Drug Information

Drug (ID: DG00948) and It's Reported Resistant Information

• Name: Balofloxacin
• Synonyms: Balofloxacin; 127294-70-6; 1-Cyclopropyl-6-fluoro-8-methoxy-7-(3-(methylamino)piperidin-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid; Bilimin; (+-)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-(methylamino)piperidino)-4-oxo-3-quinolinecarboxylic acid; 1-cyclopropyl-6-fluoro-8-methoxy-7-[3-(methylamino)piperidin-1-yl]-4-oxoquinoline-3-carboxylic acid; NCGC00167532-01; Balofloxacin [INN]; DSSTox_CID_26695; DSSTox_RID_81829; UNII-Q022B63JPM; DSSTox_GSID_46695; 3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-(methylamino)-1-piperidinyl)-4-oxo-; Q 35; 1-cyclopropyl-6-fluoro-8-methoxy-7-[3-(methylamino)piperidin-1-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid; CAS-127294-70-6; CHEMBL1210954; 3-Quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)-1-piperidinyl]-4-oxo-; BALOFLOXACIN 2-HYDRATE; SCHEMBL134163; DTXSID5046695; HMS3655N15; HY-B0159; RKL10070; Tox21_112529; MFCD00864925; s2064; AKOS015900452; Tox21_112529_1; CCG-268516; CS-1991; KS-5214; NCGC00167532-02; (+-)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-(methylamino)piperidino)-4-oxo-3-quinoline arboxylic acid; 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)-1-piperidino]-4-oxo-3-quinolinecarboxylicacid; 1-cyclopropyl-6-fluoro-8-methoxy-7-[3-(methylamino)-1-piperidyl]-4-oxo-quinoline-3-carboxylic acid; B4354; FT-0602907; SW220155-1; AB01566884_01; Balofloxacin, VETRANAL(TM), analytical standard; 294B706; A805677; SR-01000872576; J-700148; Q3633495; SR-01000872576-1; (+/-)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)piperidino]-4-oxo-3-quinolinecarboxylic acid; 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methylaminopiperidin-1-yl)-4-oxoquinoline-3-carboxylic acid; 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)-1-piperidyl]-4-oxoquinoline-3-carboxylic Acid; 1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[3-(methylamino)piperidino]-4-oxo-3-quinolinecarboxylic acid
• Indication:
  In total 1 Indication(s)
  Gram-positive bacterial infection [ICD-11: 1B74-1F40]; Approved; [1]
• Drug Resistance Disease(s):
  Disease(s) with Resistance Information Validated by in-vivo Model for This Drug (1 diseases)
  Bacterial infection [ICD-11: 1A00-1C4Z]; [1]
• Target: Bacterial Penicillin binding protein (Bact PBP); NOUNIPROTAC; [1]
• Formula: C20H24FN3O4
• IsoSMILES: CNC1CCCN(C1)C2=C(C=C3C(=C2OC)N(C=C(C3=O)C(=O)O)C4CC4)F
• InChI: 1S/C20H24FN3O4/c1-22-11-4-3-7-23(9-11)17-15(21)8-13-16(19(17)28-2)24(12-5-6-12)10-14(18(13)25)20(26)27/h8,10-12,22H,3-7,9H2,1-2H3,(H,26,27)
• InChIKey: MGQLHRYJBWGORO-UHFFFAOYSA-N
• PubChem CID: 65958
• TTD Drug ID: D00XHD

Type(s) of Resistant Mechanism of This Drug

  IDUE: Irregularity in Drug Uptake and Drug Efflux

Drug Resistance Data Categorized by Their Corresponding Diseases

ICD-01: Infectious/parasitic diseases

Bacterial infection [ICD-11: 1A00-1C4Z]

Drug Resistance Data Categorized by Their Corresponding Mechanisms

Irregularity in Drug Uptake and Drug Efflux (IDUE)

Key Molecule: (Na+)-NQR maturation NqrM (nqrM) [1]

• Molecule Alteration: Expression; Down-regulation
• Resistant Disease: Vibrio alginolyticus infection [ICD-11: 1A00-1C4Z]
• Experimental Note: Discovered Using In-vivo Testing Model
• Experiment for Molecule Alteration: Western blotting analysis
• Mechanism Description: Na(+)-NQR is a membrane-embedded NADH dehydrogenase. Down-regulation of the Na(+)-NQR is required for V. alginolyticus in resistance to BLFX. It is known that the resistant mechanisms of a quinolone antibiotic are through the inhibition of DNA-gyrase which is required for DNA synthesis, and expressional changes of OM proteins which elevate pump activity and decrease OM permeability.

References

• Ref 1: Downregulation of Na(+)-NQR complex is essential for Vibrio alginolyticus in resistance to balofloxacin .J Proteomics. 2012 May 17;75(9):2638-48. doi: 10.1016/j.jprot.2012.03.006. Epub 2012 Mar 17. 10.1016/j.jprot.2012.03.006