Details of the Drug

General Information of Drug (ID: DMPAZHC)

Drug Name

Cabazitaxel

Synonyms

Jevtana; Taxoid XRP6258; Jevtana (TN)

Indication

Disease Entry	ICD 11	Status	REF
Breast cancer	2C60-2C65	Approved	[1]
Solid tumour/cancer	2A00-2F9Z	Phase 2	[1]
Metastatic prostate carcinoma	N.A.	Investigative	[2]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 3

Molecular Weight (mw)

835.9

Logarithm of the Partition Coefficient (xlogp)

2.7

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Clearance: The drug present in the plasma can be removed from the body at the rate of 11 mL/min/kg [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 4 minutes (alpha), 2 hours (beta), and 95 hours (gamma) [3]
Metabolism: The drug is metabolized via the liver []
Unbound Fraction: The unbound fraction of drug in plasma is 0.24% [3]
Vd: The volume of distribution (Vd) of drug is 4,864 L []

Chemical Identifiers

Formula: C45H57NO14
IUPAC Name: [(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-1-hydroxy-15-[(2R,3S)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate
Canonical SMILES: CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC
InChI: InChI=1S/C45H57NO14/c1-24-28(57-39(51)33(48)32(26-17-13-11-14-18-26)46-40(52)60-41(3,4)5)22-45(53)37(58-38(50)27-19-15-12-16-20-27)35-43(8,36(49)34(55-10)31(24)42(45,6)7)29(54-9)21-30-44(35,23-56-30)59-25(2)47/h11-20,28-30,32-35,37,48,53H,21-23H2,1-10H3,(H,46,52)/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+/m0/s1
InChIKey: BMQGVNUXMIRLCK-OAGWZNDDSA-N

Cross-matching ID

PubChem CID: 9854073
ChEBI ID: CHEBI:63584
CAS Number: 183133-96-2
DrugBank ID: DB06772
TTD ID: D02HSB
INTEDE ID: DR0252
ACDINA ID: D00902

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Tubulin (TUB)	TTML2WA	NOUNIPROTAC	Inhibitor	[4]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[5]
Cytochrome P450 3A5 (CYP3A5)_{Main DME}	DEIBDNY	CP3A5_HUMAN	Substrate	[5]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Substrate	[5]

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Drug Off-Target (DOT)

DOT Name	DOT ID	UniProt ID	Interaction	REF
Forkhead box protein O3 (FOXO3)	OTHXQG4P	FOXO3_HUMAN	Gene/Protein Processing	[6]
Proline-rich AKT1 substrate 1 (AKT1S1)	OT4JHN4Y	AKTS1_HUMAN	Gene/Protein Processing	[6]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Molecular Expression Atlas of This Drug

The Studied Disease

Breast cancer

ICD Disease Classification

2C60-2C65

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Tubulin (TUB)	DTT	NO-GeName	7.94E-02	0.35	0.43
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	1.13E-01	6.17E-02	2.28E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	6.08E-01	2.08E-01	1.69E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.96E-01	-3.35E-01	-1.10E+00

Molecular Expression Atlas (MEA)

MEA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Cabazitaxel

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Tucatinib	DMBESUA	Moderate	Decreased metabolism of Cabazitaxel caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[7]
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Coadministration of a Drug Treating the Disease Different from Cabazitaxel (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Moderate	Increased metabolism of Cabazitaxel caused by Ivosidenib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[8]
Arn-509	DMT81LZ	Moderate	Increased metabolism of Cabazitaxel caused by Arn-509 mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[8]
Gilteritinib	DMTI0ZO	Moderate	Decreased clearance of Cabazitaxel due to the transporter inhibition by Gilteritinib.	Acute myeloid leukaemia [2A60]	[7]
Troleandomycin	DMUZNIG	Moderate	Decreased metabolism of Cabazitaxel caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[7]
Erdafitinib	DMI782S	Moderate	Decreased clearance of Cabazitaxel due to the transporter inhibition by Erdafitinib.	Bladder cancer [2C94]	[9]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Cabazitaxel caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[8]
Lumacaftor	DMCLWDJ	Moderate	Increased metabolism of Cabazitaxel caused by Lumacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[8]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Cabazitaxel caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[8]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Cabazitaxel caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[8]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Cabazitaxel caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[8]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Cabazitaxel caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[8]
Tazemetostat	DMWP1BH	Moderate	Increased metabolism of Cabazitaxel caused by Tazemetostat mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[8]
Boceprevir	DMBSHMF	Moderate	Decreased metabolism of Cabazitaxel caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[7]
Brentuximab vedotin	DMWLC57	Moderate	Increased risk of peripheral neuropathy by the combination of Cabazitaxel and Brentuximab vedotin.	Hodgkin lymphoma [2B30]	[10]
Cobicistat	DM6L4H2	Moderate	Decreased metabolism of Cabazitaxel caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[7]
Teriflunomide	DMQ2FKJ	Major	Additive immunosuppressive effects by the combination of Cabazitaxel and Teriflunomide.	Hyper-lipoproteinaemia [5C80]	[11]
BMS-201038	DMQTAGO	Moderate	Decreased metabolism of Cabazitaxel caused by BMS-201038 mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[8]
Berotralstat	DMWA2DZ	Moderate	Decreased metabolism of Cabazitaxel caused by Berotralstat mediated inhibition of CYP450 enzyme.	Innate/adaptive immunodeficiency [4A00]	[8]
Crizotinib	DM4F29C	Moderate	Decreased metabolism of Cabazitaxel caused by Crizotinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[8]
Ceritinib	DMB920Z	Moderate	Decreased metabolism of Cabazitaxel caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[7]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Cabazitaxel caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[8]
Capmatinib	DMYCXKL	Moderate	Decreased clearance of Cabazitaxel due to the transporter inhibition by Capmatinib.	Lung cancer [2C25]	[12]
Selpercatinib	DMZR15V	Moderate	Decreased metabolism of Cabazitaxel caused by Selpercatinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[8]
IPI-145	DMWA24P	Moderate	Decreased metabolism of Cabazitaxel caused by IPI-145 mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[13]
Vemurafenib	DM62UG5	Moderate	Increased metabolism of Cabazitaxel caused by Vemurafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[8]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Cabazitaxel caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[14]
Lasmiditan	DMXLVDT	Moderate	Decreased clearance of Cabazitaxel due to the transporter inhibition by Lasmiditan.	Migraine [8A80]	[15]
Tecfidera	DM2OVDT	Moderate	Additive immunosuppressive effects by the combination of Cabazitaxel and Tecfidera.	Multiple sclerosis [8A40]	[16]
Siponimod	DM2R86O	Major	Additive immunosuppressive effects by the combination of Cabazitaxel and Siponimod.	Multiple sclerosis [8A40]	[7]
Fingolimod	DM5JVAN	Major	Additive immunosuppressive effects by the combination of Cabazitaxel and Fingolimod.	Multiple sclerosis [8A40]	[17]
Ocrelizumab	DMEZ2KH	Moderate	Additive immunosuppressive effects by the combination of Cabazitaxel and Ocrelizumab.	Multiple sclerosis [8A40]	[18]
Ozanimod	DMT6AM2	Major	Additive immunosuppressive effects by the combination of Cabazitaxel and Ozanimod.	Multiple sclerosis [8A40]	[14]
Netupitant	DMEKAYI	Moderate	Decreased metabolism of Cabazitaxel caused by Netupitant mediated inhibition of CYP450 enzyme.	Nausea/vomiting [MD90]	[8]
Abametapir	DM2RX0I	Moderate	Decreased metabolism of Cabazitaxel caused by Abametapir mediated inhibition of CYP450 enzyme.	Pediculosis [1G00]	[19]
Lefamulin	DME6G97	Moderate	Decreased metabolism of Cabazitaxel caused by Lefamulin mediated inhibition of CYP450 enzyme.	Pneumonia [CA40]	[20]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Cabazitaxel caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[8]
Anthrax vaccine	DM9GSWY	Moderate	Antagonize the effect of Cabazitaxel when combined with Anthrax vaccine.	Sepsis [1G40-1G41]	[21]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Cabazitaxel caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[8]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Cabazitaxel caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[14]
LEE011	DMMX75K	Moderate	Decreased metabolism of Cabazitaxel caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[8]
Fostamatinib	DM6AUHV	Moderate	Decreased metabolism of Cabazitaxel caused by Fostamatinib mediated inhibition of CYP450 enzyme.	Thrombocytopenia [3B64]	[22]
Brilinta	DMBR01X	Moderate	Decreased metabolism of Cabazitaxel caused by Brilinta mediated inhibition of CYP450 enzyme.	Thrombosis [DB61-GB90]	[8]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Cabazitaxel caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[8]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Citric acid monohydrate	E00271	22230	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Polysorbate 80	E00665	Not Available	Dispersing agent; Emollient; Emulsifying agent; Plasticizing agent; Solubilizing agent; Surfactant; Suspending agent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Cabazitaxel 60mg/1.5ml solution	60mg/1.5ml	Solution	Intravenous

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References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6798).
2	Cabazitaxel FDA Label
3	Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
4	Mullard A: 2010 FDA drug approvals. Nat Rev Drug Discov. 2011 Feb;10(2):82-5.
5	DAILYMED.nlm.nih.gov: JEVTANA- cabazitaxel kit.
6	The triphenyltin carboxylate derivative triphenylstannyl 2-(benzylcarbamoyl)benzoate impedes prostate cancer progression via modulation of Akt/FOXO3a signaling. Toxicol Appl Pharmacol. 2020 Aug 15;401:115091. doi: 10.1016/j.taap.2020.115091. Epub 2020 Jun 7.
7	Cerner Multum, Inc. "Australian Product Information.".
8	Product Information. Jevtana (cabazitaxel). sanofi-aventis , Bridgewater, NJ.
9	Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
10	Carrion C, Espinosa E, Herrero A, Garcia B "Possible vincristine-isoniazid interaction." Ann Pharmacother 29 (1995): 201. [PMID: 7756727]
11	Product Information. Arava (leflunomide). Hoechst Marion-Roussel Inc, Kansas City, MO.
12	Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
13	Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
14	Cerner Multum, Inc. "UK Summary of Product Characteristics.".
15	Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
16	Product Information. Vumerity (diroximel fumarate). Alkermes, Inc, Cambridge, MA.
17	Product Information. Gilenya (fingolimod). Novartis Pharmaceuticals, East Hanover, NJ.
18	Product Information. Ocrevus (ocrelizumab). Genentech, South San Francisco, CA.
19	Product Information. Xeglyze (abametapir topical). Dr. Reddy's Laboratories Inc, Upper Saddle River, NJ.
20	Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
21	CDC. Centers for Disease Control and Prevention/ "Recommendations of the advisory committtee on immunization practices (ACIP): use of vaccines and immune globulins in persons with altered immunocompetence." MMWR Morb Mortal Wkly Rep 42(RR-04) (1993): 1-18. [PMID: 20300058]
22	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.