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Identification
NameCarboplatin
Accession NumberDB00958  (APRD00466)
TypeSmall Molecule
GroupsApproved
DescriptionAn organoplatinum compound that possesses antineoplastic activity. [PubChem]
Structure
Thumb
Synonyms
Carboplatin
CBDCA
cis-(1,1-Cyclobutanedicarboxylato)diammineplatinum(ii)
cis-Diammine(1,1-cyclobutanedicarboxylato)platinum
cis-Diammine(1,1-cyclobutanedicarboxylato)platinum(II)
Paraplatin
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Carboplatin InjectionLiquid10 mgIntravenousTeva Canada Limited1994-12-31Not applicableCanada
Carboplatin InjectionSolution10 mgIntravenousAccord Healthcare Inc2015-03-11Not applicableCanada
Carboplatin InjectionSolution10 mgIntravenousOmega Laboratories Ltd2013-06-10Not applicableCanada
Carboplatin Injection BPSolution10 mgIntravenousHospira Healthcare Corporation1997-07-30Not applicableCanada
Carboplatin Injection Liq 10mg/mlLiquid10 mgIntravenousDavid Bull Laboratories (Pty) Ltd.1992-12-311998-08-13Canada
Carboplatin Injection, BPSolution10 mgIntravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Paraplatin Inj 150mg/vialPowder, for solution150 mgIntravenousBristol Labs Division Of Bristol Myers Squibb1986-12-311996-09-09Canada
Paraplatin-AQ Inj 10mg/mlLiquid10 mgIntravenousBristol Myers Squibb Canada1989-12-312007-07-30Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CarboplatinInjection, solution10 mg/mLIntravenousSandoz Inc2010-01-31Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousTeva Parenteral Medicines, Inc.2006-05-01Not applicableUs
CarboplatinInjection10 mg/mLIntravenousTeva Parenteral Medicines, Inc.2005-11-172016-03-31Us
CarboplatinInjection10 mg/mLIntravenousMylan Institutional LLC2011-11-09Not applicableUs
CarboplatinSolution50 mg/5mLIntravenousSanja Pharmaceuticals Company2016-09-29Not applicableUs
CarboplatinInjection10 mg/mLIntravenousSun Pharma Global FZE2008-09-19Not applicableUs
CarboplatinInjection10 mg/mLIntravenousMylan Institutional LLC2011-11-09Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousTeva Parenteral Medicines, Inc.2006-02-01Not applicableUs
CarboplatinInjection10 mg/mLIntravenousSun Pharma Global FZE2008-09-19Not applicableUs
CarboplatinInjection10 mg/mLIntravenousMylan Institutional LLC2011-11-09Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousHospira Worldwide, Inc.2004-10-142016-10-13Us
CarboplatinSolution150 mg/5mLIntravenousSanja Pharmaceuticals Company2016-09-29Not applicableUs
CarboplatinInjection10 mg/mLIntravenousMylan Institutional LLC2011-11-09Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousSagent Pharmaceuticals2013-10-31Not applicableUs
CarboplatinInjection10 mg/mLIntravenousSun Pharma Global FZE2008-09-19Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousTeva Parenteral Medicines, Inc.2014-07-31Not applicableUs
CarboplatinSolution450 mg/5mLIntravenousSanja Pharmaceuticals Company2016-09-29Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousAPP Pharmaceuticals, LLC2009-09-15Not applicableUs
CarboplatinInjection10 mg/mLIntravenousMylan Institutional LLC2011-11-09Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousHospira, Inc.2004-10-14Not applicableUs
CarboplatinInjection10 mg/mLIntravenousSun Pharma Global FZE2014-03-03Not applicableUs
CarboplatinInjection, solution10 mg/mLIntravenousTeva Parenteral Medicines, Inc.2006-05-04Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ParaplatinNot Available
Paraplatin-AQNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIBG3F62OND5
CAS number41575-94-4
WeightAverage: 371.254
Monoisotopic: 371.044481331
Chemical FormulaC6H12N2O4Pt
InChI KeyOLESAACUTLOWQZ-UHFFFAOYSA-L
InChI
InChI=1S/C6H8O4.2H3N.Pt/c7-4(8)6(5(9)10)2-1-3-6;;;/h1-3H2,(H,7,8)(H,9,10);2*1H3;/q;;;+2/p-2
IUPAC Name
6,8-dioxa-7-platinaspiro[3.5]nonane-5,9-dione diamine
SMILES
N.N.O=C1O[Pt]OC(=O)C11CCC1
Pharmacology
IndicationFor the initial treatment of advanced ovarian carcinoma in established combination with other approved chemotherapeutic agents. One established combination regimen consists of PARAPLATIN and cyclophosphamide. It is also indicated for the palliative treatment of patients with ovarian carcinoma recurrent after prior chemotherapy, including patients who have been previously treated with cisplatin.
Structured Indications
PharmacodynamicsCarboplatin is an antineoplastic in the class of alkylating agents and is used to treat various forms of cancer. Alkylating agents are so named because of their ability to add alkyl groups to many electronegative groups under conditions present in cells. They stop tumor growth by cross-linking guanine bases in DNA double-helix strands - directly attacking DNA. This makes the strands unable to uncoil and separate. As this is necessary in DNA replication, the cells can no longer divide. In addition, these drugs add methyl or other alkyl groups onto molecules where they do not belong which in turn inhibits their correct utilization by base pairing and causes a miscoding of DNA. Alkylating agents are cell cycle-nonspecific. Alkylating agents work by three different mechanisms all of which achieve the same end result - disruption of DNA function and cell death.
Mechanism of actionAlkylating agents work by three different mechanisms: 1) attachment of alkyl groups to DNA bases, resulting in the DNA being fragmented by repair enzymes in their attempts to replace the alkylated bases, preventing DNA synthesis and RNA transcription from the affected DNA, 2) DNA damage via the formation of cross-links (bonds between atoms in the DNA) which prevents DNA from being separated for synthesis or transcription, and 3) the induction of mispairing of the nucleotides leading to mutations.
TargetKindPharmacological actionActionsOrganismUniProt ID
DNANucleotideyes
cross-linking/alkylation
Humannot applicabledetails
Related Articles
AbsorptionThe Cmax values and areas under the plasma concentration versus time curves from 0 to infinity (AUC inf) increase linearly with dose, although the increase was slightly more than dose proportional. Carboplatin exhibits linear pharmacokinetics.
Volume of distribution
  • 16 L [apparent volume of distribution, 30 minute IV infusion of 300 mg/m^2 to 500 mg/m^2]
Protein bindingCarboplatin is not bound to plasma protein. However, the platinum itself from carboplatin irreversibly binds to plasma proteins and is slowly eliminated with a minimum half-life of 5 days.
MetabolismNot Available
Route of eliminationThe major route of elimination of carboplatin is renal excretion. After 24 hours, all of the platinum is recovered in the urine as carboplatin. Whether biliary excretion occurs is not known.
Half lifeInitial plasma half-life (alpha) = 1.1 to 2 hours; Post distribution plasma half-life (beta) = 2.6 - 5.9 hours.
Clearance
  • 4.4 L/hour [total body clearance, 30 minute IV infusion of 300 mg/m^2 to 500 mg/m^2]
ToxicityToxic by ingestion. May be create toxic effect through inhalation or skin contact. May cause reproductive defects. May act as a sensitizer. ORL-RAT LD50 343 mg kg-1; SCN-RAT LD50 72 mg kg-1; IPN-MUS LD50 118 mg kg-1
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Carboplatin.Approved
AclarubicinAclarubicin may increase the ototoxic activities of Carboplatin.Investigational
ALT-110The risk or severity of adverse effects can be increased when Carboplatin is combined with ALT-110.Investigational
AmikacinAmikacin may increase the ototoxic activities of Carboplatin.Approved, Vet Approved
AmrubicinAmrubicin may increase the ototoxic activities of Carboplatin.Approved, Investigational
annamycinannamycin may increase the ototoxic activities of Carboplatin.Investigational
AnvirzelAnvirzel may decrease the cardiotoxic activities of Carboplatin.Investigational
ApramycinApramycin may increase the ototoxic activities of Carboplatin.Experimental, Vet Approved
ArbekacinArbekacin may increase the ototoxic activities of Carboplatin.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Carboplatin.Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Carboplatin.Approved, Investigational
BexaroteneThe serum concentration of Bexarotene can be increased when it is combined with Carboplatin.Approved, Investigational
CabazitaxelCarboplatin may increase the myelosuppressive activities of Cabazitaxel.Approved
CDX-110The risk or severity of adverse effects can be increased when Carboplatin is combined with CDX-110.Investigational
ClozapineThe risk or severity of adverse effects can be increased when Carboplatin is combined with Clozapine.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Carboplatin.Approved, Investigational
DaunorubicinDaunorubicin may increase the ototoxic activities of Carboplatin.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Carboplatin.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Carboplatin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Carboplatin.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Carboplatin.Approved
DihydrostreptomycinDihydrostreptomycin may increase the ototoxic activities of Carboplatin.Vet Approved
DocetaxelCarboplatin may increase the myelosuppressive activities of Docetaxel.Approved, Investigational
DoxorubicinDoxorubicin may increase the ototoxic activities of Carboplatin.Approved, Investigational
EltrombopagThe serum concentration of Carboplatin can be increased when it is combined with Eltrombopag.Approved
EpirubicinEpirubicin may increase the ototoxic activities of Carboplatin.Approved
FingolimodCarboplatin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FosphenytoinThe serum concentration of Fosphenytoin can be decreased when it is combined with Carboplatin.Approved
FramycetinFramycetin may increase the ototoxic activities of Carboplatin.Approved
G17DTThe risk or severity of adverse effects can be increased when Carboplatin is combined with G17DT.Investigational
GeneticinGeneticin may increase the ototoxic activities of Carboplatin.Experimental
GentamicinGentamicin may increase the ototoxic activities of Carboplatin.Approved, Vet Approved
GENTAMICIN C1AGENTAMICIN C1A may increase the ototoxic activities of Carboplatin.Experimental
GI-5005The risk or severity of adverse effects can be increased when Carboplatin is combined with GI-5005.Investigational
Hygromycin BHygromycin B may increase the ototoxic activities of Carboplatin.Vet Approved
IdarubicinIdarubicin may increase the ototoxic activities of Carboplatin.Approved
INGN 201The risk or severity of adverse effects can be increased when Carboplatin is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Carboplatin is combined with INGN 225.Investigational
INNO-206INNO-206 may increase the ototoxic activities of Carboplatin.Investigational
KanamycinKanamycin may increase the ototoxic activities of Carboplatin.Approved, Vet Approved
LeflunomideThe risk or severity of adverse effects can be increased when Carboplatin is combined with Leflunomide.Approved, Investigational
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Carboplatin.Withdrawn
MetrizamideMetrizamide may increase the ototoxic activities of Carboplatin.Approved
NatalizumabThe risk or severity of adverse effects can be increased when Carboplatin is combined with Natalizumab.Approved, Investigational
NeamineNeamine may increase the ototoxic activities of Carboplatin.Experimental
NeomycinNeomycin may increase the ototoxic activities of Carboplatin.Approved, Vet Approved
NetilmicinNetilmicin may increase the ototoxic activities of Carboplatin.Approved
OuabainOuabain may decrease the cardiotoxic activities of Carboplatin.Approved
PaclitaxelCarboplatin may increase the myelosuppressive activities of Paclitaxel.Approved, Vet Approved
ParomomycinParomomycin may increase the ototoxic activities of Carboplatin.Approved, Investigational
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Carboplatin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Carboplatin.Approved, Investigational
PirarubicinPirarubicin may increase the ototoxic activities of Carboplatin.Investigational
PlicamycinPlicamycin may increase the ototoxic activities of Carboplatin.Approved, Withdrawn
PuromycinPuromycin may increase the ototoxic activities of Carboplatin.Experimental
Rabies vaccineThe risk or severity of adverse effects can be increased when Carboplatin is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Carboplatin.Approved
RibostamycinRibostamycin may increase the ototoxic activities of Carboplatin.Approved
RoflumilastRoflumilast may increase the immunosuppressive activities of Carboplatin.Approved
RolapitantThe serum concentration of Carboplatin can be increased when it is combined with Rolapitant.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Carboplatin.Approved
SisomicinSisomicin may increase the ototoxic activities of Carboplatin.Investigational
SorafenibThe risk or severity of adverse effects can be increased when Sorafenib is combined with Carboplatin.Approved, Investigational
SP1049CSP1049C may increase the ototoxic activities of Carboplatin.Investigational
SpectinomycinSpectinomycin may increase the ototoxic activities of Carboplatin.Approved, Vet Approved
SRP 299The risk or severity of adverse effects can be increased when Carboplatin is combined with SRP 299.Investigational
StreptomycinStreptomycin may increase the ototoxic activities of Carboplatin.Approved, Vet Approved
StreptozocinStreptozocin may increase the ototoxic activities of Carboplatin.Approved
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Carboplatin.Approved, Investigational
TeriflunomideThe serum concentration of Carboplatin can be increased when it is combined with Teriflunomide.Approved
TG4010The risk or severity of adverse effects can be increased when Carboplatin is combined with TG4010.Investigational
TobramycinTobramycin may increase the ototoxic activities of Carboplatin.Approved, Investigational
TofacitinibCarboplatin may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TopotecanThe risk or severity of adverse effects can be increased when Carboplatin is combined with Topotecan.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Carboplatin.Approved, Investigational
ValrubicinValrubicin may increase the ototoxic activities of Carboplatin.Approved
ZorubicinZorubicin may increase the ototoxic activities of Carboplatin.Experimental
Food Interactions
  • Avoid echinacea as it may decrease effectiveness of immunosuppresants like carboplatin
References
Synthesis Reference

Jingzun Wang, Huisheng Qu, Lei Wang, Ting Wang, “Supermolecular carboplatin derivatives, their preparation and pharmaceutical composition containing them as active ingredient and applications of the compositions.” U.S. Patent US07259270, issued August 21, 2007.

US07259270
General References
  1. Natarajan G, Malathi R, Holler E: Increased DNA-binding activity of cis-1,1-cyclobutanedicarboxylatodiammineplatinum(II) (carboplatin) in the presence of nucleophiles and human breast cancer MCF-7 cell cytoplasmic extracts: activation theory revisited. Biochem Pharmacol. 1999 Nov 15;58(10):1625-9. [PubMed:10535754 ]
  2. Knox RJ, Friedlos F, Lydall DA, Roberts JJ: Mechanism of cytotoxicity of anticancer platinum drugs: evidence that cis-diamminedichloroplatinum(II) and cis-diammine-(1,1-cyclobutanedicarboxylato)platinum(II) differ only in the kinetics of their interaction with DNA. Cancer Res. 1986 Apr;46(4 Pt 2):1972-9. [PubMed:3512077 ]
  3. Canetta R, Rozencweig M, Carter SK: Carboplatin: the clinical spectrum to date. Cancer Treat Rev. 1985 Sep;12 Suppl A:125-36. [PubMed:3002623 ]
External Links
ATC CodesL01XA02
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (1.26 MB)
MSDSDownload (73.5 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption-0.6183
Blood Brain Barrier+0.8295
Caco-2 permeable-0.584
P-glycoprotein substrateNon-substrate0.6375
P-glycoprotein inhibitor INon-inhibitor0.9489
P-glycoprotein inhibitor IINon-inhibitor0.9968
Renal organic cation transporterNon-inhibitor0.9239
CYP450 2C9 substrateNon-substrate0.8745
CYP450 2D6 substrateNon-substrate0.8276
CYP450 3A4 substrateNon-substrate0.703
CYP450 1A2 substrateNon-inhibitor0.8142
CYP450 2C9 inhibitorNon-inhibitor0.854
CYP450 2D6 inhibitorNon-inhibitor0.9168
CYP450 2C19 inhibitorNon-inhibitor0.8607
CYP450 3A4 inhibitorNon-inhibitor0.6995
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9896
Ames testNon AMES toxic0.746
CarcinogenicityNon-carcinogens0.8906
BiodegradationReady biodegradable0.8235
Rat acute toxicity2.3469 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9596
hERG inhibition (predictor II)Non-inhibitor0.9767
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • App pharmaceuticals llc
  • Bedford laboratories div ben venue laboratories inc
  • Hospira inc
  • Pliva inc
  • Sandoz inc
  • Watson laboratories inc
  • Watson laboratories
  • Bristol myers squibb co pharmaceutical research institute
  • Akorn inc
  • Bedford laboratories
  • Bioniche pharma usa llc
  • Ebewe pharma ges mbh nfg kg
  • Fresenius kabi oncology plc
  • Pharmachemie bv
  • Pliva lachema as
  • Spectrum pharmaceuticals inc
  • Sun pharma global inc
  • Teva parenteral medicines inc
  • Bristol myers squibb co
Packagers
Dosage forms
FormRouteStrength
InjectionIntravenous10 mg/mL
Injection, solutionIntravenous10 mg/mL
SolutionIntravenous150 mg/5mL
SolutionIntravenous450 mg/5mL
SolutionIntravenous50 mg/5mL
LiquidIntravenous10 mg
SolutionIntravenous10 mg
Powder, for solutionIntravenous150 mg
Prices
Unit descriptionCostUnit
Paraplatin 450 mg vial1474.46USD vial
Paraplatin 150 mg vial491.48USD vial
Carboplatin 150 mg vial255.31USD vial
Paraplatin 50 mg vial163.84USD vial
Carboplatin 450 mg vial156.25USD vial
Carboplatin 50 mg vial85.1USD vial
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental PropertiesNot Available
Predicted Properties
PropertyValueSource
logP1.06ChemAxon
pKa (Strongest Basic)-6.6ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area52.6 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity29.01 m3·mol-1ChemAxon
Polarizability14.06 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as metalloheterocyclic compounds. These are heterocyclic compounds contain one metal ring atom.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassMetalloheterocyclic compounds
Sub ClassNot Available
Direct ParentMetalloheterocyclic compounds
Alternative Parents
Substituents
  • Oxacycle
  • Organic metal salt
  • Monocarboxylic acid or derivatives
  • Metalloheterocycle
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organic transition metal salt
  • Organooxygen compound
  • Carbonyl group
  • Amine
  • Aliphatic heteropolycyclic compound
Molecular FrameworkAliphatic heteropolycyclic compounds
External Descriptors

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
cross-linking/alkylation
General Function:
Used for biological information storage.
Specific Function:
DNA contains the instructions needed for an organism to develop, survive and reproduce.
Molecular Weight:
2.15 x 1012 Da
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. Appleton K, Mackay HJ, Judson I, Plumb JA, McCormick C, Strathdee G, Lee C, Barrett S, Reade S, Jadayel D, Tang A, Bellenger K, Mackay L, Setanoians A, Schatzlein A, Twelves C, Kaye SB, Brown R: Phase I and pharmacodynamic trial of the DNA methyltransferase inhibitor decitabine and carboplatin in solid tumors. J Clin Oncol. 2007 Oct 10;25(29):4603-9. [PubMed:17925555 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Xanthine oxidase activity
Specific Function:
Key enzyme in purine degradation. Catalyzes the oxidation of hypoxanthine to xanthine. Catalyzes the oxidation of xanthine to uric acid. Contributes to the generation of reactive oxygen species. Has also low oxidase activity towards aldehydes (in vitro).
Gene Name:
XDH
Uniprot ID:
P47989
Molecular Weight:
146422.99 Da
References
  1. Husai K, Jagannathan R, Hasan Z, Trammell GL, Rybak LP, Hazelrigg SR, Somani SM: Dose response of carboplatin-induced nephrotoxicity in rats. Pharmacol Toxicol. 2002 Aug;91(2):83-9. [PubMed:12420797 ]
  2. Husain K, Whitworth C, Rybak LP: Time response of carboplatin-induced nephrotoxicity in rats. Pharmacol Res. 2004 Sep;50(3):291-300. [PubMed:15225673 ]
  3. Husain K, Whitworth C, Somani SM, Rybak LP: Carboplatin-induced oxidative stress in rat cochlea. Hear Res. 2001 Sep;159(1-2):14-22. [PubMed:11520631 ]
  4. Husain K, Whitworth C, Hazelrigg S, Rybak L: Carboplatin-induced oxidative injury in rat inferior colliculus. Int J Toxicol. 2003 Sep-Oct;22(5):335-42. [PubMed:14555405 ]
Kind
Protein
Organism
Human
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 of hypohalous acids, primarily hypochlorous acid in physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity.
Gene Name:
MPO
Uniprot ID:
P05164
Molecular Weight:
83867.71 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
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 chloride and 4-nitrophenethyl bromide. Displays glutathione peroxidase activity with cumene hydroperoxide.
Gene Name:
GSTT1
Uniprot ID:
P30711
Molecular Weight:
27334.755 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
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
Molecular Weight:
6120.19 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
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
Molecular Weight:
6042.05 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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
Molecular Weight:
15935.685 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
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
Molecular Weight:
23355.625 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
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
Molecular Weight:
25711.555 Da
References
  1. Link [Link]
Kind
Protein
Organism
Human
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 vitamin K-dependent gamma-carboxylation of glutamate residues in prothrombin synthesis.
Gene Name:
NQO1
Uniprot ID:
P15559
Molecular Weight:
30867.405 Da
References
  1. Link [Link]

Transporters

Kind
Protein
Organism
Human
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
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
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Copper ion transmembrane transporter activity
Specific Function:
Involved in low-affinity copper uptake.
Gene Name:
SLC31A2
Uniprot ID:
O15432
Molecular Weight:
15681.29 Da
References
  1. Blair BG, Larson CA, Safaei R, Howell SB: Copper transporter 2 regulates the cellular accumulation and cytotoxicity of Cisplatin and Carboplatin. Clin Cancer Res. 2009 Jul 1;15(13):4312-21. doi: 10.1158/1078-0432.CCR-09-0311. Epub 2009 Jun 9. [PubMed:19509135 ]
Kind
Protein
Organism
Human
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 plasma membrane where it functions in the efflux of copper from cells.
Gene Name:
ATP7A
Uniprot ID:
Q04656
Molecular Weight:
163372.275 Da
References
  1. Samimi G, Katano K, Holzer AK, Safaei R, Howell SB: Modulation of the cellular pharmacology of cisplatin and its analogs by the copper exporters ATP7A and ATP7B. Mol Pharmacol. 2004 Jul;66(1):25-32. [PubMed:15213293 ]
Kind
Protein
Organism
Human
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
Molecular Weight:
157261.34 Da
References
  1. Samimi G, Katano K, Holzer AK, Safaei R, Howell SB: Modulation of the cellular pharmacology of cisplatin and its analogs by the copper exporters ATP7A and ATP7B. Mol Pharmacol. 2004 Jul;66(1):25-32. [PubMed:15213293 ]
Kind
Protein
Organism
Human
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 from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
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
Human
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
Molecular Weight:
174205.64 Da
References
  1. Link [Link]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23