title: Pharmacokinetic analysis after implantation of everolimus-eluting self-expanding stents in the peripheral vasculature.
abstract: BACKGROUND
  A novel self-expanding drug-eluting stent was designed to release everolimus 225 μg/cm(2) to prevent restenosis following peripheral arterial intervention. The purpose of this study was to measure the pharmacokinetic profile of everolimus following stent implantation.
  
  
  METHODS
  One hundred four patients with symptomatic peripheral arterial disease underwent implantation of everolimus-eluting stents in the femoropopliteal arteries. In a prespecified subset of 26 patients, blood samples for assay of everolimus content were collected prior to stent implantation, at 1, 4, and 8 hours postprocedure, prior to discharge, and at 1 month postprocedure.
  
  
  RESULTS
  A total of 39 stents, ranging from 28 mm to 100 mm in length, were implanted in 26 patients, resulting in a total delivered everolimus dose range of 3.0 to 7.6 mg. Following the procedure, the maximum observed everolimus blood concentrations (C(max)) varied from 1.83 ± 0.05 ng/mL after implantation of a single 80-mm stent to 4.66 ± 1.78 ng/mL after implantation of two 100-mm stents. The mean time to peak concentration (T(max)) varied from 6.8 hours to 35 hours. The pharmacokinetics of everolimus were dose-proportional in that dose-normalized C(max) and area under the curve values were constant over the studied dose range.
  
  
  CONCLUSIONS
  After implantation of everolimus-eluting self-expanding stents in the femoropopliteal arteries, systemic blood concentrations of everolimus are predictable and considerably lower than blood concentrations observed following safe oral administration of everolimus.
authors: Department of Cardiovascular and Interventional Radiology, Medical University, Vienna, Austria.
authors: Johannes
authors: J
authors: Lammer
authors: Dierk
authors: D
authors: Scheinert
authors: Frank
authors: F
authors: Vermassen
authors: Renate
authors: R
authors: Koppensteiner
authors: Klaus A
authors: KA
authors: Hausegger
authors: Herman
authors: H
authors: Schroë
authors: Rajeev M
authors: RM
authors: Menon
authors: Lewis B
authors: LB
authors: Schwartz
mesh_terms: D000368:Aged; D002317:Cardiovascular Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D003251:Constriction, Pathologic; D054855:Drug-Eluting Stents; D057510:Endovascular Procedures / Q000295:instrumentation*; D005060:Europe; D000068338:Everolimus; D005260:Female; D005263:Femoral Artery; D006801:Humans; D008297:Male; D008875:Middle Aged; D058729:Peripheral Arterial Disease / Q000628:therapy*; D011150:Popliteal Artery; D011446:Prospective Studies; D011474:Prosthesis Design; D012008:Recurrence; D020123:Sirolimus / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D016896:Treatment Outcome
chemical_list: D002317:Cardiovascular Agents; D000068338:Everolimus; D020123:Sirolimus