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Identification
NameTopotecan
Accession NumberDB01030  (APRD00687)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionAn antineoplastic agent used to treat ovarian cancer. It works by inhibiting DNA topoisomerases, type I. [PubChem]
Structure
Thumb
Synonyms
9-[(dimethylamino)Methyl]-10-hydroxy-(4S)-camptothecin
Topotecane
Topotecanum
External Identifiers
  • SKF-104864
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act Topotecanpowder for solution1 mgintravenousActavis Pharma CompanyNot applicableNot applicableCanada
Act Topotecanpowder for solution4 mgintravenousActavis Pharma Company2015-11-17Not applicableCanada
Hycamtininjection, powder, lyophilized, for solution4 mg/4mLintravenousGlaxo Smith Kline Llc1996-06-07Not applicableUs
Hycamtincapsule.25 mg/1oralGlaxo Smith Kline Llc2008-09-16Not applicableUs
Hycamtinpowder for solution4 mgintravenousNovartis Pharmaceuticals Canada Inc1997-06-18Not applicableCanada
Hycamtincapsule1 mg/1oralGlaxo Smith Kline Llc2008-09-16Not applicableUs
Mylan-topotecan Hydrochloride for Injectionpowder for solution4 mgintravenousMylan Pharmaceuticals UlcNot applicableNot applicableCanada
PMS-topotecanpowder for solution4 mgintravenousPharmascience Inc2013-08-29Not applicableCanada
PMS-topotecanpowder for solution1 mgintravenousPharmascience IncNot applicableNot applicableCanada
Topotecaninjection, solution, concentrate1 mg/mLintravenousTeva Parenteral Medicines, Inc.2013-05-21Not applicableUs
Topotecaninjection1 mg/mLintravenousSandoz Inc2011-02-25Not applicableUs
Topotecaninjection, solution, concentrate1 mg/mLintravenousSagent Pharmaceuticals2014-12-15Not applicableUs
Topotecaninjection, solution, concentrate1 mg/mLintravenousHospira, Inc.2011-02-02Not applicableUs
Topotecan for Injectionpowder for solution4 mgintravenousFresenius Kabi Canada Ltd2012-03-16Not applicableCanada
Topotecan for Injectionpowder for solution4 mgintravenousSandoz Canada Incorporated2009-10-02Not applicableCanada
Topotecan Hydrochloride for Injectionsolution1 mgintravenousHospira Healthcare Corporation2012-03-27Not applicableCanada
Topotecan Hydrochloride for Injectionpowder for solution4 mgintravenousMylan Pharmaceuticals Ulc2013-06-112016-07-06Canada
Topotecan Hydrochloride for Injectionpowder for solution4 mgintravenousAccord Healthcare Inc2011-06-27Not applicableCanada
Topotecan Hydrochloride for Injectionsolution1 mgintravenousAccord Healthcare Inc2013-11-21Not applicableCanada
Topotecan Injectionsolution1 mgintravenousTeva Canada Limited2013-10-21Not applicableCanada
Topotecan Injectionsolution1 mgintravenousSandoz Canada Incorporated2014-02-05Not applicableCanada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
PotactasolPowder for concentrate for solution for infusion4 mgIntravenous useActavis Group Ptc Ehf2011-01-06Not applicableEu
PotactasolPowder for concentrate for solution for infusion1 mgIntravenous useActavis Group Ptc Ehf2011-01-06Not applicableEu
Topotecan ActavisPowder for concentrate for solution for infusion4 mgIntravenous useActavis Group Ptc Ehf2009-07-24Not applicableEu
Topotecan ActavisPowder for concentrate for solution for infusion1 mgIntravenous useActavis Group Ptc Ehf2009-07-24Not applicableEu
Topotecan ActavisPowder for concentrate for solution for infusion4 mgIntravenous useActavis Group Ptc Ehf2009-07-24Not applicableEu
Topotecan ActavisPowder for concentrate for solution for infusion1 mgIntravenous useActavis Group Ptc Ehf2009-07-24Not applicableEu
Topotecan Hydrochlorideinjection, powder, for solution4 mg/4mLintravenousThree Rivers Pharmaceuticals, LLC.2010-12-02Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousPfizer Laboratories Div Pfizer Inc.2012-08-29Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousActavis Pharma, Inc.2015-01-05Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/mLintravenousMylan Institutional LLC2012-08-29Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousAccord Healthcare, Inc.2013-07-01Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousBedford Laboratories2011-04-18Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousFresenius Kabi USA, LLC2010-11-29Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousSagent Pharmaceuticals2010-11-28Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousSun Pharmaceutical Industries Limited2015-09-02Not applicableUs
Topotecan Hydrochlorideinjection, powder, lyophilized, for solution4 mg/4mLintravenousSagent Pharmaceuticals2011-06-27Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Topotecan hydrochloride
119413-54-6
Thumb
  • InChI Key: DGHHQBMTXTWTJV-BQAIUKQQSA-N
  • Monoisotopic Mass: 457.1404486
  • Average Mass: 457.907
DBSALT000322
Categories
UNII7M7YKX2N15
CAS number123948-87-8
WeightAverage: 421.4458
Monoisotopic: 421.163770861
Chemical FormulaC23H23N3O5
InChI KeyInChIKey=UCFGDBYHRUNTLO-QHCPKHFHSA-N
InChI
InChI=1S/C23H23N3O5/c1-4-23(30)16-8-18-20-12(9-26(18)21(28)15(16)11-31-22(23)29)7-13-14(10-25(2)3)19(27)6-5-17(13)24-20/h5-8,27,30H,4,9-11H2,1-3H3/t23-/m0/s1
IUPAC Name
(19S)-8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-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)-heptaene-14,18-dione
SMILES
CC[C@@]1(O)C(=O)OCC2=C1C=C1N(CC3=CC4=C(C=CC(O)=C4CN(C)C)N=C13)C2=O
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
  • Benzylamine
  • Aralkylamine
  • Pyridinone
  • Benzenoid
  • Pyridine
  • Heteroaromatic compound
  • Tertiary alcohol
  • Tertiary aliphatic amine
  • Tertiary amine
  • Lactone
  • Lactam
  • Carboxylic acid ester
  • Oxacycle
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Alcohol
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of advanced ovarian cancer in patients with disease that has recurred or progressed following therapy with platinum-based regimens. Also used as a second-line therapy for treatment-sensitive small cell lung cancer, as well as in combination with cisplatin for the treatment of stage IV-B, recurrent, or persistent cervical cancer not amenable to curative treatment with surgery and/or radiation therapy.
PharmacodynamicsTopotecan, a semi-synthetic derivative of camptothecin (a plant alkaloid obtained from the Camptotheca acuminata tree), is an anti-tumor drug with topoisomerase I-inhibitory activity similar to irinotecan. DNA topoisomerases are enzymes in the cell nucleus that regulate DNA topology (3-dimensional conformation) and facilitate nuclear processes such as DNA replication, recombination, and repair. During these processes, DNA topoisomerase I creates reversible single-stranded breaks in double-stranded DNA, allowing intact single DNA strands to pass through the break and relieve the topologic constraints inherent in supercoiled DNA. The 3'-DNA terminus of the broken DNA strand binds covalently with the topoisomerase enzyme to form a catalytic intermediate called a cleavable complex. After DNA is sufficiently relaxed and the strand passage reaction is complete, DNA topoisomerase reattaches the broken DNA strands to form the unaltered topoisomers that allow transcription to proceed. Topotecan interferes with the growth of cancer cells, which are eventually destroyed. Since the growth of normal cells can be affected by the medicine, other effects may also occur. Unlike irinotecan, topotecan is found predominantly in the inactive carboxylate form at neutral pH and it is not a prodrug.
Mechanism of actionTopotecan has the same mechanism of action as irinotecan and is believed to exert its cytotoxic effects during the S-phase of DNA synthesis. Topoisomerase I relieves torsional strain in DNA by inducing reversible single strand breaks. Topotecan binds to the topoisomerase I-DNA complex and prevents religation of these single strand breaks. This ternary complex interferes with the moving replication fork, which leads to the induction of replication arrest and lethal double-stranded breaks in DNA. As mammalian cells cannot efficiently repair these double strand breaks, the formation of this ternary complex eventually leads to apoptosis (programmed cell death). Topotecan mimics a DNA base pair and binds at the site of DNA cleavage by intercalating between the upstream (−1) and downstream (+1) base pairs. Intercalation displaces the downstream DNA, thus preventing religation of the cleaved strand. By specifically binding to the enzyme–substrate complex, Topotecan acts as an uncompetitive inhibitor.
Related Articles
AbsorptionNot Available
Volume of distributionNot Available
Protein binding35%
Metabolism

Topotecan undergoes a reversible pH dependent hydrolysis of its lactone moiety; it is the lactone form that is pharmacologically active.

Route of eliminationRenal clearance is an important determinant of topotecan elimination. In a mass balance/excretion study in 4 patients with solid tumors, the overall recovery of total topotecan and its N-desmethyl metabolite in urine and feces over 9 days averaged 73.4 ± 2.3% of the administered IV dose. Fecal elimination of total topotecan accounted for 9 ± 3.6% while fecal elimination of N-desmethyl topotecan was 1.7 ± 0.6%.
Half life2-3 hours
ClearanceNot Available
ToxicityThe primary anticipated complication of overdosage would consist of bone marrow suppression.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8911
Blood Brain Barrier-0.9659
Caco-2 permeable-0.6966
P-glycoprotein substrateSubstrate0.7918
P-glycoprotein inhibitor INon-inhibitor0.6121
P-glycoprotein inhibitor IINon-inhibitor0.9507
Renal organic cation transporterNon-inhibitor0.9
CYP450 2C9 substrateNon-substrate0.8844
CYP450 2D6 substrateNon-substrate0.8168
CYP450 3A4 substrateSubstrate0.6875
CYP450 1A2 substrateInhibitor0.5572
CYP450 2C9 inhibitorNon-inhibitor0.8305
CYP450 2D6 inhibitorNon-inhibitor0.8918
CYP450 2C19 inhibitorNon-inhibitor0.824
CYP450 3A4 inhibitorNon-inhibitor0.6464
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7184
Ames testNon AMES toxic0.6516
CarcinogenicityNon-carcinogens0.8504
BiodegradationNot ready biodegradable1.0
Rat acute toxicity3.0075 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9963
hERG inhibition (predictor II)Non-inhibitor0.8302
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
ManufacturersNot Available
Packagers
Dosage forms
FormRouteStrength
Capsuleoral.25 mg/1
Capsuleoral1 mg/1
Injection, powder, lyophilized, for solutionintravenous4 mg/4mL
Powder for solutionintravenous1 mg
Powder for concentrate for solution for infusionIntravenous use1 mg
Powder for concentrate for solution for infusionIntravenous use4 mg
Injectionintravenous1 mg/mL
Injection, solution, concentrateintravenous1 mg/mL
Powder for solutionintravenous4 mg
Injection, powder, for solutionintravenous4 mg/4mL
Injection, powder, lyophilized, for solutionintravenous4 mg/mL
Solutionintravenous1 mg
Prices
Unit descriptionCostUnit
Hycamtin 4 mg vial1306.1USD vial
Hycamtin 1 mg capsule358.92USD capsule
Hycamtin 0.25 mg capsule89.73USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA2103707 No2003-12-092012-02-07Canada
CA2103708 No2004-04-272012-02-07Canada
US5004758 No1993-05-282010-05-28Us
US5674872 No1995-04-072015-04-07Us
US8158645 No2004-12-102024-12-10Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point213-218 °CNot Available
water solubility1 mg/mlNot Available
logP0.8Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.861 mg/mLALOGPS
logP1.84ALOGPS
logP-0.36ChemAxon
logS-2.7ALOGPS
pKa (Strongest Acidic)8ChemAxon
pKa (Strongest Basic)9.83ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area103.2 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity115.02 m3·mol-1ChemAxon
Polarizability44.86 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

Venkata Raghavendra Palle, Sekhar Nariyam, Lankeshwara Matti, “PROCESS FOR PREPARING TOPOTECAN.” U.S. Patent US20070149783, issued June 28, 2007.

US20070149783
General References
  1. Kollmannsberger C, Mross K, Jakob A, Kanz L, Bokemeyer C: Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience. Oncology. 1999;56(1):1-12. [PubMed:9885371 ]
  2. Herben VM, ten Bokkel Huinink WW, Beijnen JH: Clinical pharmacokinetics of topotecan. Clin Pharmacokinet. 1996 Aug;31(2):85-102. [PubMed:8853931 ]
  3. Dennis MJ, Beijnen JH, Grochow LB, van Warmerdam LJ: An overview of the clinical pharmacology of topotecan. Semin Oncol. 1997 Feb;24(1 Suppl 5):S5-12-S5-18. [PubMed:9122737 ]
External Links
ATC CodesL01XX17
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (78.6 KB)
MSDSDownload (29.3 KB)
Interactions
Drug Interactions
Drug
AcetaminophenThe serum concentration of Topotecan can be increased when it is combined with Acetaminophen.
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Topotecan.
AfatinibThe serum concentration of Topotecan can be increased when it is combined with Afatinib.
AlbendazoleThe serum concentration of Topotecan can be increased when it is combined with Albendazole.
AldosteroneThe serum concentration of Topotecan can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Topotecan can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Topotecan can be increased when it is combined with Alfentanil.
AmantadineThe serum concentration of Topotecan can be increased when it is combined with Amantadine.
Aminohippuric acidThe serum concentration of Topotecan can be increased when it is combined with Aminohippuric acid.
AmiodaroneThe serum concentration of Topotecan can be increased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Topotecan can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Topotecan can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Topotecan can be increased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Topotecan can be increased when it is combined with Amsacrine.
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Topotecan.
AstemizoleThe serum concentration of Topotecan can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Topotecan can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Topotecan can be increased when it is combined with Atenolol.
AtorvastatinThe serum concentration of Topotecan can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Topotecan can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Topotecan can be increased when it is combined with Azithromycin.
BenzocaineThe serum concentration of Topotecan can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Topotecan can be increased when it is combined with Bepridil.
BevacizumabBevacizumab may increase the cardiotoxic activities of Topotecan.
BiperidenThe serum concentration of Topotecan can be increased when it is combined with Biperiden.
BosutinibThe serum concentration of Topotecan can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Topotecan can be increased when it is combined with Bromocriptine.
BuprenorphineThe serum concentration of Topotecan can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Topotecan can be increased when it is combined with Buspirone.
CabazitaxelThe serum concentration of Topotecan can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Topotecan can be increased when it is combined with Caffeine.
CanagliflozinThe serum concentration of Topotecan can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Topotecan can be increased when it is combined with Candesartan.
CaptoprilThe serum concentration of Topotecan can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Topotecan can be increased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Topotecan can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Topotecan can be increased when it is combined with Caspofungin.
ChloroquineThe serum concentration of Topotecan can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Topotecan can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe serum concentration of Topotecan can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Topotecan can be increased when it is combined with Chlorprothixene.
CholesterolThe serum concentration of Topotecan can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Topotecan can be decreased when it is combined with Cholic Acid.
CilazaprilThe serum concentration of Topotecan can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Topotecan can be increased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Topotecan can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Topotecan can be increased when it is combined with Citalopram.
ClarithromycinThe serum concentration of Topotecan can be increased when it is combined with Clarithromycin.
ClofazimineThe serum concentration of Topotecan can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Topotecan can be increased when it is combined with Clomipramine.
ClotrimazoleThe serum concentration of Topotecan can be increased when it is combined with Clotrimazole.
ClozapineThe risk or severity of adverse effects can be increased when Topotecan is combined with Clozapine.
CobicistatThe serum concentration of Topotecan can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Topotecan can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Topotecan can be increased when it is combined with Colforsin.
CrizotinibThe serum concentration of Topotecan can be increased when it is combined with Crizotinib.
CyclophosphamideThe serum concentration of Topotecan can be increased when it is combined with Cyclophosphamide.
CyclosporineThe serum concentration of Topotecan can be increased when it is combined with Cyclosporine.
DabrafenibThe serum concentration of Topotecan can be increased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Topotecan can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Topotecan can be increased when it is combined with Dactinomycin.
DaidzinThe serum concentration of Topotecan can be increased when it is combined with Daidzin.
DasabuvirThe serum concentration of Topotecan can be increased when it is combined with Dasabuvir.
DasatinibThe serum concentration of Topotecan can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Topotecan can be increased when it is combined with Daunorubicin.
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Topotecan.
DesipramineThe serum concentration of Topotecan can be increased when it is combined with Desipramine.
DeslanosideDeslanoside may decrease the cardiotoxic activities of Topotecan.
DesloratadineThe serum concentration of Topotecan can be increased when it is combined with Desloratadine.
DexamethasoneThe serum concentration of Topotecan can be increased when it is combined with Dexamethasone.
DextromethorphanThe serum concentration of Topotecan can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Topotecan can be increased when it is combined with Diclofenac.
DiethylstilbestrolThe serum concentration of Topotecan can be increased when it is combined with Diethylstilbestrol.
DigitoxinDigitoxin may decrease the cardiotoxic activities of Topotecan.
DigoxinThe serum concentration of Topotecan can be increased when it is combined with Digoxin.
DihydroergotamineThe serum concentration of Topotecan can be increased when it is combined with Dihydroergotamine.
DiltiazemThe serum concentration of Topotecan can be increased when it is combined with Diltiazem.
DipyridamoleThe serum concentration of Topotecan can be increased when it is combined with Dipyridamole.
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Topotecan.
DoxazosinThe serum concentration of Topotecan can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Topotecan can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Topotecan can be increased when it is combined with Doxorubicin.
DronabinolThe serum concentration of Topotecan can be increased when it is combined with Dronabinol.
DronedaroneThe serum concentration of Topotecan can be increased when it is combined with Dronedarone.
ElacridarThe serum concentration of Topotecan can be increased when it is combined with Elacridar.
ElbasvirThe serum concentration of Topotecan can be increased when it is combined with Elbasvir.
EltrombopagThe serum concentration of Topotecan can be increased when it is combined with Eltrombopag.
EnalaprilThe serum concentration of Topotecan can be increased when it is combined with Enalapril.
EnzalutamideThe serum concentration of Topotecan can be increased when it is combined with Enzalutamide.
ErgonovineThe serum concentration of Topotecan can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Topotecan can be increased when it is combined with Ergotamine.
ErlotinibThe serum concentration of Topotecan can be increased when it is combined with Erlotinib.
ErythromycinThe serum concentration of Topotecan can be increased when it is combined with Erythromycin.
EstradiolThe serum concentration of Topotecan can be increased when it is combined with Estradiol.
EstramustineThe serum concentration of Topotecan can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Topotecan can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Topotecan can be decreased when it is combined with Estrone.
EtoposideThe serum concentration of Topotecan can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Topotecan can be increased when it is combined with Etravirine.
FelodipineThe serum concentration of Topotecan can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Topotecan can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Topotecan can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Topotecan can be increased when it is combined with Fidaxomicin.
FilgrastimThe risk or severity of adverse effects can be increased when Filgrastim is combined with Topotecan.
FingolimodTopotecan may increase the immunosuppressive activities of Fingolimod.
FluconazoleThe serum concentration of Topotecan can be increased when it is combined with Fluconazole.
FluoxetineThe serum concentration of Topotecan can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Topotecan can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Topotecan can be increased when it is combined with Fluphenazine.
FlurazepamThe serum concentration of Topotecan can be increased when it is combined with Flurazepam.
FluvoxamineThe serum concentration of Topotecan can be increased when it is combined with Fluvoxamine.
FosphenytoinThe serum concentration of Topotecan can be decreased when it is combined with Fosphenytoin.
GefitinibThe serum concentration of Topotecan can be increased when it is combined with Gefitinib.
GenisteinThe serum concentration of Topotecan can be increased when it is combined with Genistein.
GlyburideThe serum concentration of Topotecan can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Topotecan can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Topotecan can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Topotecan can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Topotecan can be increased when it is combined with Haloperidol.
HesperetinThe serum concentration of Topotecan can be increased when it is combined with Hesperetin.
HydrocortisoneThe serum concentration of Topotecan can be increased when it is combined with Hydrocortisone.
IdelalisibThe serum concentration of Topotecan can be increased when it is combined with Idelalisib.
ImatinibThe serum concentration of Topotecan can be increased when it is combined with Imatinib.
ImipramineThe serum concentration of Topotecan can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Topotecan can be increased when it is combined with Indinavir.
IndomethacinThe serum concentration of Topotecan can be increased when it is combined with Indomethacin.
IsavuconazoniumThe serum concentration of Topotecan can be increased when it is combined with Isavuconazonium.
ItraconazoleThe serum concentration of Topotecan can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Topotecan can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Topotecan can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Topotecan can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Topotecan can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Topotecan can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Topotecan can be increased when it is combined with Lapatinib.
LeflunomideThe risk or severity of adverse effects can be increased when Topotecan is combined with Leflunomide.
LevofloxacinThe serum concentration of Topotecan can be increased when it is combined with Levofloxacin.
LevothyroxineThe serum concentration of Topotecan can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Topotecan can be increased when it is combined with Lidocaine.
LiothyronineThe serum concentration of Topotecan can be decreased when it is combined with Liothyronine.
LiotrixThe serum concentration of Topotecan can be decreased when it is combined with Liotrix.
LisinoprilThe serum concentration of Topotecan can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Topotecan can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Topotecan can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Topotecan can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Topotecan can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Topotecan can be increased when it is combined with Losartan.
LovastatinThe serum concentration of Topotecan can be increased when it is combined with Lovastatin.
LumacaftorThe serum concentration of Topotecan can be decreased when it is combined with Lumacaftor.
MaprotilineThe serum concentration of Topotecan can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Topotecan can be increased when it is combined with Mebendazole.
MefloquineThe serum concentration of Topotecan can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Topotecan can be increased when it is combined with Megestrol acetate.
MeprobamateThe serum concentration of Topotecan can be increased when it is combined with Meprobamate.
MetamizoleThe risk or severity of adverse effects can be increased when Metamizole is combined with Topotecan.
MethadoneThe serum concentration of Topotecan can be increased when it is combined with Methadone.
MetoprololThe serum concentration of Topotecan can be increased when it is combined with Metoprolol.
MibefradilThe serum concentration of Topotecan can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Topotecan can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Topotecan can be increased when it is combined with Midazolam.
MifepristoneThe serum concentration of Topotecan can be increased when it is combined with Mifepristone.
MitomycinThe serum concentration of Topotecan can be increased when it is combined with Mitomycin.
MitoxantroneThe serum concentration of Topotecan can be increased when it is combined with Mitoxantrone.
MorphineThe serum concentration of Topotecan can be increased when it is combined with Morphine.
NaltrexoneThe serum concentration of Topotecan can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Topotecan can be increased when it is combined with Naringenin.
NatalizumabThe risk or severity of adverse effects can be increased when Topotecan is combined with Natalizumab.
NefazodoneThe serum concentration of Topotecan can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Topotecan can be increased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Topotecan can be increased when it is combined with Neostigmine.
NicardipineThe serum concentration of Topotecan can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Topotecan can be increased when it is combined with Nifedipine.
NilotinibThe serum concentration of Topotecan can be increased when it is combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be decreased when it is combined with Topotecan.
NisoldipineThe serum concentration of Topotecan can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Topotecan can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Topotecan can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Topotecan can be decreased when it is combined with Norethisterone.
NovobiocinThe serum concentration of Topotecan can be increased when it is combined with Novobiocin.
OmeprazoleThe serum concentration of Topotecan can be increased when it is combined with Omeprazole.
OuabainOuabain may decrease the cardiotoxic activities of Topotecan.
P-NitrophenolThe serum concentration of Topotecan can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Topotecan can be increased when it is combined with Paclitaxel.
Palmitic AcidThe serum concentration of Topotecan can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Topotecan can be increased when it is combined with Pantoprazole.
ParoxetineThe serum concentration of Topotecan can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Topotecan.
PerindoprilThe serum concentration of Topotecan can be increased when it is combined with Perindopril.
PhenobarbitalThe serum concentration of Topotecan can be decreased when it is combined with Phenobarbital.
PhenytoinThe serum concentration of Topotecan can be decreased when it is combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Topotecan.
PimozideThe serum concentration of Topotecan can be increased when it is combined with Pimozide.
Platelet Activating FactorThe serum concentration of Topotecan can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Topotecan can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Topotecan can be increased when it is combined with Posaconazole.
PravastatinThe serum concentration of Topotecan can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Topotecan can be increased when it is combined with Prazosin.
PrednisoneThe serum concentration of Topotecan can be increased when it is combined with Prednisone.
ProbenecidThe serum concentration of Topotecan can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Topotecan can be increased when it is combined with Progesterone.
PromethazineThe serum concentration of Topotecan can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Topotecan can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Topotecan can be increased when it is combined with Propranolol.
ProtriptylineThe serum concentration of Topotecan can be increased when it is combined with Protriptyline.
QuercetinThe serum concentration of Topotecan can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Topotecan can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Topotecan can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Topotecan can be increased when it is combined with Quinine.
RabeprazoleThe serum concentration of Topotecan can be increased when it is combined with Rabeprazole.
Rabies vaccineThe risk or severity of adverse effects can be increased when Topotecan is combined with Rabies vaccine.
RanitidineThe serum concentration of Topotecan can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Topotecan can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Topotecan can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Topotecan can be increased when it is combined with Regorafenib.
ReserpineThe serum concentration of Topotecan can be increased when it is combined with Reserpine.
RifampicinThe serum concentration of Topotecan can be increased when it is combined with Rifampicin.
RilpivirineThe serum concentration of Topotecan can be increased when it is combined with Rilpivirine.
RitonavirThe serum concentration of Topotecan can be increased when it is combined with Ritonavir.
RoflumilastRoflumilast may increase the immunosuppressive activities of Topotecan.
RolapitantThe serum concentration of Topotecan can be increased when it is combined with Rolapitant.
SaquinavirThe serum concentration of Topotecan can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be decreased when it is combined with Topotecan.
ScopolamineThe serum concentration of Topotecan can be increased when it is combined with Scopolamine.
SelegilineThe serum concentration of Topotecan can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Topotecan can be increased when it is combined with Sertraline.
SimeprevirThe serum concentration of Topotecan can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Topotecan can be increased when it is combined with Simvastatin.
Sipuleucel-TThe therapeutic efficacy of Sipuleucel-T can be decreased when used in combination with Topotecan.
SirolimusThe serum concentration of Topotecan can be increased when it is combined with Sirolimus.
SorafenibThe serum concentration of Topotecan can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Topotecan can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Topotecan can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Topotecan can be increased when it is combined with Staurosporine.
StreptozocinThe serum concentration of Topotecan can be decreased when it is combined with Streptozocin.
SulfasalazineThe serum concentration of Topotecan can be increased when it is combined with Sulfasalazine.
SulfinpyrazoneThe serum concentration of Topotecan can be increased when it is combined with Sulfinpyrazone.
SumatriptanThe serum concentration of Topotecan can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Topotecan can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Topotecan can be increased when it is combined with Tacrine.
TacrolimusThe risk or severity of adverse effects can be increased when Tacrolimus is combined with Topotecan.
TamoxifenThe serum concentration of Topotecan can be increased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Topotecan can be increased when it is combined with Taurocholic Acid.
TelmisartanThe serum concentration of Topotecan can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Topotecan can be increased when it is combined with Temsirolimus.
TerazosinThe serum concentration of Topotecan can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Topotecan can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Topotecan can be increased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Topotecan can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Topotecan can be increased when it is combined with Testosterone.
TicagrelorThe serum concentration of Topotecan can be increased when it is combined with Ticagrelor.
TofacitinibTopotecan may increase the immunosuppressive activities of Tofacitinib.
TolvaptanThe serum concentration of Topotecan can be increased when it is combined with Tolvaptan.
TrastuzumabTrastuzumab may increase the neutropenic activities of Topotecan.
TrazodoneThe serum concentration of Topotecan can be decreased when it is combined with Trazodone.
TrifluoperazineThe serum concentration of Topotecan can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Topotecan can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Topotecan can be increased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Topotecan can be increased when it is combined with Trimipramine.
TroleandomycinThe serum concentration of Topotecan can be increased when it is combined with Troleandomycin.
VandetanibThe serum concentration of Topotecan can be increased when it is combined with Vandetanib.
VenlafaxineThe serum concentration of Topotecan can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Topotecan can be increased when it is combined with Verapamil.
VinblastineThe serum concentration of Topotecan can be increased when it is combined with Vinblastine.
VincristineThe serum concentration of Topotecan can be increased when it is combined with Vincristine.
VinorelbineThe serum concentration of Topotecan can be increased when it is combined with Vinorelbine.
VismodegibThe serum concentration of Topotecan can be increased when it is combined with Vismodegib.
ZimelidineThe serum concentration of Topotecan can be increased when it is combined with Zimelidine.
Food InteractionsNot Available

Targets

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. Schmidt F, Rieger J, Wischhusen J, Naumann U, Weller M: Glioma cell sensitivity to topotecan: the role of p53 and topotecan-induced DNA damage. Eur J Pharmacol. 2001 Jan 19;412(1):21-5. [PubMed:11166732 ]
  2. strel'tsov SA, Mikheikin AL, Nechipurenko IuD: [Interaction of topotecan--a DNA topoisomerase I inhibitor--with dual-stranded polydeoxyribonucleotides. II. Formation of a complex containing several DNA molecules in the presence of topotecan]. Mol Biol (Mosk). 2001 May-Jun;35(3):442-50. [PubMed:11443926 ]
  3. Streltsov SA: Action models for the antitumor drug camptothecin: formation of alkali-labile complex with DNA and inhibition of human DNA topoisomerase I. J Biomol Struct Dyn. 2002 Dec;20(3):447-54. [PubMed:12437383 ]
  4. Zhang J, Pu SP, Zhou YJ: [Preliminary study of apoptosis of human hepatocarcinoma cell line HepG2 induced by topotecan]. Ai Zheng. 2002 Dec;21(12):1305-9. [PubMed:12520736 ]
  5. Aisner J, Musanti R, Beers S, Smith S, Locsin S, Rubin EH: Sequencing topotecan and etoposide plus cisplatin to overcome topoisomerase I and II resistance: a pharmacodynamically based Phase I trial. Clin Cancer Res. 2003 Jul;9(7):2504-9. [PubMed:12855624 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Kollmannsberger C, Mross K, Jakob A, Kanz L, Bokemeyer C: Topotecan - A novel topoisomerase I inhibitor: pharmacology and clinical experience. Oncology. 1999;56(1):1-12. [PubMed:9885371 ]
  8. Herben VM, ten Bokkel Huinink WW, Beijnen JH: Clinical pharmacokinetics of topotecan. Clin Pharmacokinet. 1996 Aug;31(2):85-102. [PubMed:8853931 ]
  9. Dennis MJ, Beijnen JH, Grochow LB, van Warmerdam LJ: An overview of the clinical pharmacology of topotecan. Semin Oncol. 1997 Feb;24(1 Suppl 5):S5-12-S5-18. [PubMed:9122737 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
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. Kosovsky MJ, Soslau G: Immunological identification of human platelet mitochondrial DNA topoisomerase I. Biochim Biophys Acta. 1993 Jun 24;1164(1):101-7. [PubMed:8390858 ]
3. 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. Staker BL, Hjerrild K, Feese MD, Behnke CA, Burgin AB Jr, Stewart L: The mechanism of topoisomerase I poisoning by a camptothecin analog. Proc Natl Acad Sci U S A. 2002 Nov 26;99(24):15387-92. Epub 2002 Nov 8. [PubMed:12426403 ]
  2. Pourquier P, Takebayashi Y, Urasaki Y, Gioffre C, Kohlhagen G, Pommier Y: Induction of topoisomerase I cleavage complexes by 1-beta -D-arabinofuranosylcytosine (ara-C) in vitro and in ara-C-treated cells. Proc Natl Acad Sci U S A. 2000 Feb 15;97(4):1885-90. [PubMed:10677551 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitorinducer
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. 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
substrateinhibitor
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. Houghton PJ, Germain GS, Harwood FC, Schuetz JD, Stewart CF, Buchdunger E, Traxler P: Imatinib mesylate is a potent inhibitor of the ABCG2 (BCRP) transporter and reverses resistance to topotecan and SN-38 in vitro. Cancer Res. 2004 Apr 1;64(7):2333-7. [PubMed:15059881 ]
  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 ]
  3. Sugimoto Y, Tsukahara S, Imai Y, Sugimoto Y, Ueda K, Tsuruo T: Reversal of breast cancer resistance protein-mediated drug resistance by estrogen antagonists and agonists. Mol Cancer Ther. 2003 Jan;2(1):105-12. [PubMed:12533678 ]
  4. Maliepaard M, van Gastelen MA, de Jong LA, Pluim D, van Waardenburg RC, Ruevekamp-Helmers MC, Floot BG, Schellens JH: Overexpression of the BCRP/MXR/ABCP gene in a topotecan-selected ovarian tumor cell line. Cancer Res. 1999 Sep 15;59(18):4559-63. [PubMed:10493507 ]
  5. Jonker JW, Smit JW, Brinkhuis RF, Maliepaard M, Beijnen JH, Schellens JH, Schinkel AH: Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan. J Natl Cancer Inst. 2000 Oct 18;92(20):1651-6. [PubMed:11036110 ]
  6. Allen JD, Van Dort SC, Buitelaar M, van Tellingen O, Schinkel AH: Mouse breast cancer resistance protein (Bcrp1/Abcg2) mediates etoposide resistance and transport, but etoposide oral availability is limited primarily by P-glycoprotein. Cancer Res. 2003 Mar 15;63(6):1339-44. [PubMed:12649196 ]
  7. Breedveld P, Zelcer N, Pluim D, Sonmezer O, Tibben MM, Beijnen JH, Schinkel AH, van Tellingen O, Borst P, Schellens JH: Mechanism of the pharmacokinetic interaction between methotrexate and benzimidazoles: potential role for breast cancer resistance protein in clinical drug-drug interactions. Cancer Res. 2004 Aug 15;64(16):5804-11. [PubMed:15313923 ]
  8. Carcaboso AM, Elmeliegy MA, Shen J, Juel SJ, Zhang ZM, Calabrese C, Tracey L, Waters CM, Stewart CF: Tyrosine kinase inhibitor gefitinib enhances topotecan penetration of gliomas. Cancer Res. 2010 Jun 1;70(11):4499-508. doi: 10.1158/0008-5472.CAN-09-4264. Epub 2010 May 11. [PubMed:20460504 ]
  9. Shen J, Carcaboso AM, Hubbard KE, Tagen M, Wynn HG, Panetta JC, Waters CM, Elmeliegy MA, Stewart CF: Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid. Cancer Res. 2009 Jul 15;69(14):5885-92. doi: 10.1158/0008-5472.CAN-09-0700. Epub 2009 Jun 30. [PubMed:19567673 ]
  10. Rocchi E, Khodjakov A, Volk EL, Yang CH, Litman T, Bates SE, Schneider E: The product of the ABC half-transporter gene ABCG2 (BCRP/MXR/ABCP) is expressed in the plasma membrane. Biochem Biophys Res Commun. 2000 Apr 29;271(1):42-6. [PubMed:10777678 ]
  11. Ishii M, Iwahana M, Mitsui I, Minami M, Imagawa S, Tohgo A, Ejima A: Growth inhibitory effect of a new camptothecin analog, DX-8951f, on various drug-resistant sublines including BCRP-mediated camptothecin derivative-resistant variants derived from the human lung cancer cell line PC-6. Anticancer Drugs. 2000 Jun;11(5):353-62. [PubMed:10912951 ]
  12. Yang CH, Schneider E, Kuo ML, Volk EL, Rocchi E, Chen YC: BCRP/MXR/ABCP expression in topotecan-resistant human breast carcinoma cells. Biochem Pharmacol. 2000 Sep 15;60(6):831-7. [PubMed:10930538 ]
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. Collett A, Tanianis-Hughes J, Hallifax D, Warhurst G: Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo. Pharm Res. 2004 May;21(5):819-26. [PubMed:15180340 ]
  2. Carcaboso AM, Elmeliegy MA, Shen J, Juel SJ, Zhang ZM, Calabrese C, Tracey L, Waters CM, Stewart CF: Tyrosine kinase inhibitor gefitinib enhances topotecan penetration of gliomas. Cancer Res. 2010 Jun 1;70(11):4499-508. doi: 10.1158/0008-5472.CAN-09-4264. Epub 2010 May 11. [PubMed:20460504 ]
  3. Shen J, Carcaboso AM, Hubbard KE, Tagen M, Wynn HG, Panetta JC, Waters CM, Elmeliegy MA, Stewart CF: Compartment-specific roles of ATP-binding cassette transporters define differential topotecan distribution in brain parenchyma and cerebrospinal fluid. Cancer Res. 2009 Jul 15;69(14):5885-92. doi: 10.1158/0008-5472.CAN-09-0700. Epub 2009 Jun 30. [PubMed:19567673 ]
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Drug created on June 13, 2005 07:24 / Updated on September 26, 2016 02:12