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Linezolid is an antibiotic used for the treatment of infections caused by Gram-positive bacteria that are resistant to other antibiotics. [9] [10] Linezolid is active against most Gram-positive bacteria that cause disease, including streptococci, vancomycin-resistant enterococci (VRE), and methicillin-resistant Staphylococcus aureus (MRSA).
Glycopeptide antibiotics are a class of drugs of microbial origin that are composed of glycosylated cyclic or polycyclic nonribosomal peptides.Significant glycopeptide antibiotics include the anti-infective antibiotics vancomycin, teicoplanin, telavancin, ramoplanin, avoparcin and decaplanin, corbomycin, complestatin and the antitumor antibiotic bleomycin.
A set of NRPS enzymes (peptide synthase VpsA, VpsB, and VpsC) are responsible for assembling the heptapeptide. (Figure 2). [72] VpsA codes for modules 1, 2, and 3. VpsB codes for modules 4, 5, and 6, and VpsC codes for module 7. The vancomycin aglycone contains 4 D-amino acids, although the NRPSs only contain 3 epimerization domains.
When the minimum inhibitory concentration of vancomycin is > 2 µg/mL, alternative antibiotics should be used. The approach is to treat with at least one agent to which the bacteria known to be susceptible by in vitro testing. The agents that are used include daptomycin, linezolid, telavancin, ceftaroline, and quinupristin–dalfopristin.
Narrow-spectrum antibiotics have low propensity to induce bacterial resistance and are less likely to disrupt the microbiome (normal microflora). [3] On the other hand, indiscriminate use of broad-spectrum antibiotics may not only induce the development of bacterial resistance and promote the emergency of multidrug-resistant organisms, but also cause off-target effects due to dysbiosis.
Staphylococcus haemolyticus is a member of the coagulase-negative staphylococci (CoNS). [2] It is part of the skin flora of humans, [3] and its largest populations are usually found at the axillae, perineum, and inguinal areas. [4] S. haemolyticus also colonizes primates and domestic animals. [4]
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Afabicin (Debio 1450) is an experimental antibiotic developed by Debiopharm for the treatment of Staphylococcus aureus infections. It is a prodrug which is converted in vivo into the active form afabicin desphosphono (Debio 1452) which acts as an inhibitor of the staphylococcal enoyl-acyl carrier protein reductase (FabI) enzyme.