Peramivir (DB06614): A Comprehensive Pharmacological and Clinical Monograph

Executive Summary

Peramivir is a potent, intravenously administered antiviral agent belonging to the neuraminidase inhibitor class, developed for the treatment of acute uncomplicated influenza caused by influenza A and B viruses. As a small molecule drug, it functions as a transition-state analogue, selectively binding to and inhibiting the viral neuraminidase enzyme. This action is critical, as it prevents the cleavage of sialic acid residues on the surface of infected host cells, thereby blocking the release and subsequent spread of newly formed progeny virions. This mechanism of action effectively halts the progression of the infection within the host.

The pharmacological profile of Peramivir is distinguished by its unique pharmacokinetic properties. Administered as a single intravenous infusion, it achieves 100% bioavailability. It exhibits a long terminal elimination half-life of approximately 20 hours in individuals with normal renal function, low plasma protein binding of less than 30%, and a limited volume of distribution. Critically, Peramivir undergoes minimal hepatic metabolism and is primarily eliminated from the body via the kidneys, with approximately 90% of the dose excreted unchanged in the urine. This profile minimizes the potential for metabolic drug-drug interactions but renders the drug's clearance highly dependent on renal function. Consequently, precise, tiered dosage adjustments are mandatory for patients with any degree of renal impairment to prevent drug accumulation and potential toxicity.