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Identification
NameCisplatin
Accession NumberDB00515  (APRD00359)
TypeSmall Molecule
GroupsApproved
DescriptionCisplatin, cisplatinum or cis-diamminedichloroplatinum(II) (CDDP) is a platinum-based chemotherapy drug used to treat various types of cancers, including sarcomas, some carcinomas (e.g. small cell lung cancer, and ovarian cancer), lymphomas and germ cell tumors. It was the first member of its class, which now also includes carboplatin and oxaliplatin.
Structure
Thumb
Synonyms
CDDP
Cis-DDP
cis-diamminedichloroplatinum(II)
Platinol-AQ
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cisplatininjection, solution1 mg/mLintravenousWG Critical Care, LLC2012-01-13Not applicableUs
Cisplatininjection, solution1 mg/mLintravenousWG Critical Care, LLC2012-01-13Not applicableUs
Cisplatininjection, solution1 mg/mLintravenousWG Critical Care, LLC2015-04-15Not applicableUs
Cisplatin Inj 0.5mg/mlliquid.5 mgintravenousDavid Bull Laboratories (Pty) Ltd.1985-12-311996-09-10Canada
Cisplatin Inj 1mg/mlliquid1 mgintravenousDavid Bull Laboratories (Pty) Ltd.1986-12-311998-08-13Canada
Cisplatin Injectionsolution1.0 mgintravenousTeva Canada Limited2013-08-29Not applicableCanada
Cisplatin Injectionsolution1 mgintravenousFresenius Kabi Canada LtdNot applicableNot applicableCanada
Cisplatin Injectionsolution1 mgintravenousHospira Healthcare Corporation1997-05-09Not applicableCanada
Cisplatin Injectionsolution1 mgintravenousOmega Laboratories LtdNot applicableNot applicableCanada
Cisplatin Injection BPsolution1 mgintravenousSandoz Canada Incorporated2011-09-29Not applicableCanada
Cisplatin Injection, BPsolution1 mgintravenousAccord Healthcare Inc2012-04-10Not applicableCanada
Cisplatin Injection, Mylan Std.solution1 mgintravenousMylan Pharmaceuticals Ulc2013-06-122016-07-06Canada
Mylan-cisplatin Injectionsolution1 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Platinolinjection, powder, lyophilized, for solution1 mg/mLintravenousCorden Pharma Latina S.p.A.2012-01-13Not applicableUs
Platinol AQ Inj 1mg/mlliquid1 mgintravenousBristol Labs Division Of Bristol Myers Squibb1988-12-312001-07-30Canada
Platinol-AQinjection, solution1 mg/mLintravenousCorden Pharma Latina S.p.A.2012-01-13Not applicableUs
PMS-cisplatinsolution1 mgintravenousPharmascience IncNot applicableNot applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Cisplatininjection1 mg/mLintravenousAccord Healthcare, Inc.2016-03-01Not applicableUs
Cisplatininjection1 mg/mLintravenousPfizer Laboratories Div Pfizer Inc.2012-04-19Not applicableUs
Cisplatininjection, solution1 mg/mLintravenousFresenius Kabi USA, LLC2000-09-05Not applicableUs
Cisplatininjection1 mg/mLintravenousPfizer Laboratories Div Pfizer Inc.2012-04-19Not applicableUs
Cisplatininjection1 mg/mLintravenousMylan Institutional LLC2012-04-19Not applicableUs
Cisplatininjection, solution50 mg/50mLintravenousTeva Parenteral Medicines, Inc.2000-06-01Not applicableUs
Cisplatininjection1 mg/mLintravenousMylan Institutional LLC2012-04-19Not applicableUs
Cisplatininjection, solution100 mg/100mLintravenousTeva Parenteral Medicines, Inc.2000-06-01Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
AbiplatinNot Available
CisplatylNot Available
PlatidiamNot Available
PlatinCadila Healthcare
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIQ20Q21Q62J
CAS number15663-27-1
WeightAverage: 298.035
Monoisotopic: 296.939928001
Chemical FormulaCl2H4N2Pt
InChI KeyInChIKey=DQLATGHUWYMOKM-UHFFFAOYSA-L
InChI
InChI=1S/2ClH.2H2N.Pt/h2*1H;2*1H2;/q;;2*-1;+4/p-2
IUPAC Name
dichloroplatinumdiamine
SMILES
N[Pt](N)(Cl)Cl
Taxonomy
DescriptionThis compound belongs to the class of inorganic compounds known as transition metal chlorides. These are inorganic compounds in which the largest halogen atom is Chlorine, and the heaviest metal atom is a transition metal.
KingdomInorganic compounds
Super ClassMixed metal/non-metal compounds
ClassTransition metal salts
Sub ClassTransition metal chlorides
Direct ParentTransition metal chlorides
Alternative Parents
Substituents
  • Transition metal chloride
  • Inorganic chloride salt
  • Acyclic compound
Molecular FrameworkAcyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the treatment of metastatic testicular tumors, metastatic ovarian tumors and advanced bladder cancer.
PharmacodynamicsCisplatin 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.
Related Articles
AbsorptionFollowing cisplatin doses of 20 to 120 mg/m^2, the concentrations of platinum are highest in liver, prostate, and kidney; somewhat lower in bladder, muscle, testicle, pancreas, and spleen; and lowest in bowel, adrenal, heart, lung, cerebrum, and cerebellum. Platinum is present in tissues for as long as 180 days after the last administration.
Volume of distribution

Volume of distribution at steady state = 11-12 L/m^2

Protein bindingCisplatin does not undergo instantaneous and reversible binding to plasma protein that is characteristic of normal drug-protein binding. However, the platinum itself is capable of binding to plasma proteins, including albumin, transferrin, and gamma globulin. Three hours after a bolus injection and two hours after the end of a three-hour infusion, 90% of the plasma platinum is protein bound.
MetabolismNot Available
Route of eliminationThe parent compound, cisplatin, is excreted in the urine. Although small amounts of platinum are present in the bile and large intestine after administration of cisplatin, the fecal excretion of platinum appears to be insignificant.
Half lifeCisplatin decays monoexponentially with a half life of 20 to 30 minutes following administrations of 50 or 100 mg/m^2. Cisplatin has a plasma half-life of 30 minutes. The complexes between albumin and the platinum from cisplatin do not dissociate to a significant extent and are slowly eliminated with a minimum half-life of five days or more.
Clearance
  • 15-16 L/h/m^2 [total body clearance, 7-hour infusion of 100 mg/m^2]
  • 62 mL/min/m^2 [renal clearance, 2-hour infusion of 100 mg/m^2]
  • 50 mL/min/m^2 [renal clearance, 6- to 7-hour infusion of 100 mg/m^2]
    The renal clearance of free (ultrafilterable) platinum also exceeds the glomerular filtration rate indicating that cisplatin or other platinum-containing molecules are actively secreted by the kidneys. The renal clearance of free platinum is nonlinear and variable and is dependent on dose, urine flow rate, and individual variability in the extent of active secretion and possible tubular reabsorption.
ToxicityNot Available
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Glutathione S-transferase Mu 1
Gene symbol: GSTM1
UniProt: P09488
Not AvailableGSTM1presenceTinnitus, hearing impairment, Raynaud syndrome18162130
Low-density lipoprotein receptor-related protein 2
Gene symbol: LRP2
UniProt: P98164
rs2075252 Not AvailableA alleleOtotoxicity (hearing loss)17457342
Low-density lipoprotein receptor-related protein 2
Gene symbol: LRP2
UniProt: P98164
rs4668123 Not AvailableT alleleOtotoxicity (hearing loss)17457342
Glutathione S-transferase P
Gene symbol: GSTP1
UniProt: P09211
rs1695 Not AvailableA alleleTinnitus, hearing impairment, Raynaud syndrome18162130
DNA repair protein complementing XP-C cells
Gene symbol: XPC
UniProt: Q01831
rs2228001 Not AvailableG > TThose with the GG or GT genotpe have an increase risk of adverse effects21047201
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9637
Blood Brain Barrier+0.9469
Caco-2 permeable-0.5704
P-glycoprotein substrateNon-substrate0.8714
P-glycoprotein inhibitor INon-inhibitor0.9763
P-glycoprotein inhibitor IINon-inhibitor0.9843
Renal organic cation transporterNon-inhibitor0.9211
CYP450 2C9 substrateNon-substrate0.8069
CYP450 2D6 substrateNon-substrate0.7874
CYP450 3A4 substrateNon-substrate0.7495
CYP450 1A2 substrateNon-inhibitor0.7733
CYP450 2C9 inhibitorNon-inhibitor0.7808
CYP450 2D6 inhibitorNon-inhibitor0.9075
CYP450 2C19 inhibitorNon-inhibitor0.7995
CYP450 3A4 inhibitorNon-inhibitor0.8562
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9204
Ames testNon AMES toxic0.5661
CarcinogenicityCarcinogens 0.5146
BiodegradationNot ready biodegradable0.9213
Rat acute toxicity2.7612 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9774
hERG inhibition (predictor II)Non-inhibitor0.9344
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
  • Pharmachemie bv
  • Teva parenteral medicines inc
  • Bristol myers co
Packagers
Dosage forms
FormRouteStrength
Injectionintravenous1 mg/mL
Injection, solutionintravenous1 mg/mL
Injection, solutionintravenous100 mg/100mL
Injection, solutionintravenous50 mg/50mL
Liquidintravenous.5 mg
Liquidintravenous1 mg
Solutionintravenous1 mg
Solutionintravenous1.0 mg
Injection, powder, lyophilized, for solutionintravenous1 mg/mL
Prices
Unit descriptionCostUnit
Cisplatin 1 mg/ml vial0.41USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point270 dec °CPhysProp
water solubility2530 mg/L (at 25 °C)AMUNDSEN,AR & STERN,EW (1982)
logP-2.19HANSCH,C ET AL. (1995)
Predicted Properties
PropertyValueSource
logP0.041ChemAxon
pKa (Strongest Basic)5.06ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area52.04 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity22.84 m3·mol-1ChemAxon
Polarizability10.31 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Murray A. Kaplan, Alphonse P. Granatek, “Process for the preparation of microcrystalline cisplatin.” U.S. Patent US4322391, issued March 30, 1982.

US4322391
General ReferencesNot Available
External Links
ATC CodesL01XA01
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (413 KB)
MSDSDownload (76.1 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe serum concentration of Cisplatin can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Cisplatin.
AfatinibThe serum concentration of Cisplatin can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Cisplatin can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Cisplatin can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Cisplatin can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Cisplatin can be increased when it is combined with Alfentanil.
AmantadineThe serum concentration of Cisplatin can be increased when it is combined with Amantadine.
AmikacinCisplatin may increase the nephrotoxic activities of Amikacin.
Aminohippuric acidThe serum concentration of Cisplatin can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Cisplatin can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Cisplatin can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Cisplatin can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Cisplatin can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Cisplatin can be increased when it is combined with Amsacrine.
AstemizoleThe serum concentration of Cisplatin can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Cisplatin can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Cisplatin can be increased when it is combined with Atenolol.
AtorvastatinThe serum concentration of Cisplatin can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Cisplatin can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Cisplatin can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Cisplatin can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Cisplatin can be increased when it is combined with Bepridil.
BevacizumabBevacizumab may increase the cardiotoxic activities of Cisplatin.
BiperidenThe serum concentration of Cisplatin can be increased when it is combined with Biperiden.
BosutinibThe serum concentration of Cisplatin can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Cisplatin can be increased when it is combined with Bromocriptine.
BumetanideBumetanide may increase the nephrotoxic activities of Cisplatin.
BuprenorphineThe serum concentration of Cisplatin can be increased when it is combined with Buprenorphine.
BupropionThe serum concentration of Cisplatin can be increased when it is combined with Bupropion.
BuspironeThe serum concentration of Cisplatin can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Cisplatin can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Cisplatin can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Cisplatin can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Cisplatin can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Cisplatin can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Cisplatin can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Cisplatin can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Cisplatin can be increased when it is combined with Caspofungin.
ChloroquineThe serum concentration of Cisplatin can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Cisplatin can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Cisplatin can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Cisplatin can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Cisplatin can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Cisplatin can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Cisplatin can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Cisplatin can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Cisplatin can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Cisplatin can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Cisplatin can be increased when it is combined with Clarithromycin.
ClofazimineThe serum concentration of Cisplatin can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Cisplatin can be increased when it is combined with Clomipramine.
ClotrimazoleThe serum concentration of Cisplatin can be decreased when it is combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Cisplatin is combined with Clozapine.
CobicistatThe serum concentration of Cisplatin can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Cisplatin can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Cisplatin can be increased when it is combined with Colforsin.
CrizotinibThe serum concentration of Cisplatin can be increased when it is combined with Crizotinib.
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Cisplatin.
CyclosporineThe serum concentration of Cisplatin can be decreased when it is combined with Cyclosporine.
DaclatasvirThe serum concentration of Cisplatin can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Cisplatin can be increased when it is combined with Dactinomycin.
DasatinibThe serum concentration of Cisplatin can be increased when it is combined with Dasatinib.
DaunorubicinCisplatin may increase the nephrotoxic activities of Daunorubicin.
DaunorubicinThe serum concentration of Cisplatin can be decreased when it is combined with Daunorubicin.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Cisplatin.
DesipramineThe serum concentration of Cisplatin can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Cisplatin.
DesloratadineThe serum concentration of Cisplatin can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Cisplatin can be decreased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Cisplatin can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Cisplatin can be increased when it is combined with Diclofenac.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Cisplatin.
DigoxinDigoxin may decrease the cardiotoxic activities of Cisplatin.
DihydroergotamineThe serum concentration of Cisplatin can be increased when it is combined with Dihydroergotamine.
DihydrostreptomycinCisplatin may increase the nephrotoxic activities of Dihydrostreptomycin.
DiltiazemThe serum concentration of Cisplatin can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Cisplatin can be increased when it is combined with Dipyridamole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Cisplatin.
DoxazosinThe serum concentration of Cisplatin can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Cisplatin can be increased when it is combined with Doxepin.
DoxorubicinCisplatin may increase the nephrotoxic activities of Doxorubicin.
DoxorubicinThe serum concentration of Cisplatin can be decreased when it is combined with Doxorubicin.
DronabinolThe serum concentration of Cisplatin can be increased when it is combined with Dronabinol.
DronedaroneThe serum concentration of Cisplatin can be increased when it is combined with Dronedarone.
ElbasvirThe serum concentration of Cisplatin can be increased when it is combined with Elbasvir.
EltrombopagThe serum concentration of Cisplatin can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Cisplatin can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Cisplatin can be increased when it is combined with Enzalutamide.
EpirubicinCisplatin may increase the nephrotoxic activities of Epirubicin.
ErgonovineThe serum concentration of Cisplatin can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Cisplatin can be increased when it is combined with Ergotamine.
ErythromycinThe serum concentration of Cisplatin can be decreased when it is combined with Erythromycin.
EstramustineThe serum concentration of Cisplatin can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Cisplatin can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Cisplatin can be decreased when it is combined with Estrone.
Etacrynic acidEtacrynic acid may increase the nephrotoxic activities of Cisplatin.
EtoposideThe serum concentration of Cisplatin can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Cisplatin can be increased when it is combined with Etravirine.
FelodipineThe serum concentration of Cisplatin can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Cisplatin can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Cisplatin can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Cisplatin can be increased when it is combined with Fidaxomicin.
FingolimodCisplatin may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe serum concentration of Cisplatin can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Cisplatin can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Cisplatin can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Cisplatin can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Cisplatin can be increased when it is combined with Flurazepam.
FluvoxamineThe serum concentration of Cisplatin can be increased when it is combined with Fluvoxamine.
FramycetinCisplatin may increase the nephrotoxic activities of Framycetin.
FurosemideFurosemide may increase the nephrotoxic activities of Cisplatin.
GefitinibThe serum concentration of Cisplatin can be increased when it is combined with Gefitinib.
GenisteinThe serum concentration of Cisplatin can be increased when it is combined with Genistein.
GentamicinCisplatin may increase the nephrotoxic activities of Gentamicin.
GlyburideThe serum concentration of Cisplatin can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Cisplatin can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Cisplatin can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Cisplatin can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Cisplatin can be increased when it is combined with Haloperidol.
HydrocortisoneThe serum concentration of Cisplatin can be increased when it is combined with Hydrocortisone.
Hygromycin BCisplatin may increase the nephrotoxic activities of Hygromycin B.
IdarubicinCisplatin may increase the nephrotoxic activities of Idarubicin.
IdelalisibThe serum concentration of Cisplatin can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Cisplatin can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Cisplatin can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Cisplatin can be decreased when it is combined with Indinavir.
IndomethacinThe serum concentration of Cisplatin can be increased when it is combined with Indomethacin.
IsavuconazoniumThe serum concentration of Cisplatin can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Cisplatin can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Cisplatin can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Cisplatin can be increased when it is combined with Ivermectin.
KanamycinCisplatin may increase the nephrotoxic activities of Kanamycin.
KetamineThe serum concentration of Cisplatin can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Cisplatin can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Cisplatin can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Cisplatin can be increased when it is combined with Lapatinib.
LeflunomideThe risk or severity of adverse effects can be increased when Cisplatin is combined with Leflunomide.
LevofloxacinThe serum concentration of Cisplatin can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Cisplatin can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Cisplatin can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Cisplatin can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Cisplatin can be decreased when it is combined with Liotrix.
Lipoic AcidThe therapeutic efficacy of Cisplatin can be decreased when used in combination with Lipoic Acid.
LisinoprilThe serum concentration of Cisplatin can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Cisplatin can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Cisplatin can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Cisplatin can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Cisplatin can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Cisplatin can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Cisplatin can be increased when it is combined with Lovastatin.
LumacaftorThe serum concentration of Cisplatin can be decreased when it is combined with Lumacaftor.
MaprotilineThe serum concentration of Cisplatin can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Cisplatin can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Cisplatin can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Cisplatin can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Cisplatin can be increased when it is combined with Meprobamate.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Cisplatin.
MethadoneThe serum concentration of Cisplatin can be increased when it is combined with Methadone.
MetoprololThe serum concentration of Cisplatin can be increased when it is combined with Metoprolol.
MetrizamideCisplatin may increase the nephrotoxic activities of Metrizamide.
MibefradilThe serum concentration of Cisplatin can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Cisplatin can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Cisplatin can be decreased when it is combined with Midazolam.
MifepristoneThe serum concentration of Cisplatin can be decreased when it is combined with Mifepristone.
MitomycinThe serum concentration of Cisplatin can be increased when it is combined with Mitomycin.
MitoxantroneThe serum concentration of Cisplatin can be decreased when it is combined with Mitoxantrone.
MorphineThe serum concentration of Cisplatin can be increased when it is combined with Morphine.
NaltrexoneThe serum concentration of Cisplatin can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Cisplatin can be increased when it is combined with Naringenin.
NatalizumabThe risk or severity of adverse effects can be increased when Cisplatin is combined with Natalizumab.
NefazodoneThe serum concentration of Cisplatin can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Cisplatin can be decreased when it is combined with Nelfinavir.
NeomycinCisplatin may increase the nephrotoxic activities of Neomycin.
NeostigmineThe serum concentration of Cisplatin can be increased when it is combined with Neostigmine.
NetilmicinCisplatin may increase the nephrotoxic activities of Netilmicin.
NicardipineThe serum concentration of Cisplatin can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Cisplatin can be decreased when it is combined with Nifedipine.
NilotinibThe serum concentration of Cisplatin can be increased when it is combined with Nilotinib.
NisoldipineThe serum concentration of Cisplatin can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Cisplatin can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Cisplatin can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Cisplatin can be decreased when it is combined with Norethisterone.
OmeprazoleThe serum concentration of Cisplatin can be increased when it is combined with Omeprazole.
OuabainOuabain may decrease the cardiotoxic activities of Cisplatin.
P-NitrophenolThe serum concentration of Cisplatin can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Cisplatin can be increased when it is combined with Paclitaxel.
Palmitic AcidThe serum concentration of Cisplatin can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Cisplatin can be increased when it is combined with Pantoprazole.
ParomomycinCisplatin may increase the nephrotoxic activities of Paromomycin.
ParoxetineThe serum concentration of Cisplatin can be increased when it is combined with Paroxetine.
PerindoprilThe serum concentration of Cisplatin can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Cisplatin can be decreased when it is combined with Phenobarbital.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cisplatin.
PimozideThe serum concentration of Cisplatin can be increased when it is combined with Pimozide.
PiretanidePiretanide may increase the nephrotoxic activities of Cisplatin.
Platelet Activating FactorThe serum concentration of Cisplatin can be decreased when it is combined with Platelet Activating Factor.
PlicamycinCisplatin may increase the nephrotoxic activities of Plicamycin.
PonatinibThe serum concentration of Cisplatin can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Cisplatin can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Cisplatin can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Cisplatin can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Cisplatin can be increased when it is combined with Prednisone.
ProbenecidThe serum concentration of Cisplatin can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Cisplatin can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Cisplatin can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Cisplatin can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Cisplatin can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Cisplatin can be increased when it is combined with Protriptyline.
PuromycinCisplatin may increase the nephrotoxic activities of Puromycin.
QuercetinThe serum concentration of Cisplatin can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Cisplatin can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Cisplatin can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Cisplatin can be increased when it is combined with Quinine.
Rabies vaccineThe risk or severity of adverse effects can be increased when Cisplatin is combined with Rabies vaccine.
RanitidineThe serum concentration of Cisplatin can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Cisplatin can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Cisplatin can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Cisplatin can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Cisplatin can be decreased when it is combined with Reserpine.
RibostamycinCisplatin may increase the nephrotoxic activities of Ribostamycin.
RifampicinThe serum concentration of Cisplatin can be decreased when it is combined with Rifampicin.
RilpivirineThe serum concentration of Cisplatin can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Cisplatin can be decreased when it is combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Cisplatin.
RolapitantThe serum concentration of Cisplatin can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of Cisplatin can be decreased when it is combined with Saquinavir.
ScopolamineThe serum concentration of Cisplatin can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Cisplatin can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Cisplatin can be increased when it is combined with Sertraline.
SimeprevirThe serum concentration of Cisplatin can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Cisplatin can be increased when it is combined with Simvastatin.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Cisplatin.
SirolimusThe serum concentration of Cisplatin can be decreased when it is combined with Sirolimus.
SorafenibThe serum concentration of Cisplatin can be increased when it is combined with Sorafenib.
SpectinomycinCisplatin may increase the nephrotoxic activities of Spectinomycin.
SpironolactoneThe serum concentration of Cisplatin can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Cisplatin can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Cisplatin can be increased when it is combined with Staurosporine.
StreptomycinCisplatin may increase the nephrotoxic activities of Streptomycin.
StreptozocinCisplatin may increase the nephrotoxic activities of Streptozocin.
StreptozocinThe serum concentration of Cisplatin can be decreased when it is combined with Streptozocin.
SulfinpyrazoneThe serum concentration of Cisplatin can be increased when it is combined with Sulfinpyrazone.
SumatriptanThe serum concentration of Cisplatin can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Cisplatin can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Cisplatin can be increased when it is combined with Tacrine.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cisplatin.
TamoxifenThe serum concentration of Cisplatin can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Cisplatin can be increased when it is combined with Taurocholic Acid.
TelmisartanThe serum concentration of Cisplatin can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Cisplatin can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Cisplatin can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Cisplatin can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Cisplatin can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Cisplatin can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Cisplatin can be increased when it is combined with Testosterone.
TicagrelorThe serum concentration of Cisplatin can be increased when it is combined with Ticagrelor.
TobramycinCisplatin may increase the nephrotoxic activities of Tobramycin.
TofacitinibCisplatin may increase the immunosuppressive activities of Tofacitinib.
TolvaptanThe serum concentration of Cisplatin can be increased when it is combined with Tolvaptan.
TorasemideTorasemide may increase the nephrotoxic activities of Cisplatin.
TrastuzumabTrastuzumab may increase the neutropenic activities of Cisplatin.
TrazodoneThe serum concentration of Cisplatin can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Cisplatin can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Cisplatin can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Cisplatin can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Cisplatin can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Cisplatin can be increased when it is combined with Troleandomycin.
VenlafaxineThe serum concentration of Cisplatin can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Cisplatin can be decreased when it is combined with Verapamil.
VinblastineThe serum concentration of Cisplatin can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Cisplatin can be decreased when it is combined with Vincristine.
VinorelbineThe risk or severity of adverse effects can be increased when Cisplatin is combined with Vinorelbine.
VinorelbineThe serum concentration of Cisplatin can be increased when it is combined with Vinorelbine.
ZimelidineThe serum concentration of Cisplatin can be increased when it is combined with Zimelidine.
Food Interactions
  • Echinacea should be used with caution, if at all, in patients receiving therapeutic immunosuppressants. Monitor for reduced efficacy of the immunosuppressant during concomitant use.

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. Garcia Sar D, Montes-Bayon M, Aguado Ortiz L, Blanco-Gonzalez E, Sierra LM, Sanz-Medel A: In vivo detection of DNA adducts induced by cisplatin using capillary HPLC-ICP-MS and their correlation with genotoxic damage in Drosophila melanogaster. Anal Bioanal Chem. 2008 Jan;390(1):37-44. Epub 2007 Oct 12. [PubMed:17932658 ]
  4. 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 ]
  5. Bloemink MJ, Reedijk J: Cisplatin and derived anticancer drugs: mechanism and current status of DNA binding. Met Ions Biol Syst. 1996;32:641-85. [PubMed:8640534 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Erdogan S, Tosyali E, Duzguner V, Kucukgul A, Aslantas O, Celik S: Cisplatin reduces Brucella melitensis-infected cell number by inducing apoptosis, oxidant and pro-inflammatory cytokine production. Res Vet Sci. 2010 Apr;88(2):218-26. doi: 10.1016/j.rvsc.2009.09.002. Epub 2009 Oct 8. [PubMed:19818462 ]
  2. Ozen S, Akyol O, Iraz M, Sogut S, Ozugurlu F, Ozyurt H, Odaci E, Yildirim Z: Role of caffeic acid phenethyl ester, an active component of propolis, against cisplatin-induced nephrotoxicity in rats. J Appl Toxicol. 2004 Jan-Feb;24(1):27-35. [PubMed:14745844 ]
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. Yilmaz HR, Sogut S, Ozyurt B, Ozugurlu F, Sahin S, Isik B, Uz E, Ozyurt H: The activities of liver adenosine deaminase, xanthine oxidase, catalase, superoxide dismutase enzymes and the levels of malondialdehyde and nitric oxide after cisplatin toxicity in rats: protective effect of caffeic acid phenethyl ester. Toxicol Ind Health. 2005 May;21(3-4):67-73. [PubMed:15986578 ]
  2. Cetin R, Devrim E, Kilicoglu B, Avci A, Candir O, Durak I: Cisplatin impairs antioxidant system and causes oxidation in rat kidney tissues: possible protective roles of natural antioxidant foods. J Appl Toxicol. 2006 Jan-Feb;26(1):42-6. [PubMed:16158393 ]
  3. Erdogan S, Tosyali E, Duzguner V, Kucukgul A, Aslantas O, Celik S: Cisplatin reduces Brucella melitensis-infected cell number by inducing apoptosis, oxidant and pro-inflammatory cytokine production. Res Vet Sci. 2010 Apr;88(2):218-26. doi: 10.1016/j.rvsc.2009.09.002. Epub 2009 Oct 8. [PubMed:19818462 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Leukotriene-b4 20-monooxygenase activity
Specific Function:
Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 20-hydroxyeicosatetraenoic acid (20-HETE).
Gene Name:
CYP4A11
Uniprot ID:
Q02928
Molecular Weight:
59347.31 Da
References
  1. Nakamura M, Imaoka S, Tanaka E, Misawa S, Funae Y: cis-Diamminedichloroplatinum induces peroxisomes as well as CYP4A1 in rat kidney. Res Commun Mol Pathol Pharmacol. 1998 Jan;99(1):23-32. [PubMed:9523352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Constitutively expressed in some tissues in physiological conditions, such as the endothelium, kidney and brain, and in pathological conditions, such as in cancer. PTGS2 is responsible for production of inflammatory prostaglandins. Up-regulation of PTGS2 is also associated with increased cell adhesion, p...
Gene Name:
PTGS2
Uniprot ID:
P35354
Molecular Weight:
68995.625 Da
References
  1. Tusgaard B, Norregaard R, Jensen AM, Wang G, Topcu SO, Wang Y, Nielsen S, Frokiaer J: Cisplatin decreases renal cyclooxygenase-2 expression and activity in rats. Acta Physiol (Oxf). 2011 May;202(1):79-90. doi: 10.1111/j.1748-1716.2011.02257.x. Epub 2011 Mar 22. [PubMed:21272267 ]
Kind
Protein
Organism
Mycobacterium tuberculosis
Pharmacological action
unknown
Actions
inhibitor
General Function:
Not Available
Specific Function:
Not Available
Gene Name:
nat
Uniprot ID:
P0A5L8
Molecular Weight:
Not Available
References
  1. Ragunathan N, Dairou J, Pluvinage B, Martins M, Petit E, Janel N, Dupret JM, Rodrigues-Lima F: Identification of the xenobiotic-metabolizing enzyme arylamine N-acetyltransferase 1 as a new target of cisplatin in breast cancer cells: molecular and cellular mechanisms of inhibition. Mol Pharmacol. 2008 Jun;73(6):1761-8. doi: 10.1124/mol.108.045328. Epub 2008 Feb 29. [PubMed:18310302 ]
  2. Holzer AK, Samimi G, Katano K, Naerdemann W, Lin X, Safaei R, Howell SB: The copper influx transporter human copper transport protein 1 regulates the uptake of cisplatin in human ovarian carcinoma cells. Mol Pharmacol. 2004 Oct;66(4):817-23. Epub 2004 Jun 30. [PubMed:15229296 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Masek V, Anzenbacherova E, Machova M, Brabec V, Anzenbacher P: Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. Anticancer Drugs. 2009 Jun;20(5):305-11. [PubMed:19378397 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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 unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 Da
References
  1. Masek V, Anzenbacherova E, Machova M, Brabec V, Anzenbacher P: Interaction of antitumor platinum complexes with human liver microsomal cytochromes P450. Anticancer Drugs. 2009 Jun;20(5):305-11. [PubMed:19378397 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Identical protein binding
Specific Function:
Esterase with broad substrate specificity. Contributes to the inactivation of the neurotransmitter acetylcholine. Can degrade neurotoxic organophosphate esters.
Gene Name:
BCHE
Uniprot ID:
P06276
Molecular Weight:
68417.575 Da
References
  1. Bodur E: Human serum butyrylcholinesterase interactions with cisplatin and cyclophosphamide. Biochimie. 2010 Aug;92(8):979-84. doi: 10.1016/j.biochi.2010.04.010. Epub 2010 Apr 24. [PubMed:20417682 ]
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. Peters U, Preisler-Adams S, Hebeisen A, Hahn M, Seifert E, Lanvers C, Heinecke A, Horst J, Jurgens H, Lamprecht-Dinnesen A: Glutathione S-transferase genetic polymorphisms and individual sensitivity to the ototoxic effect of cisplatin. Anticancer Drugs. 2000 Sep;11(8):639-43. [PubMed:11081456 ]
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. Meijer C, Timmer A, De Vries EG, Groten JP, Knol A, Zwart N, Dam WA, Sleijfer DT, Mulder NH: Role of metallothionein in cisplatin sensitivity of germ-cell tumours. Int J Cancer. 2000 Mar 15;85(6):777-81. [PubMed:10709094 ]
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. Meijer C, Timmer A, De Vries EG, Groten JP, Knol A, Zwart N, Dam WA, Sleijfer DT, Mulder NH: Role of metallothionein in cisplatin sensitivity of germ-cell tumours. Int J Cancer. 2000 Mar 15;85(6):777-81. [PubMed:10709094 ]
Kind
Protein
Organism
Human
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
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. Peters U, Preisler-Adams S, Hebeisen A, Hahn M, Seifert E, Lanvers C, Heinecke A, Horst J, Jurgens H, Lamprecht-Dinnesen A: Glutathione S-transferase genetic polymorphisms and individual sensitivity to the ototoxic effect of cisplatin. Anticancer Drugs. 2000 Sep;11(8):639-43. [PubMed:11081456 ]
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]
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. Peters U, Preisler-Adams S, Hebeisen A, Hahn M, Seifert E, Lanvers C, Heinecke A, Horst J, Jurgens H, Lamprecht-Dinnesen A: Glutathione S-transferase genetic polymorphisms and individual sensitivity to the ototoxic effect of cisplatin. Anticancer Drugs. 2000 Sep;11(8):639-43. [PubMed:11081456 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Organic anion transmembrane transporter activity
Specific Function:
May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocytes (By similarity).
Gene Name:
ABCC3
Uniprot ID:
O15438
Molecular Weight:
169341.14 Da
References
  1. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Acts as a multispecific organic anion pump which can transport nucleotide analogs.
Gene Name:
ABCC5
Uniprot ID:
O15440
Molecular Weight:
160658.8 Da
References
  1. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inducer
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. Schrenk D, Baus PR, Ermel N, Klein C, Vorderstemann B, Kauffmann HM: Up-regulation of transporters of the MRP family by drugs and toxins. Toxicol Lett. 2001 Mar 31;120(1-3):51-7. [PubMed:11323161 ]
  2. Demeule M, Brossard M, Beliveau R: Cisplatin induces renal expression of P-glycoprotein and canalicular multispecific organic anion transporter. Am J Physiol. 1999 Dec;277(6 Pt 2):F832-40. [PubMed:10600929 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Pan BF, Sweet DH, Pritchard JB, Chen R, Nelson JA: A transfected cell model for the renal toxin transporter, rOCT2. Toxicol Sci. 1999 Feb;47(2):181-6. [PubMed:10220855 ]
  2. 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 ]
  3. Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. [PubMed:10592235 ]
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. Kurokawa T, He G, Siddik ZH: Protein kinase inhibitors emodin and dichloro-ribofuranosylbenzimidazole modulate the cellular accumulation and cytotoxicity of cisplatin in a schedule-dependent manner. Cancer Chemother Pharmacol. 2010 Feb;65(3):427-36. doi: 10.1007/s00280-009-1045-2. Epub 2009 Jun 16. [PubMed:19529937 ]
  3. Jandial DD, Farshchi-Heydari S, Larson CA, Elliott GI, Wrasidlo WJ, Howell SB: Enhanced delivery of cisplatin to intraperitoneal ovarian carcinomas mediated by the effects of bortezomib on the human copper transporter 1. Clin Cancer Res. 2009 Jan 15;15(2):553-60. doi: 10.1158/1078-0432.CCR-08-2081. [PubMed:19147760 ]
  4. Liang ZD, Stockton D, Savaraj N, Tien Kuo M: Mechanistic comparison of human high-affinity copper transporter 1-mediated transport between copper ion and cisplatin. Mol Pharmacol. 2009 Oct;76(4):843-53. doi: 10.1124/mol.109.056416. Epub 2009 Jul 1. [PubMed:19570948 ]
  5. Rabik CA, Maryon EB, Kasza K, Shafer JT, Bartnik CM, Dolan ME: Role of copper transporters in resistance to platinating agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):133-42. doi: 10.1007/s00280-008-0860-1. Epub 2008 Nov 8. [PubMed:18998134 ]
  6. Pabla N, Murphy RF, Liu K, Dong Z: The copper transporter Ctr1 contributes to cisplatin uptake by renal tubular cells during cisplatin nephrotoxicity. Am J Physiol Renal Physiol. 2009 Mar;296(3):F505-11. doi: 10.1152/ajprenal.90545.2008. Epub 2009 Jan 14. [PubMed:19144690 ]
  7. Furukawa T, Komatsu M, Ikeda R, Tsujikawa K, Akiyama S: Copper transport systems are involved in multidrug resistance and drug transport. Curr Med Chem. 2008;15(30):3268-78. [PubMed:19075668 ]
  8. Holzer AK, Samimi G, Katano K, Naerdemann W, Lin X, Safaei R, Howell SB: The copper influx transporter human copper transport protein 1 regulates the uptake of cisplatin in human ovarian carcinoma cells. Mol Pharmacol. 2004 Oct;66(4):817-23. Epub 2004 Jun 30. [PubMed:15229296 ]
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:
Transporter activity
Specific Function:
Isoform 1: May participate directly in the active transport of drugs into subcellular organelles or influence drug distribution indirectly. Transports glutathione conjugates as leukotriene-c4 (LTC4) and N-ethylmaleimide S-glutathione (NEM-GS).Isoform 2: Inhibits TNF-alpha-mediated apoptosis through blocking one or more caspases.
Gene Name:
ABCC6
Uniprot ID:
O95255
Molecular Weight:
164904.81 Da
References
  1. Belinsky MG, Chen ZS, Shchaveleva I, Zeng H, Kruh GD: Characterization of the drug resistance and transport properties of multidrug resistance protein 6 (MRP6, ABCC6). Cancer Res. 2002 Nov 1;62(21):6172-7. [PubMed:12414644 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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
Molecular Weight:
141477.255 Da
References
  1. Li D, Jang SH, Kim J, Wientjes MG, Au JL: Enhanced drug-induced apoptosis associated with P-glycoprotein overexpression is specific to antimicrotubule agents. Pharm Res. 2003 Jan;20(1):45-50. [PubMed:12608535 ]
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. Rabik CA, Maryon EB, Kasza K, Shafer JT, Bartnik CM, Dolan ME: Role of copper transporters in resistance to platinating agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):133-42. doi: 10.1007/s00280-008-0860-1. Epub 2008 Nov 8. [PubMed:18998134 ]
  2. Mangala LS, Zuzel V, Schmandt R, Leshane ES, Halder JB, Armaiz-Pena GN, Spannuth WA, Tanaka T, Shahzad MM, Lin YG, Nick AM, Danes CG, Lee JW, Jennings NB, Vivas-Mejia PE, Wolf JK, Coleman RL, Siddik ZH, Lopez-Berestein G, Lutsenko S, Sood AK: Therapeutic Targeting of ATP7B in Ovarian Carcinoma. Clin Cancer Res. 2009 Jun 1;15(11):3770-80. doi: 10.1158/1078-0432.CCR-08-2306. Epub 2009 May 26. [PubMed:19470734 ]
  3. Furukawa T, Komatsu M, Ikeda R, Tsujikawa K, Akiyama S: Copper transport systems are involved in multidrug resistance and drug transport. Curr Med Chem. 2008;15(30):3268-78. [PubMed:19075668 ]
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. Rabik CA, Maryon EB, Kasza K, Shafer JT, Bartnik CM, Dolan ME: Role of copper transporters in resistance to platinating agents. Cancer Chemother Pharmacol. 2009 Jun;64(1):133-42. doi: 10.1007/s00280-008-0860-1. Epub 2008 Nov 8. [PubMed:18998134 ]
  2. Furukawa T, Komatsu M, Ikeda R, Tsujikawa K, Akiyama S: Copper transport systems are involved in multidrug resistance and drug transport. Curr Med Chem. 2008;15(30):3268-78. [PubMed:19075668 ]
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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23