Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T22348
|
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| Former ID |
TTDI01914
|
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| Target Name |
Bacterial DNA gyrase
|
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| Target Type |
Successful
|
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| 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 [ICD9: 001-139; ICD10: A00-B99] | |||||
| Infections disease [ICD10: A00-B99] | |||||
| Ocular inflammation [ICD9: 370.33; ICD10: H16.229] | |||||
| Otitis media [ICD10: H65-H67] | |||||
| 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.
|
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| BioChemical Class |
ATP-hydrolyzing DNA topoisomerase
|
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| UniProt ID | |||||
| EC Number |
EC=5.99.1.3
|
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| Drugs and Mode of Action | |||||
| Drug(s) | Besifloxacin | Drug Info | Approved | Ocular inflammation | [1], [2] |
| Ciprofloxacin Hydrochloride | Drug Info | Approved | Bacterial infections | [3] | |
| Finafloxacin | Drug Info | Approved | Urinary tract infections | [4], [3] | |
| Gatifloxacin | Drug Info | Approved | Respiratory tract infection | [5] | |
| Gemifloxacin | Drug Info | Approved | Bacterial infections | [6] | |
| Grepafloxacin | Drug Info | Approved | Chronic bronchitis | [3] | |
| Levofloxacin | Drug Info | Approved | Bacterial infections | [7] | |
| Moxifloxacin | Drug Info | Approved | Bacterial infections | [5] | |
| Norfloxacin | Drug Info | Approved | Bacterial infections | [8] | |
| Ofloxacin | Drug Info | Approved | Bacterial infections | [9] | |
| Sparfloxacin | Drug Info | Approved | Bacterial infections | [10] | |
| Trovafloxacin | Drug Info | Approved | Bacterial infections | [11] | |
| BAY-35-3377 | Drug Info | Phase 3 | Otitis media | [12] | |
| Ciprofloxacin intratympanic - Otonomy | Drug Info | Phase 3 | Unspecified | [13] | |
| Ozenoxacin | Drug Info | Phase 3 | Bacterial infections | [14] | |
| Zabofloxacin | Drug Info | Phase 3 | Pneumonia | [15] | |
| AZD0914 | Drug Info | Phase 2 | Bacterial infections | [16] | |
| WCK-771 | Drug Info | Phase 2 | Bacterial infections | [17] | |
| Viquidacin | Drug Info | Preclinical | Bacterial infections | [18] | |
| Grepafloxacin | Drug Info | Withdrawn from market | Bacterial infections | [19] | |
| Temafloxacin | Drug Info | Withdrawn from market | Bacterial infections | [20] | |
| OLAMUFLOXACIN MESILATE | Drug Info | Discontinued in Phase 3 | Bacterial infections | [21] | |
| 99mTc-ciprofloxacin, DRAXIS | Drug Info | Discontinued in Phase 2 | Infections disease | [22] | |
| A-86719.1 | Drug Info | Discontinued in Phase 2 | Bacterial infections | [23] | |
| BAY-Y-3118 | Drug Info | Discontinued in Phase 2 | Bacterial infections | [24] | |
| Cadrofloxacin | Drug Info | Discontinued in Phase 2 | Bacterial infections | [25] | |
| CFC-222 | Drug Info | Discontinued in Phase 2 | Bacterial infections | [26] | |
| DANOFLOXACIN | Drug Info | Discontinued in Phase 2 | Bacterial infections | [27] | |
| DX-619 | Drug Info | Discontinued in Phase 2 | Bacterial infections | [28] | |
| FANDOFLOXACIN HYDROCHLORIDE | Drug Info | Discontinued in Phase 2 | Bacterial infections | [29] | |
| Ro-23-9424 | Drug Info | Discontinued in Phase 2 | Bacterial infections | [30] | |
| AZD-5099 | Drug Info | Discontinued in Phase 1 | Infections | [31] | |
| Cetefloxacin | Drug Info | Discontinued in Phase 1 | Bacterial infections | [32] | |
| DV-7751A | Drug Info | Discontinued in Phase 1 | Bacterial infections | [33] | |
| GSK945237 | Drug Info | Discontinued in Phase 1 | Bacterial infections | [34] | |
| PD-131112 | Drug Info | Discontinued in Phase 1 | Bacterial infections | [35] | |
| A-70826 | Drug Info | Terminated | Bacterial infections | [36] | |
| BMY-40062 | Drug Info | Terminated | Bacterial infections | [37] | |
| CBR-2092 | Drug Info | Terminated | Bacterial infections | [38] | |
| Clinafloxacin | Drug Info | Terminated | Pneumonia | [39] | |
| CP-67015 | Drug Info | Terminated | Bacterial infections | [40] | |
| Dual-action antibiotics | Drug Info | Terminated | Bacterial infections | [41] | |
| KB-5246 | Drug Info | Terminated | Bacterial infections | [42] | |
| MF-5137 | Drug Info | Terminated | Staphylococcus aureus infection | [43] | |
| PD-117596 | Drug Info | Terminated | Bacterial infections | [44] | |
| Protosufloxacin | Drug Info | Terminated | Bacterial infections | [45] | |
| Ro-23-7777 | Drug Info | Terminated | Fungal infections | [46] | |
| S-34109 | Drug Info | Terminated | Staphylococcus aureus infection | [47] | |
| Inhibitor | 99mTc-ciprofloxacin, DRAXIS | Drug Info | [48] | ||
| BAY-35-3377 | Drug Info | [49] | |||
| Modulator | A-70826 | Drug Info | [50] | ||
| A-86719.1 | Drug Info | ||||
| AZD-5099 | Drug Info | [51] | |||
| AZD0914 | Drug Info | ||||
| BAY-Y-3118 | Drug Info | ||||
| Besifloxacin | Drug Info | [1], [2] | |||
| BMY-40062 | Drug Info | ||||
| Cadrofloxacin | Drug Info | [52] | |||
| CBR-2092 | Drug Info | ||||
| Cetefloxacin | Drug Info | [53] | |||
| CFC-222 | Drug Info | ||||
| Ciprofloxacin Hydrochloride | Drug Info | [54] | |||
| Ciprofloxacin intratympanic - Otonomy | Drug Info | ||||
| Clinafloxacin | Drug Info | [55] | |||
| CP-67015 | Drug Info | [54] | |||
| DANOFLOXACIN | Drug Info | ||||
| Dual-action antibiotics | Drug Info | [56] | |||
| DV-7751A | Drug Info | ||||
| DX-619 | Drug Info | [57] | |||
| FANDOFLOXACIN HYDROCHLORIDE | Drug Info | [53] | |||
| Finafloxacin | Drug Info | [4] | |||
| Gatifloxacin | Drug Info | [54] | |||
| Gemifloxacin | Drug Info | [54] | |||
| Grepafloxacin | Drug Info | ||||
| GSK945237 | Drug Info | ||||
| KB-5246 | Drug Info | [58] | |||
| Levofloxacin | Drug Info | [54] | |||
| MF-5137 | Drug Info | [54] | |||
| Moxifloxacin | Drug Info | [54] | |||
| Norfloxacin | Drug Info | [54] | |||
| NSFQ-105 | Drug Info | ||||
| Ofloxacin | Drug Info | [54] | |||
| OLAMUFLOXACIN MESILATE | Drug Info | [53] | |||
| Ozenoxacin | Drug Info | ||||
| PD-117558 | Drug Info | ||||
| PD-117596 | Drug Info | ||||
| PD-131112 | Drug Info | [53] | |||
| Protosufloxacin | Drug Info | [54] | |||
| Ro-23-7777 | Drug Info | [54] | |||
| Ro-23-9424 | Drug Info | ||||
| S-34109 | Drug Info | [59] | |||
| Sparfloxacin | Drug Info | [54] | |||
| Temafloxacin | Drug Info | [60] | |||
| Trovafloxacin | Drug Info | [54] | |||
| Viquidacin | Drug Info | ||||
| WCK-771 | Drug Info | ||||
| Zabofloxacin | Drug Info | ||||
| References | |||||
| REF 1 | Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92. | ||||
| REF 2 | Besifloxacin ophthalmic suspension, 0.6%: a novel topical fluoroquinolone for bacterial conjunctivitis. Adv Ther. 2012 Jun;29(6):473-90. | ||||
| REF 3 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015 | ||||
| REF 4 | 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81. | ||||
| REF 5 | Novel agents in the management of Mycobacterium tuberculosis disease. Curr Med Chem. 2007;14(18):2000-8. | ||||
| REF 6 | Emerging drugs for bacterial urinary tract infections. Expert Opin Emerg Drugs. 2005 May;10(2):275-98. | ||||
| REF 7 | How many modes of action should an antibiotic have? Curr Opin Pharmacol. 2008 Oct;8(5):564-73. Epub 2008 Jul 30. | ||||
| REF 8 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074690. | ||||
| REF 9 | Emerging therapies for the treatment and prevention of otitis media. Expert Opin Emerg Drugs. 2006 May;11(2):251-64. | ||||
| REF 10 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020677. | ||||
| REF 11 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 050762. | ||||
| REF 12 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012837) | ||||
| REF 13 | DOI: 10.1093/jac/48.4.479 | ||||
| REF 14 | ClinicalTrials.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 15 | ClinicalTrials.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 16 | ClinicalTrials.gov (NCT02257918) Randomized, Open-label Phase 2 Study of Oral AZD0914 in the Treatment of Gonorrhea. U.S. National Institutes of Health. | ||||
| REF 17 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016734) | ||||
| REF 18 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800017450) | ||||
| REF 19 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 020695. | ||||
| REF 20 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000542) | ||||
| REF 21 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006301) | ||||
| REF 22 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016416) | ||||
| REF 23 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004047) | ||||
| REF 24 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001782) | ||||
| REF 25 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002693) | ||||
| REF 26 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004010) | ||||
| REF 27 | Pharmacokinetic 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 28 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800019670) | ||||
| REF 29 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004009) | ||||
| REF 30 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000529) | ||||
| REF 31 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800034406) | ||||
| REF 32 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001898) | ||||
| REF 33 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002052) | ||||
| REF 34 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027355) | ||||
| REF 35 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001614) | ||||
| REF 36 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001978) | ||||
| REF 37 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000465) | ||||
| REF 38 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800027165) | ||||
| REF 39 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000525) | ||||
| REF 40 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003590) | ||||
| REF 41 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001135) | ||||
| REF 42 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000463) | ||||
| REF 43 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004011) | ||||
| REF 44 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000523) | ||||
| REF 45 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003745) | ||||
| REF 46 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003620) | ||||
| REF 47 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007670) | ||||
| REF 48 | Binding 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 49 | Antibiotics 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 50 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001978) | ||||
| REF 51 | Optimization of pyrrolamide topoisomerase II inhibitors toward identification of an antibacterial clinical candidate (AZD5099). J Med Chem. 2014 Jul 24;57(14):6060-82. | ||||
| REF 52 | Hydrophilicity 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 53 | Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41. | ||||
| REF 54 | Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. | ||||
| REF 55 | DNA gyrase and topoisomerase IV are dual targets of clinafloxacin action in Streptococcus pneumoniae. Antimicrob Agents Chemother. 1998 Nov;42(11):2810-6. | ||||
| REF 56 | Mechanisms of action of cephalosporin 3'-quinolone esters, carbamates, and tertiary amines in Escherichia coli. Antimicrob Agents Chemother. 1993 Mar;37(3):559-65. | ||||
| REF 57 | DX-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 58 | Activity of KB-5246 against outer membrane mutants of Escherichia coli and Salmonella typhimurium.. Antimicrob Agents Chemother. 1990 July; 34(7): 1323-1325. | ||||
| REF 59 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007670) | ||||
| REF 60 | Mechanisms and frequency of resistance to temafloxacin. Am J Med. 1991 Dec 30;91(6A):27S-30S. | ||||
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