Twenty-eight-day efficacy and phamacokinetics of the sirolimus-eluting stent

Coron Artery Dis. 2002 May;13(3):183-8. doi: 10.1097/00019501-200205000-00008.

Abstract

Background: In-stent restenosis is caused by neointimal hyperplasia. Sirolimus (rapamycin; Wyeth Research, Radnor, Pennsylvania, USA) inhibits vascular smooth muscle cell proliferation and we evaluated the efficacy of sirolimus in reducing neointimal formation in a rabbit iliac model and in-vivo pharmacokinetics in the porcine coronary model.

Design: Randomized, blinded, prospective animal study.

Methods: Bilateral rabbit iliac artery stent implantation was performed using crossflex stents (Cordis Corporation, Warren, New Jersey, USA) coated with sirolimus incorporated in a nonerodable polymer. Arteries were randomized to one of four stent groups: uncoated stents (n = 8); polymer control stents (n = 10); low-dose sirolimus-eluting stents (n = 9); and high-dose sirolimus-eluting stents (n = 10). Histomorphometry was performed at 28 days. Arterial tissue and stents were retrieved at 8, 14 and 28 days and blood samples were obtained daily during the first week.

Results: Treatment with low-dose sirolimus was associated with a 23% (P = NS) reduction in neointimal area and treatment with high-dose sirolimus with a 45% (P < 0.05) reduction. Sustained drug release from the stent and prolonged intramural arterial deposition were confirmed for up to 28 days. No detectable sirolimus was found in the blood after 2 days.

Conclusion: Controlled-release local delivery of a cell-cycle inhibitor from a nonerodable polymer-coated stent reduced neointimal formation in rabbit iliac arteries in a dose-dependent manner and represents a promising strategy for preventing restenosis.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Vessel Prosthesis Implantation
  • Coated Materials, Biocompatible
  • Coronary Artery Disease / complications
  • Coronary Artery Disease / drug therapy
  • Coronary Artery Disease / surgery
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Evaluation
  • Graft Occlusion, Vascular / etiology
  • Immunosuppressive Agents / pharmacokinetics*
  • Immunosuppressive Agents / therapeutic use*
  • Models, Cardiovascular
  • Prospective Studies
  • Rabbits
  • Randomized Controlled Trials as Topic
  • Severity of Illness Index
  • Sirolimus / pharmacokinetics*
  • Sirolimus / therapeutic use*
  • Stents*
  • Time Factors
  • Treatment Outcome

Substances

  • Coated Materials, Biocompatible
  • Immunosuppressive Agents
  • Sirolimus