vinorelbine indications/contra

Stem definitionDrug idCAS RN
vinca alkaloids 2827 71486-22-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • vinorelbin ditartrate
  • noranhydrovinblastine tartrate
  • vinorelbine
  • navelbin
  • navelbine base
  • 5'-anhydrovinblastine
  • vinorelbine tartrate
  • vinorelbine ditartrate
  • navelbine
  • vinorelbine base
  • Molecular weight: 778.95
  • Formula: C45H54N4O8
  • CLOGP: 5.94
  • LIPINSKI: 3
  • HAC: 12
  • HDO: 2
  • TPSA: 133.87
  • ALOGS: -4.81
  • ROTB: 10

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Dec. 23, 1994 FDA PIERRE FABRE

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
Neutropenia 1076.01 41.25 322 2729 33064 3349744
Disease progression 845.22 41.25 266 2785 31993 3350815
Febrile neutropenia 780.45 41.25 222 2829 18753 3364055
Malignant neoplasm progression 566.46 41.25 171 2880 17622 3365186
Leukopenia 426.37 41.25 134 2917 15689 3367119
Neutropenic sepsis 424.48 41.25 93 2958 2613 3380195
Vomiting 383.19 41.25 201 2850 89330 3293478
Pyrexia 349.22 41.25 183 2868 80932 3301876
Metastases to liver 332.05 41.25 82 2969 3914 3378894
Diarrhoea 324.60 41.25 190 2861 104158 3278650
Nausea 323.91 41.25 205 2846 129440 3253368
Anaemia 295.92 41.25 144 2907 54189 3328619
Metastases to bone 280.56 41.25 68 2983 2993 3379815
Dyspnoea 251.75 41.25 161 2890 102773 3280035
Thrombocytopenia 239.41 41.25 109 2942 35159 3347649
Mucosal inflammation 224.40 41.25 70 2981 7913 3374895
Interstitial lung disease 211.61 41.25 77 2974 13939 3368869
Metastases to central nervous system 207.14 41.25 53 2998 2910 3379898
Constipation 205.08 41.25 94 2957 30718 3352090
Palmar-plantar erythrodysaesthesia syndrome 203.52 41.25 62 2989 6470 3376338
Breast cancer 202.51 41.25 65 2986 8052 3374756
Ejection fraction decreased 198.66 41.25 55 2996 4092 3378716
Sepsis 179.18 41.25 87 2964 32286 3350522
Haematotoxicity 172.28 41.25 43 3008 2131 3380677
Decreased appetite 169.98 41.25 91 2960 41399 3341409
Abdominal pain 168.96 41.25 94 2957 46131 3336677
Asthenia 168.00 41.25 106 2945 65559 3317249
Fatigue 157.22 41.25 123 2928 107117 3275691
Pleural effusion 155.97 41.25 67 2984 18712 3364096
Dehydration 146.75 41.25 77 2974 33572 3349236

Pharmacologic Action:

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SourceCodeDescription
ATC L01CA04 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 D000970 Antineoplastic Agents
MeSH PA D000972 Antineoplastic Agents, Phytogenic
CHEBI has role CHEBI:47868 photosensitizing agent
CHEBI has role CHEBI:35610 antineoplastic agent

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Disorder of lung contraindication 19829001 DOID:850
Infectious disease contraindication 40733004
Gastrointestinal perforation contraindication 51875005
Hepatic failure contraindication 59927004
Interstitial pneumonia contraindication 64667001 DOID:3082
Intestinal obstruction contraindication 81060008 DOID:8437
Leukopenia contraindication 84828003 DOID:615
Gastrointestinal obstruction contraindication 126765001
Pregnancy, function contraindication 289908002
Bone marrow depression contraindication 307762000
Breastfeeding (mother) contraindication 413712001
Intestinal Ischemic Necrosis contraindication
Severe Granulocytopenia contraindication
Hepatic Metastases contraindication
Kaposi's sarcoma off-label use 109385007 DOID:8632
Neoplasm of endometrium off-label use 123844007 DOID:1380
Small cell carcinoma of lung off-label use 254632001 DOID:5409
Metastatic Breast 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 13.35 acidic
pKa3 8.55 Basic
pKa4 7.39 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 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Cytochrome P450 3A4 Enzyme IC50 6 DRUG MATRIX
Substance-K receptor GPCR Ki 6.27 DRUG MATRIX

External reference:

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IDSource
DB00361 DRUGBANK_ID
4023981 VUID
N0000021986 NUI
C0078257 UMLSCUI
7105 IUPHAR_LIGAND_ID
D01935 KEGG_DRUG
253GQW851Q UNII
125317-39-7 SECONDARY_CAS_RN
4023981 VANDF
N0000007026 NDFRT
N0000021986 NDFRT
004380 NDDF
d03810 MMSL
39541 RXNORM
108792008 SNOMEDCT_US
372541004 SNOMEDCT_US
CHEMBL553025 ChEMBL_ID
CHEMBL538943 ChEMBL_ID
C030852 MESH_SUPPLEMENTAL_RECORD_UI
CHEMBL3039595 ChEMBL_ID
5311497 PUBCHEM_CID
6054 INN_ID
CHEBI:480999 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Vinorelbine HUMAN PRESCRIPTION DRUG LABEL 1 25021-204 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 18 sections
Vinorelbine HUMAN PRESCRIPTION DRUG LABEL 1 45963-607 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 18 sections
VINORELBINE HUMAN PRESCRIPTION DRUG LABEL 1 61703-341 INJECTION, SOLUTION 10 mg INTRAVENOUS ANDA 18 sections
NAVELBINE HUMAN PRESCRIPTION DRUG LABEL 1 64370-532 INJECTION 10 mg INTRAVENOUS NDA 18 sections