Cefpodoxime (free acid) exhibits moderate antibacterial activity against various bacterial strains, including Haemophilus influenzae, Escherichia coli, Neisseria gonorrhoeae, Salmonella enterica, Shigella sonnei, and Streptococcus pneumoniae. Its effectiveness is measured by Minimum Inhibitory Concentration (MIC) values, with varying degrees of potency against different strains, indicating potent activity against susceptible strains and decreased efficacy against resistant strains with specific genetic mutations. Additionally, it has shown antimicrobial activity against rifampin-resistant and beta-lactamase-nonproducing ampicillin-resistant Haemophilus influenzae isolates, with MIC values ranging from 0.03 to 8.0 µg/mL. The compound also exhibits activity against Escherichia coli strains harboring the blaTEM-168 gene, with inhibitory zone diameters enhanced by clavulanic acid, and demonstrates moderate binding to plasma proteins in both humans (25.0% to 53.45%) and rats (54.59%).
In human Caco-2 cells, Cefpodoxime (free acid) has shown insignificant binding affinity to the membrane transport protein PEPT1, with a Ki value greater than 30,000,000 nM. Additionally, the compound has a renal transport interaction with PepT2 in SKTP cells, showing a similar Ki value. It possesses moderate hepatotoxicity, indicated by elevated serum ALT or AST levels with a 33.3% observed frequency of moderate liver toxicity during clinical trials, although it showed no acute liver toxicity or severe hepatic side effects. Cefpodoxime (free acid) does not exhibit significant bioactivity in various receptor and enzyme assays, as evidenced by AC50 values exceeding 30,000 nM. The compound's pharmacokinetics reflect a low intrinsic clearance rate in rat hepatocytes and bioactivity related to specific biological compartments following oral administration, suggesting a potential for longer half-life. Overall, Cefpodoxime (free acid) demonstrates a broad spectrum of antibacterial activity with varying degrees of efficacy and moderate liver toxicity..
Note: Summary generated by AI. Data source: ChEMBL 