Identification

Name
Trovafloxacin
Accession Number
DB00685  (APRD01281)
Type
Small Molecule
Groups
Approved, Investigational, Withdrawn
Description

Trovafloxacin (sold as Trovan by Pfizer) is a broad spectrum antibiotic that inhibits the uncoiling of supercoiled DNA in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. It was withdrawn from the market due to the risk of hepatotoxicity. It had better gram-positive bacterial coverage and less gram-negative coverage than the previous fluoroquinolones. [Wikipedia]

Structure
Thumb
Synonyms
Not Available
External IDs
CP-99219
Product Ingredients
IngredientUNIICASInChI Key
Trovafloxacin hydrochloride546454T03O146961-34-4VOYNIHWZMLJQHF-AHZSKCOESA-N
Trovafloxacin mesylate0P1LKO80WN147059-75-4DYNZICQDCVYXFW-AHZSKCOESA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Trovan I.V.Liquid5 mgIntravenousPfizer1998-12-232001-11-22Canada
Trovan Tablets 100mgTablet100 mgOralPfizer1998-12-232001-11-22Canada
Trovan Tablets 200mgTablet200 mgOralPfizer1998-12-232001-11-22Canada
International/Other Brands
Trovan (Pfizer)
Categories
UNII
9F388J00UK
CAS number
147059-72-1
Weight
Average: 416.36
Monoisotopic: 416.109624848
Chemical Formula
C20H15F3N4O3
InChI Key
WVPSKSLAZQPAKQ-CDMJZVDBSA-N
InChI
InChI=1S/C20H15F3N4O3/c21-8-1-2-15(13(22)3-8)27-7-12(20(29)30)17(28)9-4-14(23)19(25-18(9)27)26-5-10-11(6-26)16(10)24/h1-4,7,10-11,16H,5-6,24H2,(H,29,30)/t10-,11+,16+
IUPAC Name
7-[(1R,5S,6S)-6-amino-3-azabicyclo[3.1.0]hexan-3-yl]-1-(2,4-difluorophenyl)-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid
SMILES
[H][[email protected]@]12CN(C[[email protected]]1([H])[[email protected]]2N)C1=NC2=C(C=C1F)C(=O)C(=CN2C1=C(F)C=C(F)C=C1)C(O)=O

Pharmacology

Indication

For treatment of infections caused by susceptible strains of the designated microorganisms in uncomplicated urethral gonorrhea in males and endocervical and rectal gonorrhea in females caused by Neisseria gonorrhoeae as well as non gonoccocal urethritis and cervicitis due to Chlamydia trachomatis.

Structured Indications
Not Available
Pharmacodynamics

Trovafloxacin is a broad spectrum antibiotic that inhibits DNA supercoiling in various bacteria by blocking the activity of DNA gyrase and topoisomerase IV. It is not used widely due to the risk of hepatotoxicity. It tends to have better gram-positive bacterial coverage and less gram-negative coverage than the previous fluoroquinolones. Mechanism of action of fluoroquinolones including trovafloxacin is different from that of penicillins, cephalosporins, aminoglycosides, macrolides, and tetracyclines. Therefore fluoroquinolones may be active against pathogens that are resistant to these antibiotics. There is no cross-resistance between trovafloxacin and the mentioned classes of antibiotics. The overall results obtained from in vitro synergy studies, testing combinations of trovafloxacin with beta-lactams and aminoglycosides, indicate that synergy is strain specific and not commonly encountered. This agrees with results obtained previously with other fluoroquinolones. Resistance to trovafloxacin in vitro develops slowly via multiple-step mutation in a manner similar to other fluoroquinolones. Resistance to trovafloxacin in vitro occurs at a general frequency of between 1x10-7 to 10-10. Although cross-resistance has been observed between trovafloxacin and some other fluoroquinolones, some microorganisms resistant to other fluoroquinolones may be susceptible to trovafloxacin.

Mechanism of action

Trovafloxacin is a fluoronaphthyridone related to the fluoroquinolones with in vitro activity against a wide range of gram-negative and gram-positive aerobic and anaerobic microorganisms. The bactericidal action of trovafloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.

TargetActionsOrganism
ADNA gyrase subunit A
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
ADNA topoisomerase 4 subunit A
inhibitor
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
UDNA topoisomerase 2-alpha
inhibitor
Human
Absorption

Well-absorbed from the gastrointestinal tract after oral administration and does not depend on concomitant food intake. The absolute bioavailability is approximately 88%.

Volume of distribution
Not Available
Protein binding

The mean plasma protein bound fraction is approximately 76%, and is concentration-independent.

Metabolism

Metabolism Trovafloxacin is metabolized by conjugation (the role of cytochrome P450 oxidative metabolism of trovafloxacin is minimal). The major metabolites include the ester glucuronide, which appears in the urine (13% of the administered dose); and the N -acetyl metabolite, which appears in the feces and serum (9% and 2.5% of the administered dose, respectively). Other minor metabolites include diacid, hydroxycarboxylic acid, and sulfamate, which have been identified in both the feces and the urine in small amounts (< 4% of the administered dose).

Route of elimination

Approximately 50% of an oral dose is excreted unchanged (43% in the feces and 6% in the urine).

Half life

Following oral administration, half-life ranged from 9.1 hours to 12.2 hours over the dosage range of 100 to 200 mg tablets. Following intravenous infusion, half-life ranged from 9.4 to 12.7 hours over a dosage range of 100 to 300 mg.

Clearance
Not Available
Toxicity

Symptoms of overdose include convulsions, decreased activity, diarrhea, sleepiness, tremors, and/or vomiting.

Affected organisms
  • Enteric bacteria and other eubacteria
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
16-BromoepiandrosteroneThe risk or severity of adverse effects can be increased when 16-Bromoepiandrosterone is combined with Trovafloxacin.Investigational
19-norandrostenedioneThe risk or severity of adverse effects can be increased when 19-norandrostenedione is combined with Trovafloxacin.Experimental, Illicit
5-androstenedioneThe risk or severity of adverse effects can be increased when 5-androstenedione is combined with Trovafloxacin.Experimental, Illicit
AcarboseTrovafloxacin may increase the hypoglycemic activities of Acarbose.Approved, Investigational
AceclofenacAceclofenac may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
AcemetacinAcemetacin may increase the neuroexcitatory activities of Trovafloxacin.Approved
AcenocoumarolTrovafloxacin may increase the anticoagulant activities of Acenocoumarol.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Trovafloxacin.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Trovafloxacin.Experimental
Acetylsalicylic acidAcetylsalicylic acid may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
AdapaleneAdapalene may increase the neuroexcitatory activities of Trovafloxacin.Approved
AlbiglutideTrovafloxacin may increase the hypoglycemic activities of Albiglutide.Approved
AlclofenacAlclofenac may increase the neuroexcitatory activities of Trovafloxacin.Approved, Withdrawn
AlclometasoneThe risk or severity of adverse effects can be increased when Alclometasone is combined with Trovafloxacin.Approved
AldosteroneThe risk or severity of adverse effects can be increased when Aldosterone is combined with Trovafloxacin.Experimental, Investigational
AlgeldrateAlgeldrate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
AlmagateAlmagate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AlmasilateAlmasilate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
AlminoprofenAlminoprofen may increase the neuroexcitatory activities of Trovafloxacin.Experimental
AlogliptinTrovafloxacin may increase the hypoglycemic activities of Alogliptin.Approved
AloglutamolAloglutamol can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
AluminiumAluminium can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Aluminium acetoacetateAluminium acetoacetate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminium glycinateAluminium glycinate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Aluminum hydroxideAluminum hydroxide can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Ambroxol acefyllinateThe metabolism of Ambroxol acefyllinate can be decreased when combined with Trovafloxacin.Experimental, Investigational
AmcinonideThe risk or severity of adverse effects can be increased when Amcinonide is combined with Trovafloxacin.Approved
AminophyllineThe metabolism of Aminophylline can be decreased when combined with Trovafloxacin.Approved
AndrographolideAndrographolide may increase the neuroexcitatory activities of Trovafloxacin.Investigational
AndrostenedioneThe risk or severity of adverse effects can be increased when Androstenedione is combined with Trovafloxacin.Experimental, Illicit
AnecortaveThe risk or severity of adverse effects can be increased when Anecortave is combined with Trovafloxacin.Investigational
anecortave acetateThe risk or severity of adverse effects can be increased when anecortave acetate is combined with Trovafloxacin.Investigational
AnisodamineAnisodamine may increase the neuroexcitatory activities of Trovafloxacin.Investigational
AntipyrineAntipyrine may increase the neuroexcitatory activities of Trovafloxacin.Approved
ApocyninApocynin may increase the neuroexcitatory activities of Trovafloxacin.Investigational
ApremilastApremilast may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
AtamestaneThe risk or severity of adverse effects can be increased when Atamestane is combined with Trovafloxacin.Investigational
AzapropazoneAzapropazone may increase the neuroexcitatory activities of Trovafloxacin.Withdrawn
AzelastineAzelastine may increase the neuroexcitatory activities of Trovafloxacin.Approved
BalsalazideBalsalazide may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
Beclomethasone dipropionateThe risk or severity of adverse effects can be increased when Beclomethasone dipropionate is combined with Trovafloxacin.Approved, Investigational
BendazacBendazac may increase the neuroexcitatory activities of Trovafloxacin.Experimental
BenorilateBenorilate may increase the neuroexcitatory activities of Trovafloxacin.Experimental
BenoxaprofenBenoxaprofen may increase the neuroexcitatory activities of Trovafloxacin.Withdrawn
BetamethasoneThe risk or severity of adverse effects can be increased when Betamethasone is combined with Trovafloxacin.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Trovafloxacin.Approved, Investigational
BevoniumBevonium may increase the neuroexcitatory activities of Trovafloxacin.Experimental
Bismuth SubcitrateBismuth Subcitrate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Bismuth subnitrateBismuth subnitrate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
BromfenacBromfenac may increase the neuroexcitatory activities of Trovafloxacin.Approved
BromocriptineTrovafloxacin may increase the hypoglycemic activities of Bromocriptine.Approved, Investigational
BucillamineBucillamine may increase the neuroexcitatory activities of Trovafloxacin.Investigational
BudesonideThe risk or severity of adverse effects can be increased when Budesonide is combined with Trovafloxacin.Approved
BufexamacBufexamac may increase the neuroexcitatory activities of Trovafloxacin.Experimental
BumadizoneBumadizone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Trovafloxacin.Approved
CalciumCalcium can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Nutraceutical
Calcium AcetateCalcium Acetate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium CarbonateCalcium Carbonate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium CitrateCalcium Citrate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium glubionateCalcium glubionate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium GluceptateCalcium Gluceptate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium gluconateCalcium gluconate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Vet Approved
Calcium lactateCalcium lactate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental, Investigational, Vet Approved
Calcium lactate gluconateCalcium lactate gluconate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium laevulateCalcium laevulate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium pangamateCalcium pangamate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Calcium PhosphateCalcium Phosphate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Calcium silicateCalcium silicate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
CanagliflozinTrovafloxacin may increase the hypoglycemic activities of Canagliflozin.Approved
Carbaspirin calciumCarbaspirin calcium may increase the neuroexcitatory activities of Trovafloxacin.Experimental, Investigational
CarprofenCarprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved, Withdrawn
CaseinCasein can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
CastanospermineCastanospermine may increase the neuroexcitatory activities of Trovafloxacin.Experimental
CelecoxibCelecoxib may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
ChloroquineChloroquine may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
ChlorpropamideTrovafloxacin may increase the hypoglycemic activities of Chlorpropamide.Approved
Choline magnesium trisalicylateCholine magnesium trisalicylate may increase the neuroexcitatory activities of Trovafloxacin.Approved
CiclesonideThe risk or severity of adverse effects can be increased when Ciclesonide is combined with Trovafloxacin.Approved, Investigational
ClobetasolThe risk or severity of adverse effects can be increased when Clobetasol is combined with Trovafloxacin.Investigational
Clobetasol propionateThe risk or severity of adverse effects can be increased when Clobetasol propionate is combined with Trovafloxacin.Approved
ClobetasoneThe risk or severity of adverse effects can be increased when Clobetasone is combined with Trovafloxacin.Approved
ClocortoloneThe risk or severity of adverse effects can be increased when Clocortolone is combined with Trovafloxacin.Approved
ClonixinClonixin may increase the neuroexcitatory activities of Trovafloxacin.Approved
ClorindioneTrovafloxacin may increase the anticoagulant activities of Clorindione.Experimental
Cortexolone 17α-propionateThe risk or severity of adverse effects can be increased when Cortexolone 17α-propionate is combined with Trovafloxacin.Investigational
CorticosteroneThe risk or severity of adverse effects can be increased when Corticosterone is combined with Trovafloxacin.Experimental
Cortisone acetateThe risk or severity of adverse effects can be increased when Cortisone acetate is combined with Trovafloxacin.Approved
CurcuminCurcumin may increase the neuroexcitatory activities of Trovafloxacin.Investigational
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Trovafloxacin.Approved, Investigational
CymarinCymarin may decrease the cardiotoxic activities of Trovafloxacin.Experimental
D-LimoneneD-Limonene may increase the neuroexcitatory activities of Trovafloxacin.Investigational
DapagliflozinTrovafloxacin may increase the hypoglycemic activities of Dapagliflozin.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Trovafloxacin.Approved
DesoximetasoneThe risk or severity of adverse effects can be increased when Desoximetasone is combined with Trovafloxacin.Approved
Desoxycorticosterone acetateThe risk or severity of adverse effects can be increased when Desoxycorticosterone acetate is combined with Trovafloxacin.Approved
Desoxycorticosterone PivalateThe risk or severity of adverse effects can be increased when Desoxycorticosterone Pivalate is combined with Trovafloxacin.Experimental, Vet Approved
DexamethasoneThe risk or severity of adverse effects can be increased when Dexamethasone is combined with Trovafloxacin.Approved, Investigational, Vet Approved
Dexamethasone isonicotinateThe risk or severity of adverse effects can be increased when Dexamethasone isonicotinate is combined with Trovafloxacin.Vet Approved
DiclofenacDiclofenac may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
DicoumarolTrovafloxacin may increase the anticoagulant activities of Dicoumarol.Approved
DidanosineThe serum concentration of Didanosine can be decreased when it is combined with Trovafloxacin.Approved
DifenpiramideDifenpiramide may increase the neuroexcitatory activities of Trovafloxacin.Experimental
DiflorasoneThe risk or severity of adverse effects can be increased when Diflorasone is combined with Trovafloxacin.Approved
DiflunisalDiflunisal may increase the neuroexcitatory activities of Trovafloxacin.Approved
DifluocortoloneThe risk or severity of adverse effects can be increased when Difluocortolone is combined with Trovafloxacin.Approved, Investigational
DifluprednateThe risk or severity of adverse effects can be increased when Difluprednate is combined with Trovafloxacin.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Trovafloxacin.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Trovafloxacin.Approved
DiphenadioneTrovafloxacin may increase the anticoagulant activities of Diphenadione.Experimental
DisopyramideTrovafloxacin may increase the hypoglycemic activities of Disopyramide.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Trovafloxacin.Approved, Investigational
DroxicamDroxicam may increase the neuroexcitatory activities of Trovafloxacin.Approved
DulaglutideTrovafloxacin may increase the hypoglycemic activities of Dulaglutide.Approved
DuvelisibDuvelisib may increase the neuroexcitatory activities of Trovafloxacin.Investigational
DyphyllineThe metabolism of Dyphylline can be decreased when combined with Trovafloxacin.Approved
E-6201E-6201 may increase the neuroexcitatory activities of Trovafloxacin.Investigational
EmpagliflozinTrovafloxacin may increase the hypoglycemic activities of Empagliflozin.Approved
EpirizoleEpirizole may increase the neuroexcitatory activities of Trovafloxacin.Approved
EquileninThe risk or severity of adverse effects can be increased when Equilenin is combined with Trovafloxacin.Experimental
EquilinThe risk or severity of adverse effects can be increased when Equilin is combined with Trovafloxacin.Approved
EstroneThe risk or severity of adverse effects can be increased when Estrone is combined with Trovafloxacin.Approved
Estrone sulfateThe risk or severity of adverse effects can be increased when Estrone sulfate is combined with Trovafloxacin.Approved
EtanerceptEtanercept may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
EthenzamideEthenzamide may increase the neuroexcitatory activities of Trovafloxacin.Experimental
Ethyl biscoumacetateTrovafloxacin may increase the anticoagulant activities of Ethyl biscoumacetate.Withdrawn
EtodolacEtodolac may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational, Vet Approved
EtofenamateEtofenamate may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
EtoricoxibEtoricoxib may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
Evening primrose oilEvening primrose oil may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
ExenatideTrovafloxacin may increase the hypoglycemic activities of Exenatide.Approved, Investigational
exisulindexisulind may increase the neuroexcitatory activities of Trovafloxacin.Investigational
FelbinacFelbinac may increase the neuroexcitatory activities of Trovafloxacin.Experimental
FenbufenFenbufen may increase the neuroexcitatory activities of Trovafloxacin.Approved
FenoprofenFenoprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved
FentiazacFentiazac may increase the neuroexcitatory activities of Trovafloxacin.Experimental
FeprazoneFeprazone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
Ferric CarboxymaltoseThe serum concentration of Trovafloxacin can be decreased when it is combined with Ferric Carboxymaltose.Approved
Ferric CitrateThe serum concentration of Trovafloxacin can be decreased when it is combined with Ferric Citrate.Approved, Investigational
Ferric pyrophosphateThe serum concentration of Trovafloxacin can be decreased when it is combined with Ferric pyrophosphate.Approved
Ferulic acidFerulic acid may increase the neuroexcitatory activities of Trovafloxacin.Experimental
FloctafenineFloctafenine may increase the neuroexcitatory activities of Trovafloxacin.Approved, Withdrawn
fluasteroneThe risk or severity of adverse effects can be increased when fluasterone is combined with Trovafloxacin.Investigational
FludrocortisoneThe risk or severity of adverse effects can be increased when Fludrocortisone is combined with Trovafloxacin.Approved
FluindioneTrovafloxacin may increase the anticoagulant activities of Fluindione.Investigational
FlumethasoneThe risk or severity of adverse effects can be increased when Flumethasone is combined with Trovafloxacin.Approved, Vet Approved
FlunixinFlunixin may increase the neuroexcitatory activities of Trovafloxacin.Vet Approved
FlunoxaprofenFlunoxaprofen may increase the neuroexcitatory activities of Trovafloxacin.Experimental
Fluocinolone AcetonideThe risk or severity of adverse effects can be increased when Fluocinolone Acetonide is combined with Trovafloxacin.Approved, Investigational, Vet Approved
FluocinonideThe risk or severity of adverse effects can be increased when Fluocinonide is combined with Trovafloxacin.Approved, Investigational
FluocortoloneThe risk or severity of adverse effects can be increased when Fluocortolone is combined with Trovafloxacin.Approved, Withdrawn
FluorometholoneThe risk or severity of adverse effects can be increased when Fluorometholone is combined with Trovafloxacin.Approved
FluprednideneThe risk or severity of adverse effects can be increased when Fluprednidene is combined with Trovafloxacin.Approved, Withdrawn
FluprednisoloneThe risk or severity of adverse effects can be increased when Fluprednisolone is combined with Trovafloxacin.Approved
FlurandrenolideThe risk or severity of adverse effects can be increased when Flurandrenolide is combined with Trovafloxacin.Approved
FlurbiprofenFlurbiprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
FormestaneThe risk or severity of adverse effects can be increased when Formestane is combined with Trovafloxacin.Approved, Investigational, Withdrawn
GitoformateGitoformate may decrease the cardiotoxic activities of Trovafloxacin.Experimental
GliclazideTrovafloxacin may increase the hypoglycemic activities of Gliclazide.Approved
GlimepirideTrovafloxacin may increase the hypoglycemic activities of Glimepiride.Approved
GlipizideTrovafloxacin may increase the hypoglycemic activities of Glipizide.Approved
GlyburideTrovafloxacin may increase the hypoglycemic activities of Glyburide.Approved
GuacetisalGuacetisal may increase the neuroexcitatory activities of Trovafloxacin.Experimental
HE3286The risk or severity of adverse effects can be increased when HE3286 is combined with Trovafloxacin.Investigational
HigenamineHigenamine may increase the neuroexcitatory activities of Trovafloxacin.Investigational
HydrocortisoneThe risk or severity of adverse effects can be increased when Hydrocortisone is combined with Trovafloxacin.Approved, Vet Approved
HydrotalciteHydrotalcite can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental, Investigational
IbuprofenIbuprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved
IbuproxamIbuproxam may increase the neuroexcitatory activities of Trovafloxacin.Withdrawn
IcatibantIcatibant may increase the neuroexcitatory activities of Trovafloxacin.Approved
Imidazole salicylateImidazole salicylate may increase the neuroexcitatory activities of Trovafloxacin.Experimental
IndobufenIndobufen may increase the neuroexcitatory activities of Trovafloxacin.Investigational
IndomethacinIndomethacin may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
IndoprofenIndoprofen may increase the neuroexcitatory activities of Trovafloxacin.Withdrawn
Insulin AspartTrovafloxacin may increase the hypoglycemic activities of Insulin Aspart.Approved
Insulin DetemirTrovafloxacin may increase the hypoglycemic activities of Insulin Detemir.Approved
Insulin GlargineTrovafloxacin may increase the hypoglycemic activities of Insulin Glargine.Approved
Insulin GlulisineTrovafloxacin may increase the hypoglycemic activities of Insulin Glulisine.Approved
Insulin HumanTrovafloxacin may increase the hypoglycemic activities of Insulin Human.Approved, Investigational
Insulin LisproTrovafloxacin may increase the hypoglycemic activities of Insulin Lispro.Approved
IronThe serum concentration of Trovafloxacin can be decreased when it is combined with Iron.Approved
Iron DextranThe serum concentration of Trovafloxacin can be decreased when it is combined with Iron Dextran.Approved, Vet Approved
Iron saccharateThe serum concentration of Trovafloxacin can be decreased when it is combined with Iron saccharate.Approved
IsoxicamIsoxicam may increase the neuroexcitatory activities of Trovafloxacin.Withdrawn
IstaroximeThe risk or severity of adverse effects can be increased when Istaroxime is combined with Trovafloxacin.Investigational
KebuzoneKebuzone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
KetoprofenKetoprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
KetorolacKetorolac may increase the neuroexcitatory activities of Trovafloxacin.Approved
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Trovafloxacin.Experimental
Lanthanum carbonateThe serum concentration of Trovafloxacin can be decreased when it is combined with Lanthanum carbonate.Approved
LeflunomideLeflunomide may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
LiraglutideTrovafloxacin may increase the hypoglycemic activities of Liraglutide.Approved
LisofyllineLisofylline may increase the neuroexcitatory activities of Trovafloxacin.Investigational
LonazolacLonazolac may increase the neuroexcitatory activities of Trovafloxacin.Experimental
LornoxicamLornoxicam may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
LoxoprofenLoxoprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
LumiracoxibLumiracoxib may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
MagaldrateMagaldrate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Withdrawn
Magnesium HydroxideMagnesium Hydroxide can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium oxideMagnesium oxide can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
Magnesium peroxideMagnesium peroxide can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Experimental
Magnesium salicylateThe serum concentration of Trovafloxacin can be decreased when it is combined with Magnesium salicylate.Approved
Magnesium silicateMagnesium silicate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved, Experimental
Magnesium SulfateThe serum concentration of Trovafloxacin can be decreased when it is combined with Magnesium Sulfate.Approved, Vet Approved
Magnesium TrisilicateMagnesium Trisilicate can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
MasoprocolMasoprocol may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
ME-609The risk or severity of adverse effects can be increased when ME-609 is combined with Trovafloxacin.Investigational
MecaserminTrovafloxacin may increase the hypoglycemic activities of Mecasermin.Approved, Investigational
Meclofenamic acidMeclofenamic acid may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
MedrysoneThe risk or severity of adverse effects can be increased when Medrysone is combined with Trovafloxacin.Approved
Mefenamic acidMefenamic acid may increase the neuroexcitatory activities of Trovafloxacin.Approved
MelengestrolThe risk or severity of adverse effects can be increased when Melengestrol is combined with Trovafloxacin.Vet Approved
MeloxicamMeloxicam may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
MesalazineMesalazine may increase the neuroexcitatory activities of Trovafloxacin.Approved
MetamizoleMetamizole may increase the neuroexcitatory activities of Trovafloxacin.Investigational, Withdrawn
MetforminTrovafloxacin may increase the hypoglycemic activities of Metformin.Approved
MethylprednisoloneThe risk or severity of adverse effects can be increased when Methylprednisolone is combined with Trovafloxacin.Approved, Vet Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Trovafloxacin.Experimental
MifepristoneTrovafloxacin may increase the hypoglycemic activities of Mifepristone.Approved, Investigational
MiglitolTrovafloxacin may increase the hypoglycemic activities of Miglitol.Approved
MizoribineMizoribine may increase the neuroexcitatory activities of Trovafloxacin.Investigational
MofebutazoneMofebutazone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
Mycophenolate mofetilMycophenolate mofetil may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
Mycophenolic acidThe serum concentration of Mycophenolic acid can be decreased when it is combined with Trovafloxacin.Approved
NabumetoneNabumetone may increase the neuroexcitatory activities of Trovafloxacin.Approved
NafamostatNafamostat may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
NaftifineNaftifine may increase the neuroexcitatory activities of Trovafloxacin.Approved
NaproxenNaproxen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
NateglinideTrovafloxacin may increase the hypoglycemic activities of Nateglinide.Approved, Investigational
NCX 1022The risk or severity of adverse effects can be increased when NCX 1022 is combined with Trovafloxacin.Investigational
NepafenacNepafenac may increase the neuroexcitatory activities of Trovafloxacin.Approved
NifenazoneNifenazone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
Niflumic AcidNiflumic Acid may increase the neuroexcitatory activities of Trovafloxacin.Approved
NimesulideNimesulide may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational, Withdrawn
NitroaspirinNitroaspirin may increase the neuroexcitatory activities of Trovafloxacin.Investigational
OleandrinOleandrin may decrease the cardiotoxic activities of Trovafloxacin.Experimental, Investigational
Oleoyl-estroneThe risk or severity of adverse effects can be increased when Oleoyl-estrone is combined with Trovafloxacin.Investigational
OlopatadineOlopatadine may increase the neuroexcitatory activities of Trovafloxacin.Approved
OlsalazineOlsalazine may increase the neuroexcitatory activities of Trovafloxacin.Approved
OrgoteinOrgotein may increase the neuroexcitatory activities of Trovafloxacin.Vet Approved
OuabainOuabain may decrease the cardiotoxic activities of Trovafloxacin.Approved
OxaprozinOxaprozin may increase the neuroexcitatory activities of Trovafloxacin.Approved
OxyphenbutazoneOxyphenbutazone may increase the neuroexcitatory activities of Trovafloxacin.Approved, Withdrawn
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Trovafloxacin.Approved, Vet Approved
ParamethasoneThe risk or severity of adverse effects can be increased when Paramethasone is combined with Trovafloxacin.Approved
ParecoxibParecoxib may increase the neuroexcitatory activities of Trovafloxacin.Approved
ParthenolideParthenolide may increase the neuroexcitatory activities of Trovafloxacin.Investigational
PentamidineTrovafloxacin may increase the hypoglycemic activities of Pentamidine.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Trovafloxacin.Experimental
PhenindioneTrovafloxacin may increase the anticoagulant activities of Phenindione.Approved, Investigational
PhenprocoumonTrovafloxacin may increase the anticoagulant activities of Phenprocoumon.Approved, Investigational
PhenylbutazonePhenylbutazone may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
PimecrolimusPimecrolimus may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
PioglitazoneTrovafloxacin may increase the hypoglycemic activities of Pioglitazone.Approved, Investigational
PirfenidonePirfenidone may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
PiroxicamPiroxicam may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
PirprofenPirprofen may increase the neuroexcitatory activities of Trovafloxacin.Experimental
PramlintideTrovafloxacin may increase the hypoglycemic activities of Pramlintide.Approved, Investigational
PranoprofenPranoprofen may increase the neuroexcitatory activities of Trovafloxacin.Experimental, Investigational
PrasteroneThe risk or severity of adverse effects can be increased when Prasterone is combined with Trovafloxacin.Approved, Nutraceutical
Prasterone sulfateThe risk or severity of adverse effects can be increased when Prasterone sulfate is combined with Trovafloxacin.Investigational
PrednicarbateThe risk or severity of adverse effects can be increased when Prednicarbate is combined with Trovafloxacin.Approved
PrednisoloneThe risk or severity of adverse effects can be increased when Prednisolone is combined with Trovafloxacin.Approved, Vet Approved
PrednisoneThe risk or severity of adverse effects can be increased when Prednisone is combined with Trovafloxacin.Approved, Vet Approved
PregnenoloneThe risk or severity of adverse effects can be increased when Pregnenolone is combined with Trovafloxacin.Experimental, Investigational
ProbenecidThe serum concentration of Trovafloxacin can be increased when it is combined with Probenecid.Approved
ProglumetacinProglumetacin may increase the neuroexcitatory activities of Trovafloxacin.Experimental
PropacetamolPropacetamol may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
PropyphenazonePropyphenazone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
ProquazoneProquazone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Trovafloxacin.Experimental
PTC299PTC299 may increase the neuroexcitatory activities of Trovafloxacin.Investigational
QuinaprilThe serum concentration of Trovafloxacin can be decreased when it is combined with Quinapril.Approved, Investigational
QuinineTrovafloxacin may increase the hypoglycemic activities of Quinine.Approved
RepaglinideTrovafloxacin may increase the hypoglycemic activities of Repaglinide.Approved, Investigational
ResveratrolResveratrol may increase the neuroexcitatory activities of Trovafloxacin.Approved, Experimental, Investigational
RimexoloneThe risk or severity of adverse effects can be increased when Rimexolone is combined with Trovafloxacin.Approved
RofecoxibRofecoxib may increase the neuroexcitatory activities of Trovafloxacin.Investigational, Withdrawn
RosiglitazoneTrovafloxacin may increase the hypoglycemic activities of Rosiglitazone.Approved, Investigational
SalicylamideSalicylamide may increase the neuroexcitatory activities of Trovafloxacin.Approved
Salicylic acidSalicylic acid may increase the neuroexcitatory activities of Trovafloxacin.Approved, Vet Approved
SalsalateSalsalate may increase the neuroexcitatory activities of Trovafloxacin.Approved
SaxagliptinTrovafloxacin may increase the hypoglycemic activities of Saxagliptin.Approved
SemapimodSemapimod may increase the neuroexcitatory activities of Trovafloxacin.Investigational
SeratrodastSeratrodast may increase the neuroexcitatory activities of Trovafloxacin.Approved
SerrapeptaseSerrapeptase may increase the neuroexcitatory activities of Trovafloxacin.Investigational
SevelamerSevelamer can cause a decrease in the absorption of Trovafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.Approved
SitagliptinTrovafloxacin may increase the hypoglycemic activities of Sitagliptin.Approved, Investigational
SRT501SRT501 may increase the neuroexcitatory activities of Trovafloxacin.Investigational
Strontium ranelateThe serum concentration of Trovafloxacin can be decreased when it is combined with Strontium ranelate.Approved
SucralfateThe serum concentration of Trovafloxacin can be decreased when it is combined with Sucralfate.Approved
SulfadiazineTrovafloxacin may increase the hypoglycemic activities of Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleTrovafloxacin may increase the hypoglycemic activities of Sulfamethoxazole.Approved
SulfasalazineSulfasalazine may increase the neuroexcitatory activities of Trovafloxacin.Approved
SulfisoxazoleTrovafloxacin may increase the hypoglycemic activities of Sulfisoxazole.Approved, Vet Approved
SulindacSulindac may increase the neuroexcitatory activities of Trovafloxacin.Approved
SunitinibTrovafloxacin may increase the hypoglycemic activities of Sunitinib.Approved, Investigational
SuprofenSuprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Withdrawn
SuxibuzoneSuxibuzone may increase the neuroexcitatory activities of Trovafloxacin.Experimental
TarenflurbilTarenflurbil may increase the neuroexcitatory activities of Trovafloxacin.Investigational
TenidapTenidap may increase the neuroexcitatory activities of Trovafloxacin.Experimental
TenoxicamTenoxicam may increase the neuroexcitatory activities of Trovafloxacin.Approved
TepoxalinTepoxalin may increase the neuroexcitatory activities of Trovafloxacin.Vet Approved
TeriflunomideTeriflunomide may increase the neuroexcitatory activities of Trovafloxacin.Approved
TheophyllineThe metabolism of Theophylline can be decreased when combined with Trovafloxacin.Approved
Tiaprofenic acidTiaprofenic acid may increase the neuroexcitatory activities of Trovafloxacin.Approved
TinoridineTinoridine may increase the neuroexcitatory activities of Trovafloxacin.Investigational
TioclomarolTrovafloxacin may increase the anticoagulant activities of Tioclomarol.Experimental
TixocortolThe risk or severity of adverse effects can be increased when Tixocortol is combined with Trovafloxacin.Approved
TolazamideTrovafloxacin may increase the hypoglycemic activities of Tolazamide.Approved
TolbutamideTrovafloxacin may increase the hypoglycemic activities of Tolbutamide.Approved
Tolfenamic AcidTolfenamic Acid may increase the neuroexcitatory activities of Trovafloxacin.Approved
TolmetinTolmetin may increase the neuroexcitatory activities of Trovafloxacin.Approved
TranilastTranilast may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Trovafloxacin.Approved, Investigational
TriamcinoloneThe risk or severity of adverse effects can be increased when Triamcinolone is combined with Trovafloxacin.Approved, Vet Approved
TribenosideTribenoside may increase the neuroexcitatory activities of Trovafloxacin.Experimental
TriptolideTriptolide may increase the neuroexcitatory activities of Trovafloxacin.Investigational
ValdecoxibValdecoxib may increase the neuroexcitatory activities of Trovafloxacin.Investigational, Withdrawn
VareniclineThe serum concentration of Varenicline can be increased when it is combined with Trovafloxacin.Approved, Investigational
WarfarinTrovafloxacin may increase the anticoagulant activities of Warfarin.Approved
ZaltoprofenZaltoprofen may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational
ZileutonZileuton may increase the neuroexcitatory activities of Trovafloxacin.Approved, Investigational, Withdrawn
ZomepiracZomepirac may increase the neuroexcitatory activities of Trovafloxacin.Withdrawn
Food Interactions
Not Available

References

General References
Not Available
External Links
KEGG Compound
C07664
PubChem Compound
62959
PubChem Substance
46508751
ChemSpider
16736478
BindingDB
50146361
ChEBI
9763
ChEMBL
CHEMBL428
Therapeutic Targets Database
DAP000652
PharmGKB
PA164749184
HET
TR6
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Trovafloxacin
ATC Codes
J01MA13 — Trovafloxacin
PDB Entries
4koe / 4z2e / 4z53

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedNot AvailableBacteremia / Endocarditis / Sepsis / Staphylococcus Aureus1

Pharmacoeconomics

Manufacturers
  • Pfizer chemicals div pfizer inc
  • Pfizer central research
Packagers
Dosage forms
FormRouteStrength
LiquidIntravenous5 mg
TabletOral100 mg
TabletOral200 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5164402No1992-11-172009-11-17Us
CA2023217No1996-12-102010-08-14Canada
US6187341No1999-01-202019-01-20Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility12.3 mg/L (at 25 °C)MCFARLAND,JW ET AL. (2001)
logP0.31DAYLIGHT (2002)
Predicted Properties
PropertyValueSource
Water Solubility0.0704 mg/mLALOGPS
logP0.86ALOGPS
logP0.14ChemAxon
logS-3.8ALOGPS
pKa (Strongest Acidic)5.41ChemAxon
pKa (Strongest Basic)9.44ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area99.76 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity101.04 m3·mol-1ChemAxon
Polarizability38.12 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9969
Blood Brain Barrier+0.8109
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.5958
P-glycoprotein inhibitor INon-inhibitor0.9513
P-glycoprotein inhibitor IINon-inhibitor0.8319
Renal organic cation transporterNon-inhibitor0.7813
CYP450 2C9 substrateNon-substrate0.8731
CYP450 2D6 substrateNon-substrate0.8237
CYP450 3A4 substrateNon-substrate0.7022
CYP450 1A2 substrateNon-inhibitor0.7515
CYP450 2C9 inhibitorNon-inhibitor0.7908
CYP450 2D6 inhibitorNon-inhibitor0.834
CYP450 2C19 inhibitorNon-inhibitor0.6968
CYP450 3A4 inhibitorNon-inhibitor0.8746
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7571
Ames testAMES toxic0.7022
CarcinogenicityNon-carcinogens0.888
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3897 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9514
hERG inhibition (predictor II)Non-inhibitor0.7112
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 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

Taxonomy

Description
This compound belongs to the class of organic compounds known as naphthyridine carboxylic acids and derivatives. These are compounds containing a naphthyridine moiety, where one of the ring atoms bears a carboxylic acid group.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazanaphthalenes
Sub Class
Naphthyridines
Direct Parent
Naphthyridine carboxylic acids and derivatives
Alternative Parents
Fluoroquinolones / Pyridinecarboxylic acids / Dialkylarylamines / Aminopiperidines / Aminopyridines and derivatives / Fluorobenzenes / Aryl fluorides / Imidolactams / Vinylogous amides / Pyrrolidines
show 11 more
Substituents
Naphthyridine carboxylic acid / Fluoroquinolone / Pyridine carboxylic acid / Pyridine carboxylic acid or derivatives / Dialkylarylamine / 4-aminopiperidine / Aminopyridine / Halobenzene / Fluorobenzene / Aryl fluoride
show 28 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
tertiary amino compound, azabicycloalkane, monocarboxylic acid, primary amino compound, amino acid, difluorobenzene, 1,8-naphthyridine derivative, quinolone antibiotic, fluoroquinolone antibiotic (CHEBI:9763)

Targets

Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function
DNA gyrase negatively supercoils closed circular double-stranded DNA in an ATP-dependent manner and also catalyzes the interconversion of other topological isomers of double-stranded DNA rings, inc...
Gene Name
gyrA
Uniprot ID
P43700
Uniprot Name
DNA gyrase subunit A
Molecular Weight
97817.145 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Brisse S, Milatovic D, Fluit AC, Verhoef J, Martin N, Scheuring S, Kohrer K, Schmitz FJ: Comparative in vitro activities of ciprofloxacin, clinafloxacin, gatifloxacin, levofloxacin, moxifloxacin, and trovafloxacin against Klebsiella pneumoniae, Klebsiella oxytoca, Enterobacter cloacae, and Enterobacter aerogenes clinical isolates with alterations in GyrA and ParC proteins. Antimicrob Agents Chemother. 1999 Aug;43(8):2051-5. [PubMed:10428935]
  4. Bebear CM, Grau O, Charron A, Renaudin H, Gruson D, Bebear C: Cloning and nucleotide sequence of the DNA gyrase (gyrA) gene from Mycoplasma hominis and characterization of quinolone-resistant mutants selected in vitro with trovafloxacin. Antimicrob Agents Chemother. 2000 Oct;44(10):2719-27. [PubMed:10991851]
  5. Gootz TD, Zaniewski RP, Haskell SL, Kaczmarek FS, Maurice AE: Activities of trovafloxacin compared with those of other fluoroquinolones against purified topoisomerases and gyrA and grlA mutants of Staphylococcus aureus. Antimicrob Agents Chemother. 1999 Aug;43(8):1845-55. [PubMed:10428901]
Kind
Protein
Organism
Haemophilus influenzae (strain ATCC 51907 / DSM 11121 / KW20 / Rd)
Pharmacological action
Yes
Actions
Inhibitor
General Function
Dna topoisomerase type ii (atp-hydrolyzing) activity
Specific Function
Topoisomerase IV is essential for chromosome segregation. It relaxes supercoiled DNA. Performs the decatenation events required during the replication of a circular DNA molecule.
Gene Name
parC
Uniprot ID
P43702
Uniprot Name
DNA topoisomerase 4 subunit A
Molecular Weight
83366.24 Da
References
  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
  3. Rafii F, Park M, Novak JS: Alterations in DNA gyrase and topoisomerase IV in resistant mutants of Clostridium perfringens found after in vitro treatment with fluoroquinolones. Antimicrob Agents Chemother. 2005 Feb;49(2):488-92. [PubMed:15673722]
  4. Daporta MT, Munoz Bellido JL, Guirao GY, Hernandez MS, Garcia-Rodriguez JA: In vitro activity of older and newer fluoroquinolones against efflux-mediated high-level ciprofloxacin-resistant Streptococcus pneumoniae. Int J Antimicrob Agents. 2004 Aug;24(2):185-7. [PubMed:15288320]
  5. Ruiz J, Jurado A, Garcia-Mendez E, Marco F, Aguilar L, Jimenez de Anta MT, Vila J: Frequency of selection of fluoroquinolone-resistant mutants of Neisseria gonorrhoeae exposed to gemifloxacin and four other quinolones. J Antimicrob Chemother. 2001 Oct;48(4):545-8. [PubMed:11581235]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Ubiquitin binding
Specific Function
Control of topological states of DNA by transient breakage and subsequent rejoining of DNA strands. Topoisomerase II makes double-strand breaks. Essential during mitosis and meiosis for proper segr...
Gene Name
TOP2A
Uniprot ID
P11388
Uniprot Name
DNA topoisomerase 2-alpha
Molecular Weight
174383.88 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]

Drug created on June 13, 2005 07:24 / Updated on November 07, 2017 01:41