vindesine ๐Ÿถ Veterinary Use | 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 ยตM/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
Myelosuppression 484.06 60.35 106 1037 23597 63464282
Bone marrow failure 170.06 60.35 48 1095 29242 63458637
Leukopenia 83.04 60.35 36 1107 77254 63410625

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
Myelosuppression 469.02 37.15 128 2146 19137 34935520
Bone marrow failure 276.39 37.15 94 2180 29159 34925498
Stomatitis 86.50 37.15 46 2228 42468 34912189
Leukopenia 64.98 37.15 44 2230 62812 34891845
Febrile neutropenia 62.04 37.15 59 2215 136790 34817867
Agranulocytosis 57.67 37.15 29 2245 23792 34930865
Large intestine infection 45.73 37.15 12 2262 1506 34953151
Pyrexia 43 37.15 77 2197 332936 34621721

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
Myelosuppression 891.46 39.94 229 3310 40067 79700782
Bone marrow failure 450.50 39.94 142 3397 50965 79689884
Leukopenia 142.34 39.94 79 3460 116434 79624415
Agranulocytosis 97.41 39.94 45 3494 44985 79695864
Febrile neutropenia 87.12 39.94 76 3463 230923 79509926
White blood cell count decreased 79.23 39.94 66 3473 188222 79552627
Pyrexia 74.36 39.94 118 3421 678591 79062258
Stomatitis 64.93 39.94 53 3486 146704 79594145
Granulocytopenia 50.39 39.94 19 3520 11412 79729437
Neutrophil count decreased 43.77 39.94 35 3504 93924 79646925
Large intestine infection 41.52 39.94 12 3527 3157 79737692
Acute myeloid leukaemia 40.50 39.94 22 3517 30863 79709986

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01CA03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS
Vinca alkaloids and analogues
CHEBI has role CHEBI:35610 antineoplastic agents
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
Acute lymphoid leukemia indication 91857003 DOID:9952
Chronic myeloid leukemia indication 92818009 DOID:8552
Malignant tumor of lung indication 363358000
Malignant melanoma indication 372244006




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

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
C0042682 UMLSCUI
CHEBI:32295 CHEBI
CHEMBL238071 ChEMBL_ID
CHEMBL219146 ChEMBL_ID
CHEMBL3989543 ChEMBL_ID
CHEMBL2105882 ChEMBL_ID
D014751 MESH_DESCRIPTOR_UI
DB00309 DRUGBANK_ID
3927 INN_ID
RSA8KO39WH UNII
40839 PUBCHEM_CID
11204 RXNORM
003505 NDDF
003506 NDDF
349851002 SNOMEDCT_US
395921004 SNOMEDCT_US
409198005 SNOMEDCT_US

Pharmaceutical products:

None