title: Comparison of peginterferon pharmacokinetic and pharmacodynamic profiles.
abstract: The pharmacokinetics and in dosing regimens of the currently available pegylated interferon (peginterferon) alfa molecules differ greatly, depending on the size and nature of their polyethylene glycol (PEG) moiety. Peginterferon alfa-2a has a branched 40 kDa PEG chain covalently attached to lysine residues and circulates as an intact molecule. On the other hand, peginterferon alfa-2b has a linear 12 kDa PEG chain covalently attached to interferon-a-2b via an unstable urethane bond that is hydrolysed after injection, releasing native interferon alfa-2b. The difference in pegylation between the two peginterferons has a significant impact on their pharmacokinetic properties. Data from comparative and non-comparative studies indicate that peginterferon alfa-2b has a shorter half-life in serum than peginterferon alfa-2a, and a significant proportion of patients receiving peginterferon alfa-2b may have trough concentrations below the limit of detection during the latter part of the 7-day dosing schedule. However, the pharmacodynamic parameters of the two drugs appear to be similar.
authors.affiliation: Department of Infectious Diseases, Foundation IRCCS Hospital San Matteo, University of Pavia, Pavia USC. Gastroenterologia, Ospedali Riuniti, Bergamo, Italy. raffaele.bruno@unipv.it
authors.forename: R
authors.initials: R
authors.lastname: Bruno
authors.forename: P
authors.initials: P
authors.lastname: Sacchi
authors.forename: S
authors.initials: S
authors.lastname: Cima
authors.forename: L
authors.initials: L
authors.lastname: Maiocchi
authors.forename: S
authors.initials: S
authors.lastname: Novati
authors.forename: G
authors.initials: G
authors.lastname: Filice
authors.forename: S
authors.initials: S
authors.lastname: Fagiuoli
mesh_terms: D000998:Antiviral Agents / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D004359:Drug Therapy, Combination; D006207:Half-Life; D016174:Hepacivirus / Q000187:drug effects*; D019698:Hepatitis C, Chronic / Q000188:drug therapy / Q000821:virology; D006801:Humans; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000627:therapeutic use*; D011092:Polyethylene Glycols / Q000493:pharmacokinetics* / Q000494:pharmacology / Q000627:therapeutic use*; D011994:Recombinant Proteins / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use; D012254:Ribavirin / Q000627:therapeutic use; D016896:Treatment Outcome
chemical_list: D000998:Antiviral Agents; D000077190:Interferon alpha-2; D016898:Interferon-alpha; D011994:Recombinant Proteins; D011092:Polyethylene Glycols; D012254:Ribavirin; C417083:peginterferon alfa-2b; C100416:peginterferon alfa-2a