Relebactam is a chemical compound used in combination with antibiotics to improve their efficacy. As a beta-lactamase inhibitor, it blocks the ability of bacteria to break down a beta-lactam antibiotic. Relebactam is a diazabicyclooctane non beta-lactam beta-lactamase inhibitor that selectively inhibits class A and class C serine beta-lactamases, thereby restoring the activity of susceptible carbapenem agents such as imipenem; it has minimal intrinsic antibacterial activity, is formulated for intravenous administration, undergoes primarily renal elimination so dose adjustment is required in renal impairment, and in the United States, relebactam is approved for use in combination with imipenem and cilastatin for certain complicated Gram negative infections and is supplied as part of that fixed combination product.
Parent: Relebactam
Typical quality specifications applied by manufacturers and pharmacopeial monographs for relebactam API include an assay of not less than 98.0 percent by HPLC, limits for individual related compounds commonly set at not more than 0.10 percent w by w, and a limit for total related compounds commonly set at not more than 0.50 percent w by w; the reporting threshold for unspecified impurities follows ICH guidance and is typically 0.05 percent, known degradants such as deacylated or oxidized derivatives are controlled as individual impurities, residual solvents are controlled in accordance with ICH Q3C, water content is monitored and commonly limited to around 2.0 percent, and elemental impurities and microbial limits are set per applicable regulatory guidance and the certificate of analysis for each batch.
Relebactam binds to the active site of serine beta-lactamases, particularly class A and class C enzymes, forming a stable inhibitory complex that prevents enzymatic hydrolysis of a coadministered beta-lactam antibiotic; by protecting the antibiotic from degradation, relebactam restores or enhances the antibiotic’s bactericidal activity against susceptible Gram negative pathogens and it has negligible direct antibacterial effect on its own.
Relebactam is not marketed as a single agent under a separate retail brand; it is available clinically only as a component of a fixed combination product with imipenem and cilastatin.
The combination product contains imipenem, a broad spectrum carbapenem antibiotic; cilastatin, an inhibitor of renal dehydropeptidase that prevents imipenem degradation in the kidney; and relebactam, a beta-lactamase inhibitor that protects imipenem from bacterial beta-lactamases; together the three components extend the effective spectrum of imipenem against certain resistant Gram negative organisms and are administered intravenously for serious infections where indicated.
The marketed brand name for the fixed combination of imipenem, cilastatin, and relebactam is Recarbrio.
