vinblastine indications/contra

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: 5.23
  • LIPINSKI: 3
  • HAC: 13
  • HDO: 3
  • TPSA: 154.10
  • ALOGS: -4.68
  • ROTB: 10

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 5, 1965 FDA

FDA Adverse Event Reporting System

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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 583.76 58.96 154 1468 18821 3365416
Pulmonary toxicity 371.79 58.96 67 1555 1307 3382930
Neutropenia 369.09 58.96 123 1499 33263 3350974
Off label use 252.51 58.96 106 1516 53871 3330366
Acute myeloid leukaemia 216.48 58.96 54 1568 5119 3379118
Hodgkin's disease 173.19 58.96 34 1588 1055 3383182
Hodgkin's disease recurrent 170.14 58.96 22 1600 28 3384209
Product use issue 164.06 58.96 56 1566 15945 3368292
Myelodysplastic syndrome 163.48 58.96 44 1578 5603 3378634
Pancytopenia 158.94 58.96 57 1565 18763 3365474
Sepsis 155.44 58.96 65 1557 32308 3351929
Haematotoxicity 155.18 58.96 35 1587 2139 3382098
Thrombocytopenia 150.07 58.96 65 1557 35203 3349034
Disease progression 142.27 58.96 61 1561 32198 3352039
Pyrexia 140.28 58.96 81 1541 81034 3303203
Second primary malignancy 127.35 58.96 28 1594 1519 3382718
Mucosal inflammation 126.85 58.96 39 1583 7944 3376293
Toxicity to various agents 126.17 58.96 63 1559 46991 3337246
Azoospermia 110.81 58.96 18 1604 180 3384057
Respiratory failure 109.30 58.96 46 1576 23095 3361142
Product use in unapproved indication 107.58 58.96 29 1593 3697 3380540
Anaemia 106.44 58.96 59 1563 54274 3329963
Neuropathy peripheral 105.49 58.96 41 1581 16766 3367471
Interstitial lung disease 97.99 58.96 37 1585 13979 3370258
Bone marrow failure 95.86 58.96 32 1590 8455 3375782
Pulmonary fibrosis 89.57 58.96 26 1596 4336 3379901
Vomiting 86.25 58.96 62 1560 89469 3294768
Testicular disorder 83.53 58.96 14 1608 172 3384065
Cardiotoxicity 81.86 58.96 20 1602 1722 3382515
Disease recurrence 76.45 58.96 24 1598 5210 3379027

Pharmacologic Action:

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SourceCodeDescription
ATC L01CA01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS
Vinca alkaloids and analogues
FDA EPC N0000175612 Vinca Alkaloid
FDA Chemical/Ingredient N0000007780 Vinca Alkaloids
MeSH PA D050256 Antimitotic Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D000972 Antineoplastic Agents, Phytogenic
MeSH PA D050258 Mitosis Modulators
MeSH PA D050257 Tubulin Modulators

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Kaposi's sarcoma indication 109385007 DOID:8632
Hodgkin's disease indication 118599009 DOID:8651
Non-Hodgkin's lymphoma indication 118601006 DOID:8675
Langerhans cell histiocytosis, disseminated indication 118614007 DOID:2571
Mycosis fungoides indication 118618005 DOID:8691
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
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 DOID:2848
Hyperuricemia contraindication 35885006 DOID:1920
Hepatic failure contraindication 59927004
Bacterial infectious disease contraindication 87628006 DOID:104
Impaired wound healing contraindication 271618001
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Peripheral nerve disease contraindication 302226006 DOID:574
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
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

Acid dissociation constants calculated using MoKa v3.0.0

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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:

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

External reference:

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IDSource
DB00570 DRUGBANK_ID
4019970 VUID
N0000148055 NUI
C0042670 UMLSCUI
6851 IUPHAR_LIGAND_ID
D01068 KEGG_DRUG
5V9KLZ54CY UNII
1101 INN_ID
CHEMBL159 ChEMBL_ID
4019970 VANDF
7980 MMSL
N0000148055 NDFRT
N0000007206 NDFRT
11198 RXNORM
12436009 SNOMEDCT_US
387051009 SNOMEDCT_US
d00400 MMSL
20303001 SNOMEDCT_US
387115000 SNOMEDCT_US
002654 NDDF
CHEMBL378544 ChEMBL_ID
CHEMBL508191 ChEMBL_ID
13342 PUBCHEM_CID
143-67-9 SECONDARY_CAS_RN
D014747 MESH_DESCRIPTOR_UI
CHEBI:27375 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Vinblastine Sulfate HUMAN PRESCRIPTION DRUG LABEL 1 63323-278 INJECTION 1 mg INTRAVENOUS ANDA 13 sections