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:

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Property	Value	Reference
t_half (Half-life)	74.50 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	48 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
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

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Approvals:

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

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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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

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FDA Adverse Event Reporting System (Geriatric)

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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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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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

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🐶 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)

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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

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Orange Book exclusivity data (new drug applications)

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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

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Bioactivity Summary:

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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

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External reference:

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ID	Source
013461	NDDF
1426815-65-7	SECONDARY_CAS_RN
173956	MMSL
27256	MMSL
4030043	VUID
4030043	VANDF
446706007	SNOMEDCT_US
447182009	SNOMEDCT_US
51F690397J	UNII
6798	IUPHAR_LIGAND_ID

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Pharmaceutical products:

None