You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
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 mgIntravenousOmega Laboratories LtdNot applicableNot applicableCanada
Cisplatin Injection BPSolution1 mgIntravenousHospira Healthcare Corporation1997-05-09Not 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/mLIntravenousBlue Point Laboratories2016-08-02Not 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 KeyDQLATGHUWYMOKM-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
Pharmacology
IndicationFor the treatment of metastatic testicular tumors, metastatic ovarian tumors and advanced bladder cancer.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
DNANucleotideyes
cross-linking/alkylation
Humannot applicabledetails
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
Interactions
Drug Interactions
DrugInteractionDrug group
AcetaminophenThe serum concentration of Cisplatin can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Cisplatin.Approved
AclarubicinCisplatin may increase the nephrotoxic activities of Aclarubicin.Investigational
AfatinibThe serum concentration of Cisplatin can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Cisplatin can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Cisplatin can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Cisplatin can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Cisplatin can be increased when it is combined with Alfentanil.Approved, Illicit
ALT-110The risk or severity of adverse effects can be increased when Cisplatin is combined with ALT-110.Investigational
AmantadineThe serum concentration of Cisplatin can be increased when it is combined with Amantadine.Approved
AmikacinCisplatin may increase the nephrotoxic activities of Amikacin.Approved, Vet Approved
Aminohippuric acidThe serum concentration of Cisplatin can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of Cisplatin can be decreased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Cisplatin can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Cisplatin can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Cisplatin can be decreased when it is combined with Amprenavir.Approved
AmrubicinCisplatin may increase the nephrotoxic activities of Amrubicin.Approved, Investigational
AmsacrineThe serum concentration of Cisplatin can be increased when it is combined with Amsacrine.Approved
annamycinCisplatin may increase the nephrotoxic activities of annamycin.Investigational
AnvirzelAnvirzel may decrease the cardiotoxic activities of Cisplatin.Investigational
ApramycinCisplatin may increase the nephrotoxic activities of Apramycin.Experimental, Vet Approved
ArbekacinCisplatin may increase the nephrotoxic activities of Arbekacin.Approved
AstemizoleThe serum concentration of Cisplatin can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Cisplatin can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Cisplatin can be increased when it is combined with Atenolol.Approved
AtorvastatinThe serum concentration of Cisplatin can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Cisplatin can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Cisplatin can be increased when it is combined with Azithromycin.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Cisplatin.Investigational
BenzocaineThe serum concentration of Cisplatin can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Cisplatin can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Cisplatin.Approved, Investigational
BiperidenThe serum concentration of Cisplatin can be increased when it is combined with Biperiden.Approved
BosutinibThe serum concentration of Cisplatin can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Cisplatin can be increased when it is combined with Bromocriptine.Approved, Investigational
BumetanideBumetanide may increase the nephrotoxic activities of Cisplatin.Approved
BuprenorphineThe serum concentration of Cisplatin can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe serum concentration of Cisplatin can be increased when it is combined with Bupropion.Approved
BuspironeThe serum concentration of Cisplatin can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelCisplatin may increase the myelosuppressive activities of Cabazitaxel.Approved
CaffeineThe serum concentration of Cisplatin can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Cisplatin can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Cisplatin can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Cisplatin can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Cisplatin can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Cisplatin can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Cisplatin can be increased when it is combined with Caspofungin.Approved
CDX-110The risk or severity of adverse effects can be increased when Cisplatin is combined with CDX-110.Investigational
ChloroquineThe serum concentration of Cisplatin can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Cisplatin can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Cisplatin can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Cisplatin can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Cisplatin can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Cisplatin can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Cisplatin can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Cisplatin can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Cisplatin can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Cisplatin can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Cisplatin can be increased when it is combined with Clarithromycin.Approved
ClofazimineThe serum concentration of Cisplatin can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Cisplatin can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe serum concentration of Cisplatin can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Cisplatin is combined with Clozapine.Approved
CobicistatThe serum concentration of Cisplatin can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Cisplatin can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Cisplatin can be increased when it is combined with Colforsin.Experimental
CrizotinibThe serum concentration of Cisplatin can be increased when it is combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Cisplatin.Approved, Investigational
CyclosporineThe serum concentration of Cisplatin can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DaclatasvirThe serum concentration of Cisplatin can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Cisplatin can be increased when it is combined with Dactinomycin.Approved
DasatinibThe serum concentration of Cisplatin can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinCisplatin may increase the nephrotoxic activities of Daunorubicin.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Cisplatin.Approved
DesipramineThe serum concentration of Cisplatin can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Cisplatin.Approved
DesloratadineThe serum concentration of Cisplatin can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Cisplatin can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Cisplatin can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Cisplatin can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Cisplatin.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Cisplatin.Approved
DihydroergotamineThe serum concentration of Cisplatin can be increased when it is combined with Dihydroergotamine.Approved
DihydrostreptomycinCisplatin may increase the nephrotoxic activities of Dihydrostreptomycin.Vet Approved
DiltiazemThe serum concentration of Cisplatin can be increased when it is combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Cisplatin can be increased when it is combined with Dipyridamole.Approved
DocetaxelCisplatin may increase the myelosuppressive activities of Docetaxel.Approved, Investigational
DoxazosinThe serum concentration of Cisplatin can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Cisplatin can be increased when it is combined with Doxepin.Approved
DoxorubicinCisplatin may increase the nephrotoxic activities of Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Cisplatin can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Cisplatin can be increased when it is combined with Dronedarone.Approved
ElbasvirThe serum concentration of Cisplatin can be increased when it is combined with Elbasvir.Approved
EltrombopagThe serum concentration of Cisplatin can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Cisplatin can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of Cisplatin can be increased when it is combined with Enzalutamide.Approved
EpirubicinCisplatin may increase the nephrotoxic activities of Epirubicin.Approved
ErgonovineThe serum concentration of Cisplatin can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Cisplatin can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Cisplatin can be decreased when it is combined with Erythromycin.Approved, Vet Approved
EstramustineThe serum concentration of Cisplatin can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Cisplatin can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Cisplatin can be decreased when it is combined with Estrone.Approved
Etacrynic acidEtacrynic acid may increase the nephrotoxic activities of Cisplatin.Approved
EtoposideThe serum concentration of Cisplatin can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Cisplatin can be increased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Cisplatin can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Cisplatin can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Cisplatin can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Cisplatin can be increased when it is combined with Fidaxomicin.Approved
FingolimodCisplatin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe serum concentration of Cisplatin can be increased when it is combined with Fluconazole.Approved
FluoxetineThe serum concentration of Cisplatin can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Cisplatin can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Cisplatin can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Cisplatin can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe serum concentration of Cisplatin can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe serum concentration of Fosphenytoin can be decreased when it is combined with Cisplatin.Approved
FramycetinCisplatin may increase the nephrotoxic activities of Framycetin.Approved
FurosemideFurosemide may increase the nephrotoxic activities of Cisplatin.Approved, Vet Approved
G17DTThe risk or severity of adverse effects can be increased when Cisplatin is combined with G17DT.Investigational
GefitinibThe serum concentration of Cisplatin can be increased when it is combined with Gefitinib.Approved, Investigational
GeneticinCisplatin may increase the nephrotoxic activities of Geneticin.Experimental
GenisteinThe serum concentration of Cisplatin can be increased when it is combined with Genistein.Investigational
GentamicinCisplatin may increase the nephrotoxic activities of Gentamicin.Approved, Vet Approved
GENTAMICIN C1ACisplatin may increase the nephrotoxic activities of GENTAMICIN C1A.Experimental
GI-5005The risk or severity of adverse effects can be increased when Cisplatin is combined with GI-5005.Investigational
GlyburideThe serum concentration of Cisplatin can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Cisplatin can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Cisplatin can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Cisplatin can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Cisplatin can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Cisplatin can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
Hygromycin BCisplatin may increase the nephrotoxic activities of Hygromycin B.Vet Approved
IdarubicinCisplatin may increase the nephrotoxic activities of Idarubicin.Approved
IdelalisibThe serum concentration of Cisplatin can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Cisplatin can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Cisplatin can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Cisplatin can be decreased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Cisplatin can be increased when it is combined with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Cisplatin is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Cisplatin is combined with INGN 225.Investigational
INNO-206Cisplatin may increase the nephrotoxic activities of INNO-206.Investigational
IsavuconazoniumThe serum concentration of Cisplatin can be increased when it is combined with Isavuconazonium.Approved, Investigational
ItraconazoleThe serum concentration of Cisplatin can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Cisplatin can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Cisplatin can be increased when it is combined with Ivermectin.Approved, Vet Approved
KanamycinCisplatin may increase the nephrotoxic activities of Kanamycin.Approved, Vet Approved
KetamineThe serum concentration of Cisplatin can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Cisplatin can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Cisplatin can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Cisplatin can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Cisplatin is combined with Leflunomide.Approved, Investigational
LevofloxacinThe serum concentration of Cisplatin can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Cisplatin can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Cisplatin can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Cisplatin can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Cisplatin can be decreased when it is combined with Liotrix.Approved
Lipoic AcidThe therapeutic efficacy of Cisplatin can be decreased when used in combination with Lipoic Acid.Approved, Nutraceutical
LisinoprilThe serum concentration of Cisplatin can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Cisplatin can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Cisplatin can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of Cisplatin can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Cisplatin can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Cisplatin can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Cisplatin can be increased when it is combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Cisplatin can be decreased when it is combined with Lumacaftor.Approved
MaprotilineThe serum concentration of Cisplatin can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Cisplatin can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Cisplatin can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Cisplatin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Cisplatin can be increased when it is combined with Meprobamate.Approved, Illicit
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Cisplatin.Withdrawn
MethadoneThe serum concentration of Cisplatin can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Cisplatin can be increased when it is combined with Metoprolol.Approved, Investigational
MetrizamideCisplatin may increase the nephrotoxic activities of Metrizamide.Approved
MibefradilThe serum concentration of Cisplatin can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Cisplatin can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Cisplatin can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Cisplatin can be decreased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Cisplatin can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Cisplatin can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Cisplatin can be increased when it is combined with Morphine.Approved, Investigational
NaltrexoneThe serum concentration of Cisplatin can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Cisplatin can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Cisplatin is combined with Natalizumab.Approved, Investigational
NeamineCisplatin may increase the nephrotoxic activities of Neamine.Experimental
NefazodoneThe serum concentration of Cisplatin can be decreased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Cisplatin can be decreased when it is combined with Nelfinavir.Approved
NeomycinCisplatin may increase the nephrotoxic activities of Neomycin.Approved, Vet Approved
NeostigmineThe serum concentration of Cisplatin can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetilmicinCisplatin may increase the nephrotoxic activities of Netilmicin.Approved
NicardipineThe serum concentration of Cisplatin can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Cisplatin can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Cisplatin can be increased when it is combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Cisplatin can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Cisplatin can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Cisplatin can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Cisplatin can be decreased when it is combined with Norethisterone.Approved
OmeprazoleThe serum concentration of Cisplatin can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OuabainOuabain may decrease the cardiotoxic activities of Cisplatin.Approved
P-NitrophenolThe serum concentration of Cisplatin can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelCisplatin may increase the myelosuppressive activities of Paclitaxel.Approved, Vet Approved
Palmitic AcidThe serum concentration of Cisplatin can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Cisplatin can be increased when it is combined with Pantoprazole.Approved
ParomomycinCisplatin may increase the nephrotoxic activities of Paromomycin.Approved, Investigational
ParoxetineThe serum concentration of Cisplatin can be increased when it is combined with Paroxetine.Approved, Investigational
PerindoprilThe serum concentration of Cisplatin can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe serum concentration of Cisplatin can be decreased when it is combined with Phenobarbital.Approved
PhenytoinThe serum concentration of Phenytoin can be decreased when it is combined with Cisplatin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Cisplatin.Approved, Investigational
PimozideThe serum concentration of Cisplatin can be increased when it is combined with Pimozide.Approved
PirarubicinCisplatin may increase the nephrotoxic activities of Pirarubicin.Investigational
PiretanidePiretanide may increase the nephrotoxic activities of Cisplatin.Experimental
Platelet Activating FactorThe serum concentration of Cisplatin can be decreased when it is combined with Platelet Activating Factor.Experimental
PlicamycinCisplatin may increase the nephrotoxic activities of Plicamycin.Approved, Withdrawn
PonatinibThe serum concentration of Cisplatin can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Cisplatin can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Cisplatin can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Cisplatin can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Cisplatin can be increased when it is combined with Prednisone.Approved, Vet Approved
ProbenecidThe serum concentration of Cisplatin can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Cisplatin can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Cisplatin can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Cisplatin can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Cisplatin can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Cisplatin can be increased when it is combined with Protriptyline.Approved
PuromycinCisplatin may increase the nephrotoxic activities of Puromycin.Experimental
QuercetinThe serum concentration of Cisplatin can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Cisplatin can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Cisplatin can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Cisplatin can be increased when it is combined with Quinine.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Cisplatin is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Cisplatin.Approved
RanitidineThe serum concentration of Cisplatin can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Cisplatin can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Cisplatin can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Cisplatin can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Cisplatin can be decreased when it is combined with Reserpine.Approved
RibostamycinCisplatin may increase the nephrotoxic activities of Ribostamycin.Approved
RifampicinThe serum concentration of Cisplatin can be decreased when it is combined with Rifampicin.Approved
RilpivirineThe serum concentration of Cisplatin can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of Cisplatin can be decreased when it is combined with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Cisplatin.Approved
RolapitantThe serum concentration of Cisplatin can be increased when it is combined with Rolapitant.Approved
SaquinavirThe serum concentration of Cisplatin can be decreased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Cisplatin can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Cisplatin can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Cisplatin can be increased when it is combined with Sertraline.Approved
SimeprevirThe serum concentration of Cisplatin can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Cisplatin can be increased when it is combined with Simvastatin.Approved
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Cisplatin.Approved
SirolimusThe serum concentration of Cisplatin can be decreased when it is combined with Sirolimus.Approved, Investigational
SisomicinCisplatin may increase the nephrotoxic activities of Sisomicin.Investigational
SorafenibThe serum concentration of Cisplatin can be increased when it is combined with Sorafenib.Approved, Investigational
SP1049CCisplatin may increase the nephrotoxic activities of SP1049C.Investigational
SpectinomycinCisplatin may increase the nephrotoxic activities of Spectinomycin.Approved, Vet Approved
SpironolactoneThe serum concentration of Cisplatin can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Cisplatin is combined with SRP 299.Investigational
St. John's WortThe serum concentration of Cisplatin can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Cisplatin can be increased when it is combined with Staurosporine.Experimental
StreptomycinCisplatin may increase the nephrotoxic activities of Streptomycin.Approved, Vet Approved
StreptozocinCisplatin may increase the nephrotoxic activities of Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Cisplatin can be increased when it is combined with Sulfinpyrazone.Approved
SumatriptanThe serum concentration of Cisplatin can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Cisplatin can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Cisplatin can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Cisplatin.Approved, Investigational
TacrolimusThe serum concentration of Cisplatin can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Cisplatin can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Cisplatin can be increased when it is combined with Taurocholic Acid.Experimental
TelmisartanThe serum concentration of Cisplatin can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Cisplatin can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Cisplatin can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Cisplatin can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Cisplatin can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Cisplatin can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Cisplatin can be increased when it is combined with Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Cisplatin is combined with TG4010.Investigational
TicagrelorThe serum concentration of Cisplatin can be increased when it is combined with Ticagrelor.Approved
TobramycinCisplatin may increase the nephrotoxic activities of Tobramycin.Approved, Investigational
TofacitinibCisplatin may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolvaptanThe serum concentration of Cisplatin can be increased when it is combined with Tolvaptan.Approved
TopotecanThe risk or severity of adverse effects can be increased when Cisplatin is combined with Topotecan.Approved, Investigational
TorasemideTorasemide may increase the nephrotoxic activities of Cisplatin.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Cisplatin.Approved, Investigational
TrazodoneThe serum concentration of Cisplatin can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Cisplatin can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Cisplatin can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Cisplatin can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Cisplatin can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Cisplatin can be increased when it is combined with Troleandomycin.Approved
ValrubicinCisplatin may increase the nephrotoxic activities of Valrubicin.Approved
VenlafaxineThe serum concentration of Cisplatin can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Cisplatin can be decreased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Cisplatin can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Cisplatin can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe risk or severity of adverse effects can be increased when Cisplatin is combined with Vinorelbine.Approved, Investigational
ZimelidineThe serum concentration of Cisplatin can be increased when it is combined with Zimelidine.Withdrawn
ZorubicinCisplatin may increase the nephrotoxic activities of Zorubicin.Experimental
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.
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)
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
SolutionIntravenous1.0 mg
SolutionIntravenous1 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
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

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 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23