cabazitaxel 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antineoplastics, taxane derivatives 4153 183133-96-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • cabazitaxel
  • jevtana
  • RPR-116258A
  • XRP-6258
  • cabazitaxel acetonate
  • cabazitaxel acetone
  • javtana
a microtubule inhibitor, cabazitaxel binds to tubulin and promotes its assembly into microtubules while simultaneously inhibiting disassembly. This leads to the stabilization of microtubules, which results in the inhibition of mitotic and interphase cellular functions
  • Molecular weight: 835.94
  • Formula: C45H57NO14
  • CLOGP: 4.59
  • LIPINSKI: 3
  • HAC: 15
  • HDO: 3
  • TPSA: 202.45
  • ALOGS: -5.31
  • ROTB: 15
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 48 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 11 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.24 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 74.50 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
June 17, 2010 FDA SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

None

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
Prostatic specific antigen increased 270.91 24.89 98 5426 12466 29556537
Febrile neutropenia 206.69 24.89 169 5355 112071 29456932
Hormone-refractory prostate cancer 176.08 24.89 37 5487 592 29568411
Metastases to bone 168.60 24.89 65 5459 9833 29559170
Malignant neoplasm progression 150.06 24.89 118 5406 73741 29495262
Prostate cancer metastatic 138.61 24.89 47 5477 4919 29564084
Osteonecrosis of jaw 106.79 24.89 55 5469 16455 29552548
Neutropenia 103.71 24.89 125 5399 131586 29437417
Hydronephrosis 71.00 24.89 34 5490 8696 29560307
Disease progression 68.01 24.89 80 5444 81836 29487167
Neutrophil count decreased 58.43 24.89 55 5469 43512 29525491
Colony stimulating factor therapy 53.50 24.89 11 5513 157 29568846
Metastases to lymph nodes 53.11 24.89 22 5502 3995 29565008
Bone lesion 50.46 24.89 19 5505 2685 29566318
Haematuria 48.53 24.89 50 5474 44089 29524914
Necrotising retinitis 41.28 24.89 12 5512 756 29568247
Pulmonary embolism 40.55 24.89 60 5464 76474 29492529
Prostate cancer recurrent 39.20 24.89 12 5512 903 29568100
Metastases to soft tissue 38.77 24.89 9 5515 231 29568772
Septic shock 34.50 24.89 50 5474 62510 29506493
Anaemia 32.96 24.89 97 5427 200854 29368149
Prostate cancer 31.86 24.89 31 5493 25496 29543507
Bone pain 30.03 24.89 26 5498 18426 29550577
Interstitial lung disease 25.99 24.89 42 5482 57676 29511327
Peripheral sensory neuropathy 25.19 24.89 15 5509 5924 29563079

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
Prostatic specific antigen increased 278.87 25.72 74 4630 8686 64485342
Febrile neutropenia 217.58 25.72 147 4557 187510 64306518
Metastases to bone 106.63 25.72 44 4660 20391 64473637
Neutropenia 105.22 25.72 107 4597 239517 64254511
Osteonecrosis of jaw 86.96 25.72 47 4657 39778 64454250
Neutrophil count decreased 67.24 25.72 51 4653 77145 64416883
Prostate cancer metastatic 64.26 25.72 19 4685 3285 64490743
Haematuria 64.11 25.72 45 4659 60426 64433602
Hydronephrosis 59.04 25.72 26 4678 14099 64479929
Hormone-refractory prostate cancer 55.10 25.72 11 4693 361 64493667
Malignant neoplasm progression 48.62 25.72 50 4654 112821 64381207
Necrotising retinitis 48.60 25.72 12 4692 1051 64492977
Prostate cancer recurrent 47.48 25.72 11 4693 734 64493294
Metastases to lymph nodes 46.22 25.72 19 4685 8698 64485330
Prostate cancer 44.96 25.72 24 4680 19771 64474257
Disease progression 42.55 25.72 52 4652 141628 64352400
Septic shock 42.34 25.72 45 4659 105392 64388636
Bone lesion 40.75 25.72 15 4689 5122 64488906
Peripheral sensory neuropathy 38.25 25.72 18 4686 11360 64482668
Metastases to soft tissue 37.11 25.72 8 4696 384 64493644
Pyrexia 35.59 25.72 105 4599 558539 63935489
Pulmonary embolism 34.99 25.72 48 4656 146308 64347720
Interstitial lung disease 32.83 25.72 38 4666 97694 64396334
Colony stimulating factor therapy 29.64 25.72 7 4697 508 64493520
Anaemia 28.80 25.72 76 4628 378604 64115424
Disseminated intravascular coagulation 27.31 25.72 21 4683 32327 64461701

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01CD04 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PLANT ALKALOIDS AND OTHER NATURAL PRODUCTS
Taxanes
FDA PE N0000175085 Microtubule Inhibition
FDA EPC N0000175592 Microtubule Inhibitor
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:61950 microtubule stabilizing role

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Metastatic Prostate Carcinoma indication
Nutritional disorder contraindication 2492009 DOID:374
Asthenia contraindication 13791008
Hyperbilirubinemia contraindication 14783006 DOID:2741
Nausea and vomiting contraindication 16932000
Dehydration contraindication 34095006
Acute nephropathy contraindication 58574008
Acute infectious disease contraindication 63171007
Leukopenia contraindication 84828003 DOID:615
Kidney disease contraindication 90708001 DOID:557
Liver function tests abnormal contraindication 166603001
Disease of liver contraindication 235856003 DOID:409
Anemia contraindication 271737000 DOID:2355
Pregnancy, function contraindication 289908002
Thrombocytopenic disorder contraindication 302215000 DOID:1588
Neutropenic disorder contraindication 303011007 DOID:1227
Severe diarrhea contraindication 409587002
Breastfeeding (mother) contraindication 413712001
Radiation Therapy Involving Bone contraindication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.2 acidic
pKa2 12.4 acidic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
60MG/1.5ML (40MG/ML) JEVTANA KIT SANOFI AVENTIS US N201023 June 17, 2010 RX SOLUTION INTRAVENOUS 10583110 Oct. 27, 2030 INCREASING SURVIVAL IN METASTATIC CASTRATION-RESISTANT PROSTATE CANCER PATIENTS PREVIOUSLY TREATED WITH DOCETAXEL BY ADMINISTERING AS A 3 WEEK CYCLE CABAZITAXEL AFTER 5 MG DEXCHLORPHENIRAMINE, 8 MG DEXAMETHASONE, AND AN H2-AGONIST
60MG/1.5ML (40MG/ML) JEVTANA KIT SANOFI AVENTIS US N201023 June 17, 2010 RX SOLUTION INTRAVENOUS 10716777 Oct. 27, 2030 INCREASING SURVIVAL IN METASTATIC CASTRATION-RESISTANT PROSTATE CANCER PATIENTS PREVIOUSLY TREATED WITH DOCETAXEL BY ADMINISTERING 20 TO 25 MG/M2 CABAZITAXEL AFTER A PREMEDICATION REGIMEN THAT INCLUDES AN H2-ANTAGONIST
60MG/1.5ML (40MG/ML) JEVTANA KIT SANOFI AVENTIS US N201023 June 17, 2010 RX SOLUTION INTRAVENOUS 8927592 Oct. 27, 2030 INCREASING SURVIVAL IN MCRPC PATIENTS PREVIOUSLY TREATED WITH DOCETAXEL BY ADMINISTERING CABAZITAXEL IN COMBINATION WITH PREDNISONE OR PREDNISOLONE AFTER A PREMEDICATION REGIMEN THAT INCLUDES AN ANTIHISTAMINE, A CORTICOSTEROID, AND AN H2-ANTAGONIST

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
60MG/1.5ML (40MG/ML) JEVTANA KIT SANOFI AVENTIS US N201023 June 17, 2010 RX SOLUTION INTRAVENOUS Dec. 18, 2023 CLINICAL TRIAL STUDY RESULTS

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tubulin beta Tumour-associated antigen INHIBITOR SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE

External reference:

IDSource
4030043 VUID
N0000181529 NUI
D09755 KEGG_DRUG
4030043 VANDF
C2830183 UMLSCUI
CHEBI:63584 CHEBI
CHEMBL1201748 ChEMBL_ID
DB06772 DRUGBANK_ID
C552428 MESH_SUPPLEMENTAL_RECORD_UI
6798 IUPHAR_LIGAND_ID
C532412 MESH_SUPPLEMENTAL_RECORD_UI
8967 INN_ID
1426815-65-7 SECONDARY_CAS_RN
51F690397J UNII
9854073 PUBCHEM_CID
996051 RXNORM
173956 MMSL
27256 MMSL
d07658 MMSL
013461 NDDF
446706007 SNOMEDCT_US
447182009 SNOMEDCT_US

Pharmaceutical products:

None