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

Stem definition	Drug id	CAS RN
antineoplastics, taxane derivatives	4153	183133-96-2

Description:

Molecule	Description
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: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

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: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
March 17, 2011	EMA	Sanofi Winthrop Industrie
June 17, 2010	FDA	SANOFI AVENTIS US

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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	292.20	25.14	106	5986	14574	34936265
Febrile neutropenia	224.16	25.14	187	5905	136662	34814177
Metastases to bone	192.60	25.14	74	6018	11896	34938943
Hormone-refractory prostate cancer	172.63	25.14	37	6055	703	34950136
Malignant neoplasm progression	159.92	25.14	128	5964	87918	34862921
Prostate cancer metastatic	146.25	25.14	50	6042	5753	34945086
Osteonecrosis of jaw	135.86	25.14	65	6027	17824	34933015
Neutropenia	97.84	25.14	128	5964	156650	34794189
Metastases to lymph nodes	86.00	25.14	32	6060	4696	34946143
Hydronephrosis	73.69	25.14	36	6056	10310	34940529
Disease progression	65.35	25.14	87	6005	107990	34842849
Colony stimulating factor therapy	59.54	25.14	12	6080	166	34950673
Neutrophil count decreased	54.22	25.14	55	6037	51049	34899790
Haematuria	51.50	25.14	53	6039	50013	34900826
Bone lesion	50.05	25.14	19	6073	2944	34947895
Prostate cancer recurrent	43.08	25.14	13	6079	1000	34949839
Metastases to lung	42.30	25.14	24	6068	9296	34941543
Necrotising retinitis	41.01	25.14	12	6080	830	34950009
Pulmonary embolism	36.47	25.14	60	6032	89686	34861153
Prostate cancer	35.49	25.14	39	6053	39610	34911229
Anaemia	34.66	25.14	104	5988	233231	34717608
BRCA1 gene mutation	34.41	25.14	6	6086	35	34950804
Metastases to soft tissue	34.05	25.14	9	6083	427	34950412
BRCA2 gene mutation	33.85	25.14	6	6086	39	34950800
Septic shock	33.28	25.14	51	6041	71783	34879056
Peri-implantitis	32.74	25.14	7	6085	131	34950708
Bone pain	29.02	25.14	26	6066	20660	34930179

FDA Adverse Event Reporting System (Geriatric)

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	303.04	28.51	80	5119	10306	79728883
Febrile neutropenia	244.82	28.51	164	5035	230835	79508354
Osteonecrosis of jaw	111.50	28.51	55	5144	43171	79696018
Metastases to bone	107.13	28.51	45	5154	24382	79714807
Neutropenia	104.14	28.51	110	5089	287600	79451589
Prostate cancer metastatic	75.84	28.51	22	5177	3985	79735204
Haematuria	68.06	28.51	47	5152	68789	79670400
Neutrophil count decreased	63.41	28.51	51	5148	93908	79645281
Hydronephrosis	62.89	28.51	28	5171	17426	79721763
Malignant neoplasm progression	61.93	28.51	59	5140	135931	79603258
Hormone-refractory prostate cancer	59.95	28.51	12	5187	448	79738741
Prostate cancer	56.38	28.51	32	5167	33236	79705953
Metastases to lymph nodes	55.28	28.51	22	5177	10375	79728814
Prostate cancer recurrent	53.06	28.51	12	5187	806	79738383
Disease progression	48.71	28.51	60	5139	184302	79554887
Necrotising retinitis	48.05	28.51	12	5187	1233	79737956
Septic shock	42.57	28.51	46	5153	122755	79616434
Bone lesion	40.31	28.51	15	5184	5904	79733285
Pyrexia	38.61	28.51	114	5085	678595	79060594
Peripheral sensory neuropathy	37.84	28.51	18	5181	13015	79726174
Peri-implantitis	36.45	28.51	7	5192	210	79738979
Colony stimulating factor therapy	35.69	28.51	8	5191	516	79738673
Metastases to soft tissue	34.49	28.51	8	5191	601	79738588
Pulmonary embolism	33.21	28.51	48	5151	171606	79567583
Interstitial lung disease	31.91	28.51	38	5161	112562	79626627
Anaemia	31.44	28.51	81	5118	444934	79294255
Sepsis	30.22	28.51	59	5140	269369	79469820
Disseminated intravascular coagulation	29.70	28.51	22	5177	35820	79703369

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.2	acidic
pKa2	12.4	acidic

Orange Book patent data (new drug applications)

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

Orange Book exclusivity data (new drug applications)

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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Tubulin beta	Tumour-associated antigen	P07437 Q9H4B7 Q13885 Q9BVA1 Q13509 P04350 P68371 Q9BUF5 Q3ZCM7	TBB5_HUMAN TBB1_HUMAN TBB2A_HUMAN TBB2B_HUMAN TBB3_HUMAN TBB4A_HUMAN TBB4B_HUMAN TBB6_HUMAN TBB8_HUMAN	INHIBITOR				SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE

External reference:

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

Pharmaceutical products:

None