Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMJFD2I)

• Drug Name: ABT-492 Drug Info
• Synonyms: Delafloxacin; 189279-58-1; ABT-492; WQ-3034; Abt 492; 1-(6-AMINO-3,5-DIFLUOROPYRIDIN-2-YL)-8-CHLORO-6-FLUORO-7-(3-HYDROXYAZETIDIN-1-YL)-4-OXO-1,4-DIHYDROQUINOLINE-3-CARBOXYLIC ACID; ABT492; RX-3341; UNII-6315412YVF; 6315412YVF; 1-(6-amino-3,5-difluoro-2-pyridyl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxo-quinoline-3-carboxylic acid; 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-carboxylic acid; Delafloxacin [USAN:INN]; Delafloxacinum; Delafloxacin (USAN)

Indication

Disease Entry	ICD 11	Status	REF
Bacterial infection	1A00-1C4Z	Phase 3	[1]

• Cross-matching ID:
  PubChem CID: 487101
  CAS Number: CAS 189279-58-1
  TTD Drug ID: DMJFD2I
  INTEDE Drug ID: DR1895
  ACDINA Drug ID: D00175

Molecule-Related Drug Atlas

Drug(s) Targeting Staphylococcus Topoisomerase IV (Stap-coc parC)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Ciprofloxacin XR	DM2NLS9	Acute gonococcal cervicitis		Approved	[4]
Levofloxacin	DMS60RB	Acute maxillary sinusitis		Approved	[4]
Gatifloxacin	DMSL679	Acute gonococcal cervicitis		Approved	[4]
Ozenoxacin	DM6KZMG	Impetigo	1B72	Approved	[5]
Sparfloxacin	DMB4HCT	Bacterial infection	1A00-1C4Z	Approved	[4]
Gemifloxacin	DMHT34O	Bacterial infection	1A00-1C4Z	Approved	[4]
Besifloxacin	DMPHXMI	Ocular inflammation	9C61.24	Approved	[6]
Finafloxacin	DMZEONG	Urinary tract infection	GC08	Approved	[7]
Delafloxacin Meglumine	DMVTU5Q	Acute bacterial skin infection	1C41	Approved	[8]
Moxifloxacin	DMU8V4S	Bacterial infection	1A00-1C4Z	Approved	[4]

Drug(s) Metabolized By UDP-glucuronosyltransferase 1A1 (UGT1A1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Tamoxifen	DMLB0EZ	Breast cancer	2C60-2C65	Approved	[9]
Estradiol	DMUNTE3	Acne vulgaris	ED80	Approved	[10]
Acetaminophen	DMUIE76	Allergic rhinitis	CA08.0	Approved	[11]
Etoposide	DMNH3PG	Acute myelogenous leukaemia	2A41	Approved	[12]
Zidovudine	DM4KI7O	Human immunodeficiency virus infection	1C62	Approved	[13]
Valproate	DMCFE9I	Epilepsy	8A60-8A68	Approved	[14]
Mycophenolate mofetil	DMPQAGE	Hepatosplenic T-cell lymphoma		Approved	[15]
Metronidazole	DMTIVEN	Abscess		Approved	[16]
Propofol	DMB4OLE	Anaesthesia	9A78.6	Approved	[17]
Ethanol	DMDRQZU	Chronic pain	MG30	Approved	[18]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Staphylococcus Topoisomerase IV (Stap-coc parC)	TTIXTO3	PARC_STAAS	Modulator	[2]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME	DEYGVN4	UD11_HUMAN	Substrate	[3]

References

• [1] Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009417)
• [2] Contrasting Effects of Acidic pH on the Extracellular and Intracellular Activities of the Anti-Gram-Positive Fluoroquinolones Moxifloxacin and Delafloxacin against Staphylococcus aureus
• [3] Delafloxacin: place in therapy and review of microbiologic, clinical and pharmacologic properties. Infect Dis Ther. 2018 Jun;7(2):197-217.
• [4] Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
• [5] In vitro and in vivo antibacterial activity of T-3912, a novel non-fluorinated topical quinolone. J Antimicrob Chemother. 2002 Mar;49(3):455-65.
• [6] Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
• [7] 2014 FDA drug approvals. Nat Rev Drug Discov. 2015 Feb;14(2):77-81.
• [8] 2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
• [9] Functional significance of UDP-glucuronosyltransferase variants in the metabolism of active tamoxifen metabolites. Cancer Res. 2009 Mar 1;69(5):1892-900.
• [10] Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8.
• [11] Effect of UDP-glucuronosyltransferase (UGT) 1A polymorphism (rs8330 and rs10929303) on glucuronidation status of acetaminophen. Dose Response. 2017 Sep 11;15(3):1559325817723731.
• [12] UDP-glucuronosyltransferase 1A1 is the principal enzyme responsible for etoposide glucuronidation in human liver and intestinal microsomes: structural characterization of phenolic and alcoholic glucuronides of etoposide and estimation of enzyme kinetics. Drug Metab Dispos. 2007 Mar;35(3):371-80.
• [13] Interindividual variability in pharmacokinetics of generic nucleoside reverse transcriptase inhibitors in TB/HIV-coinfected Ghanaian patients: UGT2B7*1c is associated with faster zidovudine clearance and glucuronidation. J Clin Pharmacol. 2009 Sep;49(9):1079-90.
• [14] Effect of aging on glucuronidation of valproic acid in human liver microsomes and the role of UDP-glucuronosyltransferase UGT1A4, UGT1A8, and UGT1A10. Drug Metab Dispos. 2009 Jan;37(1):229-36.
• [15] Characterization of rat intestinal microsomal UDP-glucuronosyltransferase activity toward mycophenolic acid. Drug Metab Dispos. 2006 Sep;34(9):1632-9.
• [16] Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
• [17] Substrate-dependent modulation of UDP-glucuronosyltransferase 1A1 (UGT1A1) by propofol in recombinant human UGT1A1 and human liver microsomes. Basic Clin Pharmacol Toxicol. 2007 Sep;101(3):211-4.
• [18] Identification and preliminary characterization of UDP-glucuronosyltransferases catalyzing formation of ethyl glucuronide. Anal Bioanal Chem. 2014 Apr;406(9-10):2325-32.