docetaxel indications/contra

Stem definitionDrug idCAS RN
antineoplastics, taxane derivatives 939 114977-28-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • docetaxel hydrate
  • docetaxel
  • docetaxol
  • docetere
  • taxotel
  • taxotere
  • docetaxel anhydrous
  • RP 56976
  • RP-56976
semisynthetic analog of taxol
  • Molecular weight: 807.89
  • Formula: C43H53NO14
  • CLOGP: 4.08
  • LIPINSKI: 2
  • HAC: 15
  • HDO: 5
  • TPSA: 224.45
  • ALOGS: -4.80
  • ROTB: 13

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
May 14, 1996 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System

scroll-->
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 5078.79 34.94 1397 15691 17578 3351193
Neutropenia 3933.39 34.94 1307 15781 32079 3336692
Diarrhoea 3769.94 34.94 1726 15362 102622 3266149
Dehydration 1992.17 34.94 796 16292 32853 3335918
Nausea 1967.18 34.94 1208 15880 128437 3240334
Pyrexia 1907.25 34.94 1008 16080 80107 3288664
Vomiting 1869.19 34.94 1028 16060 88503 3280268
Dyspnoea 1820.42 34.94 1060 16028 101874 3266897
Mucosal inflammation 1724.42 34.94 500 16588 7483 3361288
Disease progression 1620.37 34.94 679 16409 31580 3337191
Palmar-plantar erythrodysaesthesia syndrome 1307.79 34.94 386 16702 6146 3362625
Interstitial lung disease 1285.93 34.94 458 16630 13558 3355213
Fatigue 1247.90 34.94 849 16239 106391 3262380
Anaemia 1225.69 34.94 659 16429 53674 3315097
Leukopenia 1213.36 34.94 453 16635 15370 3353401
Stomatitis 1081.73 34.94 386 16702 11466 3357305
Pneumonia 1030.59 34.94 644 16444 69499 3299272
Decreased appetite 981.29 34.94 520 16568 40970 3327801
Asthenia 969.53 34.94 605 16483 65060 3303711
Pleural effusion 949.32 34.94 398 16690 18381 3350390
Neutropenic sepsis 846.74 34.94 227 16861 2479 3366292
Abdominal pain 839.42 34.94 487 16601 45738 3323033
Sepsis 805.15 34.94 420 16668 31953 3336818
Malignant neoplasm progression 792.82 34.94 345 16743 17448 3351323
Hypokalaemia 783.41 34.94 318 16770 13487 3355284
Thrombocytopenia 751.86 34.94 413 16675 34855 3333916
Bone marrow failure 742.06 34.94 268 16820 8219 3360552
Neuropathy peripheral 723.05 34.94 318 16770 16489 3352282
Hypotension 703.67 34.94 446 16642 49068 3319703
White blood cell count decreased 702.10 34.94 352 16736 24595 3344176

Pharmacologic Action:

scroll-->
SourceCodeDescription
ATC L01CD02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS
Taxanes
FDA PE N0000175085 Microtubule Inhibition
FDA EPC N0000175592 Microtubule Inhibitor
MeSH PA D050256 Antimitotic Agents
MeSH PA D000970 Antineoplastic Agents
MeSH PA D050258 Mitosis Modulators
MeSH PA D050257 Tubulin Modulators
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:47868 photosensitizing agent
CHEBI has role CHEBI:38068 antimalarial

Drug Use (View source of the data)

scroll-->
DiseaseRelationSNOMED_IDDOID
Non-small cell lung cancer indication 254637007 DOID:3908
Carcinoma of breast indication 254838004 DOID:3459
Malignant tumor of head and/or neck indication 255056009
Malignant tumor of stomach indication 363349007 DOID:10534
Malignant tumor of prostate indication 399068003 DOID:10283
Metastatic Breast Carcinoma indication
Asthenia contraindication 13791008
Hyperbilirubinemia contraindication 14783006 DOID:2741
Pulmonary edema contraindication 19242006 DOID:11396
Cardiac tamponade contraindication 35304003 DOID:115
Body fluid retention contraindication 43498006
Stomatitis contraindication 61170000 DOID:9637
Diarrhea contraindication 62315008
Acute infectious disease contraindication 63171007
Peripheral motor neuropathy contraindication 95663000 DOID:683
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Peripheral edema contraindication 271809000
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
Ascites contraindication 389026000
Breastfeeding (mother) contraindication 413712001
Pleural Effusions contraindication
Ewing's sarcoma off-label use 76909002 DOID:3369
Small cell carcinoma of lung off-label use 254632001 DOID:5409
Malignant tumor of esophagus off-label use 363402007
Malignant tumor of ovary off-label use 363443007 DOID:2394
Invasive Bladder Malignancy off-label use
Refractory Osteosarcoma off-label use

Acid dissociation constants calculated using MoKa v3.0.0

scroll-->
Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.9 acidic
pKa2 11.64 acidic
pKa3 12.4 acidic

Orange Book patent data (new drug applications)

scroll-->
Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
160MG/8ML (20MG/ML) DOCETAXEL EAGLE PHARMS N205934 Dec. 22, 2015 RX SOLUTION IV (INFUSION) 8940786 Sept. 30, 2033 METHOD OF ADMINISTERING AN ETHANOL-FREE TAXANE LIQUID NANODISPERSION FORMULATION TO A SUBJECT COMBINING THE FORMULATION WITH AN AQUEOUS MEDIUM TO PROVIDE AN ETHANOL-FREE TAXANE DILUTED SOLUTION
20MG/ML (20MG/ML) DOCETAXEL EAGLE PHARMS N205934 Dec. 22, 2015 RX SOLUTION IV (INFUSION) 8940786 Sept. 30, 2033 METHOD OF ADMINISTERING AN ETHANOL-FREE TAXANE LIQUID NANODISPERSION FORMULATION TO A SUBJECT COMBINING THE FORMULATION WITH AN AQUEOUS MEDIUM TO PROVIDE AN ETHANOL-FREE TAXANE DILUTED SOLUTION
80MG/4ML (20MG/ML) DOCETAXEL EAGLE PHARMS N205934 Dec. 22, 2015 RX SOLUTION IV (INFUSION) 8940786 Sept. 30, 2033 METHOD OF ADMINISTERING AN ETHANOL-FREE TAXANE LIQUID NANODISPERSION FORMULATION TO A SUBJECT COMBINING THE FORMULATION WITH AN AQUEOUS MEDIUM TO PROVIDE AN ETHANOL-FREE TAXANE DILUTED SOLUTION

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

scroll-->
TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Tubulin beta Structural INHIBITOR ID50 6.70 WOMBAT-PK CHEMBL
Epidermal growth factor receptor Kinase INHIBITOR Kd 9.09 WOMBAT-PK
Cytochrome P450 3A4 Enzyme IC50 5.70 DRUG MATRIX
Substance-K receptor GPCR Ki 6.28 DRUG MATRIX
Multidrug resistance-associated protein 7 Transporter WOMBAT-PK
Multidrug resistance protein 1 Transporter WOMBAT-PK
Growth hormone-releasing hormone receptor GPCR IC50 9.85 CHEMBL

External reference:

scroll-->
IDSource
4020968 VUID
N0000148441 NUI
C0246415 UMLSCUI
6809 IUPHAR_LIGAND_ID
D02165 KEGG_DRUG
CHEMBL92 ChEMBL_ID
15H5577CQD UNII
148408-66-6 SECONDARY_CAS_RN
6621 INN_ID
4020968 VANDF
N0000005739 NDFRT
N0000148441 NDFRT
005187 NDDF
178776 MMSL
72962 RXNORM
d04009 MMSL
180476 MMSL
4626 MMSL
108806006 SNOMEDCT_US
386918005 SNOMEDCT_US
C067311 MESH_SUPPLEMENTAL_RECORD_UI
DB01248 DRUGBANK_ID
CHEMBL3545252 ChEMBL_ID
148124 PUBCHEM_CID
CHEBI:4672 CHEBI

Pharmaceutical products:

scroll-->
ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
TAXOTERE HUMAN PRESCRIPTION DRUG LABEL 1 0075-8003 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS NDA 20 sections
TAXOTERE HUMAN PRESCRIPTION DRUG LABEL 1 0075-8004 INJECTION, SOLUTION, CONCENTRATE 80 mg INTRAVENOUS NDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0409-0201 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0409-0366 INJECTION, SOLUTION 20 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0409-0367 INJECTION, SOLUTION 20 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0409-0368 INJECTION, SOLUTION 20 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0703-5720 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0703-5730 INJECTION, SOLUTION, CONCENTRATE 80 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0955-1020 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS NDA authorized generic 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0955-1021 INJECTION, SOLUTION, CONCENTRATE 80 mg INTRAVENOUS NDA authorized generic 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 0955-1022 INJECTION, SOLUTION, CONCENTRATE 160 mg INTRAVENOUS NDA authorized generic 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 16714-465 INJECTION, SOLUTION 20 mg INTRAVENOUS NDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 16714-500 INJECTION, SOLUTION 80 mg INTRAVENOUS NDA 20 sections
DOCETAXEL HUMAN PRESCRIPTION DRUG LABEL 1 16729-120 KIT 40 mg None NDA 20 sections
DOCETAXEL HUMAN PRESCRIPTION DRUG LABEL 1 16729-228 KIT 40 mg None NDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 16729-231 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS NDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 16729-267 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS NDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 25021-245 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 39822-2120 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 39822-2180 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 39822-2200 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 42367-121 INJECTION 20 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43066-001 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43066-006 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43066-010 INJECTION, SOLUTION 10 mg INTRAVENOUS NDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43598-258 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43598-259 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 20 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43598-610 INJECTION, SOLUTION 80 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 43598-611 INJECTION, SOLUTION 20 mg INTRAVENOUS ANDA 19 sections
Docetaxel HUMAN PRESCRIPTION DRUG LABEL 1 45963-734 INJECTION, SOLUTION, CONCENTRATE 20 mg INTRAVENOUS NDA 19 sections