Pharmacokinetic Study of Sirolimus-Eluting BioResorbable Vascular Scaffold System for Treatment of De Novo Native Coronary Lesions: A Sub-Study of MeRes-1 Trial

Abstract

Background: MeRes100™ (Meril Life Sciences Pvt. Ltd., Vapi, India) is a novel sirolimus-eluting bioresorbable vascular scaffold (BRS). The purpose of this sub-study of MeRes-1 trial is to evaluate the systemic release of sirolimus from MeRes100 BRS implanted for the treatment of de novo native coronary artery lesions. Methods: The MeRes-1 is a prospective, multicenter, first-in-human trial of sirolimus-eluting MeRes100 BRS. The pharmacokinetic sub-study was conducted at two Indian sites in 10 patients who were implanted with the MeRes100 BRS loaded with sirolimus at a dose of 1.25 µg/mm2. Venous blood samples were collected at pre-dose and 12-time points after implantation of the scaffold. Sirolimus concentration was successively analyzed using ultra-performance liquid chromatography-electrospray ionization tandem mass spectrometry method. Results: A total of 12 scaffolds were implanted in 10 patients. Non-compartmental analysis demonstrated time to reach peak concentration of sirolimus between 0.5 h to 3 h after scaffold implantation. The peak concentration (Cmax) was deduced to be 7.47 ± 2.61 ng/mL, AUC was 436.45 ± 171.24 hng/mL, and the t½ was observed at 98.59 ± 33.58 h. The clearance was 0.66 ± 0.16 L/h and lower limit of quantification was detectable at 14.1 days. Conclusions: The MeRes-1 pharmacokinetic sub-study confirmed that MeRes100 BRS is safe and tolerable at limited systemic exposure of sirolimus.