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 185.67 27.32 135 4685 147830 50452474
Febrile neutropenia 150.05 27.32 101 4719 97566 50502738
Pulmonary toxicity 112.33 27.32 35 4785 5527 50594777
Pancytopenia 88.03 27.32 69 4751 83961 50516343
Malignant neoplasm progression 71.44 27.32 56 4764 68068 50532236
Tissue infiltration 64.23 27.32 14 4806 539 50599765
Second primary malignancy 63.01 27.32 24 4796 6890 50593414
Basal ganglion degeneration 62.62 27.32 13 4807 395 50599909
Product use in unapproved indication 61.62 27.32 65 4755 115754 50484550
Uterine enlargement 55.09 27.32 14 4806 1052 50599252
Disease progression 51.32 27.32 54 4766 95812 50504492
Febrile bone marrow aplasia 50.74 27.32 20 4800 6291 50594013
Myelodysplastic syndrome 50.71 27.32 26 4794 15106 50585198
Inguinal hernia 48.57 27.32 14 4806 1692 50598612
Interstitial lung disease 47.85 27.32 40 4780 53136 50547168
Anaesthesia 46.80 27.32 10 4810 350 50599954
Toxic neuropathy 46.21 27.32 10 4810 372 50599932
Refractory anaemia with an excess of blasts 45.53 27.32 10 4810 399 50599905
Psychogenic seizure 45.09 27.32 13 4807 1572 50598732
Ileus 42.22 27.32 22 4798 13207 50587097
Dysaesthesia 41.50 27.32 15 4805 3720 50596584
Neurological decompensation 40.49 27.32 13 4807 2257 50598047
Hypochromic anaemia 39.87 27.32 12 4808 1684 50598620
Congestive cardiomyopathy 39.20 27.32 16 4804 5502 50594802
Off label use 39.08 27.32 116 4704 474310 50125994
Premature menopause 38.98 27.32 10 4810 780 50599524
Premature baby 38.08 27.32 23 4797 18314 50581990
Monoplegia 37.89 27.32 13 4807 2770 50597534
Pyrexia 37.19 27.32 99 4721 380104 50220200
Acute myeloid leukaemia 36.82 27.32 21 4799 15053 50585251
Hyperpyrexia 36.73 27.32 13 4807 3036 50597268
Pneumocystis jirovecii pneumonia 34.67 27.32 20 4800 14643 50585661
Pleuroparenchymal fibroelastosis 33.67 27.32 5 4815 18 50600286
Foetal exposure during pregnancy 31.94 27.32 24 4796 27335 50572969
Mucosal inflammation 31.63 27.32 28 4792 40114 50560190
Lung disorder 30.91 27.32 29 4791 44770 50555534
Pericarditis constrictive 30.35 27.32 7 4813 349 50599955
Meningitis streptococcal 30.10 27.32 6 4814 148 50600156
Pseudohyponatraemia 30.10 27.32 5 4815 42 50600262
Lymphadenopathy 29.71 27.32 25 4795 33474 50566830
Klebsiella infection 28.94 27.32 14 4806 7180 50593124
Intervertebral disc disorder 28.79 27.32 12 4808 4348 50595956
Splenomegaly 27.81 27.32 15 4805 9645 50590659
Leukaemia 27.81 27.32 11 4809 3488 50596816

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 215.02 26.53 169 5059 112071 29457228
Second primary malignancy 169.14 26.53 58 5170 6647 29562652
Neutropenia 123.22 26.53 133 5095 131578 29437721
Acute myeloid leukaemia 103.81 26.53 53 5175 16460 29552839
Cardiotoxicity 96.55 26.53 35 5193 4709 29564590
Product use in unapproved indication 83.26 26.53 89 5139 86786 29482513
Off label use 78.56 26.53 167 5061 300633 29268666
Azoospermia 76.09 26.53 17 5211 388 29568911
Pulmonary toxicity 70.32 26.53 28 5200 4862 29564437
Endocarditis noninfective 69.64 26.53 13 5215 115 29569184
Neutrophil count decreased 65.03 26.53 57 5171 43510 29525789
Chronic myeloid leukaemia 61.16 26.53 20 5208 1974 29567325
Malignant neoplasm progression 57.56 26.53 68 5160 73791 29495508
Cytomegalovirus chorioretinitis 55.26 26.53 21 5207 3217 29566082
Testicular disorder 54.67 26.53 14 5214 578 29568721
Myositis 50.45 26.53 28 5200 10255 29559044
Autoimmune neutropenia 48.70 26.53 11 5217 264 29569035
Interstitial lung disease 48.05 26.53 55 5173 57663 29511636
Myelodysplastic syndrome 45.46 26.53 32 5196 17762 29551537
Pneumocystis jirovecii pneumonia 44.79 26.53 31 5197 16748 29552551
Bone marrow failure 41.09 26.53 36 5192 27413 29541886
Cytopenia 38.13 26.53 23 5205 9836 29559463
Polyneuropathy 36.12 26.53 24 5204 12128 29557171
Cardiac dysfunction 35.52 26.53 13 5215 1794 29567505
Pulmonary fibrosis 32.94 26.53 25 5203 15557 29553742
Pneumonia salmonella 32.56 26.53 6 5222 49 29569250
Myelosuppression 31.25 26.53 22 5206 12205 29557094
Treatment failure 30.37 26.53 35 5193 36904 29532395
Cryptococcal fungaemia 29.42 26.53 6 5222 87 29569212
Ichthyosis 28.75 26.53 6 5222 98 29569201
Pyrexia 28.46 26.53 113 5115 287509 29281790
Spindle cell sarcoma 27.19 26.53 6 5222 129 29569170
Lung disorder 27.05 26.53 30 5198 30332 29538967

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 315.34 23.00 239 8882 187418 64302193
Neutropenia 270.04 23.00 242 8879 239382 64250229
Second primary malignancy 239.68 23.00 83 9038 12254 64477357
Pulmonary toxicity 171.69 23.00 59 9062 8502 64481109
Acute myeloid leukaemia 157.18 23.00 77 9044 27386 64462225
Product use in unapproved indication 137.58 23.00 146 8975 176472 64313139
Malignant neoplasm progression 132.59 23.00 117 9004 112754 64376857
Off label use 91.57 23.00 244 8877 632562 63857049
Myelodysplastic syndrome 89.33 23.00 53 9068 27526 64462085
Interstitial lung disease 87.17 23.00 87 9034 97645 64391966
Pancytopenia 85.10 23.00 103 9018 143206 64346405
Cardiotoxicity 84.31 23.00 37 9084 10237 64479374
Chronic myeloid leukaemia 82.48 23.00 27 9094 3347 64486264
Disease progression 79.54 23.00 99 9022 141581 64348030
Neutrophil count decreased 78.76 23.00 74 9047 77122 64412489
Pneumocystis jirovecii pneumonia 73.91 23.00 47 9074 27587 64462024
Endocarditis noninfective 66.60 23.00 13 9108 189 64489422
Myelitis 64.39 23.00 20 9101 2094 64487517
Cytopenia 58.79 23.00 33 9088 15438 64474173
Pyrexia 56.42 23.00 190 8931 558454 63931157
Myelosuppression 52.70 23.00 36 9085 23794 64465817
Lung disorder 52.17 23.00 53 9068 60647 64428964
Tissue infiltration 47.65 23.00 12 9109 581 64489030
Basal ganglion degeneration 46.82 23.00 11 9110 397 64489214
Cytomegalovirus chorioretinitis 44.58 23.00 19 9102 4893 64484718
Uterine enlargement 44.38 23.00 12 9109 769 64488842
Myositis 44.14 23.00 28 9093 16349 64473262
Mucosal inflammation 43.80 23.00 49 9072 62535 64427076
Congestive cardiomyopathy 41.86 23.00 23 9098 10321 64479290
Autoimmune neutropenia 41.37 23.00 10 9111 408 64489203
Pleuroparenchymal fibroelastosis 38.16 23.00 6 9115 21 64489590
Neuropathy peripheral 36.36 23.00 62 9059 117463 64372148
Anaesthesia 36.27 23.00 9 9112 410 64489201
Ileus 35.60 23.00 28 9093 22938 64466673
Toxic neuropathy 34.99 23.00 10 9111 786 64488825
Thrombocytopenia 34.85 23.00 89 9032 223712 64265899
Polyneuropathy 34.66 23.00 26 9095 19868 64469743
Refractory anaemia with an excess of blasts 34.38 23.00 10 9111 836 64488775
Bone marrow failure 34.33 23.00 38 9083 47914 64441697
Psychogenic seizure 34.24 23.00 12 9109 1829 64487782
Pneumonia salmonella 33.90 23.00 6 9115 49 64489562
Pulmonary fibrosis 33.07 23.00 30 9091 29848 64459763
Febrile bone marrow aplasia 32.23 23.00 20 9101 11235 64478376
Dysaesthesia 31.55 23.00 15 9106 4980 64484631
Treatment failure 31.46 23.00 58 9063 116758 64372853
Hypothyroidism 28.85 23.00 32 9089 40425 64449186
Ichthyosis 28.61 23.00 6 9115 127 64489484
Neoplasm progression 28.52 23.00 32 9089 40932 64448679
Cryptococcal fungaemia 27.25 23.00 6 9115 161 64489450
Peripheral sensory neuropathy 27.09 23.00 18 9103 11360 64478251
Monoplegia 26.95 23.00 12 9109 3431 64486180
Ileus paralytic 26.78 23.00 16 9105 8399 64481212
Spindle cell sarcoma 25.37 23.00 6 9115 223 64489388
Oropharyngeal squamous cell carcinoma 24.68 23.00 6 9115 251 64489360
Hypochromic anaemia 24.31 23.00 10 9111 2358 64487253
Neurological decompensation 24.05 23.00 12 9109 4424 64485187
Splenic infection fungal 23.84 23.00 5 9116 106 64489505
Lymphadenopathy 23.58 23.00 31 9090 46655 64442956
Pneumonitis 23.24 23.00 32 9089 50333 64439278
Lymphopenia 23.12 23.00 23 9098 25634 64463977

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
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
Canalicular multispecific organic anion transporter 1 Transporter WOMBAT-PK
Multidrug resistance-associated protein 1 Transporter WOMBAT-PK
Multidrug resistance-associated protein 7 Transporter WOMBAT-PK
Multidrug resistance protein 1 Transporter Ki 7 CHEMBL
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