Cabazitaxel

Identification

Summary

Cabazitaxel is an antineoplastic agent used in combination with corticosteroids to treat metastatic castration-resistant prostate cancer in patients previously treated with a docetaxel-containing treatment regimen.

Brand Names
Jevtana
Generic Name
Cabazitaxel
DrugBank Accession Number
DB06772
Background

Cabazitaxel is a taxoid synthesized from 10-deacetylbaccatin III, a compound isolated from the yew tree.4 As a second-generation semisynthetic microtubule inhibitor, cabazitaxel stabilizes microtubules and induces tumour cell death.2 Due to its low affinity for the P-glycoprotein (P-gp) efflux pump, cabazitaxel can more readily penetrate the blood–brain barrier compared to other taxanes like paclitaxel and docetaxel.2,3,4

Cabazitaxel is used to treat metastatic castration-resistant prostate cancer. It was first approved by the FDA on June 17, 2010.3 It was also approved by the EMA on March 17, 2011 7 and Health Canada on December 17, 2019.6

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 835.9324
Monoisotopic: 835.377905537
Chemical Formula
C45H57NO14
Synonyms
  • 1-HYDROXY-7.BETA.,10.BETA.-DIMETHOXY-9-OXO-5.BETA.,20-EPOXYTAX-11-ENE-2.ALPHA.,4,13.ALPHA.-TRIYL 4-ACETATE 2-BENZOATE 13-((2R,3S)-3-(((TERT-BUTOXY)CARBONYL)AMINO)-2-HYDROXY-3-PHENYLPROPANOATE)
  • Cabazitaxel
  • Cabazitaxelum
External IDs
  • RPR-116258A
  • RPR116258
  • RPR116258A
  • TXD 258
  • TXD-258
  • TXD258
  • XRP 6258
  • XRP-6258
  • XRP6258

Pharmacology

Indication

Cabazitaxel is indicated, in combination with prednisone, for the treatment of patients with metastatic castration-resistant prostate cancer previously treated with a docetaxel-containing treatment regimen.5 In Europe and Canada, it can also be used in combination with prednisolone.6,7

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatMetastatic castration-resistant prostate cancer (mcrpc)Regimen in combination with: Prednisolone (DB00860)•••••••••••••••••••• ••••••••• •••••••••
Used in combination to treatMetastatic castration-resistant prostate cancer (mcrpc)Regimen in combination with: Prednisone (DB00635)•••••••••••••••••••• ••••••••• •••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Cabazitaxel demonstrates a broad spectrum of antitumour activity against advanced human tumours xenografted in mice, including intracranial human glioblastomas.6 Cabazitaxel has a low affinity to P-glycoprotein, allowing it to penetrate the blood-brain barrier without being subject to extensive P-gp-mediated active efflux.3,4 Cabazitaxel works against docetaxel-sensitive tumours and tumour models resistant to docetaxel and other chemotherapy drugs.4,6

Mechanism of action

Microtubules are cytoskeletal polymers that regulate cell shape, vesicle transport, cell signalling, and cell division. They are made up of alpha-tubulin and beta-tubulin heterodimers. Microtubules extend toward the mitotic spindle during mitosis to allow the separation and distribution of chromosomes during cell division.2 Cabazitaxel binds to the N-terminal amino acids of the beta-tubulin subunit and promotes microtubule polymerization while simultaneously inhibiting disassembly: this results in the stabilization of microtubules, preventing microtubule cell division. Cabazitaxel ultimately blocks mitotic and interphase cellular functions and tumour proliferation.2,5

TargetActionsOrganism
ATubulin beta-1 chain
inhibitor
Humans
Absorption

Based on the population pharmacokinetic analysis, after an intravenous dose of cabazitaxel 25 mg/m2 every three weeks, the mean Cmax in patients with metastatic prostate cancer was 226 ng/mL (CV 107%) and was reached at the end of the one-hour infusion (Tmax). The mean AUC in patients with metastatic prostate cancer was 991 ng x h/mL (CV 34%). No major deviation from the dose proportionality was observed from 10 to 30 mg/m2 in patients with advanced solid tumours.5

Volume of distribution

Steady-state volume of distribution (Vss) was 4,864 L (2,643 L/m2 for a patient with a median BSA of 1.84 m2).5

Protein binding

In vitro, the binding of cabazitaxel to human serum proteins was 89% to 92% and was not saturable up to 50,000 ng/mL. Cabazitaxel is mainly bound to human serum albumin (82%) and lipoproteins (88% for HDL, 70% for LDL, and 56% for VLDL). The in vitro blood-to-plasma concentration ratio in human blood ranged from 0.90 to 0.99, indicating that cabazitaxel was equally distributed between blood and plasma.5

Metabolism

More than 95% of cabazitaxel is extensively metabolized in the liver. CYP3A4 and CYP3A5 are responsible for 80% to 90% of drug metabolism, while CYP2C8 is involved to a lesser extent. While cabazitaxel is the main circulating moiety in human plasma, seven metabolites have been detected in plasma, including three active metabolites arising from O-demethylation 5 - docetaxel, RPR112698, and RPR123142.1 The main metabolite accounts for 5% of total cabazitaxel exposure.5

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Route of elimination

After a one-hour intravenous infusion [14C]-cabazitaxel 25 mg/m2, approximately 80% of the administered dose was eliminated within two weeks. Cabazitaxel is mainly excreted in the feces as numerous metabolites (76% of the dose), while renal excretion of cabazitaxel and metabolites account for 3.7% of the dose (2.3% as unchanged drug in urine). Around 20 metabolites of cabazitaxel are excreted into human urine and feces.5

Half-life

Following a one-hour intravenous infusion, plasma concentrations of cabazitaxel can be described by a three-compartment pharmacokinetic model with α-, β-, and γ- half-lives of four minutes, two hours, and 95 hours, respectively.5

Clearance

Based on the population pharmacokinetic analysis, cabazitaxel has a plasma clearance of 48.5 L/h (CV 39%; 26.4 L/h/m2 for a patient with a median BSA of 1.84 m2) in patients with metastatic prostate cancer.5

Adverse Effects
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Toxicity

The oral LD50 in rats is 500 mg/kg.8

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Cabazitaxel can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Cabazitaxel can be increased when combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Cabazitaxel.
AbirateroneThe metabolism of Cabazitaxel can be decreased when combined with Abiraterone.
AcalabrutinibThe metabolism of Cabazitaxel can be decreased when combined with Acalabrutinib.
Food Interactions
  • Avoid grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of cabazitaxel, which may increase its serum concentration.
  • Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of cabazitaxel and may reduce its serum concentration.

Products

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dosage, form, labeller, route of administration, and marketing period.
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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Cabazitaxel AccordInjection, solution, concentrate20 mg/mlIntravenousAccord Healthcare S.L.U.2020-12-23Not applicableEU flag
Cabazitaxel for InjectionKit; Solution40 mg / mLIntravenousMarcan Pharmaceuticals IncNot applicableNot applicableCanada flag
Cabazitaxel for InjectionSolution45 mg / 4.5 mLIntravenousSandoz Canada Incorporated2019-12-18Not applicableCanada flag
Cabazitaxel for InjectionSolution40 mg / mLIntravenousDr Reddy's Laboratories Ltd2020-06-01Not applicableCanada flag
Cabazitaxel for InjectionSolution60 mg / 6 mLIntravenousSandoz Canada Incorporated2019-12-18Not applicableCanada flag

Categories

ATC Codes
L01CD04 — Cabazitaxel
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as taxanes and derivatives. These are diterpenoids with a structure based either on the taxane skeleton, or a derivative thereof. In term of phytochemistry, several derivatives of the taxane skeleton exist: 2(3->20)-abeotaxane, 3,11-cyclotaxane, 11(15->1),11(10->9)-abeotaxane, 3,8-seco-taxane, and 11(15->1)-abeotaxane, among others. More complex skeletons have been found recently, which include the taxane-derived [3.3.3] propellane ring system.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Prenol lipids
Sub Class
Diterpenoids
Direct Parent
Taxanes and derivatives
Alternative Parents
Benzoic acid esters / Tricarboxylic acids and derivatives / Benzoyl derivatives / Fatty acid esters / Monosaccharides / Tertiary alcohols / Carbamate esters / Secondary alcohols / Oxetanes / Carboxylic acid esters
show 8 more
Substituents
Alcohol / Aromatic heteropolycyclic compound / Benzenoid / Benzoate ester / Benzoic acid or derivatives / Benzoyl / Carbamic acid ester / Carbonic acid derivative / Carbonyl group / Carboxylic acid derivative
show 22 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tetracyclic diterpenoid (CHEBI:63584)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
51F690397J
CAS number
183133-96-2
InChI Key
BMQGVNUXMIRLCK-OAGWZNDDSA-N
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
IUPAC Name
(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-15-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0^{3,10}.0^{4,7}]heptadec-13-en-2-yl benzoate
SMILES
[H][C@]12[C@H](OC(=O)C3=CC=CC=C3)[C@]3(O)C[C@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C4=CC=CC=C4)C(C)=C([C@@H](OC)C(=O)[C@]1(C)[C@H](C[C@H]1OC[C@@]21OC(C)=O)OC)C3(C)C

References

Synthesis Reference

Nagesh Palepu, "CABAZITAXEL FORMULATIONS AND METHODS OF PREPARING THEREOF." U.S. Patent US20120065255, issued March 15, 2012.

US20120065255
General References
  1. Kort A, Hillebrand MJ, Cirkel GA, Voest EE, Schinkel AH, Rosing H, Schellens JH, Beijnen JH: Quantification of cabazitaxel, its metabolite docetaxel and the determination of the demethylated metabolites RPR112698 and RPR123142 as docetaxel equivalents in human plasma by liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Apr 15;925:117-23. doi: 10.1016/j.jchromb.2013.02.034. Epub 2013 Mar 5. [Article]
  2. Nightingale G, Ryu J: Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. P T. 2012 Aug;37(8):440-8. [Article]
  3. Paller CJ, Antonarakis ES: Cabazitaxel: a novel second-line treatment for metastatic castration-resistant prostate cancer. Drug Des Devel Ther. 2011 Mar 10;5:117-24. doi: 10.2147/DDDT.S13029. [Article]
  4. Villanueva C, Bazan F, Kim S, Demarchi M, Chaigneau L, Thiery-Vuillemin A, Nguyen T, Cals L, Dobi E, Pivot X: Cabazitaxel: a novel microtubule inhibitor. Drugs. 2011 Jul 9;71(10):1251-8. doi: 10.2165/11591390-000000000-00000. [Article]
  5. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
  6. Health Canada Approved Drug Products: CABAZITAXEL Intravenous Injection [Link]
  7. EMA Approved Drug Products: Jevtana (cabazitaxel) Intravenous Injection [Link]
  8. Biosynth Carbosynth: Cabazitaxel MSDS [Link]
Human Metabolome Database
HMDB0015672
KEGG Drug
D09755
PubChem Compound
9854073
PubChem Substance
99443289
ChemSpider
8029779
RxNav
996051
ChEBI
63584
ChEMBL
CHEMBL1201748
ZINC
ZINC000085536932
PharmGKB
PA165958401
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cabazitaxel

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentMetastatic Prostate Cancer2
4CompletedTreatmentProstate Cancer2
3Active Not RecruitingTreatmentAdenocarcinoma of Prostate / Progression of Prostate Cancer1
3CompletedTreatmentMetastatic Prostate Cancer2
3CompletedTreatmentNeoplasm / Neoplasms of the Prostate1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, solutionIntravenous60 mg/1.5ml
Injection, solution, concentrateIntravenous
Kit; solutionIntravenous40 mg / mL
SolutionIntravenous45 mg / 4.5 mL
SolutionIntravenous60 mg / 6 mL
SolutionParenteral60 mg
InjectionParenteral60 MG
Injection, solution, concentrateIntravenous60 mg/1.5ml
Injection, solution, concentrateIntravenous10 MG/ML
Injection, solution, concentrateIntravenous20 mg/ml
InjectionIntravenous
Injection, solution, concentrateIntravenous; Parenteral60 mg/1.5ml
Injection, solution, concentrate; kitIntravenous60 mg/1.5mL
SolutionIntravenous40 mg / mL
SolutionIntravenous
InjectionParenteral60 mg/1.5ml
SolutionIntravenous60 mg/1.5ml
Injection, solution, concentrateIntravenous drip60 mg/1.5ml
SolutionIntravenous60 mg
Solution, concentrateIntravenous60 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5438072No1995-08-012014-05-22US flag
US5698582No1997-12-162012-07-03US flag
US6372780No2002-04-162016-03-26US flag
US6387946No2002-05-142016-03-26US flag
US8927592Yes2015-01-062031-04-27US flag
US7241907Yes2007-07-102026-06-10US flag
US5847170Yes1998-12-082021-09-26US flag
US6331635No2001-12-182016-03-26US flag
US10583110No2020-03-102030-10-27US flag
US10716777No2020-07-212030-10-27US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)170https://datasheets.scbt.com/sds/eghs/en/sc-396754.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.00413 mg/mLALOGPS
logP3.69ALOGPS
logP4.2Chemaxon
logS-5.3ALOGPS
pKa (Strongest Acidic)11.96Chemaxon
pKa (Strongest Basic)-3.6Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count10Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area202.45 Å2Chemaxon
Rotatable Bond Count15Chemaxon
Refractivity213.4 m3·mol-1Chemaxon
Polarizability86.25 Å3Chemaxon
Number of Rings6Chemaxon
Bioavailability0Chemaxon
Rule of FiveNoChemaxon
Ghose FilterNoChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleYesChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9535
Blood Brain Barrier-0.9825
Caco-2 permeable-0.7945
P-glycoprotein substrateSubstrate0.8287
P-glycoprotein inhibitor IInhibitor0.6646
P-glycoprotein inhibitor IIInhibitor0.5887
Renal organic cation transporterNon-inhibitor0.933
CYP450 2C9 substrateNon-substrate0.8236
CYP450 2D6 substrateNon-substrate0.882
CYP450 3A4 substrateSubstrate0.7256
CYP450 1A2 substrateNon-inhibitor0.8197
CYP450 2C9 inhibitorNon-inhibitor0.8654
CYP450 2D6 inhibitorNon-inhibitor0.8935
CYP450 2C19 inhibitorNon-inhibitor0.8429
CYP450 3A4 inhibitorNon-inhibitor0.6339
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9068
Ames testNon AMES toxic0.8028
CarcinogenicityNon-carcinogens0.9264
BiodegradationNot ready biodegradable0.9926
Rat acute toxicity2.6378 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9907
hERG inhibition (predictor II)Non-inhibitor0.7906
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-0a4i-7930410210-8f0fa9fca32aef7bc7cd
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-02h0-0260163980-752d02d253648171b42d
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0229-6600090530-9b4792c2bd9a0c1e90b4
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-01ta-1490121860-dfae29c3a71ee7088ba3
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0pi3-7760051930-8b08107a7a09a96a280f
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0a7r-2903002740-9c9de7bc5510e2c52793
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-9320000310-13de97fdca50225f819e
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-292.1316863
predicted
DarkChem Lite v0.1.0
[M-H]-293.0404863
predicted
DarkChem Lite v0.1.0
[M-H]-258.36423
predicted
DeepCCS 1.0 (2019)
[M+H]+291.2476863
predicted
DarkChem Lite v0.1.0
[M+H]+291.6275863
predicted
DarkChem Lite v0.1.0
[M+H]+260.08795
predicted
DeepCCS 1.0 (2019)
[M+Na]+290.7347863
predicted
DarkChem Lite v0.1.0
[M+Na]+292.4353863
predicted
DarkChem Lite v0.1.0
[M+Na]+266.63284
predicted
DeepCCS 1.0 (2019)

Targets

Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock new
insights and accelerate drug research.
Learn more
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Learn more
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Structural constituent of cytoskeleton
Specific Function
Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
Gene Name
TUBB1
Uniprot ID
Q9H4B7
Uniprot Name
Tubulin beta-1 chain
Molecular Weight
50326.56 Da
References
  1. Nightingale G, Ryu J: Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. P T. 2012 Aug;37(8):440-8. [Article]
  2. Smiyun G, Azarenko O, Miller H, Rifkind A, LaPointe NE, Wilson L, Jordan MA: betaIII-tubulin enhances efficacy of cabazitaxel as compared with docetaxel. Cancer Chemother Pharmacol. 2017 Jul;80(1):151-164. doi: 10.1007/s00280-017-3345-2. Epub 2017 May 31. [Article]
  3. Zhu L, Zhang C, Lu X, Song C, Wang C, Zhang M, Xie Y, Schaefer HF 3rd: Binding modes of cabazitaxel with the different human beta-tubulin isotypes: DFT and MD studies. J Mol Model. 2020 May 30;26(6):162. doi: 10.1007/s00894-020-04400-w. [Article]
  4. DailyMed Label: JEVTANA (cabazitaxel) injection, for intravenous use [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Virus receptor activity
Specific Function
Binds LDL, the major cholesterol-carrying lipoprotein of plasma, and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clat...
Gene Name
LDLR
Uniprot ID
P01130
Uniprot Name
Low-density lipoprotein receptor
Molecular Weight
95375.105 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Very-low-density lipoprotein particle receptor activity
Specific Function
Binds VLDL and transports it into cells by endocytosis. In order to be internalized, the receptor-ligand complexes must first cluster into clathrin-coated pits. Binding to Reelin induces tyrosine p...
Gene Name
VLDLR
Uniprot ID
P98155
Uniprot Name
Very low-density lipoprotein receptor
Molecular Weight
96097.45 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Mediates the transport of lipoprotein lipase LPL from the basolateral to the apical surface of endothelial cells in capillaries (By similarity). Anchors LPL on the surface of endothelial cells in the lumen of blood capillaries (By similarity). Protects LPL against loss of activity, and against ANGPTL4-mediated unfolding (PubMed:27929370, PubMed:29899144). Thereby, plays an important role in lipolytic processing of chylomicrons by LPL, triglyceride metabolism and lipid homeostasis (PubMed:19304573, PubMed:21314738). Binds chylomicrons and phospholipid particles that contain APOA5 (PubMed:17997385, PubMed:19304573). Binds high-density lipoprotein (HDL) and plays a role in the uptake of lipids from HDL (By similarity).
Specific Function
Acetylcholine receptor inhibitor activity
Gene Name
GPIHBP1
Uniprot ID
Q8IV16
Uniprot Name
Glycosylphosphatidylinositol-anchored high density lipoprotein-binding protein 1
Molecular Weight
19849.845 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Cabazitaxel inhibited this transporter in vitro; however, the in vivo risk of cabazitaxel inhibiting this transporter is low at the recommended therapeutic dose (25 mg/m^2).
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Cabazitaxel inhibited this transporter in vitro; however, the in vivo risk of cabazitaxel inhibiting this transporter is low at the recommended therapeutic dose (25 mg/m^2).
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Cabazitaxel inhibited this transporter in vitro; however, the in vivo risk of cabazitaxel inhibiting this transporter is low at the recommended therapeutic dose (25 mg/m^2).
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Cabazitaxel inhibited this transporter in vitro; however, the in vivo risk of cabazitaxel inhibiting this transporter is low at the recommended therapeutic dose (25 mg/m^2).
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]

Drug created at September 14, 2010 16:21 / Updated at April 21, 2024 05:26