Target Information

Target General Infomation
Target ID
T22348
Former ID
TTDI01914
Target Name
Bacterial DNA gyrase
Target Type
Successful
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Chronic bronchitis [ICD10: J42]
Fungal infections [ICD9: 110-118; ICD10: B35-B49]
Infections disease [ICD10: A00-B99]
Infections [ICD9: 001-139; ICD10: A00-B99]
Otitis media [ICD10: H65-H67]
Ocular inflammation [ICD9: 370.33; ICD10: H16.229]
Pneumonia [ICD10: J12-J18]
Respiratory tract infection [ICD9: 460-519; ICD10: J00-J99]
Staphylococcus aureus infection [ICD10: B95.6]
Urinary tract infections [ICD9: 599; ICD10: N39.0]
Unspecified [ICD code not available]
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, including catenanes and knotted rings.
BioChemical Class
ATP-hydrolyzing DNA topoisomerase
UniProt ID
P20831||P0A0K8
EC Number
EC=5.99.1.3
Drugs and Mode of Action
Drug(s) Besifloxacin Drug Info Approved Ocular inflammation [530677], [531950]
Ciprofloxacin Hydrochloride Drug Info Approved Bacterial infections [551871]
Finafloxacin Drug Info Approved Urinary tract infections [533123], [551871]
Gatifloxacin Drug Info Approved Respiratory tract infection [536472]
Gemifloxacin Drug Info Approved Bacterial infections [536094]
Grepafloxacin Drug Info Approved Chronic bronchitis [551871]
Levofloxacin Drug Info Approved Bacterial infections [536773]
Moxifloxacin Drug Info Approved Bacterial infections [536472]
Norfloxacin Drug Info Approved Bacterial infections [538281]
Ofloxacin Drug Info Approved Bacterial infections [536222]
Sparfloxacin Drug Info Approved Bacterial infections [538553]
Trovafloxacin Drug Info Approved Bacterial infections [538605]
BAY-35-3377 Drug Info Phase 3 Otitis media [547073]
Ciprofloxacin intratympanic - Otonomy Drug Info Phase 3 Unspecified [1559538]
Ozenoxacin Drug Info Phase 3 Bacterial infections [524682]
Zabofloxacin Drug Info Phase 3 Pneumonia [524004]
AZD0914 Drug Info Phase 2 Bacterial infections [524944]
WCK-771 Drug Info Phase 2 Bacterial infections [547481]
Viquidacin Drug Info Preclinical Bacterial infections [547573]
Grepafloxacin Drug Info Withdrawn from market Bacterial infections [538554]
Temafloxacin Drug Info Withdrawn from market Bacterial infections [544673]
OLAMUFLOXACIN MESILATE Drug Info Discontinued in Phase 3 Bacterial infections [546090]
99mTc-ciprofloxacin, DRAXIS Drug Info Discontinued in Phase 2 Infections disease [547444]
A-86719.1 Drug Info Discontinued in Phase 2 Bacterial infections [545655]
BAY-Y-3118 Drug Info Discontinued in Phase 2 Bacterial infections [544982]
Cadrofloxacin Drug Info Discontinued in Phase 2 Bacterial infections [545284]
CFC-222 Drug Info Discontinued in Phase 2 Bacterial infections [545639]
DANOFLOXACIN Drug Info Discontinued in Phase 2 Bacterial infections [526405]
DX-619 Drug Info Discontinued in Phase 2 Bacterial infections [547823]
FANDOFLOXACIN HYDROCHLORIDE Drug Info Discontinued in Phase 2 Bacterial infections [545638]
Ro-23-9424 Drug Info Discontinued in Phase 2 Bacterial infections [544670]
AZD-5099 Drug Info Discontinued in Phase 1 Infections [549270]
Cetefloxacin Drug Info Discontinued in Phase 1 Bacterial infections [545018]
DV-7751A Drug Info Discontinued in Phase 1 Bacterial infections [545076]
GSK945237 Drug Info Discontinued in Phase 1 Bacterial infections [548649]
PD-131112 Drug Info Discontinued in Phase 1 Bacterial infections [544944]
A-70826 Drug Info Terminated Bacterial infections [545052]
BMY-40062 Drug Info Terminated Bacterial infections [544661]
CBR-2092 Drug Info Terminated Bacterial infections [548625]
Clinafloxacin Drug Info Terminated Pneumonia [544668]
CP-67015 Drug Info Terminated Bacterial infections [545521]
Dual-action antibiotics Drug Info Terminated Bacterial infections [544794]
KB-5246 Drug Info Terminated Bacterial infections [544660]
MF-5137 Drug Info Terminated Staphylococcus aureus infection [545640]
PD-117596 Drug Info Terminated Bacterial infections [544667]
Protosufloxacin Drug Info Terminated Bacterial infections [545576]
Ro-23-7777 Drug Info Terminated Fungal infections [545532]
S-34109 Drug Info Terminated Staphylococcus aureus infection [546353]
Inhibitor 99mTc-ciprofloxacin, DRAXIS Drug Info [544000]
BAY-35-3377 Drug Info [525396]
Modulator A-70826 Drug Info [545053]
A-86719.1 Drug Info
AZD-5099 Drug Info [532855]
AZD0914 Drug Info
BAY-Y-3118 Drug Info
Besifloxacin Drug Info [530677], [531950]
BMY-40062 Drug Info
Cadrofloxacin Drug Info [534230]
CBR-2092 Drug Info
Cetefloxacin Drug Info [1572591]
CFC-222 Drug Info
Ciprofloxacin Hydrochloride Drug Info [556264]
Ciprofloxacin intratympanic - Otonomy Drug Info
Clinafloxacin Drug Info [534732]
CP-67015 Drug Info [556264]
DANOFLOXACIN Drug Info
Dual-action antibiotics Drug Info [534005]
DV-7751A Drug Info
DX-619 Drug Info [527893]
FANDOFLOXACIN HYDROCHLORIDE Drug Info [1572591]
Finafloxacin Drug Info [533123]
Gatifloxacin Drug Info [556264]
Gemifloxacin Drug Info [556264]
Grepafloxacin Drug Info
GSK945237 Drug Info
KB-5246 Drug Info [544015]
Levofloxacin Drug Info [556264]
MF-5137 Drug Info [556264]
Moxifloxacin Drug Info [556264]
Norfloxacin Drug Info [556264]
NSFQ-105 Drug Info
Ofloxacin Drug Info [556264]
OLAMUFLOXACIN MESILATE Drug Info [1572591]
Ozenoxacin Drug Info
PD-117558 Drug Info
PD-117596 Drug Info
PD-131112 Drug Info [1572591]
Protosufloxacin Drug Info [556264]
Ro-23-7777 Drug Info [556264]
Ro-23-9424 Drug Info
S-34109 Drug Info [546354]
Sparfloxacin Drug Info [556264]
Temafloxacin Drug Info [528147]
Trovafloxacin Drug Info [556264]
Viquidacin Drug Info
WCK-771 Drug Info
Zabofloxacin Drug Info
References
Ref 524004ClinicalTrials.gov (NCT01658020) A Study to Evaluate Efficacy and Safety Profile of Zabofloxacin Tablet 400mg and Moxifloxacin Tablet 400mg. U.S. National Institutes of Health.
Ref 524682ClinicalTrials.gov (NCT02090764) Efficacy and Safety of Ozenoxacin 1% Cream Versus Placebo in the Treatment of Patients With Impetigo. U.S. National Institutes of Health.
Ref 524944ClinicalTrials.gov (NCT02257918) Randomized, Open-label Phase 2 Study of Oral AZD0914 in the Treatment of Gonorrhea. U.S. National Institutes of Health.
Ref 526405Pharmacokinetic and pharmacodynamic profiles of danofloxacin administered by two dosing regimens in calves infected with Mannheimia (Pasteurella) haemolytica. Antimicrob Agents Chemother. 2002 Sep;46(9):3013-9.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 531950Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 536094Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98.
Ref 536222Emerging therapies for the treatment and prevention of otitis media. Expert Opin Emerg Drugs. 2006 May;11(2):251-64.
Ref 536472Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8.
Ref 536773How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30.
Ref 538281FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074690.
Ref 538553FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020677.
Ref 538554FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020695.
Ref 538605FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050762.
Ref 544660Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000463)
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Ref 546353Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007670)
Ref 547073Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012837)
Ref 547444Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016416)
Ref 547481Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016734)
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Ref 547823Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019670)
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Ref 549270Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034406)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 1559538DOI: 10.1093/jac/48.4.479
Ref
Ref 525396Antibiotics in the clinical pipeline in 2013. J Antibiot (Tokyo). 2013 Oct;66(10):571-91. doi: 10.1038/ja.2013.86. Epub 2013 Sep 4.
Ref 527893DX-619, a novel des-fluoro(6) quinolone manifesting low frequency of selection of resistant Staphylococcus aureus mutants: quinolone resistance beyond modification of type II topoisomerases. Antimicrob Agents Chemother. 2005 Dec;49(12):5051-7.
Ref 528147Mechanisms and frequency of resistance to temafloxacin. Am J Med. 1991 Dec 30;91(6A):27S-30S.
Ref 530677Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
Ref 531950Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90.
Ref 532855Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099). J Med Chem. 2014 Jul 24;57(14):6060-82.
Ref 5331232014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
Ref 534005Mechanisms of action of cephalosporin 3'-quinolone esters, carbamates, and tertiary amines in Escherichia coli. Antimicrob Agents Chemother. 1993 Mar;37(3):559-65.
Ref 534230Hydrophilicity of quinolones is not an exclusive factor for decreased activity in efflux-mediated resistant mutants of Staphylococcus aureus. Antimicrob Agents Chemother. 1996 Aug;40(8):1835-42.
Ref 534732DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae. Antimicrob Agents Chemother. 1998 Nov;42(11):2810-6.
Ref 544000Binding of ciprofloxacin labelled with technetium Tc 99m versus 99mTc-pertechnetate to a live and killed equine isolate of Escherichia coli. Can J Vet Res. 2005 October; 69(4): 272-277.
Ref 544015Activity of KB-5246 against outer membrane mutants of Escherichia coli and Salmonella typhimurium.. Antimicrob Agents Chemother. 1990 July; 34(7): 1323-1325.
Ref 545053Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001978)
Ref 546354Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007670)
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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