Identification

Name
Topotecan
Accession Number
DB01030  (APRD00687)
Type
Small Molecule
Groups
Approved, Investigational
Description

An 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 IDs
SKF-104864
Product Ingredients
IngredientUNIICASInChI Key
Topotecan hydrochloride956S425ZCY119413-54-6DGHHQBMTXTWTJV-BQAIUKQQSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Act TopotecanPowder, for solution1 mgIntravenousActavis Pharma CompanyNot applicableNot applicableCanada
Act TopotecanPowder, for solution4 mgIntravenousActavis Pharma Company2015-11-17Not applicableCanada
HycamtinCapsule1 mg/1OralNovartis2017-02-24Not applicableUs
HycamtinCapsule0.25 mgOralNovartis Europharm Limited1996-11-12Not applicableEu
HycamtinPowder, for solution4 mgIntravenousNovartis1997-06-18Not applicableCanada
HycamtinCapsule.25 mg/1OralGlaxosmithkline Inc2008-09-162017-12-31Us00007 4205 11 nlmimage10 1c198e1c
HycamtinInjection, powder, for solution4 mgIntravenousNovartis Europharm Limited1996-11-12Not applicableEu
HycamtinCapsule.25 mg/1OralNovartis2017-07-07Not applicableUs
HycamtinInjection, powder, for solution1 mgIntravenousNovartis Europharm Limited1996-11-12Not applicableEu
HycamtinInjection, powder, lyophilized, for solution4 mg/4mLIntravenousGlaxosmithkline Inc1996-06-07Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Mylan-topotecan Hydrochloride for InjectionPowder, for solution4 mgIntravenousMylan PharmaceuticalsNot applicableNot applicableCanada
PMS-topotecanPowder, for solution1 mgIntravenousPharmascience IncNot applicableNot applicableCanada
PMS-topotecanPowder, for solution4 mgIntravenousPharmascience Inc2013-08-29Not applicableCanada
PotactasolInjection, powder, for solution4 mgIntravenousActavis Group Ptc Ehf.2011-01-06Not applicableEu
PotactasolInjection, powder, for solution1 mgIntravenousActavis Group Ptc Ehf.2011-01-06Not applicableEu
TopotecanInjection, powder, lyophilized, for solution4 mg/4mLIntravenousIngenus Pharmaceuticals Llc2016-12-07Not applicableUs
TopotecanInjection, solution, concentrate1 mg/mLIntravenousMylan Institutional2018-04-09Not applicableUs
Topotecan ActavisInjection, powder, for solution1 mgIntravenousActavis Group Ptc Ehf.2009-07-24Not applicableEu
Topotecan ActavisInjection, powder, for solution4 mgIntravenousActavis Group Ptc Ehf.2009-07-24Not applicableEu
Topotecan ActavisInjection, powder, for solution4 mgIntravenousActavis Group Ptc Ehf.2009-07-24Not applicableEu
Categories
UNII
7M7YKX2N15
CAS number
123948-87-8
Weight
Average: 421.4458
Monoisotopic: 421.163770861
Chemical Formula
C23H23N3O5
InChI Key
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

Pharmacology

Indication

For 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.

Associated Conditions
Pharmacodynamics

Topotecan, 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 action

Topotecan 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.

TargetActionsOrganism
ADNA topoisomerase 1
inhibitor
Human
UDNA topoisomerase I, mitochondrial
inhibitor
Human
ADNA
intercalation
Human
Absorption
Not Available
Volume of distribution
Not Available
Protein binding

35%

Metabolism

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

Route of elimination

Renal 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 life

2-3 hours

Clearance
Not Available
Toxicity

The primary anticipated complication of overdosage would consist of bone marrow suppression.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbemaciclibThe serum concentration of Topotecan can be increased when it is combined with Abemaciclib.Approved, Investigational
AcetaminophenThe serum concentration of Topotecan can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Topotecan.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Topotecan.Experimental
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Topotecan.Approved
AfatinibThe serum concentration of Topotecan can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Topotecan can be increased when it is combined with Albendazole.Approved, Vet Approved
AldesleukinThe risk or severity of adverse effects can be increased when Topotecan is combined with Aldesleukin.Approved
AlectinibThe serum concentration of Topotecan can be increased when it is combined with Alectinib.Approved, Investigational
AlfentanilThe serum concentration of Topotecan can be increased when it is combined with Alfentanil.Approved, Illicit
AmantadineThe serum concentration of Topotecan can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Topotecan can be increased when it is combined with Aminohippuric acid.Approved, Investigational
AmiodaroneThe serum concentration of Topotecan can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Topotecan can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Topotecan can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Topotecan can be increased when it is combined with Amprenavir.Approved, Investigational
AmsacrineThe serum concentration of Topotecan can be increased when it is combined with Amsacrine.Approved, Investigational
AnakinraThe risk or severity of adverse effects can be increased when Anakinra is combined with Topotecan.Approved
AncestimThe risk or severity of cytotoxicity can be increased when Ancestim is combined with Topotecan.Approved, Investigational, Withdrawn
Anthrax immune globulin humanThe risk or severity of adverse effects can be increased when Topotecan is combined with Anthrax immune globulin human.Approved
ApalutamideThe serum concentration of Topotecan can be decreased when it is combined with Apalutamide.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be decreased when it is combined with Topotecan.Approved, Investigational
AstemizoleThe serum concentration of Topotecan can be increased when it is combined with Astemizole.Approved, Withdrawn
AsunaprevirThe serum concentration of Asunaprevir can be decreased when it is combined with Topotecan.Approved, Investigational, Withdrawn
AtazanavirThe serum concentration of Topotecan can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Topotecan can be increased when it is combined with Atenolol.Approved
AtorvastatinThe risk or severity of adverse effects can be increased when Topotecan is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Topotecan can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Topotecan can be increased when it is combined with Azithromycin.Approved
Bacillus calmette-guerin substrain connaught live antigenThe risk or severity of adverse effects can be increased when Topotecan is combined with Bacillus calmette-guerin substrain connaught live antigen.Approved, Investigational
Bacillus calmette-guerin substrain tice live antigenThe risk or severity of adverse effects can be increased when Topotecan is combined with Bacillus calmette-guerin substrain tice live antigen.Approved
BaricitinibThe serum concentration of Topotecan can be increased when it is combined with Baricitinib.Approved, Investigational
BCG vaccineThe therapeutic efficacy of BCG vaccine can be decreased when used in combination with Topotecan.Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Topotecan is combined with Beclomethasone dipropionate.Approved, Investigational
Benzyl alcoholThe serum concentration of Topotecan can be increased when it is combined with Benzyl alcohol.Approved
BepridilThe serum concentration of Topotecan can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Topotecan.Approved, Investigational
BiperidenThe serum concentration of Topotecan can be increased when it is combined with Biperiden.Approved, Investigational
BoceprevirThe serum concentration of Topotecan can be increased when it is combined with Boceprevir.Approved, Withdrawn
BosutinibThe serum concentration of Topotecan can be increased when it is combined with Bosutinib.Approved
BrigatinibThe serum concentration of Topotecan can be increased when it is combined with Brigatinib.Approved, Investigational
BromocriptineThe serum concentration of Topotecan can be increased when it is combined with Bromocriptine.Approved, Investigational
BudesonideThe risk or severity of adverse effects can be increased when Topotecan is combined with Budesonide.Approved
BuprenorphineThe serum concentration of Topotecan can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BuspironeThe serum concentration of Topotecan can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Topotecan can be increased when it is combined with Cabazitaxel.Approved
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is combined with Topotecan.Approved
CaffeineThe serum concentration of Topotecan can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Topotecan can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Topotecan can be increased when it is combined with Candesartan.Experimental
Candesartan cilexetilThe serum concentration of Topotecan can be increased when it is combined with Candesartan cilexetil.Approved
CannabidiolThe serum concentration of Topotecan can be increased when it is combined with Cannabidiol.Approved, Investigational
CaptoprilThe serum concentration of Topotecan can be increased when it is combined with Captopril.Approved
CarbamazepineThe risk or severity of adverse effects can be increased when Topotecan is combined with Carbamazepine.Approved, Investigational
CarboplatinThe risk or severity of adverse effects can be increased when Carboplatin is combined with Topotecan.Approved
CarvedilolThe serum concentration of Topotecan can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Topotecan can be increased when it is combined with Caspofungin.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Topotecan.Approved, Withdrawn
ChloroquineThe serum concentration of Topotecan can be increased when it is combined with Chloroquine.Approved, Investigational, Vet Approved
ChlorpromazineThe serum concentration of Topotecan can be increased when it is combined with Chlorpromazine.Approved, Investigational, Vet Approved
ChlorpropamideThe serum concentration of Topotecan can be increased when it is combined with Chlorpropamide.Approved, Investigational
ChlorprothixeneThe serum concentration of Topotecan can be increased when it is combined with Chlorprothixene.Approved, Investigational, Withdrawn
CholesterolThe serum concentration of Topotecan can be increased when it is combined with Cholesterol.Approved, Investigational
CilazaprilThe serum concentration of Topotecan can be increased when it is combined with Cilazapril.Approved
CisplatinThe risk or severity of adverse effects can be increased when Cisplatin is combined with Topotecan.Approved
CitalopramThe serum concentration of Topotecan can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Topotecan can be increased when it is combined with Clarithromycin.Approved
ClofazimineThe serum concentration of Topotecan can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Topotecan can be increased when it is combined with Clomipramine.Approved, Investigational, Vet Approved
Clostridium tetani toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Topotecan is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated).Approved
ClozapineThe risk or severity of adverse effects can be increased when Topotecan is combined with Clozapine.Approved
CobicistatThe serum concentration of Topotecan can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Topotecan can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Topotecan can be increased when it is combined with Colforsin.Experimental, Investigational
Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Topotecan is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated).Approved
CrizotinibThe serum concentration of Topotecan can be increased when it is combined with Crizotinib.Approved
CurcuminThe serum concentration of Topotecan can be increased when it is combined with Curcumin.Approved, Investigational
CyclophosphamideThe serum concentration of Topotecan can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Topotecan can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Topotecan.Experimental
DabrafenibThe serum concentration of Topotecan can be increased when it is combined with Dabrafenib.Approved, Investigational
DaclatasvirThe serum concentration of Topotecan can be increased when it is combined with Daclatasvir.Approved, Investigational
DactinomycinThe serum concentration of Topotecan can be increased when it is combined with Dactinomycin.Approved, Investigational
DaidzinThe serum concentration of Topotecan can be increased when it is combined with Daidzin.Experimental
DasabuvirThe serum concentration of Topotecan can be increased when it is combined with Dasabuvir.Approved
DasatinibThe serum concentration of Topotecan can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Topotecan can be increased when it is combined with Daunorubicin.Approved
DenosumabThe risk or severity of adverse effects can be increased when Denosumab is combined with Topotecan.Approved
DesipramineThe serum concentration of Topotecan can be increased when it is combined with Desipramine.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Topotecan.Approved
DesloratadineThe serum concentration of Topotecan can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Topotecan can be increased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexniguldipineThe serum concentration of Topotecan can be increased when it is combined with Dexniguldipine.Experimental
DexverapamilThe serum concentration of Topotecan can be increased when it is combined with Dexverapamil.Experimental
DiethylstilbestrolThe serum concentration of Topotecan can be increased when it is combined with Diethylstilbestrol.Approved, Investigational
DigitoxinDigitoxin may decrease the cardiotoxic activities of Topotecan.Approved, Investigational
DigoxinThe serum concentration of Topotecan can be increased when it is combined with Digoxin.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Topotecan.Approved
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Topotecan.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Topotecan.Approved, Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Topotecan.Experimental
DihydroergotamineThe serum concentration of Topotecan can be increased when it is combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe serum concentration of Topotecan can be increased when it is combined with Diltiazem.Approved, Investigational
DipyridamoleThe serum concentration of Topotecan 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 Topotecan.Approved, Investigational
DoxazosinThe serum concentration of Topotecan can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Topotecan can be increased when it is combined with Doxepin.Approved, Investigational
DoxorubicinThe serum concentration of Topotecan can be increased when it is combined with Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Topotecan can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Topotecan can be increased when it is combined with Dronedarone.Approved
ElacridarThe serum concentration of Topotecan can be increased when it is combined with Elacridar.Investigational
EltrombopagThe serum concentration of Topotecan can be increased when it is combined with Eltrombopag.Approved
EmopamilThe serum concentration of Topotecan can be increased when it is combined with Emopamil.Experimental
EnalaprilThe serum concentration of Topotecan can be increased when it is combined with Enalapril.Approved, Vet Approved
EnasidenibThe serum concentration of Topotecan can be increased when it is combined with Enasidenib.Approved, Investigational
EnzalutamideThe serum concentration of Topotecan can be increased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Topotecan can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Topotecan can be increased when it is combined with Ergotamine.Approved
ErlotinibThe serum concentration of Topotecan can be increased when it is combined with Erlotinib.Approved, Investigational
ErythromycinThe serum concentration of Topotecan can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EstradiolThe serum concentration of Topotecan can be increased when it is combined with Estradiol.Approved, Investigational, Vet Approved
Estradiol acetateThe serum concentration of Topotecan can be increased when it is combined with Estradiol acetate.Approved, Investigational, Vet Approved
Estradiol benzoateThe serum concentration of Topotecan can be increased when it is combined with Estradiol benzoate.Approved, Investigational, Vet Approved
Estradiol cypionateThe serum concentration of Topotecan can be increased when it is combined with Estradiol cypionate.Approved, Investigational, Vet Approved
Estradiol dienanthateThe serum concentration of Topotecan can be increased when it is combined with Estradiol dienanthate.Approved, Investigational, Vet Approved
Estradiol valerateThe serum concentration of Topotecan can be increased when it is combined with Estradiol valerate.Approved, Investigational, Vet Approved
EstramustineThe serum concentration of Topotecan can be increased when it is combined with Estramustine.Approved, Investigational
EstroneThe serum concentration of Topotecan can be increased when it is combined with Estrone.Approved
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Topotecan.Approved, Investigational
EtoposideThe serum concentration of Topotecan can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Topotecan can be increased when it is combined with Etravirine.Approved
EverolimusThe risk or severity of adverse effects can be increased when Everolimus is combined with Topotecan.Approved
FelodipineThe serum concentration of Topotecan can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Topotecan can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FexofenadineThe serum concentration of Topotecan can be increased when it is combined with Fexofenadine.Approved, Investigational
FidaxomicinThe serum concentration of Topotecan can be increased when it is combined with Fidaxomicin.Approved
FilgrastimThe risk or severity of adverse effects can be increased when Filgrastim is combined with Topotecan.Approved
FingolimodTopotecan may increase the immunosuppressive activities of Fingolimod.Approved, Investigational
FluconazoleThe serum concentration of Topotecan can be increased when it is combined with Fluconazole.Approved, Investigational
FluoxetineThe serum concentration of Topotecan can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Topotecan can be increased when it is combined with Flupentixol.Approved, Investigational, Withdrawn
FluphenazineThe serum concentration of Topotecan can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Topotecan can be increased when it is combined with Flurazepam.Approved, Illicit, Investigational
Fluticasone propionateThe risk or severity of adverse effects can be increased when Topotecan is combined with Fluticasone propionate.Approved
FluvoxamineThe serum concentration of Topotecan can be increased when it is combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe serum concentration of Topotecan can be decreased when it is combined with Fosphenytoin.Approved, Investigational
G17DTThe risk or severity of adverse effects can be increased when Topotecan is combined with G17DT.Investigational
GallopamilThe serum concentration of Topotecan can be increased when it is combined with Gallopamil.Investigational
GefitinibThe serum concentration of Topotecan can be increased when it is combined with Gefitinib.Approved, Investigational
GemcitabineThe risk or severity of adverse effects can be increased when Gemcitabine is combined with Topotecan.Approved
Gemtuzumab ozogamicinThe risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Topotecan.Approved, Investigational
GenisteinThe serum concentration of Topotecan can be increased when it is combined with Genistein.Investigational
GI-5005The risk or severity of adverse effects can be increased when Topotecan is combined with GI-5005.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Topotecan.Experimental
GlecaprevirThe serum concentration of Topotecan can be increased when it is combined with Glecaprevir.Approved, Investigational
GlyburideThe serum concentration of Topotecan can be increased when it is combined with Glyburide.Approved
GlycerinThe serum concentration of Topotecan can be increased when it is combined with Glycerin.Approved, Investigational
Gramicidin DThe serum concentration of Topotecan can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Topotecan can be increased when it is combined with Grepafloxacin.Approved, Investigational, Withdrawn
HaloperidolThe serum concentration of Topotecan can be increased when it is combined with Haloperidol.Approved
Hepatitis A VaccineThe risk or severity of adverse effects can be increased when Topotecan is combined with Hepatitis A Vaccine.Approved
Hepatitis B Vaccine (Recombinant)The risk or severity of adverse effects can be increased when Topotecan is combined with Hepatitis B Vaccine (Recombinant).Approved, Withdrawn
HesperetinThe serum concentration of Topotecan can be increased when it is combined with Hesperetin.Approved
Human rabies virus immune globulinThe risk or severity of adverse effects can be increased when Topotecan is combined with Human rabies virus immune globulin.Approved
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Topotecan.Approved, Vet Approved
Hydrocortisone acetateThe risk or severity of adverse effects can be increased when Topotecan is combined with Hydrocortisone acetate.Approved, Vet Approved
Hydrocortisone butyrateThe risk or severity of adverse effects can be increased when Topotecan is combined with Hydrocortisone butyrate.Approved, Vet Approved
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Topotecan.Approved
IbuprofenThe serum concentration of Topotecan can be increased when it is combined with Ibuprofen.Approved
IdelalisibThe serum concentration of Topotecan can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Topotecan can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Topotecan can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Topotecan can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Topotecan can be increased when it is combined with Indomethacin.Approved, Investigational
INGN 201The risk or severity of adverse effects can be increased when Topotecan is combined with INGN 201.Investigational
INGN 225The risk or severity of adverse effects can be increased when Topotecan is combined with INGN 225.Investigational
Interferon alfa-n3The risk or severity of adverse effects can be increased when Topotecan is combined with Interferon alfa-n3.Approved, Investigational
IrinotecanThe risk or severity of adverse effects can be increased when Irinotecan is combined with Topotecan.Approved, Investigational
IsavuconazoleThe serum concentration of Topotecan can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe serum concentration of Topotecan can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsradipineThe serum concentration of Topotecan can be increased when it is combined with Isradipine.Approved, Investigational
ItraconazoleThe serum concentration of Topotecan can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Topotecan can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Topotecan can be increased when it is combined with Ivermectin.Approved, Investigational, Vet Approved
Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated)The risk or severity of adverse effects can be increased when Topotecan is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated).Approved
KetamineThe serum concentration of Topotecan can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Topotecan can be increased when it is combined with Ketoconazole.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Topotecan.Experimental
LansoprazoleThe serum concentration of Topotecan can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Topotecan can be increased when it is combined with Lapatinib.Approved, Investigational
LeflunomideThe risk or severity of adverse effects can be increased when Topotecan is combined with Leflunomide.Approved, Investigational
LetermovirThe serum concentration of Topotecan can be increased when it is combined with Letermovir.Approved, Investigational
LevofloxacinThe serum concentration of Topotecan can be increased when it is combined with Levofloxacin.Approved, Investigational
LidocaineThe serum concentration of Topotecan can be increased when it is combined with Lidocaine.Approved, Vet Approved
LipegfilgrastimTopotecan may increase the myelosuppressive activities of Lipegfilgrastim.Approved, Investigational
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Topotecan.Approved, Investigational
LomerizineThe serum concentration of Topotecan can be increased when it is combined with Lomerizine.Experimental
LomitapideThe serum concentration of Topotecan can be increased when it is combined with Lomitapide.Approved, Investigational
LoperamideThe serum concentration of Topotecan can be increased when it is combined with Loperamide.Approved
LopinavirThe serum concentration of Topotecan can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Topotecan can be increased when it is combined with Loratadine.Approved, Investigational
LosartanThe serum concentration of Topotecan can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Topotecan can be increased when it is combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Topotecan can be increased when it is combined with Lumacaftor.Approved
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Topotecan.Illicit, Investigational, Withdrawn
MaprotilineThe serum concentration of Topotecan can be increased when it is combined with Maprotiline.Approved, Investigational
MebendazoleThe serum concentration of Topotecan can be increased when it is combined with Mebendazole.Approved, Vet Approved
Medical CannabisThe serum concentration of Topotecan can be increased when it is combined with Medical Cannabis.Experimental, Investigational
MefloquineThe serum concentration of Topotecan can be increased when it is combined with Mefloquine.Approved, Investigational
Megestrol acetateThe serum concentration of Topotecan can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
MeprobamateThe serum concentration of Topotecan can be increased when it is combined with Meprobamate.Approved, Illicit
MetamizoleThe risk or severity of myelosuppression can be increased when Metamizole is combined with Topotecan.Approved, Investigational, Withdrawn
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Topotecan.Experimental
MethadoneThe serum concentration of Topotecan can be increased when it is combined with Methadone.Approved
MethimazoleThe risk or severity of adverse effects can be increased when Topotecan is combined with Methimazole.Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Topotecan.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Topotecan.Approved, Vet Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Topotecan.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Topotecan.Experimental
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Topotecan.Experimental
MibefradilThe serum concentration of Topotecan can be increased when it is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Topotecan can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Topotecan can be increased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Topotecan can be increased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Topotecan can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Topotecan can be increased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Topotecan can be increased when it is combined with Morphine.Approved, Investigational
NabiximolsThe serum concentration of Topotecan can be increased when it is combined with Nabiximols.Approved, Investigational
NaltrexoneThe serum concentration of Topotecan can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Topotecan can be increased when it is combined with Naringenin.Experimental
NatalizumabThe risk or severity of adverse effects can be increased when Topotecan is combined with Natalizumab.Approved, Investigational
NedaplatinThe risk or severity of adverse effects can be increased when Nedaplatin is combined with Topotecan.Approved, Investigational
NelfinavirThe serum concentration of Topotecan can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Topotecan can be increased when it is combined with Neostigmine.Approved, Vet Approved
NicardipineThe serum concentration of Topotecan can be increased when it is combined with Nicardipine.Approved, Investigational
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Topotecan.Approved, Investigational
NiguldipineThe serum concentration of Topotecan can be increased when it is combined with Niguldipine.Experimental
NilotinibThe serum concentration of Topotecan can be increased when it is combined with Nilotinib.Approved, Investigational
NimodipineThe serum concentration of Topotecan can be increased when it is combined with Nimodipine.Approved, Investigational
NisoldipineThe serum concentration of Topotecan can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Topotecan can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Topotecan can be increased when it is combined with Nitrendipine.Approved, Investigational
NOV-002The risk or severity of adverse effects can be increased when NOV-002 is combined with Topotecan.Investigational
NovobiocinThe serum concentration of Topotecan can be increased when it is combined with Novobiocin.Approved, Investigational, Vet Approved
OcrelizumabOcrelizumab may increase the immunosuppressive activities of Topotecan.Approved, Investigational
OleandrinOleandrin may decrease the cardiotoxic activities of Topotecan.Experimental, Investigational
OmeprazoleThe serum concentration of Topotecan can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OuabainOuabain may decrease the cardiotoxic activities of Topotecan.Approved
OxaliplatinThe risk or severity of adverse effects can be increased when Oxaliplatin is combined with Topotecan.Approved, Investigational
P-NitrophenolThe serum concentration of Topotecan can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Topotecan can be increased when it is combined with Paclitaxel.Approved, Vet Approved
PaliferminThe therapeutic efficacy of Palifermin can be decreased when used in combination with Topotecan.Approved
Palmitic AcidThe serum concentration of Topotecan can be increased when it is combined with Palmitic Acid.Approved, Experimental
PantoprazoleThe serum concentration of Topotecan can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Topotecan can be increased when it is combined with Paroxetine.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Topotecan.Approved
PegaspargaseThe risk or severity of adverse effects can be increased when Pegaspargase is combined with Topotecan.Approved, Investigational
Peginterferon alfa-2aThe risk or severity of adverse effects can be increased when Topotecan is combined with Peginterferon alfa-2a.Approved, Investigational
Peginterferon alfa-2bThe risk or severity of adverse effects can be increased when Topotecan is combined with Peginterferon alfa-2b.Approved
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Topotecan.Approved, Investigational, Vet Approved, Withdrawn
PerindoprilThe serum concentration of Topotecan can be increased when it is combined with Perindopril.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Topotecan.Experimental
PhenytoinThe serum concentration of Topotecan can be decreased when it is combined with Phenytoin.Approved, Vet Approved
PibrentasvirThe serum concentration of Topotecan can be increased when it is combined with Pibrentasvir.Approved, Investigational
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Topotecan.Approved, Investigational
PimozideThe serum concentration of Topotecan can be increased when it is combined with Pimozide.Approved
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Topotecan.Approved
PitolisantThe serum concentration of Topotecan can be decreased when it is combined with Pitolisant.Approved, Investigational
PonatinibThe serum concentration of Topotecan can be increased when it is combined with Ponatinib.Approved, Investigational
PosaconazoleThe serum concentration of Topotecan can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Topotecan can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Topotecan can be increased when it is combined with Prazosin.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Topotecan.Approved, Vet Approved
PrednisoneThe serum concentration of Topotecan can be increased when it is combined with Prednisone.Approved, Vet Approved
ProbenecidThe serum concentration of Topotecan can be increased when it is combined with Probenecid.Approved, Investigational
ProgesteroneThe serum concentration of Topotecan can be increased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Topotecan can be increased when it is combined with Promethazine.Approved, Investigational
PropafenoneThe serum concentration of Topotecan can be increased when it is combined with Propafenone.Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Topotecan.Experimental
ProtriptylineThe serum concentration of Topotecan can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Topotecan can be increased when it is combined with Quercetin.Experimental, Investigational
QuinacrineThe serum concentration of Topotecan can be increased when it is combined with Quinacrine.Approved, Investigational
QuinidineThe serum concentration of Topotecan can be increased when it is combined with Quinidine.Approved, Investigational
QuinineThe serum concentration of Topotecan can be increased when it is combined with Quinine.Approved
RabeprazoleThe serum concentration of Topotecan can be increased when it is combined with Rabeprazole.Approved, Investigational
Rabies virus inactivated antigen, AThe risk or severity of adverse effects can be increased when Topotecan is combined with Rabies virus inactivated antigen, A.Approved, Investigational
Rabies virus inactivated antigen, AThe therapeutic efficacy of Rabies virus inactivated antigen, A can be decreased when used in combination with Topotecan.Approved, Investigational
RanitidineThe serum concentration of Topotecan can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Topotecan can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Topotecan can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Topotecan can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Topotecan can be increased when it is combined with Reserpine.Approved, Investigational
RifampicinThe serum concentration of Topotecan can be increased when it is combined with Rifampicin.Approved
RilpivirineThe serum concentration of Topotecan can be increased when it is combined with Rilpivirine.Approved
RindopepimutThe risk or severity of adverse effects can be increased when Topotecan is combined with Rindopepimut.Investigational
RitonavirThe serum concentration of Topotecan can be increased when it is combined with Ritonavir.Approved, Investigational
RoflumilastRoflumilast may increase the immunosuppressive activities of Topotecan.Approved
RolapitantThe serum concentration of Topotecan can be increased when it is combined with Rolapitant.Approved, Investigational
Rotavirus VaccineThe risk or severity of adverse effects can be increased when Topotecan is combined with Rotavirus Vaccine.Approved
Rubella virus vaccineThe risk or severity of adverse effects can be increased when Topotecan is combined with Rubella virus vaccine.Approved, Investigational
RucaparibThe serum concentration of Topotecan can be increased when it is combined with Rucaparib.Approved, Investigational
Salmonella typhi ty2 vi polysaccharide antigenThe risk or severity of adverse effects can be increased when Topotecan is combined with Salmonella typhi ty2 vi polysaccharide antigen.Approved
Salmonella typhi Ty21a live antigenThe risk or severity of adverse effects can be increased when Topotecan is combined with Salmonella typhi ty21a live antigen.Approved
SaquinavirThe serum concentration of Topotecan can be increased when it is combined with Saquinavir.Approved, Investigational
SatraplatinThe risk or severity of adverse effects can be increased when Satraplatin is combined with Topotecan.Investigational
SelegilineThe serum concentration of Topotecan can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Topotecan can be increased when it is combined with Sertraline.Approved
SimeprevirThe serum concentration of Topotecan can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Topotecan can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Topotecan can be increased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Topotecan can be increased when it is combined with Sorafenib.Approved, Investigational
SRP 299The risk or severity of adverse effects can be increased when Topotecan is combined with SRP 299.Investigational
StaurosporineThe serum concentration of Topotecan can be increased when it is combined with Staurosporine.Experimental
SulfasalazineThe serum concentration of Topotecan can be increased when it is combined with Sulfasalazine.Approved
SulfinpyrazoneThe serum concentration of Topotecan can be increased when it is combined with Sulfinpyrazone.Approved
SunitinibThe serum concentration of Topotecan can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Topotecan can be increased when it is combined with Tacrine.Investigational, Withdrawn
TacrolimusThe serum concentration of Topotecan can be increased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Topotecan can be increased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Topotecan can be increased when it is combined with Taurocholic Acid.Experimental
TecemotideThe risk or severity of adverse effects can be increased when Topotecan is combined with Tecemotide.Investigational
TelaprevirThe serum concentration of Topotecan can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelmisartanThe serum concentration of Topotecan can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Topotecan can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Topotecan can be increased when it is combined with Terazosin.Approved
TerfenadineThe serum concentration of Topotecan can be increased when it is combined with Terfenadine.Approved, Withdrawn
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Topotecan.Experimental
TeriflunomideThe serum concentration of Topotecan can be increased when it is combined with Teriflunomide.Approved
TestosteroneThe serum concentration of Topotecan can be increased when it is combined with Testosterone.Approved, Investigational
Testosterone cypionateThe serum concentration of Topotecan can be increased when it is combined with Testosterone cypionate.Approved
Testosterone enanthateThe serum concentration of Topotecan can be increased when it is combined with Testosterone enanthate.Approved
Testosterone undecanoateThe serum concentration of Topotecan can be increased when it is combined with Testosterone undecanoate.Approved, Investigational
TetrandrineThe serum concentration of Topotecan can be increased when it is combined with Tetrandrine.Experimental
TG4010The risk or severity of adverse effects can be increased when Topotecan is combined with TG4010.Investigational
TicagrelorThe serum concentration of Topotecan can be increased when it is combined with Ticagrelor.Approved
TofacitinibTopotecan may increase the immunosuppressive activities of Tofacitinib.Approved, Investigational
TolvaptanThe serum concentration of Topotecan can be increased when it is combined with Tolvaptan.Approved
TopiroxostatThe serum concentration of Topotecan can be increased when it is combined with Topiroxostat.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Topotecan.Approved, Investigational
TrifluoperazineThe serum concentration of Topotecan can be increased when it is combined with Trifluoperazine.Approved, Investigational
TriflupromazineThe serum concentration of Topotecan can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Topotecan can be increased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Topotecan can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Topotecan can be increased when it is combined with Troleandomycin.Approved
Typhoid VaccineThe risk or severity of adverse effects can be increased when Topotecan is combined with Typhoid Vaccine.Approved
VandetanibThe serum concentration of Topotecan can be increased when it is combined with Vandetanib.Approved
Varicella Zoster Vaccine (Live/Attenuated)The risk or severity of adverse effects can be increased when Topotecan is combined with Varicella Zoster Vaccine (Live/Attenuated).Approved
VelpatasvirThe serum concentration of Topotecan can be increased when it is combined with Velpatasvir.Approved, Investigational
VemurafenibThe serum concentration of Topotecan can be increased when it is combined with Vemurafenib.Approved
VenlafaxineThe serum concentration of Topotecan can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Topotecan can be increased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Topotecan can be increased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Topotecan can be increased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Topotecan can be increased when it is combined with Vinorelbine.Approved, Investigational
VismodegibThe serum concentration of Topotecan can be increased when it is combined with Vismodegib.Approved, Investigational
VoacamineThe serum concentration of Topotecan can be increased when it is combined with Voacamine.Approved, Investigational
VoxilaprevirThe serum concentration of Topotecan can be increased when it is combined with Voxilaprevir.Approved, Investigational
Yellow Fever VaccineThe risk or severity of adverse effects can be increased when Topotecan is combined with Yellow Fever Vaccine.Approved, Investigational
ZidovudineThe risk or severity of adverse effects can be increased when Topotecan is combined with Zidovudine.Approved
ZimelidineThe serum concentration of Topotecan can be increased when it is combined with Zimelidine.Withdrawn
Food Interactions
Not 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
Human Metabolome Database
HMDB0015164
KEGG Compound
C11158
PubChem Compound
60700
PubChem Substance
46505204
ChemSpider
54705
BindingDB
50034026
ChEBI
63632
ChEMBL
CHEMBL84
Therapeutic Targets Database
DAP000648
PharmGKB
PA451729
HET
TTC
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Topotecan
ATC Codes
L01XX17 — Topotecan
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
1k4t / 1rr8 / 1rrj
FDA label
Download (78.6 KB)
MSDS
Download (29.3 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedTreatmentMalignant Gliomas / WHO Grade III or IV Recurrent Glioma1
0RecruitingTreatmentGliomas1
0RecruitingTreatmentHigh Grade Glioma (HGG) / Neoplasms, Brain1
1Active Not RecruitingTreatmentAdult Acute Megakaryoblastic Leukemia / Adult Acute Monoblastic Leukemia / Adult Acute Monocytic Leukemia / Adult Acute Myeloid Leukemia With Inv(16)(p13.1q22); CBFB-MYH11 / Adult Acute Myeloid Leukemia With Maturation / Adult Acute Myeloid Leukemia With Minimal Differentiation / Adult Acute Myeloid Leukemia With t(16;16)(p13.1;q22); CBFB-MYH11 / Adult Acute Myeloid Leukemia With t(8;21)(q22;q22); RUNX1-RUNX1T1 / Adult Acute Myeloid Leukemia With t(8;21); (q22; q22.1); RUNX1-RUNX1T1 / Adult Acute Myeloid Leukemia With t(9;11)(p22.3;q23.3); MLLT3-KMT2A / Adult Acute Myeloid Leukemia With t(9;11)(p22;q23); MLLT3-MLL / Adult Acute Myeloid Leukemia Without Maturation / Adult Acute Myelomonocytic Leukemia / Adult Erythroleukemia / Adult Pure Erythroid Leukemia / Chronic Myelomonocytic Leukemia / De Novo Myelodysplastic Syndrome / Essential Thrombocythemia (ET) / Hematopoietic and Lymphoid Cell Neoplasm / Myelodysplastic Syndrome / Philadelphia Chromosome Negative, BCR-ABL1 Positive Chronic Myelogenous Leukemia / Polycythemia Vera (PV) / Previously Treated Myelodysplastic Syndromes / Recurrent Adult Acute Lymphoblastic Leukemia / Recurrent Adult Acute Myeloid Leukemia / Recurrent Disease / Secondary Myelodysplastic Syndromes1
1Active Not RecruitingTreatmentAdult Central Nervous System Germ Cell Tumor / Adult Rhabdomyosarcoma / Childhood Central Nervous System Germ Cell Tumor / Childhood Soft Tissue Sarcoma / Ewing's Sarcoma (ES) / Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Ovarian Mixed Germ Cell Tumor / Previously Untreated Childhood Rhabdomyosarcoma / Recurrent Adult Brain Tumor / Recurrent Adult Soft Tissue Sarcoma / Recurrent Childhood Brain Stem Glioma / Recurrent Childhood Cerebellar Astrocytoma / Recurrent Childhood Cerebral Astrocytoma / Recurrent Childhood Ependymoma / Recurrent Childhood Malignant Germ Cell Tumor / Recurrent Childhood Medulloblastoma / Recurrent Childhood Pineoblastoma / Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor / Recurrent Childhood Visual Pathway and Hypothalamic Glioma / Recurrent Childhood Visual Pathway Glioma / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Extragonadal Germ Cell Tumor / Recurrent Extragonadal Non-seminomatous Germ Cell Tumor / Recurrent Malignant Testicular Germ Cell Tumor / Recurrent Neuroblastoma / Recurrent Ovarian Germ Cell Tumor / Recurrent Wilms Tumor and Other Childhood Kidney Tumors / Tumors, Solid / Unspecified Adult Solid Tumor, Protocol Specific / Unspecified Childhood Solid Tumor, Protocol Specific1
1Active Not RecruitingTreatmentAdult Solid Neoplasm1
1Active Not RecruitingTreatmentCancer of the Ovary / Peritoneal Cavity Cancer1
1Active Not RecruitingTreatmentMultiple Myeloma (MM) / Plasma Cell Neoplasms1
1Active Not RecruitingTreatmentNeuroblastomas3
1Active Not RecruitingTreatmentRecurrent Childhood Anaplastic Large Cell Lymphoma / Recurrent Neuroblastoma / Unspecified Childhood Solid Tumor, Protocol Specific1
1Active Not RecruitingTreatmentRecurrent Small Cell Lung Carcinoma1
1CompletedScreeningTumors, Solid1
1CompletedSupportive CareLeptomeningeal Metastases1
1CompletedTreatmentAdvanced Solid Malignancies1
1CompletedTreatmentBrain and Central Nervous System Tumors2
1CompletedTreatmentBrenner Tumor / Ovarian Clear Cell Cystadenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mixed Epithelial Carcinoma / Ovarian Mucinous Cystadenocarcinoma / Ovarian Serous Cystadenocarcinoma / Ovarian Undifferentiated Adenocarcinoma / Stage III Ovarian Epithelial Cancer / Stage IV Ovarian Epithelial Cancer1
1CompletedTreatmentCancer of the Ovary1
1CompletedTreatmentCancer of the Ovary / Cancers / Carcinoma NOS / Fallopian Tube Cancer / Gynecological Malignancies / Metastases / Oncology / Tumors / Tumors, Solid1
1CompletedTreatmentCancer of the Ovary / Cervical Cancers / Endometrial Cancers / Fallopian Tube Cancer / Sarcomas / Vaginal Cancers / Vulvar Cancers1
1CompletedTreatmentCancer of the Ovary / Cervical Cancers / Endometrial Cancers / Lung Cancers1
1CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Peritoneal Cavity Cancer2
1CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer3
1CompletedTreatmentCancer of the Ovary / Primary Peritoneal Cavity Cancer2
1CompletedTreatmentCancer, Advanced1
1CompletedTreatmentCancers2
1CompletedTreatmentCancers / Malignancies / Solid Tumor Cancers1
1CompletedTreatmentCarcinoma, Small Cell / Lung Cancers1
1CompletedTreatmentCervical Cancers2
1CompletedTreatmentChildhood Solid Tumors / Malignant Solid Tumours1
1CompletedTreatmentChronic Myeloproliferative Disorders / Leukemias / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Myelodysplastic Syndromes / Precancerous Conditions / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentEndometrial Cancers1
1CompletedTreatmentEsophageal Cancers / Head and Neck Carcinoma / Lung Cancer Small Cell Lung Cancer (SCLC) / Malignant Neoplasm of Pancreas / Malignant Neoplasm of Stomach1
1CompletedTreatmentEsophageal Cancers / Lung Cancers / Malignant Lymphomas1
1CompletedTreatmentGenital Neoplasms, Female1
1CompletedTreatmentGynecologic Tumors1
1CompletedTreatmentLeukemias3
1CompletedTreatmentLeukemias / Malignant Lymphomas / Meningeal Neoplasms1
1CompletedTreatmentLeukemias / Myelodysplastic Syndromes1
1CompletedTreatmentLeukemias / Neutropenias1
1CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Solid Tumor Cancers1
1CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Tumors1
1CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Tumors, Solid1
1CompletedTreatmentLung Cancers3
1CompletedTreatmentLung Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentMalignant Diseases1
1CompletedTreatmentMalignant Lymphomas / Small Intestine Cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1CompletedTreatmentMalignant Lymphomas / Tumors, Solid1
1CompletedTreatmentMalignant Solid Tumours1
1CompletedTreatmentMetastatic Solid Tumors1
1CompletedTreatmentNeoplasms1
1CompletedTreatmentNeoplasms Malignant / Refractory Tumors1
1CompletedTreatmentNeuroblastomas1
1CompletedTreatmentRectal Neoplasms1
1CompletedTreatmentRetinoblastoma1
1CompletedTreatmentTumors1
1CompletedTreatmentTumors, Solid2
1CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific5
1RecruitingTreatmentAdvanced Cancers1
1RecruitingTreatmentClear Cell Sarcoma of Soft Tissue / Ewing's Sarcoma (ES) / Germ Cell Tumors / Hepatoblastomas / Neuroblastomas / Non-rhabdomyosarcoma Soft Tissue Sarcomas / Renal Cell Adenocarcinoma / Retinoblastoma / Rhabdoid Tumors / Rhabdomyosarcomas / Sarcoma, Osteogenic / Wilms' tumor1
1RecruitingTreatmentGliomas1
1RecruitingTreatmentNeoplasms1
1RecruitingTreatmentNeuroblastomas1
1TerminatedTreatmentBrain and Central Nervous System Tumors / Carcinoma of Unknown Primary / Leukemias / Malignant Lymphomas / Unspecified Childhood Solid Tumor, Protocol Specific1
1TerminatedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Peritoneal Cavity Cancer1
1TerminatedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer1
1TerminatedTreatmentCancer of the Ovary / Relapses1
1TerminatedTreatmentCervix Cancer1
1TerminatedTreatmentRectal Carcinoma / Renal Cell Adenocarcinoma1
1TerminatedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1Unknown StatusTreatmentBrain and Central Nervous System Tumors1
1Unknown StatusTreatmentCancers1
1Unknown StatusTreatmentUnspecified Childhood Solid Tumor, Protocol Specific1
1, 2Active Not RecruitingTreatmentAbdominal wall neoplasm / Cancer of the Ovary / Fallopian Tube Cancer1
1, 2Active Not RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1, 2CompletedNot AvailableCancer of the Ovary1
1, 2CompletedTreatmentCancer of the Ovary4
1, 2CompletedTreatmentCervical Cancers1
1, 2CompletedTreatmentChronic Myeloproliferative Disorders / Leukemias / Myelodysplastic Syndromes / Thrombocytopenias1
1, 2CompletedTreatmentDrug/Agent Toxicity by Tissue/Organ / Lung Cancers / Radiation Toxicity1
1, 2CompletedTreatmentLeukemias1
1, 2CompletedTreatmentLeukemias / Myelodysplastic Syndromes1
1, 2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1, 2CompletedTreatmentLung Cancers1
1, 2CompletedTreatmentMultiple Myeloma (MM)1
1, 2CompletedTreatmentTumors1
1, 2CompletedTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1, 2CompletedTreatmentRefractory Small cell lung cancer / Unspecified Adult Solid Tumor, Protocol Specific1
1, 2RecruitingTreatmentCancer of the Ovary / Lung Cancer Small Cell Lung Cancer (SCLC)1
1, 2RecruitingTreatmentCarcinoma, Non-Small -Cell Lung / Extrapulmonary Small Cell Cancer / Neoplasms, Ovarian / Neuroendocrine Carcinomas / Small Cell Lung Carcinoma / Uterine Cervical Neoplasms1
1, 2RecruitingTreatmentCarcinoma, Small Cell / Lung Cancer Small Cell Lung Cancer (SCLC) / Lung Cancers1
1, 2RecruitingTreatmentChildren, Adolescents and Young Adults With Refractory or Recurrent Malignancies1
1, 2RecruitingTreatmentTumors, Central Nervous System / Tumors, Solid1
1, 2SuspendedTreatmentAdult Solid Neoplasm / Metastatic Malignant Solid Neoplasm / Metastatic Solid Neoplasm / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Unresectable Solid Neoplasm1
1, 2TerminatedTreatmentCancer of the Ovary2
1, 2TerminatedTreatmentCervical Cancers1
1, 2TerminatedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
1, 2TerminatedTreatmentNeoplasms, Brain / Tumors, Central Nervous System1
1, 2TerminatedTreatmentTumors, Solid1
1, 2Unknown StatusTreatmentBrain Neoplasms, Primary Malignant1
1, 2Unknown StatusTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer1
1, 2Unknown StatusTreatmentUnspecified Adult Solid Tumor, Protocol Specific1
1, 2WithdrawnTreatmentLarge Cell Neuroendocrine (NE) Tumors / Lung Cancer Small Cell Lung Cancer (SCLC) / Neuroendocrine (NE) Tumors1
2Active Not RecruitingTreatmentCentral Nervous System Neoplasms / Glioblastoma Multiforme (GBM) / Glioblastomas / Gliosarcoma / Neoplasms, Brain1
2Active Not RecruitingTreatmentGlioblastoma Multiforme (GBM) / Glioblastomas / Gliosarcoma / Malignant Gliomas1
2Active Not RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2Active Not RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Small Cell Lung Cancer Extensive Stage / Small Cell Lung Cancer Limited Stage1
2Active Not RecruitingTreatmentNeuroblastomas / Sarcomas1
2CompletedNot AvailableLeukemias / Non-Hodgkin's Lymphoma (NHL)1
2CompletedTreatmentAIDS-Related Diffuse Large Cell Lymphoma / AIDS-Related Diffuse Mixed Cell Lymphoma / AIDS-Related Diffuse Small Cleaved Cell Lymphoma / AIDS-related Immunoblastic Large Cell Lymphoma / AIDS-Related Lymphoblastic Lymphoma / AIDS-related Peripheral/Systemic Lymphoma / AIDS-related Primary CNS Lymphoma / AIDS-related Small Noncleaved Cell Lymphoma / Childhood Diffuse Large Cell Lymphoma / Childhood Immunoblastic Large Cell Lymphoma / HIV-associated Hodgkin Lymphoma / Leptomeningeal Metastases / Recurrent Childhood Acute Lymphoblastic Leukemia / Recurrent Childhood Acute Myeloid Leukemia / Recurrent Childhood Large Cell Lymphoma / Recurrent Childhood Lymphoblastic Lymphoma / Recurrent Childhood Medulloblastoma / Recurrent Childhood Small Noncleaved Cell Lymphoma / Recurrent/Refractory Childhood Hodgkin Lymphoma / Unspecified Childhood Solid Tumor, Protocol Specific1
2CompletedTreatmentAdenocarcinoma of Colon / Adenocarcinoma of Rectum / Metastatic Disease1
2CompletedTreatmentAdenocarcinoma of the Cervix / Adenosquamous carcinoma of the cervix / Cervical Small Cell Carcinoma / Cervical Squamous Cell Carcinoma / Recurrent Cervical Carcinoma / Stage III Cervical Cancer / Stage IVA Cervical Cancer / Stage IVB Cervical Cancer1
2CompletedTreatmentAdult Acute Megakaryoblastic Leukemia (M7) / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Recurrent Adult Acute Myeloid Leukemia1
2CompletedTreatmentBrain and Central Nervous System Tumors2
2CompletedTreatmentBrain and Central Nervous System Tumors / Metastatic Cancers / Unspecified Adult Solid Tumor, Protocol Specific1
2CompletedTreatmentCancer of the Ovary6
2CompletedTreatmentCancer of the Ovary / Childhood Germ Cell Tumor / Extragonadal Germ Cell Tumor / Head and Neck Carcinoma / Liver Cancer / Malignant Lymphomas / Neuroblastomas / Renal Cancers / Retinoblastoma / Sarcomas / Testicular germ cell tumour1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm / Neoplasms, Ovarian1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Malignant Tumor of Peritoneum1
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Peritoneal Cavity Cancer2
2CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cavity Cancer3
2CompletedTreatmentCancer of the Ovary / Neoplasms, Ovarian1
2CompletedTreatmentCancer of the Ovary / Peritoneal Cavity Cancer1
2CompletedTreatmentCarcinoma of Unknown Primary / Lung Cancers1
2CompletedTreatmentCarcinoma, Small Cell1
2CompletedTreatmentCarcinoma, Small Cell / Lung Cancer Small Cell Lung Cancer (SCLC)1
2CompletedTreatmentCervical Cancers5
2CompletedTreatmentEndometrial Cancers / Neoplasms, Endometrial1
2CompletedTreatmentEwing Sarcoma of Bone / Extraosseous Ewing Sarcoma / Peripheral Primitive Neuroectodermal Tumor / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor1
2CompletedTreatmentEwing's Sarcoma (ES) / Neuroblastomas / Rhabdomyosarcomas1
2CompletedTreatmentExtensive Stage Small Cell Lung Cancer1
2CompletedTreatmentExtensive Stage Small Cell Lung Cancer / Refractory Small cell lung cancer2
2CompletedTreatmentHuman Immunodeficiency Virus (HIV) Infections / Progressive Multifocal Leukoencephalopathy1
2CompletedTreatmentLeukemias4
2CompletedTreatmentLeukemias / Myelodysplastic Syndromes1
2CompletedTreatmentLeukemias / Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Diseases1
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)4
2CompletedTreatmentLung Cancers11
2CompletedTreatmentMalignant Lymphomas2
2CompletedTreatmentMalignant Neoplasm of Colon1
2CompletedTreatmentNeoplasms, Brain / Neuroblastomas / Tumors, Solid1
2CompletedTreatmentNeoplasms, Ovarian1
2CompletedTreatmentNeoplasms, Ovarian / Uterine Neoplasms1
2CompletedTreatmentNeuroblastomas3
2CompletedTreatmentNeutropenias / Sarcomas1
2CompletedTreatmentNon-Hodgkin's Lymphoma (NHL)1
2CompletedTreatmentOvarian Epithelial Cancer1
2CompletedTreatmentOvarian Epithelial Cancer / Primary Peritoneal Cancer1
2CompletedTreatmentPlasma Cell Myeloma1
2CompletedTreatmentRecurrent Small Cell Lung Carcinoma1
2CompletedTreatmentRetinoblastoma1
2CompletedTreatmentSarcomas1
2CompletedTreatmentSoft Tissue Sarcoma (STS)1
2CompletedTreatmentTumors, Solid1
2Not Yet RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2Not Yet RecruitingTreatmentVery High Risk Neuroblastoma1
2RecruitingTreatmentAdult Liposarcoma / Metastatic Bone Sarcomas / Metastatic Liposarcoma / Recurrent Adult Soft Tissue Sarcoma / Recurrent Liposarcoma / Recurrent Osteosarcoma / Stage IV Adult Soft Tissue Sarcoma1
2RecruitingTreatmentAtypical Teratoid Rhabdoid Tumors (ATRT) / Malignant Rhabdoid Tumors (MRT)1
2RecruitingTreatmentChildhood Atypical Teratoid/Rhabdoid Tumor / Embryonal Tumor With Abundant Neuropil and True Rosettes / Metastatic Malignant Neoplasm to the Leptomeninges / Recurrent Childhood Ependymoma / Recurrent Childhood Medulloblastoma1
2RecruitingTreatmentEndometrial Clear Cell Carcinoma / Ovarian Clear Cell Carcinoma1
2RecruitingTreatmentFallopian Tube Transitional Cell Carcinoma / Malignant Ovarian Clear Cell Tumor / Malignant Ovarian Endometrioid Tumor / Malignant Ovarian Mixed Epithelial Tumor / Malignant Ovarian Serous Tumor / Ovarian Seromucinous Carcinoma / Ovarian Transitional Cell Carcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Undifferentiated Fallopian Tube Carcinoma / Undifferentiated Ovarian Carcinoma1
2RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2RecruitingTreatmentMedulloblastomas / Neuroblastomas1
2RecruitingTreatmentMetastatic Small Cell Lung Cancer1
2RecruitingTreatmentNeuroblastomas2
2RecruitingTreatmentRecurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2RecruitingTreatmentRetinoblastoma1
2SuspendedTreatmentAcute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome / Agnogenic Myeloid Metaplasia / Atypical Chronic Myeloid Leukemia, BCR-ABL1 Negative / Chronic Myelomonocytic Leukemia / Essential Thrombocythemia (ET) / Leukemia Acute Myeloid Leukemia (AML) / Myelodysplastic/Myeloproliferative Neoplasms / Polycythemia Vera (PV) / Recurrent Adult Acute Myeloid Leukemia / Refractory Acute Myeloid Leukemia1
2TerminatedTreatmentCancer of the Ovary2
2TerminatedTreatmentCancer of the Ovary / Primary Peritoneal Cavity Cancer1
2TerminatedTreatmentCancer, Breast1
2TerminatedTreatmentCancer treatment / Cancers / Ovarian / Relapses1
2TerminatedTreatmentEpithelial Ovarian Carcinoma1
2TerminatedTreatmentExtensive Stage Small Cell Lung Cancer / Refractory Small cell lung cancer1
2TerminatedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2TerminatedTreatmentLung Cancers1
2TerminatedTreatmentMalignant Ovarian Endometrioid Tumor / Malignant Ovarian Serous Tumor / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2TerminatedTreatmentMalignant Ovarian Mixed Epithelial Tumor / Ovarian Clear Cell Cystadenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mucinous Cystadenocarcinoma / Ovarian Serous Cystadenocarcinoma / Primary Peritoneal Carcinoma / Stage III Ovarian Cancer / Undifferentiated Ovarian Carcinoma1
2TerminatedTreatmentMediastinal Neoplasms1
2TerminatedTreatmentNeoplasms, Breast1
2TerminatedTreatmentNeuroblastomas1
2TerminatedTreatmentRecurrent Ovarian Epithelial Cancer1
2TerminatedTreatmentSarcomas1
2Unknown StatusTreatmentCancer of the Ovary1
2Unknown StatusTreatmentCentral Nervous System (CNS) Metastases / Metastatic Brain Tumors1
2Unknown StatusTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2Unknown StatusTreatmentLeukemias / Myelodysplastic Syndromes1
2Unknown StatusTreatmentLung Cancer Small Cell Lung Cancer (SCLC)1
2Unknown StatusTreatmentLung Cancers / Refractory to Chemotherapy1
2Unknown StatusTreatmentNeoplasms, Brain1
2Unknown StatusTreatmentNeuroblastomas1
2WithdrawnTreatmentCervical Cancers1
2WithdrawnTreatmentLung Cancers1
2WithdrawnTreatmentNeuroblastomas1
2WithdrawnTreatmentProstate Cancer1
2, 3Active Not RecruitingTreatmentLow Grade Ovarian Serous Adenocarcinoma / Micropapillary Serous Carcinoma / Ovarian Serous Adenocarcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma1
2, 3RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)2
2, 3SuspendedTreatmentDeleterious BRCA1 Gene Mutation / Deleterious BRCA2 Gene Mutation / Fallopian Tube Clear Cell Adenocarcinoma / Fallopian Tube Endometrioid Adenocarcinoma / Fallopian Tube Mucinous Adenocarcinoma / Fallopian Tube Serous Adenocarcinoma / Fallopian Tube Transitional Cell Carcinoma / Malignant Ovarian Mixed Epithelial Tumor / Ovarian Clear Cell Adenocarcinoma / Ovarian Endometrioid Adenocarcinoma / Ovarian Mucinous Adenocarcinoma / Ovarian Seromucinous Carcinoma / Ovarian Serous Adenocarcinoma / Ovarian Transitional Cell Carcinoma / Primary Peritoneal Serous Adenocarcinoma / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Undifferentiated Fallopian Tube Carcinoma / Undifferentiated Ovarian Carcinoma1
3Active Not RecruitingTreatmentAdult Supratentorial Primitive Neuroectodermal Tumor (PNET) / Childhood Supratentorial Primitive Neuroectodermal Tumor / Ewing Sarcoma of Bone / Extraosseous Ewing Sarcoma / Extraosseous Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Localized Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Non-Metastatic Extraskeletal Ewing Sarcoma / Peripheral Primitive Neuroectodermal Tumor of Bone / Peripheral Primitive Neuroectodermal Tumor of Soft Tissues / Peripheral Primitive Neuroectodermal Tumor of the Kidney / Untreated Childhood Supratentorial Primitive Neuroectodermal Tumor1
3Active Not RecruitingTreatmentCancer of the Ovary2
3Active Not RecruitingTreatmentCancer of the Ovary / Fallopian Tube Cancer / Ovarian Epithelial Cancer / Primary Fallopian Tube Cancer / Primary Peritoneal Carcinoma1
3Active Not RecruitingTreatmentLocalized Resectable Neuroblastoma / Localized Unresectable Neuroblastoma / Recurrent Neuroblastoma / Regional Neuroblastoma / Stage 4 Neuroblastoma / Stage 4S Neuroblastoma1
3Active Not RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)2
3Active Not RecruitingTreatmentLung Cancers1
3Active Not RecruitingTreatmentRetinal Neoplasms / Retinoblastoma1
3CompletedTreatmentAcute Lymphoblastic Leukaemias (ALL)1
3CompletedTreatmentAdenocarcinoma of the Cervix / Adenosquamous carcinoma of the cervix / Cervical Squamous Cell Carcinoma / Recurrent Cervical Carcinoma / Stage IVB Cervical Cancer2
3CompletedTreatmentAdult Malignant Mesenchymoma / Adult Rhabdomyosarcoma / Alveolar Childhood Rhabdomyosarcoma / Childhood Malignant Mesenchymoma / Embryonal Childhood Rhabdomyosarcoma / Embryonal-botryoid Childhood Rhabdomyosarcoma / Nonmetastatic Childhood Soft Tissue Sarcoma / Previously Untreated Childhood Rhabdomyosarcoma / Stage I Adult Soft Tissue Sarcoma / Stage II Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma1
3CompletedTreatmentCancer of the Ovary6
3CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer1
3CompletedTreatmentCancer of the Ovary / Fallopian Tube Cancer / Peritoneal Cavity Cancer1
3CompletedTreatmentCervical Cancers1
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
3CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC)4
3CompletedTreatmentLung Cancers2
3CompletedTreatmentNeoplasms, Ovarian1
3CompletedTreatmentNeuroblastomas3
3CompletedTreatmentPrimary Peritoneal Carcinoma / Primary Peritoneal Cavity Cancer / Stage III Ovarian Cancer / Stage III Ovarian Epithelial Cancer / Stage IV Ovarian Cancer / Stage IV Ovarian Epithelial Cancer1
3CompletedTreatmentTumors, Solid1
3RecruitingTreatmentChildhood Ganglioneuroblastoma / Childhood Neuroblastoma / INRG Stage L2 / INRG Stage M / INRG Stage MS / NMYC Gene Amplification / Recurrent Neuroblastoma1
3RecruitingTreatmentLung Cancer Small Cell Lung Cancer (SCLC)2
3RecruitingTreatmentNeoplasms, Ovarian1
3TerminatedTreatmentExtensive Disease / First-Line / Lung Cancer Small Cell Lung Cancer (SCLC)1
3TerminatedTreatmentOvarian Epithelial Cancer1
3Unknown StatusTreatmentNeuroblastomas1
3Unknown StatusTreatmentSarcomas1
3WithdrawnTreatmentSarcomas1
4CompletedTreatmentLeukemia Acute Myeloid Leukemia (AML)1
Not AvailableCompletedNot AvailableCervical Intraepithelial Neoplasia (CIN)2
Not AvailableCompletedNot AvailableLung Cancer Small Cell Lung Cancer (SCLC)2
Not AvailableCompletedTreatmentDisseminated Neuroblastoma / Ganglioneuroblastoma / Localized Resectable Neuroblastoma / Localized Unresectable Neuroblastoma / Regional Neuroblastoma / Stage 4S Neuroblastoma1
Not AvailableCompletedTreatmentEwing Sarcoma of Bone / Localized Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor1
Not AvailableRecruitingNot AvailableCancer of the Ovary1
Not AvailableRecruitingTreatmentNeuroblastomas2
Not AvailableSuspendedTreatmentDisseminated Neuroblastoma / Localized Resectable Neuroblastoma / Localized Unresectable Neuroblastoma / Regional Neuroblastoma / Stage 4S Neuroblastoma1
Not AvailableTerminatedTreatmentCancer of the Ovary1
Not AvailableWithdrawnTreatmentAdult Supratentorial Primitive Neuroectodermal Tumor (PNET) / Ewing Sarcoma of Bone / Extraosseous Ewing Sarcoma / Metastatic Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Recurrent Childhood Supratentorial Primitive Neuroectodermal Tumor / Recurrent Ewing Sarcoma/Peripheral Primitive Neuroectodermal Tumor / Untreated Childhood Supratentorial Primitive Neuroectodermal Tumor1
Not AvailableWithdrawnTreatmentMalignant Lymphomas / Tumors, Central Nervous System1
Not AvailableWithdrawnTreatmentRetinoblastoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • GlaxoSmithKline Inc.
  • Pfizer Animal Health
Dosage forms
FormRouteStrength
CapsuleOral.25 mg/1
CapsuleOral0.25 mg
CapsuleOral1 mg/1
CapsuleOral1 mg
Powder, for solutionIntravenous4 mg
Powder, for solutionIntravenous1 mg
Injection, powder, for solutionIntravenous1 mg
Injection, powder, for solutionIntravenous4 mg
InjectionIntravenous1 mg/mL
Injection, solution, concentrateIntravenous1 mg/mL
Injection, powder, for solutionIntravenous4 mg/4mL
Injection, powder, lyophilized, for solutionIntravenous4 mg/4mL
Injection, powder, lyophilized, for solutionIntravenous4 mg/mL
SolutionIntravenous1 mg
Injection, solution, concentrateIntravenous1 mg/1ml
Injection, solution, concentrateIntravenous4 mg/4ml
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)
US5674872No1995-04-072015-04-07Us
US5004758No1993-05-282010-05-28Us
CA2103708No2004-04-272012-02-07Canada
CA2103707No2003-12-092012-02-07Canada
US8158645No2004-12-102024-12-10Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)213-218 °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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00b9-0019400000-11f24a2a9b88f6c67514

Taxonomy

Description
This 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).
Kingdom
Organic compounds
Super Class
Alkaloids and derivatives
Class
Camptothecins
Sub Class
Not Available
Direct Parent
Camptothecins
Alternative Parents
Hydroxyquinolines / Pyranopyridines / Pyridinones / 1-hydroxy-2-unsubstituted benzenoids / Aralkylamines / Tertiary alcohols / Heteroaromatic compounds / Trialkylamines / Amino acids and derivatives / Lactones
show 9 more
Substituents
Camptothecin / Hydroxyquinoline / Pyranopyridine / Quinoline / 1-hydroxy-2-unsubstituted benzenoid / Pyridinone / Aralkylamine / Benzenoid / Pyridine / Heteroaromatic compound
show 23 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
pyranoindolizinoquinoline (CHEBI:63632)

Targets

Details
1. DNA topoisomerase 1
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 singl...
Gene Name
TOP1
Uniprot ID
P11387
Uniprot Name
DNA topoisomerase 1
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-str...
Gene Name
TOP1MT
Uniprot ID
Q969P6
Uniprot Name
DNA topoisomerase I, mitochondrial
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
Inhibitor
Inducer
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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
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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
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
Uniprot Name
Multidrug resistance protein 1
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]

Drug created on June 13, 2005 07:24 / Updated on August 15, 2018 09:48