Introducing the first polymer-free leflunomide eluting stent

Deuse, T.; Erben, Reinhold G.; Ikeno, Fumiaki; Behnisch, Boris; Böeger, Rainer; Connolly, Andrew J.; Reichenspurner, Hermann; Bergow, Claudia; Pelletier, Marc; Robbins, Robert C.; Schrepfer, Sonja

doi:10.1016/j.atherosclerosis.2007.12.055

Cited by 19 publications

(7 citation statements)

References 43 publications

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“…Another drug that has been used in a polymer-free stent is the prodrug leflunomide, which has a long half-life of several days. The active metabolite teriflunomide inhibits de novo pyrimidine biosynthesis which is a critical process in rapidly dividing cells such as T-leukocytes, while other anti-inflammaotry and antiproliferative effects have also been ascribed to this inhibitor. Promising in vivo results have been reported for leflunomide-eluting DES such as a significant reduction in neointimal area and stent thickness ratios …”

Section: Drugsmentioning

confidence: 99%

“…Many drugs have been incorporated in the Yukon stent and they all have similar elution rates. In a test comparing a Yukon stent loaded with either sirolimus or leflunomide, interchangeable elution rates were found in vitro …”

Section: Drug Release Kinetics From Stentsmentioning

confidence: 99%

“…Promising in vivo results have been reported for leflunomide-eluting DES such as a significant reduction in neointimal area and stent thickness ratios. 47…”

Section: ■ Coating Technologiesmentioning

confidence: 99%

“…In a test comparing a Yukon stent loaded with either sirolimus or leflunomide, interchangeable elution rates were found in vitro. 47 According to the in vitro release experiment of Mani et al, flufenamic acid was released from the SAMs in a sustained pattern for 2 weeks up to 1 month. 40,82 Approximately 80% of the flufenamic acid was released after 4 weeks, and the release behavior was governed, as assumed by the authors, by the hydrolysis of the ester bond between flufenamic acid and SAM.…”

Section: ■ Drug Release Kinetics From Stentsmentioning

confidence: 99%

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Polymer-Free Drug-Eluting Stents: An Overview of Coating Strategies and Comparison with Polymer-Coated Drug-Eluting Stents

et al. 2015

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Clinical evaluations have proven the efficacy of drug-elution stents (DES) in reduction of in-stent restenosis rates as compared to drug-free bare metal stents (BMS). Typically, DES are metal stents that are covered with a polymer film loaded with anti-inflammatory or antiproliferative drugs that are released in a sustained manner. However, although favorable effects of the released drugs have been observed, the polymer coating as such has been associated with several adverse clinical effects, such as late stent thrombosis. Elimination of the polymeric carrier of DES may therefore potentially lead to safer DES. Several technologies have been developed to design polymer-free DES, such as the use of microporous stents and inorganic coatings that can be drug loaded. Several drugs, including sirolimus, tacrolimus, paclitaxel, and probucol have been used in the design of carrier-free stents. Due to the function of the polymeric coating to control the release kinetics of a drug, polymer-free stents are expected to have a faster drug elution rate, which may affect the therapeutic efficacy. However, several polymer-free stents have shown similar efficacy and safety as the first-generation DES, although the superiority of polymer-free DES has not been established in clinical trials.

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Section: Drugsmentioning

confidence: 99%

Section: Drug Release Kinetics From Stentsmentioning

confidence: 99%

“…Promising in vivo results have been reported for leflunomide-eluting DES such as a significant reduction in neointimal area and stent thickness ratios. 47…”

Section: ■ Coating Technologiesmentioning

confidence: 99%

Section: ■ Drug Release Kinetics From Stentsmentioning

confidence: 99%

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Polymer-Free Drug-Eluting Stents: An Overview of Coating Strategies and Comparison with Polymer-Coated Drug-Eluting Stents

et al. 2015

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“…The polymer and its degraded products may influence intimal regeneration and neo-endothelial cell function. A polymer-free leflunomide-eluting stent was developed, and its efficacy was demonstrated in an animal model [31•].…”

Section: New Stents and The Futurementioning

confidence: 99%

Angioscopic Evaluation of Neointimal Coverage of Coronary Stents

Uchida¹,

Uchida

2010

Curr Cardiovasc Imaging Rep

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Drug-eluting stents (DES) reduce coronary restenosis significantly; however, late stent thrombosis (LST) occurs, which requires long-term antiplatelet therapy. Angioscopic grading of neointimal coverage of coronary stent struts was established, and it was revealed that neointimal formation is incomplete and prevalence of LST is higher in DES when compared to bare-metal stents. It was also observed that the neointima is thicker and LST is less frequent in paclitaxel-eluting and zotarolimus-eluting stents than in sirolimus-eluting stents. Many new stents were devised and they are now under experimental or clinical investigations to overcome the shortcomings of the stents that have been employed clinically. Endothelial cells are highly anti-thrombotic. Neo-endothelial cell damage is considered to be caused by friction between the cells and stent struts due to the thin neointima between them which might act as a cushion. Therefore, development of a DES that causes an appropriate thickness (around 100 μm) of the neointima is a potential option with which to prevent neo-endothelial cell damage and consequent LST while preventing restenosis.

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