Drug intelligence / Profile preview

cloxacillin + gentamicin

Development stage
Unknown
Lead developer
GSK
Modality
Small Molecules
Administration
Intravenous, Intramuscular, Intrathecal
01

Overview

Cloxacillin + gentamicin is a combination of two antibiotics used primarily for the treatment of serious bacterial infections, including right-sided Staphylococcus aureus endocarditis and neonatal sepsis. Cloxacillin is a penicillinase-resistant penicillin antibiotic that inhibits bacterial cell wall synthesis by binding to penicillin-binding proteins, leading to cell lysis and death. Gentamicin is an aminoglycoside antibiotic that binds to the 30S subunit of bacterial ribosomes, inhibiting protein synthesis and causing misreading of mRNA, which results in bactericidal activity. The combination leverages the broad-spectrum activity of gentamicin (especially against Gram-negative bacteria) with cloxacillin’s efficacy against beta-lactamase-producing staphylococci (Gram-positive bacteria). This regimen has been studied for short-course therapy in right-sided endocarditis among intravenous drug users and for severe infections in neonates where staphylococcal infection risk is high[1][3][4][5][7].

02

Targets

Bacterial RibosomePBP (Penicillin-binding protein family)Bacterial 50S ribosomal subunit

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