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Identification
NameIrinotecan
Accession NumberDB00762  (APRD00579)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionIrinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. It is a derivative of camptothecin that inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex, and causes double-strand DNA breakage and cell death. It is a derivative of camptothecin. Irinotecan was approved for the treatment of advanced pancreatic cancer in October, 2015 (irinotecan liposome injection, trade name Onivyde).
Structure
Thumb
Synonyms
Biotecan
Camptothecin-11
External Identifiers
  • CPT-11
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
CamptosarInjection, solution20 mg/mLIntravenousPharmacia And Upjohn Company Llc1996-06-14Not applicableUs
CamptosarInjection, solution20 mg/mLIntravenousPharmacia And Upjohn Company Llc1996-06-14Not applicableUs
Camptosar InjectionSolution20 mgIntravenousPfizer Canada Inc1997-08-27Not applicableCanada
IrinotecanSolution20 mgIntravenousPfizer Canada Inc2014-03-07Not applicableCanada
Irinotecan for InjectionSolution20 mgIntravenousTeva Canada Limited2008-10-31Not applicableCanada
Irinotecan Hydrochloride InjectionSolution20 mgIntravenousTeligent Ou2015-05-28Not applicableCanada
Irinotecan Hydrochloride InjectionSolution20 mgIntravenousHospira Healthcare Corporation2006-02-01Not applicableCanada
Irinotecan Hydrochloride Injection, USPSolution20 mgIntravenousQilu Pharmaceuticals Co. LtdNot applicableNot applicableCanada
Irinotecan Hydrochloride Trihydrate for InjectionSolution20 mgIntravenousAccord Healthcare Inc2013-05-06Not applicableCanada
Irinotecan Hydrochloride Trihydrate for InjectionSolution20 mgIntravenousFresenius Kabi Canada Ltd2011-05-27Not applicableCanada
Irinotecan Hydrochloride Trihydrate InjectionSolution20 mgIntravenousSandoz Canada Incorporated2008-01-30Not applicableCanada
OnivydeInjection4.3 mg/mLIntravenousMerrimack Pharmaceuticals2015-10-22Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Irinotecan HydrochlorideInjection100 mg/5mLIntravenousSun Pharma Global FZE2008-04-21Not applicableUs
Irinotecan HydrochlorideInjection20 mg/mLIntravenousWest ward Pharmaceutical Corp2010-12-20Not applicableUs
Irinotecan HydrochlorideInjection, solution20 mg/mLIntravenousActavis Pharma, Inc.2015-01-05Not applicableUs
Irinotecan HydrochlorideInjection20 mg/mLIntravenousAreva Pharmaceuticals,Inc.2008-02-20Not applicableUs
Irinotecan HydrochlorideInjection20 mg/mLIntravenousHeritage Pharmaceuticals Inc.2012-06-20Not applicableUs
Irinotecan HydrochlorideInjection, solution20 mg/mLIntravenousSandoz Inc2009-11-30Not applicableUs
Irinotecan HydrochlorideInjection20 mg/mLIntravenousWest ward Pharmaceutical Corp2010-12-20Not applicableUs
Irinotecan HydrochlorideInjection, solution20 mg/mLIntravenousSagent Pharmaceuticals2014-08-15Not applicableUs
Irinotecan HydrochlorideInjection, solution20 mg/mLIntravenousSagent Pharmaceuticals2012-04-20Not applicableUs
Irinotecan HydrochlorideInjection, solution20 mg/mLIntravenousFresenius Kabi USA, LLC2009-04-01Not applicableUs
Irinotecan HydrochlorideInjection, solution40 mg/2mLIntravenousTeva Parenteral Medicines, Inc.2008-02-28Not applicableUs
Irinotecan HydrochlorideInjection20 mg/mLIntravenousBlue Point Laboratories2008-02-20Not applicableUs
Irinotecan HydrochlorideInjection40 mg/2mLIntravenousSun Pharma Global FZE2008-04-21Not applicableUs
Irinotecan HydrochlorideInjection20 mg/mLIntravenousWest Ward Pharmaceuticals Corp2010-12-20Not applicableUs
Irinotecan HydrochlorideInjection, solution100 mg/5mLIntravenousTeva Parenteral Medicines, Inc.2008-02-27Not applicableUs
Irinotecan HydrochlorideInjection, solution20 mg/mLIntravenousHospira, Inc.2008-02-27Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
CamptoYakultHonsha Co. Ltd.
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Irinotecan hydrochloride
100286-90-6
Thumb
  • InChI Key: GURKHSYORGJETM-WAQYZQTGSA-N
  • Monoisotopic Mass: 622.255812707
  • Average Mass: 623.139
DBSALT000103
Irinotecan hydrochloride hydrate
136572-09-3
Thumb
  • InChI Key: OHNBIIZWIUBGTK-NYPSMHOZSA-N
  • Monoisotopic Mass: 640.2663774
  • Average Mass: 641.16
DBSALT001805
Categories
UNII7673326042
CAS number97682-44-5
WeightAverage: 586.678
Monoisotopic: 586.279134968
Chemical FormulaC33H38N4O6
InChI KeyUWKQSNNFCGGAFS-XIFFEERXSA-N
InChI
InChI=1S/C33H38N4O6/c1-3-22-23-16-21(43-32(40)36-14-10-20(11-15-36)35-12-6-5-7-13-35)8-9-27(23)34-29-24(22)18-37-28(29)17-26-25(30(37)38)19-42-31(39)33(26,41)4-2/h8-9,16-17,20,41H,3-7,10-15,18-19H2,1-2H3/t33-/m0/s1
IUPAC Name
(19S)-10,19-diethyl-19-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.0²,¹¹.0⁴,⁹.0¹⁵,²⁰]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-7-yl 4-(piperidin-1-yl)piperidine-1-carboxylate
SMILES
CCC1=C2CN3C(=CC4=C(COC(=O)[C@]4(O)CC)C3=O)C2=NC2=C1C=C(OC(=O)N1CCC(CC1)N1CCCCC1)C=C2
Pharmacology
IndicationFor the treatment of metastatic colorectal cancer (first-line therapy when administered with 5-fluorouracil and leucovorin). Also used in combination with cisplatin for the treatment of extensive small cell lung cancer. Irinotecan is currently under investigation for the treatment of metastatic or recurrent cervical cancer. Also used in combination with fluorouracil and leucovorin for the treatment of patients with metastatic adenocarcinoma of the pancreas after disease progression following gemcitabine-based therapy.
Structured Indications
PharmacodynamicsIrinotecan is an antineoplastic enzyme inhibitor primarily used in the treatment of colorectal cancer. Irinotecan is a semisynthetic derivative of camptothecin. Camptothecins interact specifically with topoisomerase I, an enzyme in the cell nucleus that regulates DNA topology and facilitates nuclear processes such as DNA replication, recombination, and repair. During these processes, topoisomerase I relieves torsional strain in DNA by inducing reversible single-strand breaks, allowing single DNA strands to pass through the break. The 3'-DNA terminus of the broken DNA strands bind covalently with the topoisomerase enzyme to form a catalytic intermediate called a cleavable complex. After the DNA is sufficiently relaxed and the strand passage reaction is complete, DNA topoisomerase reattaches the broken DNA strands to form the chemically unaltered topoisomers that allow transcription to proceed. Irinotecan and its active metabolite SN-38 bind to the topoisomerase I-DNA complex and prevent religation of these single-strand breaks. Current research suggests that the cytotoxicity of irinotecan is due to double-strand DNA damage produced during DNA synthesis when replication enzymes interact with the ternary complex formed by topoisomerase I, DNA, and either Irinotecan or SN-38. Mammalian cells cannot efficiently repair these double-strand breaks. The precise contribution of SN-38 to the activity of irinotecan in humans is not known. Irinotecan is cell cycle phase-specific (S-phase).
Mechanism of actionIrinotecan inhibits the action of topoisomerase I. Irinotecan prevents religation of the DNA strand by binding to topoisomerase I-DNA complex. The formation of this ternary complex interferes with the moving replication fork, which induces replication arrest and lethal double-stranded breaks in DNA. As a result, DNA damage is not efficiently repaired and apoptosis (programmed cell death) occurs.
TargetKindPharmacological actionActionsOrganismUniProt ID
DNA topoisomerase I, mitochondrialProteinyes
inhibitor
HumanQ969P6 details
DNA topoisomerase 1Proteinyes
inhibitor
HumanP11387 details
Related Articles
AbsorptionThe maximum plasma concentration (Cmax) when a dose of 125 mg/m^2 is given to patients with solid tumours is 1660 ng/mL. The AUC (0-24) is 10,200 ng·h/mL. The Cmax when a dose of 340 mg/m^2 is given to patients with solid tumours is 3392 ng/mL. The AUC (0-24) is 20,604 ng·h/mL.
Volume of distribution

The volume of distribution of terminal elimination phase is 110 L/m^2 when a dose of 125 mg/m^2 is given to patients with solid tumours. The volume of distribution of terminal elimination phase is 234 L/m^2 when a dose of 340 mg/m^2 is given to patients with solid tumours.

Protein binding30%-68% protein bound, mainly to albumin.
Metabolism

Hepatic. The metabolic conversion of irinotecan to the active metabolite SN-38 is mediated by carboxylesterase enzymes and primarily occurs in the liver. SN-38 is subsequently conjugated predominantly by the enzyme UDP-glucuronosyl transferase 1A1 (UGT1A1) to form a glucuronide metabolite.

SubstrateEnzymesProduct
Irinotecan
SN-38Details
Route of eliminationThe cumulative biliary and urinary excretion of irinotecan and its metabolites (SN-38 and SN-38 glucuronide) over a period of 48 hours following administration of irinotecan in two patients ranged from approximately 25% (100 mg/m2) to 50% (300 mg/m2).
Half lifeThe half life of irinotecan is about 6 - 12 hours. The terminal elimination half-life of the active metabolite, SN-38 is 10 - 20 hours.
Clearance
  • 13.3 L/h/m^2 [Dose of 125 mg/m^2, patients with solid tumours]
  • 13.9 L/h/m^2 [Dose of 340 mg/m^2, patients with solid tumours]
ToxicityGastrointestinal complications, such as nausea, vomiting, abdominal cramping, diarrhea, and infection.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Irinotecan Action PathwayDrug actionSMP00433
Irinotecan Metabolism PathwayDrug metabolismSMP00600
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug Reactions
Interacting Gene/EnzymeSNP RS IDAllele nameDefining changeAdverse ReactionReference(s)
Solute carrier organic anion transporter family member 1B1
Gene symbol: SLCO1B1
UniProt: Q9Y6L6
rs4149056 SLCO1B1*15C AlleleDiarrhea, leucopenia, neutropenia17898662
Solute carrier organic anion transporter family member 1B1
Gene symbol: SLCO1B1
UniProt: Q9Y6L6
rs2306283 SLCO1B1*15G AlleleDiarrhea, leucopenia, neutropenia17898662
UDP-glucuronosyltransferase 1-1
Gene symbol: UGT1A1
UniProt: P22309
rs8175347 UGT1A1*28 or UGT1A 7/7extra TA in promoterLeukopenia, thrombpocytopenia17681105
UDP-glucuronosyltransferase 1-7
Gene symbol: UGT1A7
UniProt: Q9HAW7
rs17868323 Not AvailableG alleleLeukopenia, thrombpocytopenia18349289
UDP-glucuronosyltransferase 1-7
Gene symbol: UGT1A7
UniProt: Q9HAW7
rs17863778 Not AvailableA alleleLeukopenia, thrombpocytopenia18349289
UDP-glucuronosyltransferase 1-7
Gene symbol: UGT1A7
UniProt: Q9HAW7
rs17868324 Not AvailableA alleleLeukopenia, thrombpocytopenia18349289
UDP-glucuronosyltransferase 1-1
Gene symbol: UGT1A1
UniProt: P22309
rs10929302 Not AvailableA AlleleHematological toxicity, neutropenia17510208
Interactions
Drug Interactions
DrugInteractionDrug group
AcetaminophenThe serum concentration of Irinotecan can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Irinotecan.Approved
AdenineThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Adenine.Approved, Nutraceutical
AfatinibThe serum concentration of Irinotecan can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Irinotecan can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Irinotecan can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Irinotecan can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Irinotecan can be increased when it is combined with Alfentanil.Approved, Illicit
ALT-110The risk or severity of adverse effects can be increased when Irinotecan is combined with ALT-110.Investigational
AmantadineThe serum concentration of Irinotecan can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Irinotecan can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Irinotecan can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Irinotecan can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Irinotecan can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Irinotecan can be increased when it is combined with Amsacrine.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Irinotecan.Investigational
AprepitantThe serum concentration of Irinotecan can be increased when it is combined with Aprepitant.Approved, Investigational
AstemizoleThe serum concentration of Irinotecan can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Irinotecan can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Irinotecan can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Irinotecan can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Irinotecan can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Irinotecan can be increased when it is combined with Azithromycin.Approved
BcgThe therapeutic efficacy of Bcg can be decreased when used in combination with Irinotecan.Investigational
BenzocaineThe serum concentration of Irinotecan can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Irinotecan can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabThe risk or severity of adverse effects can be increased when Bevacizumab is combined with Irinotecan.Approved, Investigational
BexaroteneThe serum concentration of Irinotecan can be decreased when it is combined with Bexarotene.Approved, Investigational
BiperidenThe serum concentration of Irinotecan can be increased when it is combined with Biperiden.Approved
BoceprevirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Boceprevir.Approved
BortezomibThe metabolism of Irinotecan can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Irinotecan can be decreased when it is combined with Bosentan.Approved, Investigational
BosutinibThe serum concentration of Irinotecan can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Irinotecan can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Irinotecan can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Irinotecan can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Irinotecan.Approved
CaffeineThe serum concentration of Irinotecan can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Irinotecan can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Irinotecan can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Irinotecan can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Carbamazepine resulting in a loss in efficacy.Approved, Investigational
CarvedilolThe serum concentration of Irinotecan can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Irinotecan can be increased when it is combined with Caspofungin.Approved
CDX-110The risk or severity of adverse effects can be increased when Irinotecan is combined with CDX-110.Investigational
CeritinibThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Ceritinib.Approved
ChloroquineThe serum concentration of Irinotecan can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Irinotecan can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Irinotecan can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Irinotecan can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Irinotecan can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Irinotecan can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Irinotecan can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Irinotecan can be decreased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Irinotecan can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Irinotecan can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Clarithromycin.Approved
ClemastineThe metabolism of Irinotecan can be decreased when combined with Clemastine.Approved
ClofazimineThe serum concentration of Irinotecan can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Irinotecan can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClopidogrelThe metabolism of Irinotecan can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Irinotecan can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe risk or severity of adverse effects can be increased when Irinotecan is combined with Clozapine.Approved
CobicistatThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Cobicistat.Approved
ColchicineThe serum concentration of Irinotecan can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Irinotecan can be increased when it is combined with Colforsin.Experimental
ConivaptanThe serum concentration of Irinotecan can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Irinotecan can be decreased when combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Irinotecan.Approved, Investigational
CyclosporineThe metabolism of Irinotecan can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Irinotecan can be decreased when it is combined with Dabrafenib.Approved
DaclatasvirThe serum concentration of Irinotecan can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Irinotecan can be increased when it is combined with Dactinomycin.Approved
DarunavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Darunavir.Approved
DasatinibThe serum concentration of Irinotecan can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Irinotecan can be decreased when it is combined with Daunorubicin.Approved
DeferasiroxThe serum concentration of Irinotecan can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Irinotecan can be decreased when combined with Delavirdine.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Irinotecan.Approved
DesipramineThe serum concentration of Irinotecan can be increased when it is combined with Desipramine.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Irinotecan.Approved
DesloratadineThe serum concentration of Irinotecan can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Irinotecan can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe serum concentration of Irinotecan can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Irinotecan can be increased when it is combined with Diclofenac.Approved, Vet Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Irinotecan.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Irinotecan.Approved
DihydroergotamineThe metabolism of Irinotecan can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Irinotecan can be decreased when combined with Diltiazem.Approved
DipyridamoleThe serum concentration of Irinotecan can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Irinotecan.Approved, Investigational
DoxazosinThe serum concentration of Irinotecan can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Irinotecan can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Irinotecan can be decreased when it is combined with Doxorubicin.Approved, Investigational
DoxycyclineThe metabolism of Irinotecan can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Irinotecan can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe metabolism of Irinotecan can be decreased when combined with Dronedarone.Approved
EfavirenzThe serum concentration of Irinotecan can be decreased when it is combined with Efavirenz.Approved, Investigational
ElbasvirThe serum concentration of Irinotecan can be increased when it is combined with Elbasvir.Approved
EltrombopagThe serum concentration of Irinotecan can be increased when it is combined with Eltrombopag.Approved
EnalaprilThe serum concentration of Irinotecan can be increased when it is combined with Enalapril.Approved, Vet Approved
EnzalutamideThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Enzalutamide resulting in a loss in efficacy.Approved
ErgonovineThe serum concentration of Irinotecan can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Irinotecan can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Erlotinib.Approved, Investigational
ErythromycinThe metabolism of Irinotecan can be decreased when combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Irinotecan can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstramustineThe serum concentration of Irinotecan can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Irinotecan can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Irinotecan can be decreased when it is combined with Estrone.Approved
EtoposideThe serum concentration of Irinotecan can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Irinotecan can be decreased when it is combined with Etravirine.Approved
FelodipineThe serum concentration of Irinotecan can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Irinotecan can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Irinotecan can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Irinotecan can be increased when it is combined with Fidaxomicin.Approved
FingolimodIrinotecan may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe metabolism of Irinotecan can be decreased when combined with Fluconazole.Approved
FlunitrazepamThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Flunitrazepam.Approved, Illicit
FluoxetineThe serum concentration of Irinotecan can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Irinotecan can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Irinotecan can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Irinotecan can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe metabolism of Irinotecan can be decreased when combined with Fluvoxamine.Approved, Investigational
FosamprenavirThe metabolism of Irinotecan can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Irinotecan can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Fosphenytoin resulting in a loss in efficacy.Approved
Fusidic AcidThe serum concentration of Irinotecan can be increased when it is combined with Fusidic Acid.Approved
G17DTThe risk or severity of adverse effects can be increased when Irinotecan is combined with G17DT.Investigational
GefitinibThe serum concentration of Irinotecan can be increased when it is combined with Gefitinib.Approved, Investigational
GemfibrozilThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Gemfibrozil.Approved
GenisteinThe serum concentration of Irinotecan can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Irinotecan is combined with GI-5005.Investigational
GlyburideThe serum concentration of Irinotecan can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Irinotecan can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Irinotecan can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Irinotecan can be increased when it is combined with Grepafloxacin.Withdrawn
HaloperidolThe serum concentration of Irinotecan can be increased when it is combined with Haloperidol.Approved
HydrocortisoneThe serum concentration of Irinotecan can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Irinotecan can be increased when it is combined with Idelalisib.Approved
ImatinibThe metabolism of Irinotecan can be decreased when combined with Imatinib.Approved
ImipramineThe serum concentration of Irinotecan can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Indinavir.Approved
IndomethacinThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Irinotecan is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Irinotecan is combined with INGN 225.Investigational
IsavuconazoniumThe metabolism of Irinotecan can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Irinotecan can be decreased when combined with Isradipine.Approved
ItraconazoleThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Irinotecan can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Irinotecan can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Irinotecan can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Irinotecan can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Irinotecan can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Irinotecan is combined with Leflunomide.Approved, Investigational
LevofloxacinThe serum concentration of Irinotecan can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Irinotecan can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Irinotecan can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Irinotecan can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Irinotecan can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Irinotecan can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Irinotecan can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Irinotecan can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Lopinavir.Approved
LoratadineThe serum concentration of Irinotecan can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Irinotecan can be increased when it is combined with Losartan.Approved
LovastatinThe metabolism of Irinotecan can be decreased when combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Irinotecan can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Lumacaftor resulting in a loss in efficacy.Approved
MaprotilineThe serum concentration of Irinotecan can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Irinotecan can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Irinotecan can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Irinotecan can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Irinotecan 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 Irinotecan.Withdrawn
MethadoneThe serum concentration of Irinotecan can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Irinotecan can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Irinotecan can be increased when it is combined with Mibefradil.Withdrawn
MiconazoleThe serum concentration of Irinotecan can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Irinotecan can be decreased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Irinotecan can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Irinotecan can be increased when it is combined with Mitomycin.Approved
MitotaneThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Mitotane resulting in a loss in efficacy.Approved
MitoxantroneThe serum concentration of Irinotecan can be decreased when it is combined with Mitoxantrone.Approved, Investigational
ModafinilThe serum concentration of Irinotecan can be decreased when it is combined with Modafinil.Approved, Investigational
MorphineThe serum concentration of Irinotecan can be increased when it is combined with Morphine.Approved, Investigational
NafcillinThe serum concentration of Irinotecan can be decreased when it is combined with Nafcillin.Approved
NaltrexoneThe serum concentration of Irinotecan can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Irinotecan can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Irinotecan is combined with Natalizumab.Approved, Investigational
NefazodoneThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Nelfinavir.Approved
NeostigmineThe serum concentration of Irinotecan can be increased when it is combined with Neostigmine.Approved, Vet Approved
NetupitantThe serum concentration of Irinotecan can be increased when it is combined with Netupitant.Approved
NevirapineThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Nevirapine resulting in a loss in efficacy.Approved
NicardipineThe serum concentration of Irinotecan can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Irinotecan can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Irinotecan can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Irinotecan can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Irinotecan can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Irinotecan can be decreased when it is combined with Norethisterone.Approved
OlaparibThe metabolism of Irinotecan can be decreased when combined with Olaparib.Approved
OmeprazoleThe serum concentration of Irinotecan can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OsimertinibThe serum concentration of Irinotecan can be increased when it is combined with Osimertinib.Approved
OuabainOuabain may decrease the cardiotoxic activities of Irinotecan.Approved
P-NitrophenolThe serum concentration of Irinotecan can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Irinotecan.Approved, Vet Approved
PalbociclibThe serum concentration of Irinotecan can be increased when it is combined with Palbociclib.Approved
Palmitic AcidThe serum concentration of Irinotecan can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Irinotecan can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Irinotecan can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Pazopanib.Approved
PentobarbitalThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Pentobarbital resulting in a loss in efficacy.Approved, Vet Approved
PerindoprilThe serum concentration of Irinotecan can be increased when it is combined with Perindopril.Approved
PhenobarbitalThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Phenobarbital resulting in a loss in efficacy.Approved
PhenytoinThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Phenytoin resulting in a loss in efficacy.Approved, Vet Approved
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Irinotecan.Approved, Investigational
PimozideThe serum concentration of Irinotecan can be increased when it is combined with Pimozide.Approved
Platelet Activating FactorThe serum concentration of Irinotecan can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Irinotecan can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Irinotecan can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Irinotecan can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Irinotecan can be increased when it is combined with Prednisone.Approved, Vet Approved
PrimidoneThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Primidone resulting in a loss in efficacy.Approved, Vet Approved
ProbenecidThe serum concentration of Irinotecan can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Irinotecan can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Irinotecan can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Irinotecan can be increased when it is combined with Propafenone.Approved
PropofolThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Propofol.Approved, Investigational, Vet Approved
PropranololThe serum concentration of Irinotecan can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Irinotecan can be increased when it is combined with Protriptyline.Approved
QuazepamThe serum concentration of Irinotecan can be increased when it is combined with Quazepam.Approved, Illicit
QuercetinThe serum concentration of Irinotecan can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Irinotecan can be increased when it is combined with Quinacrine.Approved
QuinidineThe serum concentration of Irinotecan can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Irinotecan can be increased when it is combined with Quinine.Approved
Rabies vaccineThe risk or severity of adverse effects can be increased when Irinotecan is combined with Rabies vaccine.Approved
Rabies vaccineThe therapeutic efficacy of Rabies vaccine can be decreased when used in combination with Irinotecan.Approved
RanitidineThe serum concentration of Irinotecan can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Irinotecan can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Irinotecan can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Regorafenib.Approved
ReserpineThe serum concentration of Irinotecan can be decreased when it is combined with Reserpine.Approved
RifabutinThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Rifabutin resulting in a loss in efficacy.Approved
RifampicinThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Rifampicin resulting in a loss in efficacy.Approved
RifapentineThe serum concentration of the active metabolites of Irinotecan can be reduced when Irinotecan is used in combination with Rifapentine resulting in a loss in efficacy.Approved
RilpivirineThe serum concentration of Irinotecan can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Irinotecan.Approved
RolapitantThe serum concentration of Irinotecan can be increased when it is combined with Rolapitant.Approved
SaquinavirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Irinotecan can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Irinotecan can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Irinotecan can be increased when it is combined with Sertraline.Approved
SildenafilThe metabolism of Irinotecan can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Irinotecan can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Irinotecan can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Irinotecan 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 Irinotecan.Approved
SirolimusThe serum concentration of Irinotecan can be decreased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Irinotecan can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Irinotecan can be increased when it is combined with Spironolactone.Approved
SRP 299The risk or severity of adverse effects can be increased when Irinotecan is combined with SRP 299.Investigational
St. John's WortThe therapeutic efficacy of Irinotecan can be decreased when used in combination with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Irinotecan can be increased when it is combined with Staurosporine.Experimental
StiripentolThe serum concentration of Irinotecan can be increased when it is combined with Stiripentol.Approved
StreptozocinThe serum concentration of Irinotecan can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Irinotecan can be increased when it is combined with Sulfinpyrazone.Approved
SulfisoxazoleThe metabolism of Irinotecan can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SumatriptanThe serum concentration of Irinotecan can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Irinotecan can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Irinotecan 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 Irinotecan.Approved, Investigational
TacrolimusThe serum concentration of Irinotecan can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Irinotecan can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Irinotecan can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Telaprevir.Approved
TelithromycinThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Telithromycin.Approved
TelmisartanThe serum concentration of Irinotecan can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Irinotecan can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Irinotecan can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Irinotecan can be increased when it is combined with Terfenadine.Withdrawn
TeriflunomideThe serum concentration of Irinotecan can be increased when it is combined with Teriflunomide.Approved
TesmilifeneThe serum concentration of Irinotecan can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Irinotecan can be increased when it is combined with Testosterone.Approved, Investigational
TG4010The risk or severity of adverse effects can be increased when Irinotecan is combined with TG4010.Investigational
ThiotepaThe metabolism of Irinotecan can be decreased when combined with Thiotepa.Approved
TicagrelorThe serum concentration of Irinotecan can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Irinotecan can be decreased when combined with Ticlopidine.Approved
TocilizumabThe serum concentration of Irinotecan can be decreased when it is combined with Tocilizumab.Approved
TofacitinibIrinotecan may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolvaptanThe serum concentration of Irinotecan can be increased when it is combined with Tolvaptan.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Irinotecan.Approved, Investigational
TrazodoneThe serum concentration of Irinotecan can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Irinotecan can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Irinotecan can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Irinotecan can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Irinotecan can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Irinotecan can be increased when it is combined with Troleandomycin.Approved
VenlafaxineThe metabolism of Irinotecan can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Irinotecan can be decreased when combined with Verapamil.Approved
VinblastineThe serum concentration of Irinotecan can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Irinotecan can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Irinotecan can be increased when it is combined with Vinorelbine.Approved, Investigational
VoriconazoleThe serum concentration of the active metabolites of Irinotecan can be increased when Irinotecan is used in combination with Voriconazole.Approved, Investigational
ZimelidineThe serum concentration of Irinotecan can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Irinotecan can be decreased when combined with Ziprasidone.Approved
Food InteractionsNot Available
References
Synthesis ReferenceUS4604463
General References
  1. Innocenti F, Undevia SD, Iyer L, Chen PX, Das S, Kocherginsky M, Karrison T, Janisch L, Ramirez J, Rudin CM, Vokes EE, Ratain MJ: Genetic variants in the UDP-glucuronosyltransferase 1A1 gene predict the risk of severe neutropenia of irinotecan. J Clin Oncol. 2004 Apr 15;22(8):1382-8. Epub 2004 Mar 8. [PubMed:15007088 ]
  2. O'Dwyer PJ, Catalano RB: Uridine diphosphate glucuronosyltransferase (UGT) 1A1 and irinotecan: practical pharmacogenomics arrives in cancer therapy. J Clin Oncol. 2006 Oct 1;24(28):4534-8. [PubMed:17008691 ]
  3. Ramesh M, Ahlawat P, Srinivas NR: Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23. doi: 10.1002/bmc.1345. [PubMed:19852077 ]
  4. Chabot GG: Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 1997 Oct;33(4):245-59. [PubMed:9342501 ]
External Links
ATC CodesL01XX19
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (132 KB)
MSDSDownload (36.3 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.969
Blood Brain Barrier+0.6284
Caco-2 permeable-0.6065
P-glycoprotein substrateSubstrate0.7861
P-glycoprotein inhibitor IInhibitor0.7092
P-glycoprotein inhibitor IINon-inhibitor0.5337
Renal organic cation transporterNon-inhibitor0.8178
CYP450 2C9 substrateNon-substrate0.8174
CYP450 2D6 substrateNon-substrate0.9115
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.8564
CYP450 2C9 inhibitorNon-inhibitor0.7377
CYP450 2D6 inhibitorNon-inhibitor0.7779
CYP450 2C19 inhibitorNon-inhibitor0.6625
CYP450 3A4 inhibitorInhibitor0.8295
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.5081
Ames testNon AMES toxic0.6977
CarcinogenicityNon-carcinogens0.8045
BiodegradationNot ready biodegradable0.9956
Rat acute toxicity2.7960 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9457
hERG inhibition (predictor II)Inhibitor0.5413
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Pfizer inc
  • Accord healthcare inc
  • Actavis totowa llc
  • Akorn inc
  • App pharmaceuticals
  • Bedford laboratories
  • Dr reddys laboratories ltd
  • Ebewe pharma ges mbh nfg kg
  • Fresenius kabi oncology plc
  • Hospira inc
  • Pharmaforce inc
  • Pliva lachema as
  • Sandoz inc
  • Sun pharma global inc
  • Teva parenteral medicines inc
  • Watson laboratories inc
Packagers
Dosage forms
FormRouteStrength
SolutionIntravenous20 mg
InjectionIntravenous100 mg/5mL
InjectionIntravenous20 mg/mL
InjectionIntravenous40 mg/2mL
Injection, solutionIntravenous100 mg/5mL
Injection, solutionIntravenous20 mg/mL
Injection, solutionIntravenous40 mg/2mL
InjectionIntravenous4.3 mg/mL
Prices
Unit descriptionCostUnit
Irinotecan hcl 40 mg/2 ml inj138.07USD ml
Camptosar 20 mg/ml vial36.0USD ml
Irinotecan hcl 40 mg/2 ml vial22.2USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2202531 No2005-05-032015-10-11Canada
CA2294031 No2005-01-182018-07-27Canada
US6403569 Yes2000-10-282020-10-28Us
US6794370 Yes2000-11-012020-11-01Us
US8147867 No2008-08-292028-08-29Us
US8329213 No2005-05-022025-05-02Us
US8703181 No2005-05-022025-05-02Us
US8992970 No2005-05-022025-05-02Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point222-223 °CNot Available
water solubilitySolubleNot Available
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.107 mg/mLALOGPS
logP3.94ALOGPS
logP2.78ChemAxon
logS-3.7ALOGPS
pKa (Strongest Acidic)11.71ChemAxon
pKa (Strongest Basic)9.47ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area112.51 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity161.33 m3·mol-1ChemAxon
Polarizability65.27 Å3ChemAxon
Number of Rings7ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as camptothecins. These are heterocyclic compounds comprising a planar pentacyclic ring structure, that includes a pyrrolo[3,4-beta]-quinoline moiety (rings A, B and C), conjugated pyridone moiety (ring D) and one chiral center at position 20 within the alpha-hydroxy lactone ring with (S) configuration (the E-ring).
KingdomOrganic compounds
Super ClassAlkaloids and derivatives
ClassCamptothecins
Sub ClassNot Available
Direct ParentCamptothecins
Alternative Parents
Substituents
  • Camptothecin
  • Hydroxyquinoline
  • Quinoline
  • Pyranopyridine
  • Piperidinecarboxylic acid
  • Pyridinone
  • 4-aminopiperidine
  • Benzenoid
  • Pyridine
  • Piperidine
  • Dicarboxylic acid or derivatives
  • Heteroaromatic compound
  • Tertiary alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Lactone
  • Lactam
  • Carboxylic acid ester
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function:
Releases the supercoiling and torsional tension of DNA introduced during duplication of mitochondrial DNA by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a single-strand break via transesterification at a target site in duplex DNA. The scissile phosphodiester is attacked by the catalytic tyrosine of the enzyme, resulting in the formation of a DNA-(3'-phosphotyrosy...
Gene Name:
TOP1MT
Uniprot ID:
Q969P6
Molecular Weight:
69871.39 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. Yoshikawa M, Ikegami Y, Hayasaka S, Ishii K, Ito A, Sano K, Suzuki T, Togawa T, Yoshida H, Soda H, Oka M, Kohno S, Sawada S, Ishikawa T, Tanabe S: Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells. Int J Cancer. 2004 Jul 20;110(6):921-7. [PubMed:15170677 ]
  4. Yoshikawa M, Ikegami Y, Sano K, Yoshida H, Mitomo H, Sawada S, Ishikawa T: Transport of SN-38 by the wild type of human ABC transporter ABCG2 and its inhibition by quercetin, a natural flavonoid. J Exp Ther Oncol. 2004 Apr;4(1):25-35. [PubMed:15255290 ]
  5. Yang X, Hu Z, Chan SY, Chan E, Goh BC, Duan W, Zhou S: Novel agents that potentially inhibit irinotecan-induced diarrhea. Curr Med Chem. 2005;12(11):1343-58. [PubMed:15975002 ]
  6. Nakagawa H, Saito H, Ikegami Y, Aida-Hyugaji S, Sawada S, Ishikawa T: Molecular modeling of new camptothecin analogues to circumvent ABCG2-mediated drug resistance in cancer. Cancer Lett. 2006 Mar 8;234(1):81-9. Epub 2005 Nov 23. [PubMed:16309825 ]
  7. Ishikawa T, Ikegami Y, Sano K, Nakagawa H, Sawada S: Transport mechanism-based drug molecular design: novel camptothecin analogues to circumvent ABCG2-associated drug resistance of human tumor cells. Curr Pharm Des. 2006;12(3):313-25. [PubMed:16454746 ]
  8. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  9. Ramesh M, Ahlawat P, Srinivas NR: Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23. doi: 10.1002/bmc.1345. [PubMed:19852077 ]
  10. Chabot GG: Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 1997 Oct;33(4):245-59. [PubMed:9342501 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Poly(a) rna binding
Specific Function:
Releases the supercoiling and torsional tension of DNA introduced during the DNA replication and transcription by transiently cleaving and rejoining one strand of the DNA duplex. Introduces a single-strand break via transesterification at a target site in duplex DNA. The scissile phosphodiester is attacked by the catalytic tyrosine of the enzyme, resulting in the formation of a DNA-(3'-phosphot...
Gene Name:
TOP1
Uniprot ID:
P11387
Molecular Weight:
90725.19 Da
References
  1. Yoshikawa M, Ikegami Y, Hayasaka S, Ishii K, Ito A, Sano K, Suzuki T, Togawa T, Yoshida H, Soda H, Oka M, Kohno S, Sawada S, Ishikawa T, Tanabe S: Novel camptothecin analogues that circumvent ABCG2-associated drug resistance in human tumor cells. Int J Cancer. 2004 Jul 20;110(6):921-7. [PubMed:15170677 ]
  2. Yoshikawa M, Ikegami Y, Sano K, Yoshida H, Mitomo H, Sawada S, Ishikawa T: Transport of SN-38 by the wild type of human ABC transporter ABCG2 and its inhibition by quercetin, a natural flavonoid. J Exp Ther Oncol. 2004 Apr;4(1):25-35. [PubMed:15255290 ]
  3. Yang X, Hu Z, Chan SY, Chan E, Goh BC, Duan W, Zhou S: Novel agents that potentially inhibit irinotecan-induced diarrhea. Curr Med Chem. 2005;12(11):1343-58. [PubMed:15975002 ]
  4. Nakagawa H, Saito H, Ikegami Y, Aida-Hyugaji S, Sawada S, Ishikawa T: Molecular modeling of new camptothecin analogues to circumvent ABCG2-mediated drug resistance in cancer. Cancer Lett. 2006 Mar 8;234(1):81-9. Epub 2005 Nov 23. [PubMed:16309825 ]
  5. Ishikawa T, Ikegami Y, Sano K, Nakagawa H, Sawada S: Transport mechanism-based drug molecular design: novel camptothecin analogues to circumvent ABCG2-associated drug resistance of human tumor cells. Curr Pharm Des. 2006;12(3):313-25. [PubMed:16454746 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Ramesh M, Ahlawat P, Srinivas NR: Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23. doi: 10.1002/bmc.1345. [PubMed:19852077 ]
  8. Chabot GG: Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 1997 Oct;33(4):245-59. [PubMed:9342501 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Ramesh M, Ahlawat P, Srinivas NR: Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23. doi: 10.1002/bmc.1345. [PubMed:19852077 ]
  2. 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 ]
  3. Kuhn JG: Pharmacology of irinotecan. Oncology (Williston Park). 1998 Aug;12(8 Suppl 6):39-42. [PubMed:9726089 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
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.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 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 ]
  2. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
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. Acts as a 1,4-cineole 2-exo-monooxygenase.
Gene Name:
CYP2B6
Uniprot ID:
P20813
Molecular Weight:
56277.81 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
substrate
General Function:
Oxygen binding
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.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Kuhn JG: Pharmacology of irinotecan. Oncology (Williston Park). 1998 Aug;12(8 Suppl 6):39-42. [PubMed:9726089 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
References
  1. Chabot GG: Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 1997 Oct;33(4):245-59. [PubMed:9342501 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Triglyceride lipase activity
Specific Function:
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester. Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine. Catalyzes the transesterification of cocaine to form cocaethylene. Displays fatty acid ethyl ester synthase activity,...
Gene Name:
CES1
Uniprot ID:
P23141
Molecular Weight:
62520.62 Da
References
  1. Chabot GG: Clinical pharmacokinetics of irinotecan. Clin Pharmacokinet. 1997 Oct;33(4):245-59. [PubMed:9342501 ]
  2. Ramesh M, Ahlawat P, Srinivas NR: Irinotecan and its active metabolite, SN-38: review of bioanalytical methods and recent update from clinical pharmacology perspectives. Biomed Chromatogr. 2010 Jan;24(1):104-23. doi: 10.1002/bmc.1345. [PubMed:19852077 ]
  3. Kuhn JG: Pharmacology of irinotecan. Oncology (Williston Park). 1998 Aug;12(8 Suppl 6):39-42. [PubMed:9726089 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Methylumbelliferyl-acetate deacetylase activity
Specific Function:
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Shows high catalytic efficiency for hydrolysis of cocaine, 4-methylumbelliferyl acetate, heroin and 6-monoacetylmorphine.
Gene Name:
CES2
Uniprot ID:
O00748
Molecular Weight:
61806.41 Da
References
  1. Sanghani SP, Quinney SK, Fredenburg TB, Davis WI, Murry DJ, Bosron WF: Hydrolysis of irinotecan and its oxidative metabolites, 7-ethyl-10-[4-N-(5-aminopentanoic acid)-1-piperidino] carbonyloxycamptothecin and 7-ethyl-10-[4-(1-piperidino)-1-amino]-carbonyloxycamptothecin, by human carboxylesterases CES1A1, CES2, and a newly expressed carboxylesterase isoenzyme, CES3. Drug Metab Dispos. 2004 May;32(5):505-11. [PubMed:15100172 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Link [Link]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Toxin transporter activity
Specific Function:
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name:
SLC22A3
Uniprot ID:
O75751
Molecular Weight:
61279.485 Da
References
  1. Shnitsar V, Eckardt R, Gupta S, Grottker J, Muller GA, Koepsell H, Burckhardt G, Hagos Y: Expression of human organic cation transporter 3 in kidney carcinoma cell lines increases chemosensitivity to melphalan, irinotecan, and vincristine. Cancer Res. 2009 Feb 15;69(4):1494-501. doi: 10.1158/0008-5472.CAN-08-2483. Epub 2009 Feb 3. [PubMed:19190342 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Nozawa T, Minami H, Sugiura S, Tsuji A, Tamai I: Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms. Drug Metab Dispos. 2005 Mar;33(3):434-9. Epub 2004 Dec 17. [PubMed:15608127 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
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. Chen ZS, Furukawa T, Sumizawa T, Ono K, Ueda K, Seto K, Akiyama SI: ATP-Dependent efflux of CPT-11 and SN-38 by the multidrug resistance protein (MRP) and its inhibition by PAK-104P. Mol Pharmacol. 1999 May;55(5):921-8. [PubMed:10220571 ]
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. Wang X, Furukawa T, Nitanda T, Okamoto M, Sugimoto Y, Akiyama S, Baba M: Breast cancer resistance protein (BCRP/ABCG2) induces cellular resistance to HIV-1 nucleoside reverse transcriptase inhibitors. Mol Pharmacol. 2003 Jan;63(1):65-72. [PubMed:12488537 ]
  2. Maliepaard M, van Gastelen MA, Tohgo A, Hausheer FH, van Waardenburg RC, de Jong LA, Pluim D, Beijnen JH, Schellens JH: Circumvention of breast cancer resistance protein (BCRP)-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. Clin Cancer Res. 2001 Apr;7(4):935-41. [PubMed:11309344 ]
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. Kroetz DL: Role for drug transporters beyond tumor resistance: hepatic functional imaging and genotyping of multidrug resistance transporters for the prediction of irinotecan toxicity. J Clin Oncol. 2006 Sep 10;24(26):4225-7. Epub 2006 Aug 8. [PubMed:16895999 ]
  2. Han JY, Lim HS, Park YH, Lee SY, Lee JS: Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer. Lung Cancer. 2009 Jan;63(1):115-20. doi: 10.1016/j.lungcan.2007.12.003. Epub 2008 Jan 24. [PubMed:18221820 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Organic anion transmembrane transporter activity
Specific Function:
Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name:
ABCC2
Uniprot ID:
Q92887
Molecular Weight:
174205.64 Da
References
  1. Kroetz DL: Role for drug transporters beyond tumor resistance: hepatic functional imaging and genotyping of multidrug resistance transporters for the prediction of irinotecan toxicity. J Clin Oncol. 2006 Sep 10;24(26):4225-7. Epub 2006 Aug 8. [PubMed:16895999 ]
  2. Han JY, Lim HS, Park YH, Lee SY, Lee JS: Integrated pharmacogenetic prediction of irinotecan pharmacokinetics and toxicity in patients with advanced non-small cell lung cancer. Lung Cancer. 2009 Jan;63(1):115-20. doi: 10.1016/j.lungcan.2007.12.003. Epub 2008 Jan 24. [PubMed:18221820 ]
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 03:54