Identification
- Summary
Oxaliplatin is a platinum based chemotherapy agent used to treat carcinoma of the colon or rectum or stage III colon cancer.
- Generic Name
- Oxaliplatin
- DrugBank Accession Number
- DB00526
- Background
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
Structure for Oxaliplatin (DB00526)
- 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.
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
- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- 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.
Target Actions Organism ADNA cross-linking/alkylationHumans - 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
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- 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.
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The risk or severity of adverse effects can be increased when Oxaliplatin is combined with Abatacept. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Oxaliplatin. Abemaciclib Abemaciclib may decrease the excretion rate of Oxaliplatin which could result in a higher serum level. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Oxaliplatin. Acetylsalicylic acid The risk or severity of bleeding can be increased when Acetylsalicylic acid is combined with Oxaliplatin. Acrivastine The risk or severity of QTc prolongation can be increased when Acrivastine is combined with Oxaliplatin. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Oxaliplatin. Adenosine The risk or severity of QTc prolongation can be increased when Oxaliplatin is combined with Adenosine. Adenovirus type 7 vaccine live The risk or severity of infection can be increased when Adenovirus type 7 vaccine live is combined with Oxaliplatin. Afatinib Afatinib may decrease the excretion rate of Oxaliplatin which could result in a higher serum level. 
Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - Food Interactions
- No interactions found.
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 Act Oxaliplatin Powder, for solution 50 mg / vial Intravenous Actavis Pharma Company Not applicable Not applicable Canada 
Act Oxaliplatin Powder, for solution 100 mg / vial Intravenous Actavis Pharma Company Not applicable Not applicable Canada Act Oxaliplatin Solution 5 mg / mL Intravenous Actavis Pharma Company 2015-12-16 2018-07-09 Canada Eloxatin Injection, solution, concentrate 5 mg/1mL Intravenous sanofi-aventis U.S. LLC 2006-06-02 2018-10-30 US 
Eloxatin Powder, for solution 50 mg / vial Intravenous Sanofi Aventis 2008-06-27 2016-08-03 Canada Eloxatin Powder, for solution 50 mg/1 Intravenous Sanofi Aventis 2002-08-09 2008-11-30 US Eloxatin Injection, solution, concentrate 5 mg/1mL Intravenous sanofi-aventis U.S. LLC 2006-06-02 2018-12-01 US Eloxatin Solution 5 mg / mL Intravenous Sanofi Aventis 2007-07-17 2018-11-09 Canada Eloxatin Powder, for solution 100 mg/1 Intravenous Sanofi Aventis 2002-08-09 2009-04-30 US Eloxatin Solution, concentrate 200 mg/40mL Intravenous sanofi-aventis U.S. LLC 2008-04-01 2008-04-01 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Oxaliplatin Injection, solution 5 mg/1mL Intravenous Sanja Pharmaceuticals Company 2017-09-21 Not applicable US Oxaliplatin Injection, solution, concentrate 5 mg/1mL Intravenous Fresenius Kabi USA, LLC 2010-06-11 Not applicable US Oxaliplatin Injection, solution 5 mg/1mL Intravenous AuroMedics Pharma LLC 2017-09-21 Not applicable US Oxaliplatin Injection, solution, concentrate 5 mg/1mL Intravenous Winthrop U.S. 2015-09-01 Not applicable US Oxaliplatin Injection, solution 5 mg/1mL Intravenous Pfizer Laboratories Div Pfizer Inc. 2012-08-09 2016-12-31 US Oxaliplatin Injection, solution 50 mg/10mL Intravenous Breckenridge Pharmaceutical, Inc. 2017-02-20 2019-05-31 US Oxaliplatin Injection, powder, lyophilized, for solution 5 mg/1mL Intravenous Actavis Pharma, Inc. 2015-01-05 Not applicable US Oxaliplatin Injection, powder, lyophilized, for solution 100 mg/20mL Intravenous Breckenridge Pharmaceutical, Inc. 2017-09-01 2020-10-31 US Oxaliplatin Injection, powder, lyophilized, for solution 5 mg/1mL Intravenous Hospira, Inc. 2009-09-30 2009-10-01 US Oxaliplatin Injection, solution 5 mg/1mL Intravenous Meitheal Pharmaceuticals Inc. 2017-10-01 Not applicable US
Categories
- ATC Codes
- L01XA03 — Oxaliplatin
- Drug Categories
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- BCRP/ABCG2 Substrates
- Coordination Complexes
- Immunosuppressive Agents
- Moderate Risk QTc-Prolonging Agents
- Myelosuppressive Agents
- Narrow Therapeutic Index Drugs
- OCT2 Substrates
- OCT2 Substrates with a Narrow Therapeutic Index
- Platinum Compounds
- QTc Prolonging Agents
- 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)
- Affected organisms
- Humans and other mammals
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])[C@@H]2CCCC[C@H]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
- External Links
- KEGG Drug
- D01790
- PubChem Compound
- 6857599
- PubChem Substance
- 46509083
- ChemSpider
- 8062727
- 32592
- ChEBI
- 31941
- ChEMBL
- CHEMBL414804
- Therapeutic Targets Database
- DAP000062
- PharmGKB
- PA131285527
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Oxaliplatin
- FDA label
- Download (2.35 MB)
- MSDS
- Download (38.4 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Colon Neoplasm 1 4 Completed Treatment Colorectal Cancer 4 4 Completed Treatment Colorectal Cancer / Cytokine-Induced Killer Cells / Postoperative Complications / Survival 1 4 Completed Treatment Colorectal Neoplasms 1 4 Completed Treatment Stage-Ⅱ Colorectal Cancer 1 4 Recruiting Treatment Esophagus Adenocarcinoma / 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 Cancer 1 4 Terminated Health Services Research Colon Cancer / Unresectable Metastasis Originating in Colonic Cancer 1 4 Terminated Treatment Colorectal Cancer 1 4 Unknown Status Treatment Advanced Adult Primary Liver Cancer 1 4 Unknown Status Treatment Cancer 1
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
Form Route Strength Solution, concentrate Intravenous 5 mg Injection, powder, for solution Injection, powder, lyophilized, for solution Injection, solution, concentrate Intravenous 200 mg/40ml Injection, powder, for solution 100 mg Injection, powder, for solution 50 mg Injection, solution, concentrate Intravenous Powder, for solution Intravenous 100 mg/1 Powder, for solution Intravenous 5 MG/ML Powder, for solution Intravenous 50 mg/1 Solution Intravenous 5 mg / mL Solution, concentrate Intravenous 200 mg/40mL Solution, concentrate Intravenous 50 mg Injection Intravenous 200 mg/40ml Solution, concentrate Intravenous 100 mg Injection, powder, lyophilized, for solution Intravenous 100 mg Solution Intravenous 100 mg Injection, solution, concentrate Intravenous 150 mg/30ml Solution Intravenous 50 mg/10ml Injection, powder, lyophilized, for solution Parenteral 50 mg Injection, solution Intravenous Solution Intravenous 5 mg Injection Intravenous 100 mg/20mL Injection Intravenous 5 mg/1mL Injection Intravenous 50 mg/10mL Injection, powder, lyophilized, for solution Intravenous 100 mg/20mL Injection, powder, lyophilized, for solution Intravenous 5 mg/1mL Injection, powder, lyophilized, for solution Intravenous 50 mg/10mL Injection, solution Intravenous 100 mg/20mL Injection, solution Intravenous 100 mg/1mL Injection, solution Intravenous 200 mg/40mL Injection, solution Intravenous 5 mg/1mL Injection, solution Intravenous 50 mg/10mL Injection, solution Intravenous 50 mg/1mL Injection, solution, concentrate Intravenous 100 mg/20mL Injection, solution, concentrate Intravenous 5 mg/1mL Injection, solution, concentrate Intravenous 50 mg/10mL Injection; injection, solution, concentrate Intravenous 5 mg/ml Powder, for solution Intravenous 100 mg/20mL Powder, for solution Intravenous 50 mg/10mL Injection, powder, for solution Parenteral Powder, for solution Intravenous 100 mg / vial Powder, for solution Intravenous 50 mg / vial Injection, solution, concentrate Intravenous 5 mg/ml Injection, solution Intravenous 5 mg/ml Solution Intravenous 200 mg Injection, powder, for solution Intravenous Powder 100 mg/1vial Solution Intravenous 5 mg/ml Injection, powder, lyophilized, for solution Intravenous 5 mg/ml Injection, powder, for solution Intravenous 50 mg Solution Intravenous 50 mg Powder, for solution Intravenous Injection, solution, concentrate Intravenous; Parenteral 5 MG/ML Injection, powder, for solution Intravenous Injection Intravenous 100 MG Injection Intravenous 50 MG Injection, solution Intravenous 2 MG/ML Injection Intravenous 5 mg/ml Injection, powder, lyophilized, for solution Intravenous 200 mg Solution Intravenous 100 mg/20ml Solution Intravenous 200 mg/40ml Injection Intravenous Injection, powder, lyophilized, for solution Intravenous 100.00 mg Injection, powder, lyophilized, for solution Intravenous 50.00 mg Injection, powder, lyophilized, for solution Intravenous 50 mg Solution Intravenous 2 mg/1ml Solution Intravenous 5 mg/1ml Powder 50 mg/1vial Injection, powder, for solution 100 mg/1vial Injection, powder, for solution 50 mg/1vial Injection, solution Intravenous 2 mg/1ml - Prices
Unit description Cost Unit Oxaliplatin 100 mg vial 1650.0USD vial Oxaliplatin 50 mg vial 825.0USD vial DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5290961 No 1994-03-01 2013-01-12 US CA2196922 No 2004-06-01 2015-08-07 Canada US5420319 Yes 1995-05-30 2017-02-09 US US5716988 Yes 1998-02-10 2016-02-07 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 27.5 mg/mL ALOGPS logP -0.47 ALOGPS logS -1.2 ALOGPS Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 0 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 85.82 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 67.52 m3·mol-1 Chemaxon Polarizability 21.9 Å3 Chemaxon Number of Rings 3 Chemaxon Bioavailability 1 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.8638 Blood Brain Barrier + 0.7667 Caco-2 permeable - 0.6453 P-glycoprotein substrate Substrate 0.5056 P-glycoprotein inhibitor I Non-inhibitor 0.9332 P-glycoprotein inhibitor II Non-inhibitor 1.0 Renal organic cation transporter Non-inhibitor 0.9289 CYP450 2C9 substrate Non-substrate 0.8846 CYP450 2D6 substrate Non-substrate 0.8094 CYP450 3A4 substrate Non-substrate 0.6064 CYP450 1A2 substrate Non-inhibitor 0.8403 CYP450 2C9 inhibitor Non-inhibitor 0.8686 CYP450 2D6 inhibitor Non-inhibitor 0.8997 CYP450 2C19 inhibitor Non-inhibitor 0.8189 CYP450 3A4 inhibitor Non-inhibitor 0.8337 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9872 Ames test Non AMES toxic 0.6034 Carcinogenicity Non-carcinogens 0.938 Biodegradation Not ready biodegradable 0.9796 Rat acute toxicity 2.3765 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.8879 hERG inhibition (predictor II) Non-inhibitor 0.938
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets
Build, predict & validate machine-learning models
Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
Yes
Cross-linking/alkylation
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- 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. [Article]
- 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
- 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. [Article]
- 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. [Article]
- 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
- 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. [Article]
- 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
- 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. [Article]
- 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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [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
- PharmGKB: Platinum Pathway, Pharmacokinetics/Pharmacodynamics [Link]
Drug created at June 13, 2005 13:24 / Updated at June 02, 2023 16:39