Cilastatin is a specific inhibitor of the renal enzyme dehydropeptidase-I and is widely used in pharmaceutical formulations to prevent the degradation of certain β-lactam antibiotics. It is most commonly combined with imipenem to protect the antibiotic from enzymatic hydrolysis in the kidneys. Cilastatin itself has no antibacterial activity but enhances the therapeutic effectiveness of imipenem. It improves the stability and bioavailability of the drug during systemic circulation. Cilastatin is well characterized chemically and pharmacologically. It is routinely analyzed in quality control laboratories to ensure product safety and efficacy. Accurate analytical methods are essential for its determination. Chromatographic techniques are commonly employed for its analysis. Reference standards of cilastatin support method development and validation. Overall, cilastatin plays a critical role in both clinical therapy and pharmaceutical analysis.
