Stem definition | Drug id | CAS RN |
---|---|---|
antineoplastics, taxane derivatives | 4153 | 183133-96-2 |
None
Property | Value | Reference |
---|---|---|
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 |
Date | Agency | Company | Orphan |
---|---|---|---|
June 17, 2010 | FDA | SANOFI AVENTIS US |
None
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients 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 |
None
Source | Code | Description |
---|---|---|
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 |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
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 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 10.2 | acidic |
pKa2 | 12.4 | acidic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
60MG/1.5ML (40MG/ML) | JEVTANA KIT | SANOFI AVENTIS US | N201023 | June 17, 2010 | RX | SOLUTION | INTRAVENOUS | Dec. 18, 2023 | CLINICAL TRIAL STUDY RESULTS |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Tubulin beta | Tumour-associated antigen | INHIBITOR | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE |
ID | Source |
---|---|
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 |
None