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
Structure for Cabazitaxel (DB06772)
- 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
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to treat Metastatic castration-resistant prostate cancer (mcrpc) Regimen in combination with: Prednisolone (DB00860) •••••••••••• •••••••• ••••••••• ••••••••• Used in combination to treat Metastatic castration-resistant prostate cancer (mcrpc) Regimen in combination with: Prednisone (DB00635) •••••••••••• •••••••• ••••••••• ••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- 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
Target Actions Organism ATubulin beta-1 chain inhibitorHumans - 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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The oral LD50 in rats is 500 mg/kg.8
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbametapir The serum concentration of Cabazitaxel can be increased when it is combined with Abametapir. Abatacept The metabolism of Cabazitaxel can be increased when combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Cabazitaxel. Abiraterone The metabolism of Cabazitaxel can be decreased when combined with Abiraterone. Acalabrutinib The 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
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Cabazitaxel Accord Injection, solution, concentrate 20 mg/ml Intravenous Accord Healthcare S.L.U. 2020-12-23 Not applicable EU 
Cabazitaxel for Injection Solution 40 mg / mL Intravenous Dr Reddy's Laboratories Ltd 2020-06-01 Not applicable Canada 
Cabazitaxel for Injection Solution 60 mg / 6 mL Intravenous Sandoz Canada Incorporated 2019-12-18 Not applicable Canada Cabazitaxel for Injection Kit; Solution 40 mg / mL Intravenous Marcan Pharmaceuticals Inc Not applicable Not applicable Canada Cabazitaxel for Injection Solution 45 mg / 4.5 mL Intravenous Sandoz Canada Incorporated 2019-12-18 Not applicable Canada
Categories
- ATC Codes
- L01CD04 — Cabazitaxel
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Inhibitors
- Cardiotoxic antineoplastic agents
- Cyclodecanes
- Cycloparaffins
- Cytochrome P-450 CYP2C8 Substrates
- Cytochrome P-450 CYP2C8 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 CYP3A5 Substrates
- Cytochrome P-450 CYP3A5 Substrates with a Narrow Therapeutic Index
- Cytochrome P-450 Substrates
- Diterpenes
- Immunosuppressive Agents
- Microtubule Inhibition
- Microtubule Inhibitors
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B3 inhibitors
- P-glycoprotein inhibitors
- P-glycoprotein substrates
- P-glycoprotein substrates with a Narrow Therapeutic Index
- Taxane Derivatives
- Taxoids
- Terpenes
- 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
- 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]
- Nightingale G, Ryu J: Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. P T. 2012 Aug;37(8):440-8. [Article]
- 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]
- 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]
- FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
- Health Canada Approved Drug Products: CABAZITAXEL Intravenous Injection [Link]
- EMA Approved Drug Products: Jevtana (cabazitaxel) Intravenous Injection [Link]
- Biosynth Carbosynth: Cabazitaxel MSDS [Link]
- External Links
- Human Metabolome Database
- HMDB0015672
- KEGG Drug
- D09755
- PubChem Compound
- 9854073
- PubChem Substance
- 99443289
- ChemSpider
- 8029779
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Treatment Metastatic Prostate Cancer 2 4 Completed Treatment Prostate Cancer 2 3 Active Not Recruiting Treatment Adenocarcinoma of Prostate / Progression of Prostate Cancer 1 3 Completed Treatment Metastatic Prostate Cancer 2 3 Completed Treatment Neoplasm / Neoplasms of the Prostate 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 60 mg/1.5ml Injection, solution, concentrate Intravenous Kit; solution Intravenous 40 mg / mL Solution Intravenous 45 mg / 4.5 mL Solution Intravenous 60 mg / 6 mL Solution Parenteral 60 mg Injection Parenteral 60 MG Injection, solution, concentrate Intravenous 60 mg/1.5ml Injection, solution, concentrate Intravenous 10 MG/ML Injection, solution, concentrate Intravenous 20 mg/ml Injection Intravenous Injection, solution, concentrate Intravenous; Parenteral 60 mg/1.5ml Injection, solution, concentrate; kit Intravenous 60 mg/1.5mL Solution Intravenous 40 mg / mL Solution Intravenous Injection Parenteral 60 mg/1.5ml Solution Intravenous 60 mg/1.5ml Injection, solution, concentrate Intravenous drip 60 mg/1.5ml Solution Intravenous 60 mg Solution, concentrate Intravenous 60 mg - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5438072 No 1995-08-01 2014-05-22 US 
US5698582 No 1997-12-16 2012-07-03 US US6372780 No 2002-04-16 2016-03-26 US US6387946 No 2002-05-14 2016-03-26 US US8927592 Yes 2015-01-06 2031-04-27 US US7241907 Yes 2007-07-10 2026-06-10 US US5847170 Yes 1998-12-08 2021-09-26 US US6331635 No 2001-12-18 2016-03-26 US US10583110 No 2020-03-10 2030-10-27 US US10716777 No 2020-07-21 2030-10-27 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 170 https://datasheets.scbt.com/sds/eghs/en/sc-396754.pdf - Predicted Properties
Property Value Source Water Solubility 0.00413 mg/mL ALOGPS logP 3.69 ALOGPS logP 4.2 Chemaxon logS -5.3 ALOGPS pKa (Strongest Acidic) 11.96 Chemaxon pKa (Strongest Basic) -3.6 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 10 Chemaxon Hydrogen Donor Count 3 Chemaxon Polar Surface Area 202.45 Å2 Chemaxon Rotatable Bond Count 15 Chemaxon Refractivity 213.4 m3·mol-1 Chemaxon Polarizability 86.25 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9535 Blood Brain Barrier - 0.9825 Caco-2 permeable - 0.7945 P-glycoprotein substrate Substrate 0.8287 P-glycoprotein inhibitor I Inhibitor 0.6646 P-glycoprotein inhibitor II Inhibitor 0.5887 Renal organic cation transporter Non-inhibitor 0.933 CYP450 2C9 substrate Non-substrate 0.8236 CYP450 2D6 substrate Non-substrate 0.882 CYP450 3A4 substrate Substrate 0.7256 CYP450 1A2 substrate Non-inhibitor 0.8197 CYP450 2C9 inhibitor Non-inhibitor 0.8654 CYP450 2D6 inhibitor Non-inhibitor 0.8935 CYP450 2C19 inhibitor Non-inhibitor 0.8429 CYP450 3A4 inhibitor Non-inhibitor 0.6339 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9068 Ames test Non AMES toxic 0.8028 Carcinogenicity Non-carcinogens 0.9264 Biodegradation Not ready biodegradable 0.9926 Rat acute toxicity 2.6378 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9907 hERG inhibition (predictor II) Non-inhibitor 0.7906
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 292.1316863 predictedDarkChem Lite v0.1.0 [M-H]- 293.0404863 predictedDarkChem Lite v0.1.0 [M-H]- 258.36423 predictedDeepCCS 1.0 (2019) [M+H]+ 291.2476863 predictedDarkChem Lite v0.1.0 [M+H]+ 291.6275863 predictedDarkChem Lite v0.1.0 [M+H]+ 260.08795 predictedDeepCCS 1.0 (2019) [M+Na]+ 290.7347863 predictedDarkChem Lite v0.1.0 [M+Na]+ 292.4353863 predictedDarkChem Lite v0.1.0 [M+Na]+ 266.63284 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- 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
- Nightingale G, Ryu J: Cabazitaxel (jevtana): a novel agent for metastatic castration-resistant prostate cancer. P T. 2012 Aug;37(8):440-8. [Article]
- 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]
- 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]
- 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
- 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
- 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
- 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
- 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
- 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
- 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
- FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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
- 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
- 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
- FDA Approved Drug Products: JEVTANA (cabazitaxel) injection, for intravenous use (June 2023) [Link]
Drug created at September 14, 2010 16:21 / Updated at February 20, 2024 23:54