Topoisomerase Inhibitors

Name
Topoisomerase Inhibitors
Accession Number
DBCAT000548
Description

Compounds that inhibit the activity of DNA TOPOISOMERASES.

Drugs
DrugDrug Description
TeniposideA cytotoxic drug used as an adjunct for chemotherapy induction in the treatment of refractory childhood acute lymphoblastic leukemia.
IrinotecanAn antineoplastic enzyme inhibitor used to treat metastatic carcinoma of the colon or rectum.
EtoposideA podophyllotoxin derivative used to treat testicular and small cell lung tumors.
TopotecanAn antineoplastic agent used to treat ovarian cancer, small cell lung cancer, or cervical cancer.
MitoxantroneA chemotherapeutic agent used for the treatment of secondary progressive, progressive relapsing, or worsening relapsing-remitting multiple sclerosis.
MoxifloxacinA fluoroquinolone antibiotic used to treat various bacterial infections.
GrepafloxacinA fluoroquinolone antibiotic used to treat various gram positive and gram negative bacterial infections.
DexrazoxaneA cytoprotective drug used to prevent and improve cardiomyopathy associated with doxorubicin treatment for metastatic breast cancer.
ValrubicinAn anthracycline used intravesically in the treatment of BCG-resistant bladder carcinoma.
EpirubicinAn anthracycline topoisomerase II inhibitor used as an adjuvant to treating axillary node metastases in patients who have undergone surgical resection of primary breast cancer.
EnoxacinFor the treatment of adults (≥18 years of age) with the following infections caused by susceptible strains of the designated microorganisms: (1) uncomplicated urethral or cervical gonorrhea due to Neisseria...
PefloxacinAn antibiotic used to treat a variety of bacterial infections.
CiprofloxacinA second generation fluoroquinolone used to treat various susceptible bacterial infections.
TrovafloxacinAn antibiotic used to treat gonorrhea and chlamydia.
DaunorubicinAn anthracycline aminoglycoside used to induce remission of nonlymphocytic leukemia and acute lymphocytic leukemia.
Nalidixic acidA quinolone antibiotic used to treat urinary tract infections.
CinoxacinFor the treatment of initial and recurrent urinary tract infections in adults caused by the following susceptible microorganisms: Escherichia coli, Proteus mirabilis, Proteus vulgaris, Klebsiella species (including K. pneumoniae), and...
LomefloxacinA fluoroquinolone used to prevent and treat a wide variety of infections in the body.
DoxorubicinA medication used to treat various cancers, including AIDS-associated Kaposi's Sarcoma and metastatic cancers.
GatifloxacinA fourth generation fluoroquinolone used to treat a wide variety of infections in the body.
NorfloxacinA broad-spectrum fluoroquinolone antibiotic with variable activity against gram-positive and gram-negative bacteria. Typically reserved for the treatment of UTIs due to accumulation in the urine.
LevofloxacinA fluoroquinolone antibiotic used to treat infections caused by susceptible bacteria of the upper respiratory tract, skin and skin structures, urinary tract, and prostate, as well as for post-exposure treatment of inhaled anthrax and the plague.
GemifloxacinA quinolone antibacterial agent used for the treatment of acute bacterial exacerbation of chronic bronchitis and mild to moderate community-acquired pneumonia caused by susceptible bacteria.
OfloxacinAn antibacterial agent used for the treatment of bacterial infections in many parts of the body, including the respiratory tract, kidney, skin, soft tissue, and urinary tract.
IdarubicinAn anthracycline antineoplastic agent used to treat acute myeloid leukemia (AML) in adults.
SparfloxacinA fluoroquinolone antibiotic used to treat bacterial respiratory infections and sinusitis.
TemafloxacinFor the treatment of lower respiratory tract infections, genital and urinary infections like prostatitis, and skin infections.
FleroxacinFleroxacin is a broad-spectrum antimicrobial fluoroquinolone.
CamptothecinInvestigated for the treatment of cancer.
RubitecanInvestigated for use/treatment in pancreatic cancer, leukemia (unspecified), melanoma, ovarian cancer, and cancer/tumors (unspecified).
GarenoxacinInvestigated for use/treatment in bacterial infection.
PixantroneAn antineoplastic agent use to treat patients with relapsed or refractory aggressive Non-Hodgkin B-cell Lymphomas (NHL).
MLN576Investigated for use/treatment in solid tumors.
BesifloxacinA fluoroquinolone antibiotic agent used for the treatment of bacterial conjunctivitis.
FlumequineFlumequine is a synthetic chemotherapeutic antibiotic of the fluoroquinolone drug class used to treat bacterial infections.
AlatrofloxacinA fluoroquinolone antibiotic used to treat a variety of bacterial infections.
AclarubicinNot Annotated
PazufloxacinPazufloxacin is under investigation in clinical trial NCT02592096 (Pazufloxacin Mesilate Ear Drops Clinical Trial Protocol).
Acridine CarboxamideAcridine Carboxamide has been used in trials studying the treatment of Lung Cancer and Brain and Central Nervous System Tumors.
PrulifloxacinA broad-spectrum fluoroquinolone antibiotic used to treat a variety of susceptible bacterial infections.
ExatecanExatecan has been used in trials studying the treatment of Sarcoma, Leukemia, Lymphoma, Lung Cancer, and Liver Cancer, among others.
NadifloxacinA topical fluoroquinolone used in the treatment of acne and topical bacterial skin infections.
BelotecanBelotecan has been investigated for the treatment of Epithelial Ovarian Cancer.
TU-100TU-100 has been used in trials studying the treatment of Abdominal Pain, Colonic Transit, Crohn's Disease, Rectal Sensation, and Gastric Emptying, among others.
DaidzeinNot Annotated
SitafloxacinA fluoroquinolone antibiotic indicated in the treatment of susceptible bacterial infections.
Oxolinic acidNot Annotated
RufloxacinA fluoroquinolone antibiotic indicated in the treatment of susceptible respiratory infections and uncomplicated cystitis.
Coumermycin A1Not Annotated
ClinafloxacinClinafloxacin is a fluoroquinolone antibacterial currently under research. It has been proven to present good antibiotic properties. However, its approval and release have been halted due to the presence of...
SN-38Investigated for use/treatment in colorectal cancer.
FinafloxacinFinafloxacin is indicated for the treatment of acute otitis externa (AOE) with or without an otowick, caused by susceptible strains of Pseudomonas aeruginosa and Staphylococcus aureus in patients age 1...
Etirinotecan pegolEtirinotecan pegol is under investigation in clinical trial NCT01663012 (Phase II NKTR-102 In Bevacizumab-Resistant High Grade Glioma).
Sacituzumab govitecanSacituzumab govitecan targets TROP-2-expressing cancer cells through a humanized antibody (RS7) before subsequently becoming internalized and releasing the topoisomerase I inhibitor SN-38 to induce DNA damage-mediated apoptosis.
Trastuzumab deruxtecanAn antibody used to treat certain types of unresectable or metastatic HER2 positive breast cancer.
Etoposide toniribateNot Annotated
GepotidacinGepotidacin has been used in trials studying the treatment of Gonorrhea, Infections, Bacterial, and Infections, Respiratory Tract.
ZoliflodacinZoliflodacin has been used in trials studying the basic science and treatment of Gonorrhoea.
OzenoxacinA quinolone antibiotic used to treat impetigo caused by susceptible bacteria.
Drugs & Drug Targets
DrugTargetType
TeniposideDNA topoisomerase 2-alphatarget
TeniposideCytochrome P450 2C19enzyme
TeniposideCytochrome P450 2C9enzyme
TeniposideCytochrome P450 3A4enzyme
TeniposideMultidrug resistance-associated protein 6transporter
TeniposideATP-binding cassette sub-family G member 2transporter
TeniposideCytochrome P450 3A5enzyme
IrinotecanDNA topoisomerase I, mitochondrialtarget
IrinotecanDNA topoisomerase 1target
IrinotecanCytochrome P450 3A4enzyme
IrinotecanCytochrome P450 3A5enzyme
IrinotecanUDP-glucuronosyltransferase 1-1enzyme
IrinotecanUDP-glucuronosyltransferase 1-9enzyme
IrinotecanLiver carboxylesterase 1enzyme
IrinotecanCytochrome P450 3A7enzyme
IrinotecanCytochrome P450 2B6enzyme
IrinotecanSolute carrier family 22 member 3transporter
IrinotecanSolute carrier organic anion transporter family member 1B1transporter
IrinotecanMultidrug resistance-associated protein 1transporter
IrinotecanATP-binding cassette sub-family G member 2transporter
IrinotecanSerum albumincarrier
IrinotecanCocaine esteraseenzyme
IrinotecanCholinesteraseenzyme
IrinotecanP-glycoprotein 1transporter
IrinotecanCanalicular multispecific organic anion transporter 1transporter
EtoposideDNA topoisomerase 2-alphatarget
EtoposideCytochrome P450 3A4enzyme
EtoposideCanalicular multispecific organic anion transporter 2transporter
EtoposideMultidrug resistance-associated protein 6transporter
EtoposideP-glycoprotein 1transporter
EtoposideMultidrug resistance-associated protein 1transporter
EtoposideMultidrug resistance-associated protein 7transporter
EtoposideCanalicular multispecific organic anion transporter 1transporter
EtoposideATP-binding cassette sub-family G member 2transporter
EtoposideCytochrome P450 1A2enzyme
EtoposideCytochrome P450 2E1enzyme
EtoposideCytochrome P450 3A5enzyme
EtoposideUDP-glucuronosyltransferase 1-1enzyme
EtoposideDNA topoisomerase 2-betatarget
EtoposideGlutathione S-transferase theta-1enzyme
EtoposideGlutathione S-transferase Penzyme
EtoposideProstaglandin G/H synthase 2enzyme
EtoposideProstaglandin G/H synthase 1enzyme
TopotecanDNA topoisomerase I, mitochondrialtarget
TopotecanDNA topoisomerase 1target
TopotecanATP-binding cassette sub-family G member 2transporter
TopotecanP-glycoprotein 1transporter
TopotecanDNAtarget
TopotecanMultidrug and toxin extrusion protein 1transporter
TopotecanMultidrug and toxin extrusion protein 2transporter
MitoxantroneDNA topoisomerase 2-alphatarget
MitoxantroneCytochrome P450 2E1enzyme
MitoxantroneP-glycoprotein 1transporter
MitoxantroneMultidrug resistance-associated protein 1transporter
MitoxantroneATP-binding cassette sub-family G member 2transporter
MitoxantroneDNAtarget
MitoxantroneCytochrome P450 1B1enzyme
MitoxantroneCytochrome P450 3A4enzyme
MoxifloxacinDNA gyrase subunit Atarget
MoxifloxacinDNA topoisomerase 4 subunit Atarget
MoxifloxacinDNA topoisomerase 2-alphatarget
MoxifloxacinCytochrome P450 1A2enzyme
MoxifloxacinSerum paraoxonase/arylesterase 1target
GrepafloxacinDNA gyrase subunit Atarget
GrepafloxacinDNA topoisomerase 4 subunit Atarget
GrepafloxacinCytochrome P450 3A4enzyme
GrepafloxacinCytochrome P450 1A2enzyme
GrepafloxacinSolute carrier family 22 member 2transporter
GrepafloxacinSolute carrier family 22 member 5transporter
GrepafloxacinCanalicular multispecific organic anion transporter 1transporter
GrepafloxacinP-glycoprotein 1transporter
GrepafloxacinMultidrug resistance-associated protein 1transporter
GrepafloxacinSolute carrier family 22 member 6transporter
DexrazoxaneDNA topoisomerase 2-alphatarget
DexrazoxaneDNA topoisomerase 2-betatarget
ValrubicinDNA topoisomerase 2-alphatarget
ValrubicinDNAtarget
EpirubicinDNA topoisomerase 2-alphatarget
EpirubicinDNAtarget
EpirubicinMultidrug resistance-associated protein 1transporter
EpirubicinUDP-glucuronosyltransferase 2B7enzyme
EpirubicinCytosolic phospholipase A2enzyme
EnoxacinDNA gyrase subunit Atarget
EnoxacinDNA topoisomerase 4 subunit Atarget
EnoxacinDNA topoisomerase 2-alphatarget
EnoxacinCytochrome P450 1A2enzyme
PefloxacinDNA gyrase subunit Atarget
PefloxacinDNA topoisomerase 4 subunit Atarget
PefloxacinDNA topoisomerase 2-alphatarget
PefloxacinCytochrome P450 1A2enzyme
PefloxacinDNA topoisomerase 1target
CiprofloxacinDNA gyrase subunit Atarget
CiprofloxacinDNA topoisomerase 4 subunit Atarget
CiprofloxacinDNA topoisomerase 2-alphatarget
CiprofloxacinCytochrome P450 1A2enzyme
CiprofloxacinCytochrome P450 3A4enzyme
CiprofloxacinCytochrome P450 3A5enzyme
CiprofloxacinCytochrome P450 3A7enzyme
CiprofloxacinP-glycoprotein 1transporter
CiprofloxacinPotassium voltage-gated channel subfamily H member 2target
CiprofloxacinDNA gyrase subunit Atarget
CiprofloxacinDNA topoisomerase 4 subunit Atarget
CiprofloxacinDNA topoisomerase 4 subunit Btarget
CiprofloxacinDNA gyrase subunit Atarget
CiprofloxacinMultidrug resistance protein MdtKtarget
CiprofloxacinGyrase Atarget
CiprofloxacinDNA gyrase subunit Atarget
CiprofloxacinMultidrug and toxin extrusion protein 1transporter
CiprofloxacinMultidrug and toxin extrusion protein 2transporter
CiprofloxacinSerum albumincarrier
TrovafloxacinDNA gyrase subunit Atarget
TrovafloxacinDNA topoisomerase 4 subunit Atarget
TrovafloxacinDNA topoisomerase 2-alphatarget
TrovafloxacinCytochrome P450 1A2enzyme
DaunorubicinDNAtarget
DaunorubicinCytochrome P450 3A5enzyme
DaunorubicinNADPH--cytochrome P450 reductaseenzyme
DaunorubicinP-glycoprotein 1transporter
DaunorubicinMultidrug resistance-associated protein 1transporter
DaunorubicinMultidrug resistance-associated protein 6transporter
DaunorubicinMultidrug resistance-associated protein 7transporter
DaunorubicinATP-binding cassette sub-family G member 2transporter
DaunorubicinDNA topoisomerase 2-alphatarget
DaunorubicinDNA topoisomerase 2-betatarget
DaunorubicinCytochrome P450 1B1enzyme
DaunorubicinCytochrome P450 3A4enzyme
DaunorubicinAldose reductaseenzyme
DaunorubicinCarbonyl reductase [NADPH] 1enzyme
DaunorubicinCarbonyl reductase [NADPH] 3enzyme
Nalidixic acidDNAtarget
Nalidixic acidSolute carrier family 22 member 6transporter
Nalidixic acidTryptophan 2,3-dioxygenaseenzyme
Nalidixic acidCytochrome P450 1A2enzyme
CinoxacinDNAtarget
CinoxacinDNA gyrase subunit Atarget
CinoxacinSolute carrier family 22 member 6transporter
CinoxacinCytochrome P450 1A2enzyme
LomefloxacinDNA gyrase subunit Atarget
LomefloxacinDNA topoisomerase 4 subunit Atarget
LomefloxacinDNA topoisomerase 2-alphatarget
LomefloxacinCytochrome P450 1A2enzyme
LomefloxacinSolute carrier family 22 member 5transporter
LomefloxacinCanalicular multispecific organic anion transporter 1transporter
DoxorubicinDNA topoisomerase 2-alphatarget
DoxorubicinDNAtarget
DoxorubicinCytochrome P450 3A4enzyme
DoxorubicinCytochrome P450 2D6enzyme
DoxorubicinCytochrome P450 2B6enzyme
DoxorubicinP-glycoprotein 1transporter
DoxorubicinCanalicular multispecific organic anion transporter 2transporter
DoxorubicinMultidrug resistance-associated protein 6transporter
DoxorubicinMultidrug resistance-associated protein 1transporter
DoxorubicinMultidrug resistance-associated protein 7transporter
DoxorubicinATP-binding cassette sub-family G member 2transporter
DoxorubicinBile salt export pumptransporter
DoxorubicinSolute carrier family 22 member 16transporter
DoxorubicinATP-binding cassette sub-family B member 8, mitochondrialtransporter
DoxorubicinCytochrome P450 1B1enzyme
DoxorubicinCarbonyl reductase [NADPH] 1enzyme
DoxorubicinCarbonyl reductase [NADPH] 3enzyme
DoxorubicinAlcohol dehydrogenase [NADP(+)]enzyme
DoxorubicinAldo-keto reductase family 1 member C3enzyme
DoxorubicinNAD(P)H dehydrogenase [quinone] 1enzyme
DoxorubicinXanthine dehydrogenase/oxidaseenzyme
DoxorubicinNitric oxide synthase, endothelialenzyme
DoxorubicinNitric oxide synthase, inducibleenzyme
DoxorubicinNitric oxide synthase, brainenzyme
DoxorubicinNADH dehydrogenase [ubiquinone] iron-sulfur protein 2, mitochondrialenzyme
DoxorubicinNADH dehydrogenase [ubiquinone] iron-sulfur protein 3, mitochondrialenzyme
DoxorubicinNADH dehydrogenase [ubiquinone] iron-sulfur protein 7, mitochondrialenzyme
DoxorubicinNADPH--cytochrome P450 reductaseenzyme
DoxorubicinRalA-binding protein 1transporter
DoxorubicinCanalicular multispecific organic anion transporter 1transporter
DoxorubicinSerum albumincarrier
DoxorubicinNucleolar and coiled-body phosphoprotein 1target
DoxorubicinDNA topoisomerase 1target
DoxorubicinDNA topoisomerase 2-betatarget
DoxorubicinAldose reductaseenzyme
DoxorubicinAldo-keto reductase family 1 member B10enzyme
DoxorubicinAldo-keto reductase family 1 member C4enzyme
GatifloxacinSerum albumincarrier
GatifloxacinDNA gyrase subunit Atarget
GatifloxacinDNA gyrase subunit Btarget
GatifloxacinDNA topoisomerase 4 subunit Atarget
GatifloxacinDNA topoisomerase 4 subunit Btarget
GatifloxacinCytochrome P450 1A2enzyme
NorfloxacinDNA gyrase subunit Atarget
NorfloxacinDNA topoisomerase 4 subunit Atarget
NorfloxacinDNA topoisomerase 2-alphatarget
NorfloxacinCytochrome P450 1A2enzyme
NorfloxacinCytochrome P450 3A4enzyme
NorfloxacinSolute carrier family 22 member 5transporter
NorfloxacinSolute carrier family 22 member 6transporter
NorfloxacinCytochrome P450 1A1enzyme
NorfloxacinCytochrome P450 3A7enzyme
NorfloxacinDNA gyrase subunit Atarget
NorfloxacinDNA topoisomerase 2target
NorfloxacinDNA topoisomerase 4 subunit Atarget
LevofloxacinDNA gyrase subunit Atarget
LevofloxacinDNA topoisomerase 4 subunit Atarget
LevofloxacinSolute carrier family 22 member 2transporter
LevofloxacinP-glycoprotein 1transporter
LevofloxacinSolute carrier family 22 member 4transporter
LevofloxacinMultidrug and toxin extrusion protein 1transporter
LevofloxacinMultidrug and toxin extrusion protein 2transporter
LevofloxacinCytochrome P450 2C9enzyme
LevofloxacinSerum albumincarrier
LevofloxacinSolute carrier organic anion transporter family member 4C1transporter
LevofloxacinSolute carrier family 22 member 1transporter
LevofloxacinSolute carrier organic anion transporter family member 1A2transporter
GemifloxacinDNA gyrase subunit Atarget
GemifloxacinDNA topoisomerase 4 subunit Atarget
GemifloxacinCytochrome P450 1A2enzyme
OfloxacinDNA gyrase subunit Atarget
OfloxacinDNA topoisomerase 4 subunit Atarget
OfloxacinDNA topoisomerase 2-alphatarget
OfloxacinCytochrome P450 1A2enzyme
OfloxacinSolute carrier family 22 member 5transporter
OfloxacinMultidrug resistance-associated protein 1transporter
OfloxacinSolute carrier family 22 member 6transporter
OfloxacinCanalicular multispecific organic anion transporter 1transporter
OfloxacinSolute carrier family 22 member 4transporter
OfloxacinBile salt export pumptransporter
IdarubicinDNA topoisomerase 2-alphatarget
IdarubicinDNAtarget
IdarubicinMultidrug resistance-associated protein 1transporter
IdarubicinCytochrome P450 2C9enzyme
IdarubicinCytochrome P450 2D6enzyme
SparfloxacinDNA gyrase subunit Atarget
SparfloxacinDNA topoisomerase 4 subunit Atarget
SparfloxacinDNA topoisomerase 2-alphatarget
SparfloxacinSolute carrier family 22 member 5transporter
SparfloxacinCanalicular multispecific organic anion transporter 1transporter
SparfloxacinP-glycoprotein 1transporter
SparfloxacinCytochrome P450 1A2enzyme
TemafloxacinDNA gyrase subunit Atarget
TemafloxacinDNA topoisomerase 4 subunit Atarget
TemafloxacinCytochrome P450 1A2enzyme
FleroxacinDNA topoisomerase 2-alphatarget
FleroxacinDNA gyrase subunit Atarget
FleroxacinDNA topoisomerase 4 subunit Atarget
CamptothecinDNA topoisomerase 1target
CamptothecinP-glycoprotein 1transporter
CamptothecinATP-binding cassette sub-family G member 2transporter
CamptothecinSerum albumincarrier
RubitecanDNA topoisomerase 1target
GarenoxacinCytochrome P450 1A2enzyme
BesifloxacinDNA topoisomerase 4 subunit Atarget
BesifloxacinDNA topoisomerase 4 subunit Atarget
BesifloxacinDNA gyrase subunit Atarget
BesifloxacinDNA gyrase subunit Atarget
BesifloxacinCytochrome P450 1A2enzyme
FlumequineCytochrome P450 1A2enzyme
PazufloxacinCytochrome P450 1A2enzyme
PrulifloxacinCytochrome P450 1A2enzyme
SitafloxacinCytochrome P450 1A2enzyme
RufloxacinCytochrome P450 1A2enzyme
ClinafloxacinCytochrome P450 1A2enzyme
ClinafloxacinCytochrome P450 2C19enzyme
ClinafloxacinCytochrome P450 2D6enzyme
ClinafloxacinCytochrome P450 2C9enzyme
SN-38DNA topoisomerase 1target
SN-38Cytochrome P450 3A4enzyme
FinafloxacinDNA gyrase subunit Atarget
FinafloxacinDNA topoisomerase 4 subunit Atarget
FinafloxacinDNA topoisomerase 2-alphatarget
Sacituzumab govitecanTumor-associated calcium signal transducer 2target
Sacituzumab govitecanDNA topoisomerase 1target
Sacituzumab govitecanFar upstream element-binding protein 1target
Sacituzumab govitecanUDP-glucuronosyltransferase 1-1enzyme
Trastuzumab deruxtecanP-glycoprotein 1transporter
Trastuzumab deruxtecanHigh affinity immunoglobulin gamma Fc receptor Itarget
Trastuzumab deruxtecanDNA topoisomerase 1target
Trastuzumab deruxtecanLysosomal alpha-glucosidaseenzyme
Trastuzumab deruxtecanDNA topoisomerase 1enzyme
Trastuzumab deruxtecanCathepsin Benzyme
Trastuzumab deruxtecanCathepsin L1enzyme
Trastuzumab deruxtecanCytochrome P450 3A4enzyme
Trastuzumab deruxtecanSolute carrier organic anion transporter family member 1B1transporter
Trastuzumab deruxtecanSolute carrier organic anion transporter family member 1B3transporter
Trastuzumab deruxtecanMultidrug and toxin extrusion protein 2transporter
Trastuzumab deruxtecanMultidrug resistance-associated protein 1transporter
Trastuzumab deruxtecanATP-binding cassette sub-family G member 2transporter
OzenoxacinDNA gyrase subunit Atarget
OzenoxacinDNA topoisomerase 4 subunit Atarget