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
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)
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 |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/26119479Curator'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
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 |
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Target ID: CHEMBL355 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479 |
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Target ID: CHEMBL614429 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479 |
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Target ID: CHEMBL614430 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479 |
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Target ID: CHEMBL350 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26119479 |
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Target ID: CHEMBL352 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22875850 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Curative | BAXDELA Approved UseBAXDELA 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 Date2017 |
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Curative | BAXDELA Approved UseBAXDELA 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 Date2017 |
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Curative | BAXDELA Approved UseBAXDELA 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 Date2017 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
8.94 μg/mL |
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 |
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 |
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 |
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 | Co-administered | Analyte | Population |
---|---|---|---|---|
21.8 μg × h/mL |
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 |
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 |
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 |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.7 h |
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
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
16% |
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: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Other AEs: Nausea, Gastrointestinal disorders... Other AEs: Nausea (50%) Sources: 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 |
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: |
unhealthy, adult Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Age Group: adult Sources: |
Disc. AE: Tendinitis, Tendon rupture... AEs leading to discontinuation/dose reduction: Tendinitis (serious) Sources: Tendon rupture (serious) Peripheral neuropathy (serious) Myasthenia gravis (serious) |
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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: Page: p. 163 |
Disc. AE: Hypersensitivity... AEs leading to discontinuation/dose reduction: Hypersensitivity (0.1%) Sources: 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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: Page: p. 163 |
Disc. AE: Vomiting, Hypersensitivity... AEs leading to discontinuation/dose reduction: Vomiting (0.1%) Sources: Page: p. 163Hypersensitivity (0.1%) Urticaria (0.3%) Dermatitis allergic (0.1%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Pruritus | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
|
Dizziness | 12.5% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Feeling hot | 12.5% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Nervous system disorders | 12.5% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
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: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Retching | 12.5% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Rhinorrhea | 12.5% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
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: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Diarrhea | 25% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Nausea | 50% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Vomiting | 75% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
Gastrointestinal disorders | 87.5% | 1200 mg single, intravenous Highest studied dose Dose: 1200 mg Route: intravenous Route: single Dose: 1200 mg Sources: |
healthy, 19- 64 years n = 8 Health Status: healthy Age Group: 19- 64 years Sex: M+F Population Size: 8 Sources: |
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: |
unhealthy, adult Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Age Group: adult Sources: |
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: |
unhealthy, adult Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Age Group: adult Sources: |
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: |
unhealthy, adult Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Age Group: adult Sources: |
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: |
unhealthy, adult Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Age Group: adult Sources: |
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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: 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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: 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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: 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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: 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: Page: p. 163 |
unhealthy n = 741 Health Status: unhealthy Condition: acute bacterial skin and skin structure infections Population Size: 741 Sources: Page: p. 163 |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
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 | Metabolite | Clinical evidence |
---|---|---|---|---|
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
no | ||||
yes | ||||
yes | ||||
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 |
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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 |
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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 |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02015637
900mg orally (2 x 450 mg tablets) administered once
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/22875850
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
Edited
Sat Dec 16 17:34:51 GMT 2023
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admin
on
Sat Dec 16 17:34:51 GMT 2023
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Record UNII |
6315412YVF
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Record Status |
Validated (UNII)
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Record Version |
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NDF-RT |
N0000193223
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J01MA23
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NCI_THESAURUS |
C795
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487101
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CHEMBL2105637
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189279-58-1
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Delafloxacin
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DTXSID40172331
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Related Record | Type | Details | ||
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TARGET ORGANISM->INHIBITOR |
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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
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TRANSPORTER -> SUBSTRATE |
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TRANSPORTER -> SUBSTRATE |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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METABOLIC ENZYME -> SUBSTRATE |
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METABOLIC ENZYME -> INDUCER |
Delafloxacin was a mild inducer (less than 2 fold) of CYP3A4 at a clinically relevant concentration.
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TARGET ORGANISM->INHIBITOR |
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METABOLIC ENZYME -> SUBSTRATE |
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TARGET ORGANISM->INHIBITOR |
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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
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BINDER->LIGAND |
BINDING
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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METABOLIC ENZYME -> SUBSTRATE |
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SALT/SOLVATE -> PARENT |
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TARGET ORGANISM->INHIBITOR |
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METABOLIC ENZYME -> INDUCER |
Delafloxacin was a mild inducer (less than 2 fold) of CYP2C9 at a concentration of 100 μM
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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TARGET ORGANISM->INHIBITOR |
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Related Record | Type | Details | ||
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ACTIVE MOIETY |
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Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Biological Half-life | PHARMACOKINETIC |
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MULTIPLE ORAL ADMINISTRATION |
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Tmax | PHARMACOKINETIC |
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FASTED CONDITION |
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NOAEL | TOXICITY |
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ORGAN SYSTEM OR TYPE OF EFFECT TOXICITY TOXICITY TOXICITY |
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Volume of Distribution | PHARMACOKINETIC |
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INTRAVENOUS ADMINISTRATION |
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