API | gemifloxacin

gemifloxacin (factive) Report issue

Small molecule Approved ^FDA

AACT ChEMBL DrugBank Drug Central Drugs@FDA KEGG MeSH PubChem repoDB

Active Ingredient History

NOW

Gemifloxacin is an oral broad-spectrum quinolone antibacterial agent used in the treatment of acute bacterial exacerbation of chronic bronchitis and mild-to-moderate pneumonia. Gemifloxacin mesylate is marketed under the brand name Factive, indicated for the treatment of bacterial infection caused by susceptible strains such as S. pneumoniae, H. influenzae, H. parainfluenzae, or M. catarrhalis, S. pneumoniae (including multi-drug resistant strains [MDRSP]), M. pneumoniae, C. pneumoniae, or K. pneumoniae. Gemifloxacin has in vitro activity against a wide range of Gram-negative and Grampositive microorganisms. Gemifloxacin is bactericidal with minimum bactericidal concentrations (MBCs) generally within one dilution of the minimum inhibitory concentrations (MICs). Gemifloxacin acts by inhibiting DNA synthesis through the inhibition of both DNA gyrase and topoisomerase IV (TOPO IV), which are essential for bacterial growth. Streptococcus pneumoniae showing mutations in both DNA gyrase and TOPO IV (double mutants) are resistant to most fluoroquinolones. Gemifloxacin has the ability to inhibit both enzyme systems at therapeutically relevant drug levels in S. pneumoniae (dual targeting), and has MIC values that are still in the susceptible range for some of these double mutants. ^NCATS

Chemistry

SMILES: CO/N=C1\CN(c2nc3c(cc2F)c(=O)c(C(=O)O)cn3C2CC2)CC1CN
InChIKey: ZRCVYEYHRGVLOC-HYARGMPZSA-N
Mol. Mass: 389.39
ALogP: 0.97 Partition coefficient
ChEMBL Molecules:

gemifloxacin

gemifloxacin mesylate

More Chemistry

Pharmacology

Mechanisms of Action:
- DNA gyrase subunit A (Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)) ^UniProt
- DNA gyrase subunit B (Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)) ^UniProt
- DNA topoisomerase 4 subunit A (Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)) ^UniProt
- DNA topoisomerase 4 subunit B (Streptococcus pneumoniae serotype 4 (strain ATCC BAA-334 / TIGR4)) ^UniProt
Multi-specific: Missing data
Black Box: Yes
Availability: Prescription Only
Delivery Methods: Oral
Pro Drug: No

7-(3-aminomethyl-4-methoxyimino-pyrrolidine-1-yl)-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-(1,8)-naphthyridine-3-carboxylic acid | factiv | factive | gemifloxacin | gemifloxacin mesilate | gemifloxacin mesylate | lb20304 | lb 20304 | lb-20304 | lb-20304a | sb 265805 | sb-265805 | sb-265805-s

Organizations (10)

Research & Development (8)

Organization	Org Type	FDA approvals	Clinical Trials involvement	Org ID	Force Sort

Marketing (3)

Organization	Org Type	FDA approvals	Clinical Trials involvement	Org ID	Force Sort

Indications (9)

Approved Indications (2)

Bronchitis, Chronic (approved 2003)

Pneumonia, Bacterial (approved 2003)

Experimental Indications - Clinical Trial Phases 1-4 (7)

Blood Glucose (Phase 1)

Communicable Diseases (Phase 1)

Gonorrhea (Phase 4)

Helicobacter pylori (Phase 3)

Hypoglycemia (Phase 1)

Peritonitis (Phase 3)

Rhinoscleroma (Early Phase 1)

Overview

Highest Phase: Phase 4
# of Trials: 6
# of Trial Organizations: 8

Trials by Phase

Trial	Phase	Start Date	Organizations	Indications

Feedback

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