DELAFLOXACIN

Details

Stereochemistry	ACHIRAL
Molecular Formula	C18H12ClF3N4O4
Molecular Weight	440.76
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

NC1=NC(N2C=C(C(O)=O)C(=O)C3=C2C(Cl)=C(N4CC(O)C4)C(F)=C3)=C(F)C=C1F

InChI

InChIKey=DYDCPNMLZGFQTM-UHFFFAOYSA-N

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)

HIDE SMILES / InChI

Molecular Formula	C18H12ClF3N4O4
Molecular Weight	440.76
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/history/baxdela.html http://www.malinplc.com/wp-content/uploads/2015/10/Melinta-Therapeutics-Presents-Complete-Delafloxacin-Results-09.10.15.pdf

Delafloxacin (CAS registry number 189279-58-1) was described as WQ-3034 by Wakunaga Pharmaceutical Co., Ltd., Osaka & Hiroshima, Japan. It was first licensed in 1999 to Abbott Park, IL, and further developed as ABT-492. Delafloxacin (Baxdela), a fluoroquinolone antibiotic, is currently being developed by Melinta Therapeutics. It is a novel investigational fluoroquinolone in development for the treatment of uncomplicated gonorrhea, and acute bacterial skin and skin structure infections. Delafloxacin shows MICs remarkably low against Gram-positive organisms and anaerobes and similar to those of ciprofloxacin against Gram-negative bacteria. It remains active against most fluoroquinolone-resistant strains, except enterococci. Its potency is further increased in acidic environments (found in many infection sites). Delafloxacin is active on staphylococci growing intracellularly or in biofilms. Delafloxacin is a dual-targeting fluoroquinolone, capable of forming cleavable complexes with DNA and topoisomerase IV or DNA gyrase and of inhibiting the activity of these enzymes in both Gram-positive and Gram-negative bacteria. On Oct 24, 2016, Melinta Therapeutics Submitted Baxdela New Drug Application for hospital-treated skin infections.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Haemophilus influenzae 10 Target ID: CHEMBL355 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479	Inhibitor 8504
Moraxella catarrhalis 10 Target ID: CHEMBL614429 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479	Inhibitor 8504
Neisseria gonorrhoeae 5 Target ID: CHEMBL614430 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479	Inhibitor 8504
Klebsiella pneumoniae 2 Target ID: CHEMBL350 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479	Inhibitor 8504
Staphylococcus aureus 70 Target ID: CHEMBL352 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22875850	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Community-acquired bacterial pneumonia 11 Sources: https://clinicaltrials.gov/ct2/show/NCT02679573	Curative	Phase III 665	BAXDELA Approved Use BAXDELA is a fluoroquinolone antibacterial indicated in adults for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria. (1.1) To reduce the development of drug-resistant bacteria and maintain the effectiveness of BAXDELA and other antibacterial drugs, BAXDELA should be used only to treat infections that are proven or strongly suspected to be caused by bacteria. (1.2) Launch Date 2017
Gonorrhea 30 Sources: https://clinicaltrials.gov/ct2/show/NCT02015637	Curative	Phase III 665	BAXDELA Approved Use BAXDELA is a fluoroquinolone antibacterial indicated in adults for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria. (1.1) To reduce the development of drug-resistant bacteria and maintain the effectiveness of BAXDELA and other antibacterial drugs, BAXDELA should be used only to treat infections that are proven or strongly suspected to be caused by bacteria. (1.2) Launch Date 2017
Acute bacterial skin and skin structure infection 16 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf	Curative	Approved 8583	BAXDELA Approved Use BAXDELA is a fluoroquinolone antibacterial indicated in adults for the treatment of acute bacterial skin and skin structure infections (ABSSSI) caused by designated susceptible bacteria. (1.1) To reduce the development of drug-resistant bacteria and maintain the effectiveness of BAXDELA and other antibacterial drugs, BAXDELA should be used only to treat infections that are proven or strongly suspected to be caused by bacteria. (1.2) Launch Date 2017

C_max

Value	Dose	Analyte	Population
8.94 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
9.29 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	300 mg 2 times / day steady-state, intravenous dose: 300 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
7.17 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
7.45 μg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	450 mg 2 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
21.8 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
23.4 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	300 mg 2 times / day steady-state, intravenous dose: 300 mg route of administration: Intravenous experiment type: STEADY-STATE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
22.7 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
30.8 μg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	450 mg 2 times / day steady-state, oral dose: 450 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
3.7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:		DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
16% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/208610s007,208611s006lbl.pdf	300 mg single, intravenous dose: 300 mg route of administration: Intravenous experiment type: SINGLE co-administered:		DELAFLOXACIN MEGLUMINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: https://pubmed.ncbi.nlm.nih.gov/26718605	healthy, 19- 64 years Health Status: healthy Age Group: 19- 64 years Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/26718605	Other AEs: Nausea, Gastrointestinal disorders... Other AEs: Nausea (50%) Gastrointestinal disorders (87.5%) Vomiting (75%) Diarrhea (25%) Retching (12.5%) Nervous system disorders (12.5%) Dizziness (12.5%) Feeling hot (12.5%) Respiratory, thoracic and mediastinal disorders (12.5%) Rhinorrhea (12.5%) Skin and subcutaneous tissue disorders (12.5%) Pruritus Sources: https://pubmed.ncbi.nlm.nih.gov/26718605
300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf	Disc. AE: Tendinitis, Tendon rupture... AEs leading to discontinuation/dose reduction: Tendinitis (serious) Tendon rupture (serious) Peripheral neuropathy (serious) Myasthenia gravis (serious) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf
300 mg 2 times / day multiple, intravenous Recommended Dose: 300 mg, 2 times / day Route: intravenous Route: multiple Dose: 300 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf	Disc. AE: Hypersensitivity... AEs leading to discontinuation/dose reduction: Hypersensitivity (0.1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
300 \|450 mg\|mg 2 times / day multiple, intravenous\|oral Recommended Dose: 300 \|450 mg\|mg, 2 times / day Route: intravenous\|oral Route: multiple Dose: 300 \|450 mg\|mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf	Disc. AE: Vomiting, Hypersensitivity... AEs leading to discontinuation/dose reduction: Vomiting (0.1%) Hypersensitivity (0.1%) Urticaria (0.3%) Dermatitis allergic (0.1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087	inhibitor 2438 inducer 440	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2A6 879 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP2E1 1060 CYP3A4/5 296 P-gp 1741 BCRP 910 OAT1 725 OAT3 747 OATP1B1 1079 OATP1B3 961 BSEP 550 OCT1 620 OCT2 779 UGT1A1 246 UGT1A3 89 UGT1A4 98 UGT1A6 136 UGT1A9 148 UGT2B7 197 UGT2B15 84	UGT1A1 479 UGT1A3 470 UGT2B15 236 OAT1 395 OAT3 391 OCT1 393 OCT2 434 OATP1B1 503 OATP1B3 435 BCRP 697 P-gp 2052	CYP1A2 832 CYP2B6 669 CYP2C19 329 CYP2C8 198

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	no
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
UGT1A3 99	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
UGT1A4 100	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
UGT1A6 171	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
UGT1A9 155	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
UGT2B15 84	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
UGT2B7 210	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=36 Page: 36.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	yes	no (co-administration study) Comment: An in vivo DDI study (Study ML-3341-118) of multiple oral doses of delafloxacin (450 mg Q12h) on a single oral dose of midazolam (5 mg) demonstrated no impact on midazolam PK, and minimal impact on 1-hydroxymidazolam PK Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=16 Page: 16.0

Drug as victim

Target	Modality	Activity	Clinical evidence
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	no
UGT1A1 479	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=15 Page: 15.0	yes
UGT1A3 470	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=15 Page: 15.0	yes
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	yes	no (co-administration study) Comment: Delafloxacin AUC0-24 values from patients who received P-gp/BCRP inhibitors along with delafloxacin are overlayed with the values from patients who received no P-gp/BCRP inhibitors. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0	yes	no (co-administration study) Comment: Delafloxacin AUC0-24 values from patients who received P-gp/BCRP inhibitors along with delafloxacin are overlayed with the values from patients who received no P-gp/BCRP inhibitors. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=37 Page: 37.0
UGT2B15 236	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=15 Page: 15.0	yes	yes (pharmacogenomic study) Comment: The Cmin data from Study M00-224 seems significantly correlated with UGT2B15*2 genotype. Due to the small sample size (N=27), Applicant concluded that further confirmation is required to elucidate the role of UGT2B15. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000ClinPharmR.pdf#page=15 Page: 15.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000PharmR.pdf#page=85 Page: 85.0

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY10497	https://www.001chemical.com/chem/189279-58-1
AA Blocks	AA002I3C	https://www.aablocks.com/goods/Goods/detail?id=AA002I3C
Aaron Chemicals	AR002IV4	http://www.aaronchem.com/189279-58-1
Achemtek	0104-035792	http://www.achemtek.com/189279-58-1
Acorn PharmaTech	ACN-052287	http://www.acornpharmatech.com/
Adooq BioScience	A10023	https://www.adooq.com/abt-492.html
Adooq BioScience	ABT-492	http://www.adooq.com/abt-492.html
AK Scientific, Inc. (AKSCI)	X5822	http://www.aksci.com/item_detail.php?cat=X5822
Ambinter	Amb22520781	http://www.ambinter.com/reference/22520781
Angene	AGN-PC-0QIQPJ	http://www.angenechemical.com/productshow/AGN-PC-0QIQPJ.html
Ark Pharm	AK232294	http://www.arkpharminc.com/products/189279-58-1.html
Aurum Pharmatech LLC	W-5433	http://www.Aurumpharmatech.com/Product/ProductDetails/W_5433
BioCrick	BCC1522	http://www.biocrick.com/Delafloxacin-BCC1522.html
BLD Pharm	BD360873	http://www.bldpharm.com/products/189279-58-1.html
BOC Sciences	189279-58-1	https://www.bocsci.com/product/delafloxacin-cas-189279-58-1-292324.html
Chem Scene	CS-1478	http://www.chemscene.com/189279-58-1.html
Chemspace	CSSB00020648435	https://chem-space.com/CSSB00020648435
Clearsynth	CS-DS-00004	https://www.clearsynth.com/en/CSDS00004.html
CSNpharm	CSN16520	https://www.csnpharm.com/products/delafloxacin.html
DC Chemicals	DC10458	http://www.dcchemicals.com/product_show-Delafloxacin_ABT_492.html
eNovation Chemicals	D520374	https://www.enovationchem.com/ProductDetails.asp?ProductID=D520374
eNovation Chemicals	D571807	https://www.enovationchem.com/ProductDetails.asp?ProductID=D571807
eNovation Chemicals	Y0975525	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0975525
Excenen	EX-A2331	https://www.excenen.com/searchresultlist.php?id=189279-58-1
Finetech	FT-0697895	http://www.finetechnology-ind.com/prod/detail/pub/189279-58-1.html
iChemical	EBD246564	http://www.ichemical.com/products/189279-58-1.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
Lab Network	LN01342002	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01342002
LGC Standards	DRE-A12117300AL-100	https://www.lgcstandards.com/US/en/p/DRE-A12117300AL-100
LGC Standards	DRE-C12117300	https://www.lgcstandards.com/US/en/p/DRE-C12117300
MedChem Express	HY-14814	https://www.medchemexpress.com/Delafloxacin.html
Molcore	MC10497	https://www.molcore.com/product/189279-58-1
MuseChem	I011446	https://www.musechem.com/product/I011446.html
Selleck Chemicals	S1553	http://www.selleckchem.com/products/ABT-492.html
Sigma-Aldrich	SML1869_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/sml1869?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S525586	http://www.smolecule.com/products/s525586
Sun-shine Chemical	Delafloxacin	http://www.sun-shinechem.com/Details/Delafloxacin/2077/1256037-58-7.html
Synblock Inc	SB16746	http://www.synblock.com/product/189279-58-1.html
THE BioTek	bt-266634	https://www.thebiotek.com/product/inhibitors/bt-266634

PubMed

Title	Date	PubMed
Comparative antimicrobial activities of the newly synthesized quinolone WQ-3034, levofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis and Mycobacterium avium complex.	2000 Feb	10639351
New antibiotics for antibiotic-resistant bacteria.	2009 May 28	20948644
Methicillin-resistant Staphylococcus aureus: a pervasive pathogen highlights the need for new antimicrobial development.	2010 Dec	21165342

Patents

Sample Use Guides

In Vivo Use Guide

900mg orally (2 x 450 mg tablets) administered once

Route of Administration: Oral

In Vitro Use Guide

Delafloxacin demonstrated potent in vitro activity against this set of Staphylococcus aureus (MRSA) isolates, with MICs of 0.008-1 mg/L and an MIC(50) and MIC(90) of 0.03 and 0.5 mg/L, respectively.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 09:19:38 GMT 2025` Edited by `admin` on `Wed Apr 02 09:19:38 GMT 2025`
Record UNII	6315412YVF
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BAXDELA

Preferred Name

English

DELAFLOXACIN

Official Name

English

DELAFLOXACIN [MI]

Common Name

English

delafloxacin [INN]

Common Name

English

RX-3341

Code

English

ABT-492

Code

English

WQ-3034

Code

English

3-QUINOLINECARBOXYLIC ACID, 1-(6-AMINO-3,5-DIFLUORO-2-PYRIDINYL)-8-CHLORO-6-FLUORO-1,4-DIHYDRO-7-(3-HYDROXY-1-AZETIDINYL)-4-OXO-

Common Name

English

Delafloxacin [WHO-DD]

Common Name

English

DELAFLOXACIN [USAN]

Common Name

English

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

Systematic Name

English

Classification Tree Code System Code

NDF-RT

N0000193223