U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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 of DELAFLOXACIN

SMILES

NC1=C(F)C=C(F)C(=N1)N2C=C(C(O)=O)C(=O)C3=CC(F)=C(N4CC(O)C4)C(Cl)=C23

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
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

2017
422
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8297
Inhibitor
8297
Inhibitor
8297
Inhibitor
8297
Inhibitor
8297
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
Phase III
656
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

1.49774402E12
Curative
Phase III
656
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

1.49774402E12
Curative
Approved
8429
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

1.49774402E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
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
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
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
7.45 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

AUC

ValueDoseCo-administeredAnalytePopulation
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
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
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
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
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

Doses

DosePopulationAdverse 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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
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
Condition: acute bacterial skin and skin structure infections
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
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
Page: p. 163
300 |450 mg|mg 2 times / day multiple, intravenous|oral (complex)
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
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
Page: p. 163
AEs

AEs

AESignificanceDosePopulation
Pruritus
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Dizziness 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Feeling hot 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Nervous system disorders 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Respiratory, thoracic and mediastinal disorders 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Retching 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Rhinorrhea 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Skin and subcutaneous tissue disorders 12.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Diarrhea 25%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Nausea 50%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Vomiting 75%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Gastrointestinal disorders 87.5%
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
n = 8
Health Status: healthy
Age Group: 19- 64 years
Sex: M+F
Population Size: 8
Sources:
https://pubmed.ncbi.nlm.nih.gov/26718605
Myasthenia gravis serious
Disc. AE
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
Condition: acute bacterial skin and skin structure infections
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf
Peripheral neuropathy serious
Disc. AE
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
Condition: acute bacterial skin and skin structure infections
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf
Tendinitis serious
Disc. AE
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
Condition: acute bacterial skin and skin structure infections
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf
Tendon rupture serious
Disc. AE
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
Condition: acute bacterial skin and skin structure infections
Age Group: adult
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208610s000,208611s000lbl.pdf
Hypersensitivity 0.1%
Disc. AE
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
Dermatitis allergic 0.1%
Disc. AE
300 |450 mg|mg 2 times / day multiple, intravenous|oral (complex)
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
Hypersensitivity 0.1%
Disc. AE
300 |450 mg|mg 2 times / day multiple, intravenous|oral (complex)
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
Vomiting 0.1%
Disc. AE
300 |450 mg|mg 2 times / day multiple, intravenous|oral (complex)
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
Urticaria 0.3%
Disc. AE
300 |450 mg|mg 2 times / day multiple, intravenous|oral (complex)
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
Page: p. 163
unhealthy
n = 741
Health Status: unhealthy
Condition: acute bacterial skin and skin structure infections
Population Size: 741
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208610Orig1s000,208611Orig1s000MedR.pdf
Page: p. 163
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
781
inhibitor
1767

inducer
389
inhibitor
1852
inhibitor
1612

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1524

CYP2A6
707

CYP2B6
810

CYP2C8
911

CYP2C19
1478

CYP2E1
882

CYP3A4/5
278

P-gp
1461

BCRP
699

OAT1
599

OAT3
642

OATP1B1
788

OATP1B3
706

BSEP
402

OCT1
512

OCT2
647

UGT1A1
204

UGT1A3
84

UGT1A4
77

UGT1A6
108

UGT1A9
116

UGT2B7
146

UGT2B15
64
UGT1A1
418

UGT1A3
422

UGT2B15
203

OAT1
326

OAT3
339

OCT1
327

OCT2
355

OATP1B1
406

OATP1B3
350

BCRP
561

P-gp
1537
CYP1A2
701

CYP2B6
547

CYP2C19
293

CYP2C8
168
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
BCRP
773
 no
BSEP
403
 no
CYP1A2
1692
 no
CYP1A2
1692
 no
CYP2A6
739
 no
CYP2B6
1001
 no
CYP2B6
1001
 no
CYP2C19
1553
 no
CYP2C19
1553
 no
CYP2C8
965
 no
CYP2C8
965
 no
CYP2C9
1819
 no
CYP2D6
1891
 no
CYP2E1
970
 no
CYP3A4/5
335
 no
OAT1
603
 no
OAT3
644
 no
OATP1B1
803
 no
OATP1B3
715
 no
OCT1
543
 no
OCT2
648
 no
P-gp
1650
 no
UGT1A1
254
 no
UGT1A3
93
 no
UGT1A4
80
 no
UGT1A6
141
 no
UGT1A9
121
 no
UGT2B15
64
 no
UGT2B7
157
 no
CYP2C9
1819
 yes
CYP3A4
1925
 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
Page: 16.0
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
OAT1
326
 no
OAT3
339
 no
OATP1B1
406
 no
OATP1B3
350
 no
OCT1
327
 no
OCT2
355
 no
UGT1A1
418
 yes
UGT1A3
422
 yes
BCRP
561
 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.
Page: 37.0
P-gp
1537
 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.
Page: 37.0
UGT2B15
203
 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.
Page: 15.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1647
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY10497
https://www.001chemical.com/chem/189279-58-1
AA Blocks
AA002I3C
https://www.aablocks.com/goods/Goods/detail?id=AA002I3C
AK Scientific, Inc. (AKSCI)
X5822
http://www.aksci.com/item_detail.php?cat=X5822
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
ABT-492
http://www.adooq.com/abt-492.html
Adooq BioScience
A10023
https://www.adooq.com/abt-492.html
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
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
BioCrick
BCC1522
http://www.biocrick.com/Delafloxacin-BCC1522.html
CSNpharm
CSN16520
https://www.csnpharm.com/products/delafloxacin.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
DC Chemicals
DC10458
http://www.dcchemicals.com/product_show-Delafloxacin_ABT_492.html
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
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
Lab Network
LN01342002
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01342002
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
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
iChemical
EBD246564
http://www.ichemical.com/products/189279-58-1.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs
PubMed

PubMed

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

Patents

05998436
2
06133284
2
06156903
3
JP2000136191A
2

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 Sat Dec 16 17:34:51 UTC 2023
Edited
by admin
on Sat Dec 16 17:34:51 UTC 2023
Record UNII
6315412YVF
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
DELAFLOXACIN
INN   USAN   WHO-DD  
USAN   INN  
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
BAXDELA
Brand 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
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
WHO-ATC J01MA23
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
NCI_THESAURUS C795
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
Code System Code Type Description
DAILYMED
6315412YVF
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
INN
9064
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
PUBCHEM
487101
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
ChEMBL
CHEMBL2105637
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
SMS_ID
100000176638
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
MERCK INDEX
m12032
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
RXCUI
1927663
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
DRUG BANK
DB11943
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
CAS
189279-58-1
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
LACTMED
Delafloxacin
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
DRUG CENTRAL
5238
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
FDA UNII
6315412YVF
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
NCI_THESAURUS
C87390
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
USAN
TT-116
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
EPA CompTox
DTXSID40172331
Created by admin on Sat Dec 16 17:34:54 UTC 2023 , Edited by admin on Sat Dec 16 17:34:54 UTC 2023
PRIMARY
Related Record Type Details
NEISSERIA MENINGITIDIS
TARGET ORGANISM->INHIBITOR
Structure of DELAFLOXACIN
EXCRETED UNCHANGED
Following a single oral dose of 14C-labeled delafloxacin, 50% of the radioactivity is excreted in urine as unchanged delafloxacin and glucuronide metabolites and 48% is excreted in feces as unchanged delafloxacin.
FECAL; URINE
MULTIDRUG RESISTANCE PROTEIN 1
TRANSPORTER -> SUBSTRATE
ATP-BINDING CASSETTE SUB-FAMILY G MEMBER 2
TRANSPORTER -> SUBSTRATE
STAPHYLOCOCCUS HAEMOLYTICUS
TARGET ORGANISM->INHIBITOR
METHICILLIN-RESISTANT STAPHYLOCOCCUS AUREUS
TARGET ORGANISM->INHIBITOR
ENTEROCOCCUS FAECALIS
TARGET ORGANISM->INHIBITOR
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A1
METABOLIC ENZYME -> SUBSTRATE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INDUCER
Delafloxacin was a mild inducer (less than 2 fold) of CYP3A4 at a clinically relevant concentration.
STREPTOCOCCUS ANGINOSUS
TARGET ORGANISM->INHIBITOR
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 2B15
METABOLIC ENZYME -> SUBSTRATE
CLOSTRIDIUM PERFRINGENS
TARGET ORGANISM->INHIBITOR
Structure of DELAFLOXACIN
EXCRETED UNCHANGED
After single intravenous dose of 14C-labeled delafloxacin, 65% of the radioactivity is excreted in urine as unchanged delafloxacin and glucuronide metabolites and 28% is excreted in feces as unchanged delafloxacin.
FECAL; URINE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
STREPTOCOCCUS PYOGENES
TARGET ORGANISM->INHIBITOR
CLOSTRIDIUM DIFFICILE
TARGET ORGANISM->INHIBITOR
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A3
METABOLIC ENZYME -> SUBSTRATE
Structure of DELAFLOXACIN MEGLUMINE
SALT/SOLVATE -> PARENT
STREPTOCOCCUS AGALACTIAE
TARGET ORGANISM->INHIBITOR
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INDUCER
Delafloxacin was a mild inducer (less than 2 fold) of CYP2C9 at a concentration of 100 μM
MORAXELLA CATARRHALIS
TARGET ORGANISM->INHIBITOR
STAPHYLOCOCCUS AUREUS
TARGET ORGANISM->INHIBITOR
NEISSERIA GONORRHOEAE
TARGET ORGANISM->INHIBITOR
HAEMOPHILUS INFLUENZAE
TARGET ORGANISM->INHIBITOR
PSEUDOMONAS AERUGINOSA
TARGET ORGANISM->INHIBITOR
Related Record Type Details
Structure of DELAFLOXACIN
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Biological Half-life PHARMACOKINETIC MULTIPLE ORAL ADMINISTRATION

Tmax PHARMACOKINETIC FASTED CONDITION

ORAL ADMINISTRATION

NOAEL TOXICITY ORGAN SYSTEM OR TYPE OF EFFECT
TOXICITY
SPECIES
TOXICITY
ROUTE OF ADMINISTRATION
TOXICITY
COMMENTS

Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

SINGLE DOSE

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