
Pulmonary fibrosis 25.32 22.06 30 10374 44082 79689902
Oropharyngeal squamous cell carcinoma 24.95 22.06 6 10398 260 79733724
Lymphopenia 24.91 22.06 25 10379 30532 79703452
Respiratory failure 24.53 22.06 65 10339 180846 79553138
Intervertebral disc disorder 24.01 22.06 12 10392 4813 79729171
Splenic infection fungal 23.98 22.06 5 10399 112 79733872
Left ventricular dysfunction 23.92 22.06 20 10384 19341 79714643
Inguinal hernia 23.37 22.06 13 10391 6475 79727509
Invasive lobular breast carcinoma 23.36 22.06 7 10397 704 79733280
Pseudohyponatraemia 23.19 22.06 5 10399 132 79733852
Infusion site ulcer 23.11 22.06 4 10400 31 79733953
Treatment failure 22.86 22.06 61 10343 170425 79563559
Sepsis 22.72 22.06 82 10322 269346 79464638
Joint swelling 22.61 22.06 5 10399 288641 79445343
Infusion site hypoaesthesia 22.57 22.06 4 10400 36 79733948
Anxiety 22.32 22.06 3 10401 248509 79485475
Headache 22.06 22.06 32 10372 653740 79080244

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01CA01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS
Vinca alkaloids and analogues
FDA CS M0022674 Vinca Alkaloids
FDA EPC N0000175612 Vinca Alkaloid
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:35705 immunosuppressive agents
CHEBI has role CHEBI:61951 microtubule destabilizing role
CHEBI has role CHEBI:76924 plant metabolites
MeSH PA D050256 Antimitotic Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000972 Antineoplastic Agents, Phytogenic
MeSH PA D050257 Tubulin Modulators

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Kaposi's sarcoma indication 109385007
Hodgkin's disease indication 118599009
Non-Hodgkin's lymphoma indication 118601006
Langerhans cell histiocytosis, disseminated indication 118614007
Mycosis fungoides indication 118618005
Malignant tumor of testis indication 363449006 DOID:2998
Carcinoma of female breast indication 447782002
Gestational trophoblastic neoplasia indication 609519004 DOID:3590
Metastatic Breast Carcinoma indication
Non-small cell lung cancer off-label use 254637007 DOID:3908
Malignant tumor of head and/or neck off-label use 255056009
Malignant tumor of urinary bladder off-label use 399326009 DOID:11054
Neuroblastoma off-label use 432328008 DOID:769
Ovarian Germ Cell Tumor Carcinoma off-label use
Mycosis contraindication 3218000 DOID:1564
Hyperbilirubinemia contraindication 14783006 DOID:2741
Disorder of lung contraindication 19829001 DOID:850
Viral disease contraindication 34014006 DOID:934
Depressive disorder contraindication 35489007
Hyperuricemia contraindication 35885006 DOID:1920
Hepatic failure contraindication 59927004
Bacterial infectious disease contraindication 87628006
Impaired wound healing contraindication 271618001
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Peripheral nerve disease contraindication 302226006
Neutropenic disorder contraindication 303011007 DOID:1227
Bone marrow depression contraindication 307762000
Breastfeeding (mother) contraindication 413712001
Myocardial ischemia contraindication 414795007 DOID:3393
Protozoal Infection contraindication
Severe Leukopenia contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.32 acidic
pKa2 13.81 acidic
pKa3 7.54 Basic
pKa4 6.84 Basic
pKa5 6.11 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tubulin beta Tumour-associated antigen INHIBITOR IC50 9 IUPHAR SCIENTIFIC LITERATURE
Multidrug resistance-associated protein 7 Transporter WOMBAT-PK
Multidrug resistance protein 1 Transporter Ki 7 CHEMBL
Canalicular multispecific organic anion transporter 1 Transporter WOMBAT-PK
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK
Thromboxane-A synthase Enzyme IC50 5.73 DRUG MATRIX
Arachidonate 15-lipoxygenase Enzyme IC50 5.30 DRUG MATRIX
Amine oxidase [flavin-containing] B Enzyme Ki 4.11 CHEMBL

External reference:

IDSource
4019970 VUID
N0000148055 NUI
D01068 KEGG_DRUG
143-67-9 SECONDARY_CAS_RN
4017457 VANDF
4019970 VANDF
C0042670 UMLSCUI
CHEBI:27375 CHEBI
VLB PDB_CHEM_ID
CHEMBL159 ChEMBL_ID
CHEMBL508191 ChEMBL_ID
CHEMBL378544 ChEMBL_ID
D014747 MESH_DESCRIPTOR_UI
DB00570 DRUGBANK_ID
6851 IUPHAR_LIGAND_ID
1101 INN_ID
5V9KLZ54CY UNII
13342 PUBCHEM_CID
11198 RXNORM
5674 MMSL
7980 MMSL
856 MMSL
d00400 MMSL
002654 NDDF
002655 NDDF
12436009 SNOMEDCT_US
387051009 SNOMEDCT_US
387115000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Vinblastine Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 63323-278 INJECTION 1 mg INTRAVENOUS ANDA 12 sections