Details of the Drug

General Information of Drug (ID: DMJFD2I)

• Drug Name: ABT-492
• 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]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 1:
  Molecular Weight (mw); 440.8
  Logarithm of the Partition Coefficient (xlogp); 2.7
  Rotatable Bond Count (rotbonds); 3
  Hydrogen Bond Donor Count (hbonddonor); 3
  Hydrogen Bond Acceptor Count (hbondacc); 11
• ADMET Property:
  Bioavailability: The bioavailability of drug is 58.8% []
  Clearance: The mean total clearance of drug is 16.3 L/h []
  Elimination: After a single intravenous dose, 65% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 28% excreted unchanged in the feces []
  Half-life: The concentration or amount of drug in body reduced by one-half in 3.7 hours []
  Metabolism: The drug is metabolized via the glucuronidation []
  Unbound Fraction: The unbound fraction of drug in plasma is 0.16% [2]
  Vd: The volume of distribution (Vd) of drug is 30-48 L []
• Chemical Identifiers:
  Formula: C18H12ClF3N4O4
  IUPAC Name: 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6-fluoro-7-(3-hydroxyazetidin-1-yl)-4-oxoquinoline-3-carboxylic acid
  Canonical SMILES: C1C(CN1C2=C(C=C3C(=C2Cl)N(C=C(C3=O)C(=O)O)C4=C(C=C(C(=N4)N)F)F)F)O
  InChI: InChI=1S/C18H12ClF3N4O4/c19-12-13-7(1-9(20)14(12)25-3-6(27)4-25)15(28)8(18(29)30)5-26(13)17-11(22)2-10(21)16(23)24-17/h1-2,5-6,27H,3-4H2,(H2,23,24)(H,29,30)
  InChIKey: DYDCPNMLZGFQTM-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 487101
  CAS Number: 189279-58-1
  DrugBank ID: DB11943
  TTD ID: D0V9BU
  INTEDE ID: DR1895
  ACDINA ID: D00175

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	[3]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME	DEYGVN4	UD11_HUMAN	Substrate	[4]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from ABT-492 (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Gilteritinib	DMTI0ZO	Moderate	Decreased clearance of ABT-492 due to the transporter inhibition by Gilteritinib.	Acute myeloid leukaemia [2A60]	[5]
Ag-221	DMS0ZBI	Moderate	Decreased clearance of ABT-492 due to the transporter inhibition by Ag-221.	BCR-ABL1-negative chronic myeloid leukaemia [2A41]	[5]
Erdafitinib	DMI782S	Moderate	Decreased clearance of ABT-492 due to the transporter inhibition by Erdafitinib.	Bladder cancer [2C94]	[6]
PF-04449913	DMSB068	Moderate	Decreased clearance of ABT-492 due to the transporter inhibition by PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[7]
Lurbinectedin	DMEFRTZ	Minor	Decreased absorption of ABT-492 due to intestinal mucosa variation caused by Lurbinectedin.	Lung cancer [2C25]	[8]
Rucaparib	DM9PVX8	Moderate	Decreased metabolism of ABT-492 caused by Rucaparib mediated inhibition of UGT.	Ovarian cancer [2C73]	[9]
Choline salicylate	DM8P137	Moderate	Additive CNS depression effects by the combination of ABT-492 and Choline salicylate.	Postoperative inflammation [1A00-CA43]	[10]
Darolutamide	DMV7YFT	Moderate	Decreased clearance of ABT-492 due to the transporter inhibition by Darolutamide.	Prostate cancer [2C82]	[11]
Tedizolid	DMG2SKR	Moderate	Decreased clearance of ABT-492 due to the transporter inhibition by Tedizolid.	Skin and skin-structure infection [1F28-1G0Z]	[7]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Kyselina citronova	E00014	311	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
Meglumine	E00181	8567	Buffering agent
Crospovidone	E00626	Not Available	Disintegrant
Edetate disodium	E00186	8759	Complexing agent
Magnesium palmitostearate	E00532	18763844	Other agent
Magnesium stearate	E00208	11177	lubricant
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Sodium bicarbonate	E00424	516892	Alkalizing agent; Diluent
Sodium dihydrogenorthophosphate	E00559	23672064	Buffering agent; Complexing agent
Sodium phosphate monobasic monohydrate	E00428	516949	Buffering agent; Complexing agent
Vinylpyrrolidone	E00668	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Water	E00035	962	Solvent
Betadex sulfobutyl ether sodium	E00589	66577045	Solubilizing agent
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Delafloxacin 450 mg tablet	450 mg	Oral Tablet	Oral
Delafloxacin Meglumine 300 mg For Injection	300 mg	For Injection	Intravenous
Delafloxacin Meglumine 450 mg tablet	450 mg	Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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] Trend Analysis of a Database of Intravenous Pharmacokinetic Parameters in Humans for 1352 Drug Compounds
• [3] Contrasting Effects of Acidic pH on the Extracellular and Intracellular Activities of the Anti-Gram-Positive Fluoroquinolones Moxifloxacin and Delafloxacin against Staphylococcus aureus
• [4] Delafloxacin: place in therapy and review of microbiologic, clinical and pharmacologic properties. Infect Dis Ther. 2018 Jun;7(2):197-217.
• [5] Cerner Multum, Inc. "Australian Product Information.".
• [6] Product Information. Balversa (erdafitinib). Janssen Products, LP, Horsham, PA.
• [7] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [8] Johnson EJ, MacGowan AP, Potter MN, et al "Reduced absorption of oral ciprofloxacin after chemotherapy for haematological malignancy." J Antimicrob Chemother 25 (1990): 837-42. [PMID: 2373666]
• [9] EMA. European Medicines Agency. European Union "EMA - List of medicines under additional monitoring.".
• [10] Product Information. Factive (gemifloxacin). GeneSoft Inc, San Francisco, CA.
• [11] Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.