title: Comparative pharmacokinetics of a tumour-targeting therapy candidate rh-IFNα2a-NGR with rh-IFNα2a administered intravenously in mice and rats.
abstract: OBJECTIVE
  rh-IFNα2a-NGR is a promising anti-tumor candidate. The aim of present study was to compare pharmacokinetics of rh-IFNα2a-NGR with rh-IFNα2a.
  
  
  METHODS
  Pharmacokinetics and elimination were investigated after intravenous administration to mice and rats. Compared tumor and tissue distribution profiles between rh-IFNα2a-NGR and rh-IFNα2a were illustrated in the tumor transplanted mice of SP2/0 myeloma. Double antibody sandwich ELISA method was used to assess the level of both rh-IFNα2a-NGR and rh-IFNα2a in serum, tissue, bile and urine.
  
  
  RESULTS
  After a single intravenous administration, the pharmacokinetic characters of rh-IFNα2a-NGR and rh-IFNα2a were described using a two-compartment model. No significant differences were observed between the two drugs in pharmacokinetic and elimination data. However, the concentration of rh-IFNα2a-NGR in tumor was 5.34 times and 1.52 times as high as that of rh-IFNα2a at 0.5 h (P < 0.01) and 1 h. In addition, immunohistochemical stain displayed rh-IFNα2a-NGR was predominantly located in tumor vascular tissues.
  
  
  CONCLUSIONS
  rh-IFNα2a-NGR could be an agent for tumor vascular-targeting therapy and these findings provided references for further clinical study.
authors.affiliation: Institute of Integrative Traditional & Western Medicine, Lanzhou University, Lanzhou, Gansu, China.
authors.forename: Xue-Xi
authors.initials: XX
authors.lastname: Wang
authors.forename: Li
authors.initials: L
authors.lastname: Lu
authors.forename: Chun-Li
authors.initials: CL
authors.lastname: Song
authors.forename: Wei-Na
authors.initials: WN
authors.lastname: Qian
authors.forename: Sheng-Yan
authors.initials: SY
authors.lastname: Zhang
authors.forename: Ying-Qi
authors.initials: YQ
authors.lastname: Zhang
authors.forename: Yong-Jie
authors.initials: YJ
authors.lastname: Wu
mesh_terms: D020533:Angiogenesis Inhibitors / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D000818:Animals; D001646:Bile / Q000378:metabolism; D016503:Drug Delivery Systems; D015507:Drugs, Investigational / Q000008:administration & dosage / Q000378:metabolism / Q000493:pharmacokinetics*; D006801:Humans; D007275:Injections, Intravenous; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000008:administration & dosage / Q000235:genetics / Q000378:metabolism / Q000493:pharmacokinetics*; D051379:Mice; D008815:Mice, Inbred Strains; D008954:Models, Biological; D009368:Neoplasm Transplantation; D009842:Oligopeptides / Q000008:administration & dosage / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D010954:Plasmacytoma / Q000098:blood supply / Q000378:metabolism* / Q000473:pathology; D011897:Random Allocation; D051381:Rats; D017207:Rats, Sprague-Dawley; D011993:Recombinant Fusion Proteins / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics* / Q000652:urine; D011994:Recombinant Proteins / Q000008:administration & dosage / Q000097:blood / Q000235:genetics / Q000378:metabolism / Q000493:pharmacokinetics / Q000652:urine; D014018:Tissue Distribution
chemical_list: D020533:Angiogenesis Inhibitors; D015507:Drugs, Investigational; D000077190:Interferon alpha-2; D016898:Interferon-alpha; C526428:NGR peptide; D009842:Oligopeptides; D011993:Recombinant Fusion Proteins; D011994:Recombinant Proteins