Identification

Name
Oxaliplatin
Accession Number
DB00526
Description

Oxaliplatin is a platinum-based chemotherapy drug in the same family as cisplatin and carboplatin. It is typically administered in combination with fluorouracil and leucovorin in a combination known as Folfox for the treatment of colorectal cancer. Compared to cisplatin the two amine groups are replaced by cyclohexyldiamine for improved antitumour activity. The chlorine ligands are replaced by the oxalato bidentate derived from oxalic acid in order to improve water solubility. Oxaliplatin is marketed by Sanofi-Aventis under the trademark Eloxatin®.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 397.294
Monoisotopic: 397.060149
Chemical Formula
C8H14N2O4Pt
Synonyms
  • Diaminocyclohexane Oxalatoplatinum
  • L-OHP
  • Oxalatoplatin
  • Oxalatoplatinum
  • Oxaliplatin
  • oxaliplatine
  • oxaliplatino
  • oxaliplatinum
External IDs
  • JM-83
  • NSC-266046
  • RP-54780
  • SR-96669

Pharmacology

Indication

Used in combination with infusional 5-FU/LV, is indicated for the treatment of advanced carcinoma of the colon or rectum and for adjuvant treatment of stage III colon cancer patients who have undergone complete resection of the primary tumor.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More
Pharmacodynamics

Oxaliplatin selectively inhibits the synthesis of deoxyribonucleic acid (DNA). The guanine and cytosine content correlates with the degree of Oxaliplatin-induced cross-linking. At high concentrations of the drug, cellular RNA and protein synthesis are also suppressed.

Mechanism of action

Oxaliplatin undergoes nonenzymatic conversion to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo DACH platinum, which covalently bind with macromolecules. After activation, oxaliplatin binds preferentially to the guanine and cytosine moieties of DNA, leading to cross-linking of DNA, thus inhibiting DNA synthesis and transcription. Cytotoxicity is cell-cycle nonspecific.

TargetActionsOrganism
ADNA
cross-linking/alkylation
Humans
Absorption

Bioavailability is complete following intravenous administration. When a single 2-hour intravenous infusion of oxaliplatin at a dose of 85 mg/m^2 is given, the peak serum concentration was 0.814 mcg/mL.

Volume of distribution
  • 440 L [single 2-hour IV infusion at dose of 85 mg/m^2] At the end of a 2-hour infusion of oxaliplatin, approximately 15% of the administered platinum is present in the systemic circulation. The remaining 85% is rapidly distributed into tissues or eliminated in the urine.
Protein binding

Plasma protein binding of platinum (active metabolite) is irreversible and is greater than 90%, primarily to albumin and gamma-globulins. It is also irreversibly binds to erythrocytes.

Metabolism

Oxaliplatin undergoes nonenzymatic conversion in physiologic solutions to active derivatives via displacement of the labile oxalate ligand. Several transient reactive species are formed, including monoaquo and diaquo DACH platinum, which covalently bind with macromolecules. There is no evidence of cytochrome P450-mediated metabolism in vitro.

Route of elimination

The major route of platinum elimination is renal excretion. At five days after a single 2-hour infusion of oxaliplatin, urinary elimination accounted for about 54% of the platinum eliminated, with fecal excretion accounting for only about 2%.

Half-life

The decline of ultrafilterable platinum levels following oxaliplatin administartion is triphasic, with two distribution phases: t1/2α; 0.43 hours and t1/2β; 16.8 hours. This is followed by a long terminal elimination phase that lasts 391 hours (t1/2γ).

Clearance
  • 10 - 17 L/h [renal clearance]
Adverse Effects
Learn about our commercial Adverse Effects data.
Learn More
Toxicity

There have been five cases of oxaliplatin overdose reported. One patient received two 130 mg/m2 doses of oxaliplatin (cumulative dose of 260 mg/m2) within a 24-hour period. The patient experienced Grade 4 thrombocytopenia (<25,000/mm3) without any bleeding, which resolved. Two other patients were mistakenly administered oxaliplatin instead of carboplatin. One patient received a total oxaliplatin dose of 500 mg and the other received 650 mg. The first patient experienced dyspnea, wheezing, paresthesia, profuse vomiting and chest pain on the day of administration. She developed respiratory failure and severe bradycardia, and subsequently did not respond to resuscitation efforts. The other patient also experienced dyspnea, wheezing, paresthesia, and vomiting. Most common adverse reactions (incidence ≥ 40%) were peripheral sensory neuropathy, neutropenia, thrombocytopenia, anemia, nausea, increase in transaminases and alkaline phosphatase, diarrhea, emesis, fatigue and stomatitis.

Affected organisms
  • Humans and other mammals
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
AbataceptThe risk or severity of adverse effects can be increased when Oxaliplatin is combined with Abatacept.
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Oxaliplatin.
AbemaciclibAbemaciclib may decrease the excretion rate of Oxaliplatin which could result in a higher serum level.
AcebutololThe risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Acebutolol.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Oxaliplatin.
Acetylsalicylic acidThe risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Oxaliplatin.
AcrivastineThe risk or severity of QTc prolongation can be increased when Acrivastine is combined with Oxaliplatin.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Oxaliplatin.
AdenosineThe risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Adenosine.
Adenovirus type 7 vaccine liveThe risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Oxaliplatin.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
No interactions found.

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Act OxaliplatinSolutionIntravenousActavis Pharma Company2015-12-162018-07-09Canada flag
Act OxaliplatinPowder, for solutionIntravenousActavis Pharma CompanyNot applicableNot applicableCanada flag
Act OxaliplatinPowder, for solutionIntravenousActavis Pharma CompanyNot applicableNot applicableCanada flag
EloxatinPowder, for solution100 mg/1IntravenousSanofi Aventis2002-08-092009-04-30US flag
EloxatinInjection, solution, concentrate5 mg/1mLIntravenoussanofi-aventis U.S. LLC2006-06-022018-12-01US flag
EloxatinPowder, for solution50 mgIntravenousSanofi Aventis2008-06-272016-08-03Canada flag
EloxatinSolution, concentrate200 mg/40mLIntravenoussanofi-aventis U.S. LLC2008-04-012008-04-01US flag
EloxatinInjection, solution, concentrate5 mg/1mLIntravenousRecipharm HC Limited2009-07-222009-07-22US flag
EloxatinPowder, for solution50 mg/1IntravenousSanofi Aventis2002-08-092008-11-30US flag
EloxatinInjection, solution, concentrate5 mg/1mLIntravenoussanofi-aventis U.S. LLC2006-06-022018-10-30US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
OxaliplatinInjection, solution5 mg/1mLIntravenousSandoz Inc2015-03-01Not applicableUS flag
OxaliplatinInjection5 mg/1mLIntravenousBlue Point Laboratories2018-02-09Not applicableUS flag
OxaliplatinPowder, for solution50 mg/10mLIntravenousPfizer Laboratories Div Pfizer Inc.2012-08-092016-12-31US flag
OxaliplatinInjection, solution5 mg/1mLIntravenousNorthStar Rx LLC2019-06-17Not applicableUS flag
OxaliplatinInjection, powder, lyophilized, for solution50 mg/10mLIntravenousSun Pharmaceutical Industries, Inc.2009-08-19Not applicableUS flag
OxaliplatinInjection, powder, lyophilized, for solution100 mg/20mLIntravenousBreckenridge Pharmaceutical, Inc.2017-09-012020-10-31US flag
OxaliplatinInjection, solution100 mg/20mLIntravenousIngenus Pharmaceuticals, LLC2018-10-29Not applicableUS flag
OxaliplatinInjection, solution5 mg/1mLIntravenousSagent Pharmaceuticals2014-09-15Not applicableUS flag
OxaliplatinInjection, solution5 mg/1mLIntravenousBaxter Healthcare Corporation2018-02-19Not applicableUS flag
OxaliplatinInjection, solution5 mg/1mLIntravenousFosun Pharma USA Inc.2020-03-30Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more

Categories

ATC Codes
L01XA03 — Oxaliplatin
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as cyclohexylamines. These are organic compounds containing a cyclohexylamine moiety, which consist of a cyclohexane ring attached to an amine group.
Kingdom
Organic compounds
Super Class
Organic nitrogen compounds
Class
Organonitrogen compounds
Sub Class
Cyclohexylamines
Direct Parent
Cyclohexylamines
Alternative Parents
Dicarboxylic acids and derivatives / Organic transition metal salts / Carboxylic acids / Organopnictogen compounds / Organic oxides / Monoalkylamines / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Aliphatic homomonocyclic compound / Amine / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Cyclohexylamine / Dicarboxylic acid or derivatives / Hydrocarbon derivative / Organic oxide / Organic oxygen compound
Molecular Framework
Not Available
External Descriptors
platinum coordination entity (CHEBI:31941)

Chemical Identifiers

UNII
04ZR38536J
CAS number
61825-94-3
InChI Key
ZROHGHOFXNOHSO-BNTLRKBRSA-L
InChI
InChI=1S/C6H14N2.C2H2O4.Pt/c7-5-3-1-2-4-6(5)8;3-1(4)2(5)6;/h5-6H,1-4,7-8H2;(H,3,4)(H,5,6);/q;;+2/p-2/t5-,6-;;/m1../s1
IUPAC Name
(3aR,7aR)-octahydro-2',5'-dioxaspiro[cyclohexa[d]1,3-diaza-2-platinacyclopentane-2,1'-cyclopentane]-3',4'-dione
SMILES
[H][N]1([H])[[email protected]@H]2CCCC[[email protected]]2[N]([H])([H])[Pt]11OC(=O)C(=O)O1

References

Synthesis Reference

Masazumi Eriguchi, "Liposome preparations containing oxaliplatin." U.S. Patent US20040022842, issued February 05, 2004.

US20040022842
General References
  1. Pasetto LM, D'Andrea MR, Rossi E, Monfardini S: Oxaliplatin-related neurotoxicity: how and why? Crit Rev Oncol Hematol. 2006 Aug;59(2):159-68. Epub 2006 Jun 27. [PubMed:16806962]
  2. Graham J, Mushin M, Kirkpatrick P: Oxaliplatin. Nat Rev Drug Discov. 2004 Jan;3(1):11-2. [PubMed:14756144]
KEGG Drug
D01790
PubChem Compound
6857599
PubChem Substance
46509083
ChemSpider
8062727
RxNav
32592
ChEBI
31941
ChEMBL
CHEMBL414804
Therapeutic Targets Database
DAP000062
PharmGKB
PA131285527
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Oxaliplatin
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
FDA label
Download (2.35 MB)
MSDS
Download (38.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingHealth Services ResearchMalignant Neoplasm of Colon / Unresectable Metastasis Originating in Colonic Cancer1
4CompletedTreatmentColonic Neoplasms1
4CompletedTreatmentColorectal Cancers4
4CompletedTreatmentColorectal Cancers / Cytokine-Induced Killer Cells / Postoperative Complications / Survival1
4CompletedTreatmentNeoplasms, Colorectal1
4CompletedTreatmentStage-Ⅱ Colorectal Cancer1
4RecruitingTreatmentAdenocarcinoma Of Esophagus / Gastric Adenocarcinoma / Stage IIB Gastric Cancer / Stage IIIA Esophageal Adenocarcinoma / Stage IIIA Gastric Cancer / Stage IIIB Esophageal Adenocarcinoma / Stage IIIB Gastric Cancer / Stage IIIC Esophageal Adenocarcinoma / Stage IIIC Gastric Cancer1
4TerminatedTreatmentColorectal Cancers1
4Unknown StatusTreatmentAdvanced Adult Primary Liver Cancer1
4Unknown StatusTreatmentColon Cancer Liver Metastasis1

Pharmacoeconomics

Manufacturers
  • Sanofi aventis us llc
  • App pharmaceuticals llc
  • Ebewe pharma ges mbh nfg kg
  • Fresenius kabi oncology plc
  • Hospira inc
  • Hospira worldwide pty
  • Sun pharma global inc
  • Teva parenteral medicines inc
Packagers
  • APP Pharmaceuticals
  • Ben Venue Laboratories Inc.
  • Ebewe Pharma
  • Hospira Inc.
  • Sanofi-Aventis Inc.
  • Sun Pharmaceutical Industries Ltd.
  • Teva Pharmaceutical Industries Ltd.
Dosage Forms
FormRouteStrength
Injection, solution, concentrateIntravenous200 mg/40ml
Injection, powder, for solutionIntravenous100 mg
Injection, powder, for solutionIntravenous50 mg
Injection, solution, concentrateIntravenous5 mg/ml
InjectionIntravenous
Powder, for solution5 MG/ML
Powder, for solutionIntravenous100 mg/1
Powder, for solutionIntravenous100 mg
Powder, for solutionIntravenous50 mg
Powder, for solutionIntravenous50 mg/1
Solution, concentrateIntravenous200 mg/40mL
Solution, concentrateIntravenous50 mg
InjectionIntravenous200 mg/40ml
Powder
Injection, solution, concentrateIntravenous150 mg/30ml
SolutionIntravenous50 mg/10ml
Injection, solution
Injection
InjectionIntravenous100 mg/20mL
InjectionIntravenous5 mg/1mL
InjectionIntravenous50 mg/10mL
Injection, powder, lyophilized, for solutionIntravenous100 mg/20mL
Injection, powder, lyophilized, for solutionIntravenous5 mg/1mL
Injection, powder, lyophilized, for solutionIntravenous50 mg/10mL
Injection, solutionIntravenous100 mg/20mL
Injection, solutionIntravenous100 mg/1mL
Injection, solutionIntravenous200 mg/40mL
Injection, solutionIntravenous5 mg/1mL
Injection, solutionIntravenous50 mg/10mL
Injection, solutionIntravenous50 mg/1mL
Injection, solution, concentrateIntravenous
Injection, solution, concentrateIntravenous100 mg/20mL
Injection, solution, concentrateIntravenous5 mg/1mL
Injection, solution, concentrateIntravenous50 mg/10mL
Powder, for solutionIntravenous100 mg/20mL
Powder, for solutionIntravenous50 mg/10mL
SolutionIntravenous5 mg
Injection, powder, for solutionParenteral5 mg/ml
Powder, for solutionIntravenous
SolutionIntravenous
Injection, powder, for solution
Injection, powder, lyophilized, for solutionIntravenous100 mg
Injection, solution, concentrateIntravenous; Parenteral5 MG/ML
SolutionIntravenous100 mg
Injection, powder, lyophilized, for solutionIntravenous50 mg
Injection, powder, for solutionIntravenous150 mg
Solution
InjectionIntravenous50 mg
InjectionIntravenous100 mg
Injection, solution, concentrateIntravenous100 mg/50mL
Injection, solution, concentrateIntravenous50 mg/25mL
Injection, powder, lyophilized, for solutionIntravenous200 mg
SolutionIntravenous100 mg/20ml
SolutionIntravenous200 mg/40ml
Prices
Unit descriptionCostUnit
Oxaliplatin 100 mg vial1650.0USD vial
Oxaliplatin 50 mg vial825.0USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5290961No1994-03-012013-01-12US flag
CA2196922No2004-06-012015-08-07Canada flag
US5420319Yes1995-05-302017-02-09US flag
US5716988Yes1998-02-102016-02-07US flag
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility27.5 mg/mLALOGPS
logP-0.47ALOGPS
logS-1.2ALOGPS
Physiological Charge0ChemAxon
Hydrogen Acceptor Count0ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area85.82 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity67.52 m3·mol-1ChemAxon
Polarizability21.9 Å3ChemAxon
Number of Rings3ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.8638
Blood Brain Barrier+0.7667
Caco-2 permeable-0.6453
P-glycoprotein substrateSubstrate0.5056
P-glycoprotein inhibitor INon-inhibitor0.9332
P-glycoprotein inhibitor IINon-inhibitor1.0
Renal organic cation transporterNon-inhibitor0.9289
CYP450 2C9 substrateNon-substrate0.8846
CYP450 2D6 substrateNon-substrate0.8094
CYP450 3A4 substrateNon-substrate0.6064
CYP450 1A2 substrateNon-inhibitor0.8403
CYP450 2C9 inhibitorNon-inhibitor0.8686
CYP450 2D6 inhibitorNon-inhibitor0.8997
CYP450 2C19 inhibitorNon-inhibitor0.8189
CYP450 3A4 inhibitorNon-inhibitor0.8337
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9872
Ames testNon AMES toxic0.6034
CarcinogenicityNon-carcinogens0.938
BiodegradationNot ready biodegradable0.9796
Rat acute toxicity2.3765 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8879
hERG inhibition (predictor II)Non-inhibitor0.938
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Nucleotide
Organism
Humans
Pharmacological action
Yes
Actions
Cross-linking/alkylation
DNA is the molecule of heredity, as it is responsible for the genetic propagation of most inherited traits. It is a polynucleic acid that carries genetic information on cell growth, division, and function. DNA consists of two long strands of nucleotides twisted into a double helix and held together by hydrogen bonds. The sequence of nucleotides determines hereditary characteristics. Each strand serves as the template for subsequent DNA replication and as a template for mRNA production, leading to protein synthesis via ribosomes.
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Sharma S, Gong P, Temple B, Bhattacharyya D, Dokholyan NV, Chaney SG: Molecular dynamic simulations of cisplatin- and oxaliplatin-d(GG) intrastand cross-links reveal differences in their conformational dynamics. J Mol Biol. 2007 Nov 9;373(5):1123-40. Epub 2007 Aug 23. [PubMed:17900616]
  4. Zhu G, Chang P, Lippard SJ: Recognition of platinum-DNA damage by poly(ADP-ribose) polymerase-1. Biochemistry. 2010 Jul 27;49(29):6177-83. doi: 10.1021/bi100775t. [PubMed:20550106]
  5. Ramachandran S, Temple BR, Chaney SG, Dokholyan NV: Structural basis for the sequence-dependent effects of platinum-DNA adducts. Nucleic Acids Res. 2009 May;37(8):2434-48. doi: 10.1093/nar/gkp029. Epub 2009 Mar 2. [PubMed:19255091]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Glutathione transferase activity
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Acts on 1,2-epoxy-3-(4-nitrophenoxy)propane, phenethylisothiocyanate 4-nitrobenzyl chlorid...
Gene Name
GSTT1
Uniprot ID
P30711
Uniprot Name
Glutathione S-transferase theta-1
Molecular Weight
27334.755 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Metallothioneins have a high content of cysteine residues that bind various heavy metals; these proteins are transcriptionally regulated by both heavy metals and glucocorticoids.
Gene Name
MT1A
Uniprot ID
P04731
Uniprot Name
Metallothionein-1A
Molecular Weight
6120.19 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Metallothioneins have a high content of cysteine residues that bind various heavy metals; these proteins are transcriptionally regulated by both heavy metals and glucocorticoids.
Gene Name
MT2A
Uniprot ID
P02795
Uniprot Name
Metallothionein-2
Molecular Weight
6042.05 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Peroxidase activity
Specific Function
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production o...
Gene Name
MPO
Uniprot ID
P05164
Uniprot Name
Myeloperoxidase
Molecular Weight
83867.71 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Zinc ion binding
Specific Function
Destroys radicals which are normally produced within the cells and which are toxic to biological systems.
Gene Name
SOD1
Uniprot ID
P00441
Uniprot Name
Superoxide dismutase [Cu-Zn]
Molecular Weight
15935.685 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
S-nitrosoglutathione binding
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles. Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration.
Gene Name
GSTP1
Uniprot ID
P09211
Uniprot Name
Glutathione S-transferase P
Molecular Weight
23355.625 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein homodimerization activity
Specific Function
Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
Gene Name
GSTM1
Uniprot ID
P09488
Uniprot Name
Glutathione S-transferase Mu 1
Molecular Weight
25711.555 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Superoxide dismutase activity
Specific Function
The enzyme apparently serves as a quinone reductase in connection with conjugation reactions of hydroquinons involved in detoxification pathways as well as in biosynthetic processes such as the vit...
Gene Name
NQO1
Uniprot ID
P15559
Uniprot Name
NAD(P)H dehydrogenase [quinone] 1
Molecular Weight
30867.405 Da
References
  1. Link [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Burger H, Zoumaro-Djayoon A, Boersma AW, Helleman J, Berns EM, Mathijssen RH, Loos WJ, Wiemer EA: Differential transport of platinum compounds by the human organic cation transporter hOCT2 (hSLC22A2). Br J Pharmacol. 2010 Feb;159(4):898-908. doi: 10.1111/j.1476-5381.2009.00569.x. Epub 2010 Jan 8. [PubMed:20067471]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper uptake transmembrane transporter activity
Specific Function
High-affinity, saturable copper transporter involved in dietary copper uptake.
Gene Name
SLC31A1
Uniprot ID
O15431
Uniprot Name
High affinity copper uptake protein 1
Molecular Weight
21090.545 Da
References
  1. Howell SB, Safaei R, Larson CA, Sailor MJ: Copper transporters and the cellular pharmacology of the platinum-containing cancer drugs. Mol Pharmacol. 2010 Jun;77(6):887-94. doi: 10.1124/mol.109.063172. Epub 2010 Feb 16. [PubMed:20159940]
  2. Song IS, Savaraj N, Siddik ZH, Liu P, Wei Y, Wu CJ, Kuo MT: Role of human copper transporter Ctr1 in the transport of platinum-based antitumor agents in cisplatin-sensitive and cisplatin-resistant cells. Mol Cancer Ther. 2004 Dec;3(12):1543-9. [PubMed:15634647]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Yokoo S, Masuda S, Yonezawa A, Terada T, Katsura T, Inui K: Significance of organic cation transporter 3 (SLC22A3) expression for the cytotoxic effect of oxaliplatin in colorectal cancer. Drug Metab Dispos. 2008 Nov;36(11):2299-306. doi: 10.1124/dmd.108.023168. Epub 2008 Aug 18. [PubMed:18710896]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Ceckova M, Vackova Z, Radilova H, Libra A, Buncek M, Staud F: Effect of ABCG2 on cytotoxicity of platinum drugs: interference of EGFP. Toxicol In Vitro. 2008 Dec;22(8):1846-52. doi: 10.1016/j.tiv.2008.09.001. Epub 2008 Sep 9. [PubMed:18801423]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Organic anion transmembrane transporter activity
Specific Function
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name
ABCC2
Uniprot ID
Q92887
Uniprot Name
Canalicular multispecific organic anion transporter 1
Molecular Weight
174205.64 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Copper-exporting atpase activity
Specific Function
Involved in the export of copper out of the cells, such as the efflux of hepatic copper into the bile.
Gene Name
ATP7B
Uniprot ID
P35670
Uniprot Name
Copper-transporting ATPase 2
Molecular Weight
157261.34 Da
References
  1. Link [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Superoxide dismutase copper chaperone activity
Specific Function
May supply copper to copper-requiring proteins within the secretory pathway, when localized in the trans-Golgi network. Under conditions of elevated extracellular copper, it relocalized to the plas...
Gene Name
ATP7A
Uniprot ID
Q04656
Uniprot Name
Copper-transporting ATPase 1
Molecular Weight
163372.275 Da
References
  1. Link [Link]

Drug created on June 13, 2005 07:24 / Updated on October 23, 2020 21:53

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