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

Stem definitionDrug idCAS RN
vinca alkaloids 2826 53643-48-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • eldisine
  • desacetylvinblastine amide
  • vindesine sulfate
  • vindesine
  • compound 112531
Vinblastine derivative with antineoplastic activity against CANCER. Major side effects are myelosuppression and neurotoxicity. Vindesine is used extensively in chemotherapy protocols (ANTINEOPLASTIC COMBINED CHEMOTHERAPY PROTOCOLS).
  • Molecular weight: 753.94
  • Formula: C43H55N5O7
  • CLOGP: 3.42
  • LIPINSKI: 2
  • HAC: 12
  • HDO: 5
  • TPSA: 164.82
  • ALOGS: -4.03
  • ROTB: 7

Drug dosage:

None

ADMET properties:

PropertyValueReference
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.14 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
Vd (Volume of distribution) 5 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 2.20 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 35 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1979 YEAR INTRODUCED

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
Bone marrow failure 186.39 53.05 52 818 29617 46655575
Leukopenia 79.57 53.05 34 836 68309 46616883
Acute myeloid leukaemia 73.50 53.05 22 848 15756 46669436
Myelosuppression 64.47 53.05 17 853 7686 46677506

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
Bone marrow failure 288.46 37.94 96 1744 29689 29920949
Stomatitis 88.81 37.94 44 1796 37235 29913403
Leukopenia 69.36 37.94 43 1797 56116 29894522
Myelosuppression 52.67 37.94 19 1821 7303 29943335
Febrile neutropenia 52.60 37.94 47 1793 106646 29843992
Large intestine infection 48.24 37.94 12 1828 1291 29949347

Pharmacologic Action:

SourceCodeDescription
ATC L01CA03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS
Vinca alkaloids and analogues
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 cytostatic

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute lymphoid leukemia indication 91857003 DOID:9952
Chronic myeloid leukemia indication 92818009 DOID:8552
Malignant tumor of lung indication 363358000
Malignant melanoma indication 372244006

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.64 acidic
pKa2 13.81 acidic
pKa3 7.86 Basic
pKa4 6.98 Basic
pKa5 6.15 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
Cytochrome P450 3A4 Enzyme Km 4.61 WOMBAT-PK

External reference:

IDSource
4025282 VUID
N0000171809 NUI
D01769 KEGG_DRUG
59917-39-4 SECONDARY_CAS_RN
4025282 VANDF
4025283 VANDF
C0877923 UMLSCUI
CHEBI:36373 CHEBI
CHEMBL238071 ChEMBL_ID
CHEMBL3989543 ChEMBL_ID
DB00309 DRUGBANK_ID
CHEMBL219146 ChEMBL_ID
CHEMBL2105882 ChEMBL_ID
D014751 MESH_DESCRIPTOR_UI
11643449 PUBCHEM_CID
3927 INN_ID
RSA8KO39WH UNII
11204 RXNORM
003505 NDDF
003506 NDDF
349851002 SNOMEDCT_US
395921004 SNOMEDCT_US
409198005 SNOMEDCT_US

Pharmaceutical products:

None