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 190.38 27.27 138 4963 158029 56128937
Febrile neutropenia 169.23 27.27 110 4991 105435 56181531
Pulmonary toxicity 102.04 27.27 35 5066 7848 56279118
Pancytopenia 87.74 27.27 69 5032 88646 56198320
Malignant neoplasm progression 70.08 27.27 56 5045 73531 56213435
Second primary malignancy 69.83 27.27 26 5075 7376 56279590
Tissue infiltration 68.77 27.27 15 5086 610 56286356
Basal ganglion degeneration 67.86 27.27 14 5087 434 56286532
Disease progression 63.91 27.27 62 5039 105111 56181855
Uterine enlargement 59.25 27.27 15 5086 1168 56285798
Product use in unapproved indication 55.50 27.27 66 5035 140756 56146210
Inguinal hernia 53.08 27.27 15 5086 1776 56285190
Anaesthesia 51.67 27.27 11 5090 398 56286568
Febrile bone marrow aplasia 50.91 27.27 20 5081 6552 56280414
Myelodysplastic syndrome 49.95 27.27 26 5075 16380 56270586
Psychogenic seizure 49.73 27.27 14 5087 1635 56285331
Interstitial lung disease 49.19 27.27 41 5060 57022 56229944
Pleuroparenchymal fibroelastosis 47.32 27.27 7 5094 26 56286940
Toxic neuropathy 46.71 27.27 10 5091 372 56286594
Refractory anaemia with an excess of blasts 45.43 27.27 10 5091 424 56286542
Dysaesthesia 44.54 27.27 16 5085 4100 56282866
Neurological decompensation 44.24 27.27 14 5087 2440 56284526
Hypochromic anaemia 43.83 27.27 13 5088 1825 56285141
Ileus 42.26 27.27 22 5079 13860 56273106
Astrocytoma, low grade 41.86 27.27 7 5094 65 56286901
Monoplegia 41.59 27.27 14 5087 2960 56284006
Hyperpyrexia 40.30 27.27 14 5087 3254 56283712
Premature menopause 39.25 27.27 10 5091 798 56286168
Pyrexia 39.23 27.27 104 4997 418669 55868297
Congestive cardiomyopathy 39.15 27.27 16 5085 5803 56281163
Premature baby 38.16 27.27 23 5078 19182 56267784
Acute myeloid leukaemia 35.47 27.27 21 5080 16951 56270015
Off label use 34.98 27.27 120 4981 556060 55730906
Pneumocystis jirovecii pneumonia 34.32 27.27 20 5081 15681 56271285
Lymphadenopathy 33.91 27.27 27 5074 35181 56251785
Foetal exposure during pregnancy 32.71 27.27 26 5075 33797 56253169
Intervertebral disc disorder 32.36 27.27 13 5088 4513 56282453
Klebsiella infection 31.63 27.27 15 5086 7741 56279225
Mucosal inflammation 31.28 27.27 28 5073 42782 56244184
Splenomegaly 30.62 27.27 16 5085 10152 56276814
Pericarditis constrictive 30.60 27.27 7 5094 354 56286612
Meningitis streptococcal 30.40 27.27 6 5095 148 56286818
Pseudohyponatraemia 30.35 27.27 5 5096 42 56286924
Lung disorder 30.02 27.27 30 5071 52567 56234399
Renal cyst 29.04 27.27 15 5086 9294 56277672
Abdominal tenderness 28.84 27.27 14 5087 7607 56279359
Respiratory failure 28.60 27.27 39 5062 95023 56191943
Hypothyroidism 27.94 27.27 25 5076 38171 56248795
Neuropathy peripheral 27.67 27.27 40 5061 102853 56184113
Leukaemia 27.53 27.27 11 5090 3764 56283202

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 228.32 25.98 180 5342 121669 31570153
Second primary malignancy 186.80 25.98 63 5459 6969 31684853
Neutropenia 126.44 25.98 138 5384 140226 31551596
Acute myeloid leukaemia 121.37 25.98 61 5461 18611 31673211
Cardiotoxicity 95.06 25.98 35 5487 4992 31686830
Product use in unapproved indication 81.34 25.98 93 5429 99078 31592744
Azoospermia 76.33 25.98 17 5505 388 31691434
Off label use 71.51 25.98 174 5348 347100 31344722
Endocarditis noninfective 69.72 25.98 13 5509 116 31691706
Pulmonary toxicity 68.14 25.98 28 5494 5349 31686473
Neutrophil count decreased 66.60 25.98 59 5463 46335 31645487
Malignant neoplasm progression 61.21 25.98 72 5450 78926 31612896
Chronic myeloid leukaemia 58.82 25.98 21 5501 2740 31689082
Cytomegalovirus chorioretinitis 54.40 25.98 21 5501 3407 31688415
Testicular disorder 53.94 25.98 14 5508 619 31691203
Myositis 51.54 25.98 29 5493 11065 31680757
Pneumocystis jirovecii pneumonia 49.83 25.98 34 5488 18217 31673605
Autoimmune neutropenia 48.82 25.98 11 5511 265 31691557
Interstitial lung disease 45.93 25.98 55 5467 61348 31630474
Myelodysplastic syndrome 45.89 25.98 33 5489 19218 31672604
Bone marrow failure 40.91 25.98 36 5486 27972 31663850
Cytopenia 38.60 25.98 24 5498 10986 31680836
Desmoid tumour 38.38 25.98 8 5514 132 31691690
Polyneuropathy 34.93 25.98 24 5498 12998 31678824
Cardiac dysfunction 34.50 25.98 13 5509 1974 31689848
Pneumonia salmonella 32.65 25.98 6 5516 49 31691773
Optic glioma 32.54 25.98 6 5516 50 31691772
Myelosuppression 31.99 25.98 24 5498 14896 31676926
Pulmonary fibrosis 31.78 25.98 25 5497 16635 31675187
Cryptococcal fungaemia 28.90 25.98 6 5516 97 31691725
Ichthyosis 28.72 25.98 6 5516 100 31691722
Treatment failure 27.98 25.98 35 5487 40757 31651065
Spindle cell sarcoma 27.10 25.98 6 5516 133 31691689
Neuropathy peripheral 26.05 25.98 47 5475 75602 31616220
Pancytopenia 26.03 25.98 51 5471 87265 31604557

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 343.38 22.99 256 9374 204062 70714752
Neutropenia 277.50 22.99 249 9381 256907 70661907
Second primary malignancy 253.91 22.99 87 9543 12964 70905850
Pulmonary toxicity 171.82 22.99 62 9568 10736 70908078
Acute myeloid leukaemia 160.24 22.99 80 9550 30860 70887954
Malignant neoplasm progression 136.97 22.99 121 9509 121618 70797196
Product use in unapproved indication 131.49 22.99 151 9479 207327 70711487
Pancytopenia 90.63 22.99 107 9523 151000 70767814
Myelodysplastic syndrome 90.13 22.99 54 9576 29731 70889083
Disease progression 87.51 22.99 107 9523 156565 70762249
Interstitial lung disease 86.94 22.99 88 9542 104597 70814217
Cardiotoxicity 83.10 22.99 37 9593 11033 70907781
Neutrophil count decreased 82.03 22.99 77 9553 83479 70835335
Chronic myeloid leukaemia 81.63 22.99 28 9602 4173 70914641
Off label use 80.78 22.99 252 9378 742808 70176006
Pneumocystis jirovecii pneumonia 79.44 22.99 50 9580 30032 70888782
Endocarditis noninfective 67.00 22.99 13 9617 191 70918623
Pleuroparenchymal fibroelastosis 66.00 22.99 11 9619 63 70918751
Myelitis 63.72 22.99 20 9610 2257 70916557
Cytopenia 59.22 22.99 34 9596 17289 70901525
Pyrexia 56.03 22.99 195 9435 606757 70312057
Myelosuppression 55.35 22.99 40 9590 30105 70888709
Tissue infiltration 51.73 22.99 13 9617 651 70918163
Basal ganglion degeneration 51.48 22.99 12 9618 436 70918378
Lung disorder 49.75 22.99 54 9576 69430 70849384
Desmoid tumour 48.83 22.99 10 9620 196 70918618
Neuropathy peripheral 48.35 22.99 72 9558 126824 70791990
Uterine enlargement 47.99 22.99 13 9617 874 70917940
Astrocytoma, low grade 46.15 22.99 9 9621 136 70918678
Myositis 45.98 22.99 29 9601 17460 70901354
Cytomegalovirus chorioretinitis 43.94 22.99 19 9611 5279 70913535
Mucosal inflammation 43.87 22.99 50 9580 67800 70851014
Optic glioma 43.71 22.99 8 9622 84 70918730
Congestive cardiomyopathy 41.55 22.99 23 9607 10903 70907911
Autoimmune neutropenia 40.36 22.99 10 9620 472 70918342
Astrocytoma 40.31 22.99 9 9621 269 70918545
Anaesthesia 40.28 22.99 10 9620 476 70918338
Psychogenic seizure 38.25 22.99 13 9617 1883 70916931
Ileus 35.27 22.99 28 9602 24209 70894605
Bone marrow failure 34.92 22.99 38 9592 48972 70869842
Toxic neuropathy 34.42 22.99 10 9620 868 70917946
Thrombocytopenia 34.41 22.99 90 9540 239020 70679794
Refractory anaemia with an excess of blasts 34.20 22.99 10 9620 888 70917926
Dysaesthesia 34.16 22.99 16 9614 5352 70913462
Polyneuropathy 33.90 22.99 26 9604 21389 70897425
Neoplasm progression 33.86 22.99 36 9594 45192 70873622
Pneumonia salmonella 33.14 22.99 6 9624 59 70918755
Febrile bone marrow aplasia 31.81 22.99 20 9610 11971 70906843
Hypothyroidism 31.77 22.99 35 9595 45720 70873094
Pulmonary fibrosis 30.57 22.99 30 9600 34280 70884534
Monoplegia 30.04 22.99 13 9617 3618 70915196
Ichthyosis 28.42 22.99 6 9624 137 70918677
Guillain-Barre syndrome 28.06 22.99 16 9614 8024 70910790
Hypochromic anaemia 27.49 22.99 11 9619 2516 70916298
Cryptococcal fungaemia 27.15 22.99 6 9624 171 70918643
Treatment failure 26.88 22.99 60 9570 144082 70774732
Ileus paralytic 26.79 22.99 16 9614 8745 70910069
Peripheral sensory neuropathy 26.73 22.99 18 9612 12092 70906722
Neurological decompensation 26.68 22.99 13 9617 4743 70914071
Lymphadenopathy 26.65 22.99 33 9597 48758 70870056
Spindle cell sarcoma 25.45 22.99 6 9624 229 70918585
Pneumonitis 25.24 22.99 34 9596 54563 70864251
Respiratory failure 24.75 22.99 64 9566 168671 70750143
Oropharyngeal squamous cell carcinoma 24.74 22.99 6 9624 259 70918555
Left ventricular dysfunction 24.55 22.99 20 9610 17937 70900877
Inguinal hernia 24.15 22.99 13 9617 5832 70912982
Intervertebral disc disorder 24.14 22.99 12 9618 4573 70914241
Splenic infection fungal 23.99 22.99 5 9625 107 70918707
Pseudohyponatraemia 22.99 22.99 5 9625 132 70918682

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
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

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