Gipodacin for treatment of bacterial urinary tract infections
A technology of urinary tract infection and gepodacin, applied in antibacterial drugs, urinary system diseases, organic active ingredients, etc., can solve problems such as limited treatment methods and affecting the efficacy of oral antibacterial treatment programs
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Embodiment 1
[0267] Biological activity assay (in vitro assay)
[0268] Studies were conducted to evaluate the in vitro activity of compounds of the invention and specific comparative compounds identified in the following methods.
[0269] method 1
[0270] Antibacterial activity was determined by broth microdilution using CLSI recommended procedures.
[0271] Gepodacin was tested in serial two-fold dilutions and the minimum inhibitory concentration (MIC) was determined as the lowest concentration of the compound that inhibited visible growth.
[0272] Gepodacin was tested against 28 strains of Staphylococcus saprophyticus collected from several hospitals.
[0273] Amoxicillin, azithromycin, levofloxacin, and cefuroxime were included as positive controls. The MICs of gepodacin and positive controls were determined by the broth microdilution method according to the CLSI method.
[0274] For 28 S. saprophyticus isolates, the MIC90 of gepodacin (a test isolate with 90% MIC inhibition)...
Embodiment 2
[0315] Example 2: Distribution and Exposure of Gepodacin in Tissues and Fluids of Healthy and Infected Participants
[0316] Antibiotic target exposure plays a key role, as suboptimal levels can lead to treatment failure and resistance. Gepodacin exposure in plasma and other matrices such as urine, saliva, epithelial lining fluid (ELF), and alveolar macrophages (AM) has been assessed in multiple clinical studies.
[0317] Bronchoalveolar lavage samples were collected to determine gepodacin exposure in ELF and AM following a 2-hour single 1000 mg IV infusion in healthy subjects. Salivary exposure was assessed in healthy volunteers following a single oral dose of 150 mg. In women with acute uUTI, urinary exposure to gepodacin was assessed following oral administration of 1500 mg BID for 5 days.
[0318] The ratios of ELF and AM AUC(0-12) to unbound plasma were 1.84 and 178, respectively, indicating good ELF exposure and excellent cell penetration. There was a linear relatio...
Embodiment 3
[0320] Example 3: Phase II Study Evaluating Gepodacin in the Treatment of Uncomplicated Urinary Tract Infections
[0321] method:
[0322] This phase IIa single-center study evaluated the safety, tolerability, pharmacokinetics, and efficacy of oral gepodacin 1500 mg BID for 5 days in female subjects with acute cystitis. Clean-captured midstream urine samples were obtained by standard methods for quantitative culture. Urine samples were collected from all participants at pre-treatment (baseline) and at all post-baseline visits. All urine samples were sent to a central laboratory (PPD Global Clinical Laboratories, Highland Heights, KY, USA) for Gram staining, quantitative culture, pathogen identification and drug susceptibility testing. The distribution of participants and the study outline are shown in Figure 1.
[0323] A. Microbiological research
[0324] Susceptibility testing was performed by CLSI broth microdilution and gradient diffusion (fosfomycin only) (CLSI,...
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