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Identification
NameIdarubicin
Accession NumberDB01177  (APRD00126)
TypeSmall Molecule
GroupsApproved
DescriptionAn orally administered anthracycline antineoplastic. The compound has shown activity against breast cancer, lymphomas and leukemias, together with the potential for reduced cardiac toxicity. [PubChem]
Structure
Thumb
Synonyms
(1S,3S)-3-Acetyl-3,5,12-trihydroxy-6,11-dioxo-1,2,3,4,6,11-hexahydronaphthacen-1-yl 3-amino-2,3,6-trideoxy-alpha-L-lyxo-hexopyranoside
4-Demethoxydaunomycin
4-Demethoxydaunorubicin
5,12-Naphthacenedione, 9-acetyl-7-((3-amino-2,3,6-trideoxy-alpha-L-lyxo-hexopyranosyl)oxy)-7,8,9,10-tetrahydro-6,9,11-trihydroxy-, (7S-cis)-
Idarubicina
Idarubicine
Idarubicinum
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aj-idarubicinSolution1 mgIntravenousAgila Jamp Canada IncNot applicableNot applicableCanada
Idamycin - Cap 10mgCapsule10 mgOralPfizer Canada Inc1996-12-312006-08-02Canada
Idamycin - Cap 25mgCapsule25 mgOralPfizer Canada Inc1996-12-302006-08-02Canada
Idamycin - Cap 5mgCapsule5 mgOralPfizer Canada Inc1996-12-312006-08-02Canada
Idamycin PFSSolution1 mg/mLIntravenousPharmacia and Upjohn Company1997-02-17Not applicableUs
Idamycin PFSSolution1 mg/mLIntravenousPharmacia and Upjohn Company1997-02-17Not applicableUs
Idamycin PFSSolution1 mg/mLIntravenousPharmacia and Upjohn Company1997-02-17Not applicableUs
Idamycin PFSSolution1 mgIntravenousPfizer Canada Inc2006-11-25Not applicableCanada
Idamycin Powder -5mg/vialPowder, for solution5 mgIntravenousPfizer Canada Inc1995-12-312014-03-21Canada
Idamycin Powder -10mg/vialPowder, for solution10 mgIntravenousPfizer Canada Inc1995-12-312014-03-21Canada
Idamycin Pws 10mg/vialPowder, for solution10 mgIntravenousAdria Laboratories Of Canada Ltd.1991-12-311996-09-10Canada
Idamycin Pws 5mg/vialPowder, for solution5 mgIntravenousAdria Laboratories Of Canada Ltd.1991-12-311996-09-10Canada
IdarubicinSolution1 mgIntravenousPfizer Canada Inc2014-11-04Not applicableCanada
Idarubicin Hydrochloride InjectionSolution1 mgIntravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
Idarubicin Hydrochloride InjectionSolution1 mgIntravenousFresenius Kabi Canada Ltd2010-04-13Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Idarubicin HydrochlorideInjection, solution1 mg/mLIntravenousTeva Parenteral Medicines, Inc.2002-10-01Not applicableUs
Idarubicin HydrochlorideInjection5 mg/5mLIntravenousAmneal Agila, Llc2013-04-30Not applicableUs
Idarubicin HydrochlorideInjection1 mg/mLIntravenousSandoz Inc2011-03-29Not applicableUs
Idarubicin HydrochlorideInjection10 mg/10mLIntravenousAmneal Agila, Llc2013-04-30Not applicableUs
Idarubicin HydrochlorideInjection, solution1 mg/mLIntravenousTeva Parenteral Medicines, Inc.2002-10-01Not applicableUs
Idarubicin HydrochlorideInjection20 mg/20mLIntravenousAmneal Agila, Llc2013-04-30Not applicableUs
Idarubicin HydrochlorideInjection, solution1 mg/mLIntravenousTeva Parenteral Medicines, Inc.2002-10-01Not applicableUs
Idarubicin HydrochlorideInjection, solution1 mg/mLIntravenousFresenius Kabi USA, LLC2009-08-11Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
IdamycinNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Idarubicin Hydrochloride
Thumb
  • InChI Key: JVHPTYWUBOQMBP-RVFAQHLVSA-N
  • Monoisotopic Mass: 533.145259206
  • Average Mass: 533.955
DBSALT000341
Categories
UNIIZRP63D75JW
CAS number58957-92-9
WeightAverage: 497.4939
Monoisotopic: 497.168581467
Chemical FormulaC26H27NO9
InChI KeyXDXDZDZNSLXDNA-TZNDIEGXSA-N
InChI
InChI=1S/C26H27NO9/c1-10-21(29)15(27)7-17(35-10)36-16-9-26(34,11(2)28)8-14-18(16)25(33)20-19(24(14)32)22(30)12-5-3-4-6-13(12)23(20)31/h3-6,10,15-17,21,29,32-34H,7-9,27H2,1-2H3/t10-,15-,16-,17-,21+,26-/m0/s1
IUPAC Name
(7S,9S)-9-acetyl-7-{[(2R,4S,5S,6S)-4-amino-5-hydroxy-6-methyloxan-2-yl]oxy}-6,9,11-trihydroxy-5,7,8,9,10,12-hexahydrotetracene-5,12-dione
SMILES
C[C@@H]1O[[email protected]](C[[email protected]](N)[C@@H]1O)O[[email protected]]1C[C@@](O)(CC2=C1C(O)=C1C(=O)C3=CC=CC=C3C(=O)C1=C2O)C(C)=O
Pharmacology
IndicationFor the treatment of acute myeloid leukemia (AML) in adults. This includes French-American-British (FAB) classifications M1 through M7.
Structured Indications
PharmacodynamicsIdarubicin is an antineoplastic in the anthracycline class. General properties of drugs in this class include: interaction with DNA in a variety of different ways including intercalation (squeezing between the base pairs), DNA strand breakage and inhibition with the enzyme topoisomerase II. Most of these compounds have been isolated from natural sources and antibiotics. However, they lack the specificity of the antimicrobial antibiotics and thus produce significant toxicity. The anthracyclines are among the most important antitumor drugs available. Doxorubicin is widely used for the treatment of several solid tumors while daunorubicin and idarubicin are used exclusively for the treatment of leukemia. Idarubicin may also inhibit polymerase activity, affect regulation of gene expression, and produce free radical damage to DNA. Idarubicin possesses an antitumor effect against a wide spectrum of tumors, either grafted or spontaneous. The anthracyclines are cell cycle-nonspecific.
Mechanism of actionIdarubicin has antimitotic and cytotoxic activity through a number of proposed mechanisms of action: Idarubicin forms complexes with DNA by intercalation between base pairs, and it inhibits topoisomerase II activity by stabilizing the DNA-topoisomerase II complex, preventing the religation portion of the ligation-religation reaction that topoisomerase II catalyzes.
TargetKindPharmacological actionActionsOrganismUniProt ID
DNANucleotideyes
intercalation
Humannot applicabledetails
DNA topoisomerase 2-alphaProteinyes
inhibitor
HumanP11388 details
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding97%
MetabolismNot Available
Route of eliminationThe drug is eliminated predominately by biliary and to a lesser extent by renal excretion, mostly in the form of idarubicinol.
Half life22 hours
ClearanceNot Available
ToxicityNot Available
Affected organisms
  • Humans and other mammals
  • Bacteria
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Idarubicin can be increased when it is combined with Abiraterone.Approved
AceclofenacAceclofenac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
AcetovanilloneAcetovanillone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Idarubicin.Approved
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
AdapaleneAdapalene may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
Alendronic acidIdarubicin may increase the hypocalcemic activities of Alendronic acid.Approved
ALT-110The risk or severity of adverse effects can be increased when Idarubicin is combined with ALT-110.Investigational
AmdinocillinThe serum concentration of Idarubicin can be decreased when it is combined with Amdinocillin.Withdrawn
AmiodaroneThe metabolism of Idarubicin can be decreased when combined with Amiodarone.Approved, Investigational
AmoxicillinThe serum concentration of Idarubicin can be decreased when it is combined with Amoxicillin.Approved, Vet Approved
Amphotericin BAmphotericin B may increase the nephrotoxic activities of Idarubicin.Approved, Investigational
AmpicillinThe serum concentration of Idarubicin can be decreased when it is combined with Ampicillin.Approved, Vet Approved
AnisodamineAnisodamine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
AntipyrineAntipyrine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Idarubicin.Investigational
ApremilastApremilast may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
AprepitantThe metabolism of Idarubicin can be increased when combined with Aprepitant.Approved, Investigational
ArtemetherThe metabolism of Idarubicin can be decreased when combined with Artemether.Approved
AtomoxetineThe metabolism of Idarubicin can be decreased when combined with Atomoxetine.Approved
Atracurium besylateIdarubicin may increase the respiratory depressant activities of Atracurium besylate.Approved
AzapropazoneAzapropazone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
AzelastineAzelastine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
AzidocillinThe serum concentration of Idarubicin can be decreased when it is combined with Azidocillin.Approved
AzlocillinThe serum concentration of Idarubicin can be decreased when it is combined with Azlocillin.Approved
BacampicillinThe serum concentration of Idarubicin can be decreased when it is combined with Bacampicillin.Approved
BalsalazideBalsalazide may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Idarubicin.Investigational
BenoxaprofenBenoxaprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
Benzathine benzylpenicillinThe serum concentration of Idarubicin can be decreased when it is combined with Benzathine benzylpenicillin.Approved, Vet Approved
BenzylpenicillinThe serum concentration of Idarubicin can be decreased when it is combined with Benzylpenicillin.Approved, Vet Approved
Benzylpenicillin PotassiumThe serum concentration of Idarubicin can be decreased when it is combined with Benzylpenicillin Potassium.Approved
Benzylpenicilloyl PolylysineThe serum concentration of Idarubicin can be decreased when it is combined with Benzylpenicilloyl Polylysine.Approved
BetaxololThe metabolism of Idarubicin can be decreased when combined with Betaxolol.Approved
Betulinic AcidBetulinic Acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Idarubicin.Approved, Investigational
Botulinum Toxin Type AIdarubicin may increase the neuromuscular blocking activities of Botulinum Toxin Type A.Approved, Investigational
Botulinum Toxin Type BIdarubicin may increase the neuromuscular blocking activities of Botulinum Toxin Type B.Approved
BromfenacBromfenac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
BucillamineBucillamine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
BumetanideThe risk or severity of adverse effects can be increased when Bumetanide is combined with Idarubicin.Approved
BupropionThe metabolism of Idarubicin can be decreased when combined with Bupropion.Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Idarubicin.Approved
CapecitabineThe metabolism of Idarubicin can be decreased when combined with Capecitabine.Approved, Investigational
CapreomycinCapreomycin may increase the neuromuscular blocking activities of Idarubicin.Approved
CarbamazepineThe metabolism of Idarubicin can be increased when combined with Carbamazepine.Approved, Investigational
CarbenicillinThe serum concentration of Idarubicin can be decreased when it is combined with Carbenicillin.Approved
CarboplatinIdarubicin may increase the ototoxic activities of Carboplatin.Approved
CarindacillinThe serum concentration of Idarubicin can be decreased when it is combined with Carindacillin.Approved
CarprofenCarprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved, Withdrawn
CastanospermineCastanospermine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Experimental
CDX-110The risk or severity of adverse effects can be increased when Idarubicin is combined with CDX-110.Investigational
CelecoxibCelecoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
CeritinibThe serum concentration of Idarubicin can be increased when it is combined with Ceritinib.Approved
ChloroquineChloroquine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
ChlorpromazineThe metabolism of Idarubicin can be decreased when combined with Chlorpromazine.Approved, Vet Approved
CholecalciferolThe metabolism of Idarubicin can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Idarubicin can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Idarubicin can be decreased when combined with Cinacalcet.Approved
Cisatracurium besylateIdarubicin may increase the respiratory depressant activities of Cisatracurium besylate.Approved
CisplatinCisplatin may increase the nephrotoxic activities of Idarubicin.Approved
CitalopramThe metabolism of Idarubicin can be decreased when combined with Citalopram.Approved
ClemastineThe metabolism of Idarubicin can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Idarubicin can be decreased when combined with Clobazam.Approved, Illicit
ClodronateIdarubicin may increase the hypocalcemic activities of Clodronate.Approved, Investigational, Vet Approved
ClomipramineThe metabolism of Idarubicin can be decreased when combined with Clomipramine.Approved, Vet Approved
ClonixinClonixin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
ClotrimazoleThe metabolism of Idarubicin can be decreased when combined with Clotrimazole.Approved, Vet Approved
CloxacillinThe serum concentration of Idarubicin can be decreased when it is combined with Cloxacillin.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Idarubicin is combined with Clozapine.Approved
CobicistatThe serum concentration of Idarubicin can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Idarubicin can be decreased when combined with Cocaine.Approved, Illicit
ColistimethateIdarubicin may increase the nephrotoxic activities of Colistimethate.Approved, Vet Approved
CurcuminCurcumin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
CyclacillinThe serum concentration of Idarubicin can be decreased when it is combined with Cyclacillin.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Idarubicin.Approved, Investigational
CyclosporineIdarubicin may increase the nephrotoxic activities of Cyclosporine.Approved, Investigational, Vet Approved
CyclosporineThe metabolism of Idarubicin can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
D-LimoneneD-Limonene may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
DabrafenibThe serum concentration of Idarubicin can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe metabolism of Idarubicin can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Idarubicin can be increased when it is combined with Darunavir.Approved
DecamethoniumIdarubicin may increase the respiratory depressant activities of Decamethonium.Approved
DelavirdineThe metabolism of Idarubicin can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Idarubicin.Approved
DesipramineThe metabolism of Idarubicin can be decreased when combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Idarubicin.Approved
DiclofenacDiclofenac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
DicloxacillinThe serum concentration of Idarubicin can be decreased when it is combined with Dicloxacillin.Approved, Vet Approved
DiflunisalDiflunisal may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Idarubicin.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Idarubicin.Approved
DiphenhydramineThe metabolism of Idarubicin can be decreased when combined with Diphenhydramine.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Idarubicin.Approved, Investigational
Domoic AcidIdarubicin may increase the respiratory depressant activities of Domoic Acid.Experimental
Doxacurium chlorideIdarubicin may increase the respiratory depressant activities of Doxacurium chloride.Approved
DronedaroneThe metabolism of Idarubicin can be decreased when combined with Dronedarone.Approved
DroxicamDroxicam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
DuloxetineThe metabolism of Idarubicin can be decreased when combined with Duloxetine.Approved
DuvelisibDuvelisib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
E6201E6201 may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
EbselenEbselen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
EfavirenzThe metabolism of Idarubicin can be decreased when combined with Efavirenz.Approved, Investigational
EliglustatThe metabolism of Idarubicin can be decreased when combined with Eliglustat.Approved
EpirizoleEpirizole may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
Etacrynic acidThe risk or severity of adverse effects can be increased when Etacrynic acid is combined with Idarubicin.Approved
EtanerceptEtanercept may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
Etidronic acidIdarubicin may increase the hypocalcemic activities of Etidronic acid.Approved
EtodolacEtodolac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
EtoricoxibEtoricoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
EtravirineThe metabolism of Idarubicin can be decreased when combined with Etravirine.Approved
Evening primrose oilEvening primrose oil may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
exisulindexisulind may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
FenbufenFenbufen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
FenoprofenFenoprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Idarubicin.Approved
FingolimodIdarubicin may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FloctafenineFloctafenine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Withdrawn
FloxuridineThe metabolism of Idarubicin can be decreased when combined with Floxuridine.Approved
FlucloxacillinThe serum concentration of Idarubicin can be decreased when it is combined with Flucloxacillin.Approved
FluconazoleThe metabolism of Idarubicin can be decreased when combined with Fluconazole.Approved
FlunixinFlunixin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Vet Approved
FluorouracilThe metabolism of Idarubicin can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Idarubicin can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlurbiprofenFlurbiprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
FluvastatinThe metabolism of Idarubicin can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Idarubicin can be decreased when combined with Fluvoxamine.Approved, Investigational
FoscarnetFoscarnet may increase the nephrotoxic activities of Idarubicin.Approved
FosphenytoinThe metabolism of Idarubicin can be increased when combined with Fosphenytoin.Approved
FurosemideThe risk or severity of adverse effects can be increased when Furosemide is combined with Idarubicin.Approved, Vet Approved
G17DTThe risk or severity of adverse effects can be increased when Idarubicin is combined with G17DT.Investigational
Gallamine TriethiodideIdarubicin may increase the respiratory depressant activities of Gallamine Triethiodide.Approved
GemfibrozilThe metabolism of Idarubicin can be decreased when combined with Gemfibrozil.Approved
GI-5005The risk or severity of adverse effects can be increased when Idarubicin is combined with GI-5005.Investigational
HaloperidolThe metabolism of Idarubicin can be decreased when combined with Haloperidol.Approved
HigenamineHigenamine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
HMPL-004HMPL-004 may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
IbandronateIdarubicin may increase the hypocalcemic activities of Ibandronate.Approved, Investigational
IbuprofenIbuprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
IbuproxamIbuproxam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
IcatibantIcatibant may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
ImipramineThe metabolism of Idarubicin can be decreased when combined with Imipramine.Approved
IndinavirThe metabolism of Idarubicin can be decreased when combined with Indinavir.Approved
IndomethacinIndomethacin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
IndoprofenIndoprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
INGN 201The risk or severity of adverse effects can be increased when Idarubicin is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Idarubicin is combined with INGN 225.Investigational
IrbesartanThe metabolism of Idarubicin can be decreased when combined with Irbesartan.Approved, Investigational
IsoniazidThe metabolism of Idarubicin can be decreased when combined with Isoniazid.Approved
IsoxicamIsoxicam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
KebuzoneKebuzone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Experimental
KetoconazoleThe metabolism of Idarubicin can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenKetoprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
KetorolacKetorolac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
LeflunomideThe risk or severity of adverse effects can be increased when Idarubicin is combined with Leflunomide.Approved, Investigational
LisofyllineLisofylline may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
LopinavirThe metabolism of Idarubicin can be decreased when combined with Lopinavir.Approved
LorcaserinThe metabolism of Idarubicin can be decreased when combined with Lorcaserin.Approved
LornoxicamLornoxicam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
LosartanThe metabolism of Idarubicin can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Idarubicin can be decreased when combined with Lovastatin.Approved, Investigational
LoxoprofenLoxoprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
LumacaftorThe serum concentration of Idarubicin can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Idarubicin can be decreased when combined with Lumefantrine.Approved
LumiracoxibLumiracoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
Magnesium salicylateMagnesium salicylate may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
MannitolMannitol may increase the nephrotoxic activities of Idarubicin.Approved, Investigational
MasoprocolMasoprocol may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
MecamylamineIdarubicin may increase the neuromuscular blocking activities of Mecamylamine.Approved
Meclofenamic acidMeclofenamic acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
Mefenamic acidMefenamic acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
MeloxicamMeloxicam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
MesalazineMesalazine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Idarubicin.Withdrawn
MethadoneThe metabolism of Idarubicin can be decreased when combined with Methadone.Approved
MethotrimeprazineThe metabolism of Idarubicin can be decreased when combined with Methotrimeprazine.Approved
MeticillinThe serum concentration of Idarubicin can be decreased when it is combined with Meticillin.Approved
MetocurineIdarubicin may increase the respiratory depressant activities of Metocurine.Approved
Metocurine IodideIdarubicin may increase the respiratory depressant activities of Metocurine Iodide.Withdrawn
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Idarubicin.Approved, Investigational
MezlocillinThe serum concentration of Idarubicin can be decreased when it is combined with Mezlocillin.Approved
MifepristoneThe serum concentration of Idarubicin can be increased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Idarubicin can be decreased when combined with Mirabegron.Approved
MivacuriumIdarubicin may increase the respiratory depressant activities of Mivacurium.Approved
MizoribineMizoribine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
Mycophenolate mofetilMycophenolate mofetil may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
Mycophenolic acidMycophenolic acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
NabumetoneNabumetone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
NafamostatNafamostat may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
NafcillinThe serum concentration of Idarubicin can be decreased when it is combined with Nafcillin.Approved
NaftifineNaftifine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
NaproxenNaproxen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
NatalizumabThe risk or severity of adverse effects can be increased when Idarubicin is combined with Natalizumab.Approved, Investigational
NCX 4016NCX 4016 may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
NeosaxitoxinIdarubicin may increase the respiratory depressant activities of Neosaxitoxin.Investigational
NepafenacNepafenac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
NevirapineThe metabolism of Idarubicin can be decreased when combined with Nevirapine.Approved
NicardipineThe metabolism of Idarubicin can be decreased when combined with Nicardipine.Approved
Niflumic AcidNiflumic Acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
NilotinibThe metabolism of Idarubicin can be decreased when combined with Nilotinib.Approved, Investigational
NimesulideNimesulide may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Withdrawn
NitroaspirinNitroaspirin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
OlopatadineOlopatadine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
OlsalazineOlsalazine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
OmeprazoleThe metabolism of Idarubicin can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OrgoteinOrgotein may decrease the excretion rate of Idarubicin which could result in a higher serum level.Vet Approved
OuabainOuabain may decrease the cardiotoxic activities of Idarubicin.Approved
OxacillinThe serum concentration of Idarubicin can be decreased when it is combined with Oxacillin.Approved
OxaprozinOxaprozin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
OxyphenbutazoneOxyphenbutazone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Idarubicin.Approved, Vet Approved
PamidronateIdarubicin may increase the hypocalcemic activities of Pamidronate.Approved
PancuroniumIdarubicin may increase the respiratory depressant activities of Pancuronium.Approved
PanobinostatThe serum concentration of Idarubicin can be increased when it is combined with Panobinostat.Approved, Investigational
ParecoxibParecoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
ParoxetineThe metabolism of Idarubicin can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Idarubicin can be decreased when it is combined with Peginterferon alfa-2b.Approved
PhenobarbitalThe metabolism of Idarubicin can be increased when combined with Phenobarbital.Approved
PhenoxymethylpenicillinThe serum concentration of Idarubicin can be decreased when it is combined with Phenoxymethylpenicillin.Approved, Vet Approved
PhenylbutazonePhenylbutazone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
PhenytoinThe metabolism of Idarubicin can be increased when combined with Phenytoin.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Idarubicin.Approved, Investigational
PipecuroniumIdarubicin may increase the respiratory depressant activities of Pipecuronium.Approved
PiperacillinThe serum concentration of Idarubicin can be decreased when it is combined with Piperacillin.Approved
PiretanideThe risk or severity of adverse effects can be increased when Piretanide is combined with Idarubicin.Experimental
PirfenidonePirfenidone may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
PiroxicamPiroxicam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
PivampicillinThe serum concentration of Idarubicin can be decreased when it is combined with Pivampicillin.Approved
PivmecillinamThe serum concentration of Idarubicin can be decreased when it is combined with Pivmecillinam.Approved
PrimidoneThe metabolism of Idarubicin can be increased when combined with Primidone.Approved, Vet Approved
Procaine benzylpenicillinThe serum concentration of Idarubicin can be decreased when it is combined with Procaine benzylpenicillin.Approved, Vet Approved
PromazineThe metabolism of Idarubicin can be decreased when combined with Promazine.Approved, Vet Approved
PropacetamolPropacetamol may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
PTC299PTC299 may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
PyrantelIdarubicin may increase the respiratory depressant activities of Pyrantel.Approved, Vet Approved
PyrimethamineThe metabolism of Idarubicin can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuinidineThe metabolism of Idarubicin can be decreased when combined with Quinidine.Approved
QuinineThe metabolism of Idarubicin can be decreased when combined with Quinine.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Idarubicin is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Idarubicin.Approved
RanolazineThe metabolism of Idarubicin can be decreased when combined with Ranolazine.Approved, Investigational
RapacuroniumIdarubicin may increase the respiratory depressant activities of Rapacuronium.Withdrawn
ResveratrolResveratrol may decrease the excretion rate of Idarubicin which could result in a higher serum level.Experimental, Investigational
RifampicinThe metabolism of Idarubicin can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Idarubicin can be increased when combined with Rifapentine.Approved
RisedronateIdarubicin may increase the hypocalcemic activities of Risedronate.Approved, Investigational
RitonavirThe metabolism of Idarubicin can be decreased when combined with Ritonavir.Approved, Investigational
RocuroniumIdarubicin may increase the respiratory depressant activities of Rocuronium.Approved
RofecoxibRofecoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational, Withdrawn
RoflumilastRoflumilast may increase the immunosuppressive activities of Idarubicin.Approved
RolapitantThe metabolism of Idarubicin can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Idarubicin can be decreased when combined with Ropinirole.Approved, Investigational
SalicylamideSalicylamide may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
Salicylic acidSalicylic acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Vet Approved
SalsalateSalsalate may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
SecobarbitalThe metabolism of Idarubicin can be increased when combined with Secobarbital.Approved, Vet Approved
SeratrodastSeratrodast may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
SertralineThe metabolism of Idarubicin can be decreased when combined with Sertraline.Approved
SildenafilThe metabolism of Idarubicin can be decreased when combined with Sildenafil.Approved, Investigational
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Idarubicin.Approved
SorafenibThe metabolism of Idarubicin can be decreased when combined with Sorafenib.Approved, Investigational
SRP 299The risk or severity of adverse effects can be increased when Idarubicin is combined with SRP 299.Investigational
SRT501SRT501 may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
StiripentolThe metabolism of Idarubicin can be decreased when combined with Stiripentol.Approved
SuccinylcholineIdarubicin may increase the respiratory depressant activities of Succinylcholine.Approved
SulbactamThe serum concentration of Idarubicin can be decreased when it is combined with Sulbactam.Approved
SulfadiazineThe metabolism of Idarubicin can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Idarubicin can be decreased when combined with Sulfamethoxazole.Approved
SulfasalazineSulfasalazine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
SulfisoxazoleThe metabolism of Idarubicin can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
SultamicillinThe serum concentration of Idarubicin can be decreased when it is combined with Sultamicillin.Investigational
SuprofenSuprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Withdrawn
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Idarubicin.Approved, Investigational
TazobactamThe serum concentration of Idarubicin can be decreased when it is combined with Tazobactam.Approved
Technetium tc 99m etidronateIdarubicin may increase the hypocalcemic activities of Technetium tc 99m etidronate.Approved
Technetium Tc-99m MedronateIdarubicin may increase the hypocalcemic activities of Technetium Tc-99m Medronate.Approved
TenofovirThe serum concentration of Idarubicin can be increased when it is combined with Tenofovir.Approved, Investigational
TenoxicamTenoxicam may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
TepoxalinTepoxalin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Vet Approved
TerbinafineThe metabolism of Idarubicin can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TeriflunomideTeriflunomide may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
TG4010The risk or severity of adverse effects can be increased when Idarubicin is combined with TG4010.Investigational
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Idarubicin.Approved
Tiaprofenic acidTiaprofenic acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
TicagrelorThe metabolism of Idarubicin can be decreased when combined with Ticagrelor.Approved
TicarcillinThe serum concentration of Idarubicin can be decreased when it is combined with Ticarcillin.Approved, Vet Approved
TiclopidineThe metabolism of Idarubicin can be decreased when combined with Ticlopidine.Approved
TiludronateIdarubicin may increase the hypocalcemic activities of Tiludronate.Approved, Vet Approved
TinoridineTinoridine may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational
TipranavirThe metabolism of Idarubicin can be decreased when combined with Tipranavir.Approved, Investigational
TofacitinibIdarubicin may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolbutamideThe metabolism of Idarubicin can be decreased when combined with Tolbutamide.Approved
Tolfenamic AcidTolfenamic Acid may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
TolmetinTolmetin may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
TorasemideThe risk or severity of adverse effects can be increased when Torasemide is combined with Idarubicin.Approved
TranilastTranilast may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational
TranylcypromineThe metabolism of Idarubicin can be decreased when combined with Tranylcypromine.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Idarubicin.Approved, Investigational
TrimethoprimThe metabolism of Idarubicin can be decreased when combined with Trimethoprim.Approved, Vet Approved
Trisalicylate-cholineTrisalicylate-choline may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
TubocurarineIdarubicin may increase the respiratory depressant activities of Tubocurarine.Approved
ValdecoxibValdecoxib may decrease the excretion rate of Idarubicin which could result in a higher serum level.Investigational, Withdrawn
Valproic AcidThe metabolism of Idarubicin can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Idarubicin can be decreased when combined with Valsartan.Approved, Investigational
VancomycinVancomycin may increase the nephrotoxic activities of Idarubicin.Approved
VecuroniumIdarubicin may increase the respiratory depressant activities of Vecuronium.Approved
VenlafaxineThe metabolism of Idarubicin can be decreased when combined with Venlafaxine.Approved
VoriconazoleThe metabolism of Idarubicin can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Idarubicin can be decreased when combined with Zafirlukast.Approved, Investigational
ZaltoprofenZaltoprofen may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved
ZileutonZileuton may decrease the excretion rate of Idarubicin which could result in a higher serum level.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Idarubicin can be decreased when combined with Ziprasidone.Approved
Zoledronic acidIdarubicin may increase the hypocalcemic activities of Zoledronic acid.Approved
ZomepiracZomepirac may decrease the excretion rate of Idarubicin which could result in a higher serum level.Withdrawn
Food InteractionsNot Available
References
Synthesis Reference

Marco Villa, Roberto Arosio, Roberta Fretta, Nicola Diulgheroff, “Synthesis of idarubicin aglycone.” U.S. Patent US20060047108, issued March 02, 2006.

US20060047108
General ReferencesNot Available
External Links
ATC CodesL01DB06
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelNot Available
MSDSNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.5153
Blood Brain Barrier-0.975
Caco-2 permeable-0.7492
P-glycoprotein substrateSubstrate0.7862
P-glycoprotein inhibitor INon-inhibitor0.7328
P-glycoprotein inhibitor IINon-inhibitor0.956
Renal organic cation transporterNon-inhibitor0.9214
CYP450 2C9 substrateNon-substrate0.8004
CYP450 2D6 substrateNon-substrate0.8937
CYP450 3A4 substrateSubstrate0.5419
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.9439
CYP450 2D6 inhibitorNon-inhibitor0.9382
CYP450 2C19 inhibitorNon-inhibitor0.9316
CYP450 3A4 inhibitorNon-inhibitor0.9514
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.9516
Ames testAMES toxic0.9107
CarcinogenicityNon-carcinogens0.9456
BiodegradationNot ready biodegradable0.9762
Rat acute toxicity4.3474 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9896
hERG inhibition (predictor II)Non-inhibitor0.882
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
CapsuleOral10 mg
CapsuleOral25 mg
CapsuleOral5 mg
SolutionIntravenous1 mg/mL
SolutionIntravenous1 mg
Powder, for solutionIntravenous10 mg
Powder, for solutionIntravenous5 mg
InjectionIntravenous1 mg/mL
InjectionIntravenous10 mg/10mL
InjectionIntravenous20 mg/20mL
InjectionIntravenous5 mg/5mL
Injection, solutionIntravenous1 mg/mL
Prices
Unit descriptionCostUnit
Idamycin pfs 1 mg/ml vial60.0USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
PatentsNot Available
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP0.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.772 mg/mLALOGPS
logP1.69ALOGPS
logP1.9ChemAxon
logS-2.8ALOGPS
pKa (Strongest Acidic)9.55ChemAxon
pKa (Strongest Basic)8.95ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count10ChemAxon
Hydrogen Donor Count5ChemAxon
Polar Surface Area176.61 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity126.43 m3·mol-1ChemAxon
Polarizability50.33 Å3ChemAxon
Number of Rings5ChemAxon
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 organic compounds known as anthracyclines. These are polyketides containing a tetracenequinone ring structure with a sugar attached by glycosidic linkage.
KingdomOrganic compounds
Super ClassPhenylpropanoids and polyketides
ClassAnthracyclines
Sub ClassNot Available
Direct ParentAnthracyclines
Alternative Parents
Substituents
  • Anthracyclinone-skeleton
  • Anthracycline
  • Tetracenequinone
  • 1,4-anthraquinone
  • 9,10-anthraquinone
  • Anthracene
  • Amino sugar
  • Tetralin
  • Aryl ketone
  • Hydroquinone
  • Amino saccharide
  • Benzenoid
  • Oxane
  • Monosaccharide
  • Saccharide
  • Vinylogous acid
  • Tertiary alcohol
  • Alpha-hydroxy ketone
  • Secondary alcohol
  • Polyol
  • Ketone
  • 1,2-aminoalcohol
  • Oxacycle
  • Organoheterocyclic compound
  • Acetal
  • Hydrocarbon derivative
  • Primary amine
  • Organooxygen compound
  • Organonitrogen compound
  • Primary aliphatic amine
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

1. DNA
Kind
Nucleotide
Organism
Human
Pharmacological action
yes
Actions
intercalation
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. Zahraei Z, Rabbani-Chadegani A: A comparison of the effect of anticancer drugs, idarubicin and adriamycin, on soluble chromatin. Eur J Pharmacol. 2007 Dec 1;575(1-3):28-33. Epub 2007 Jul 31. [PubMed:17716648 ]
  2. Hollingshead LM, Faulds D: Idarubicin. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in the chemotherapy of cancer. Drugs. 1991 Oct;42(4):690-719. [PubMed:1723369 ]
  3. Bigioni M, Zunino F, Capranico G: Base mutation analysis of topoisomerase II-idarubicin-DNA ternary complex formation. Evidence for enzyme subunit cooperativity in DNA cleavage. Nucleic Acids Res. 1994 Jun 25;22(12):2274-81. [PubMed:8036155 ]
  4. Fukushima T, Ueda T, Uchida M, Nakamura T: Action mechanism of idarubicin (4-demethoxydaunorubicin) as compared with daunorubicin in leukemic cells. Int J Hematol. 1993 Apr;57(2):121-30. [PubMed:8494991 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Ubiquitin binding
Specific Function:
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segregation of daughter chromosomes. May play a role in regulating the period length of ARNTL/BMAL1 transcriptional oscillation (By similarity).
Gene Name:
TOP2A
Uniprot ID:
P11388
Molecular Weight:
174383.88 Da
References
  1. Willmore E, Errington F, Tilby MJ, Austin CA: Formation and longevity of idarubicin-induced DNA topoisomerase II cleavable complexes in K562 human leukaemia cells. Biochem Pharmacol. 2002 May 15;63(10):1807-15. [PubMed:12034365 ]
  2. Zhou R, Wang Y, Gruber A, Larsson R, Castanos-Velez E, Liliemark E: Topoisomerase II-mediated alterations of K562 drug resistant sublines. Med Oncol. 1999 Sep;16(3):191-8. [PubMed:10523799 ]
  3. De Renzo A, Santoro LF, Notaro R, Pane F, Buonaiuto MR, Luciano L, Rotoli B: Acute promyelocytic leukemia after treatment for non-Hodgkin's lymphoma with drugs targeting topoisomerase II. Am J Hematol. 1999 Apr;60(4):300-4. [PubMed:10203104 ]
  4. Gonzalez-Cid M, Fundia AF, Cuello MT, Larripa I: Correlation between chromosome damage and apoptosis induced by fludarabine and idarubicin in normal human lymphocytes. Toxicology. 2002 Feb 28;171(2-3):215-22. [PubMed:11836027 ]
  5. Bigioni M, Zunino F, Capranico G: Base mutation analysis of topoisomerase II-idarubicin-DNA ternary complex formation. Evidence for enzyme subunit cooperativity in DNA cleavage. Nucleic Acids Res. 1994 Jun 25;22(12):2274-81. [PubMed:8036155 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Transporter activity
Specific Function:
Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotrexate, antiviral drugs and other xenobiotics. Confers resistance to anticancer drugs. Hydrolyzes ATP with low efficiency.
Gene Name:
ABCC1
Uniprot ID:
P33527
Molecular Weight:
171589.5 Da
References
  1. Heijn M, Hooijberg JH, Scheffer GL, Szabo G, Westerhoff HV, Lankelma J: Anthracyclines modulate multidrug resistance protein (MRP) mediated organic anion transport. Biochim Biophys Acta. 1997 May 22;1326(1):12-22. [PubMed:9188796 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23