SAR236553/REGN727 drug found to lower LDL-C levels

SAR236553/REGN727 is a fully human monoclonal antibody that acts by inhibiting PCSK9, a determinant of circulating low-density-lipoprotein cholesterol (LDL-C) levels in the blood, thereby increasing the number of free LDL receptors which can bind to circulating LDL-C and clear it from the bloodstream.

The double-blind placebo-controlled dose-finding study randomized 77 heFH patients to either placebo or one of four active dose regimens of 150mg at four-week intervals (Q4W), 200mg Q4W, 300mg Q4W, or 150mg at two-week intervals (Q2W) to evaluate the efficacy of various subcutaneous doses and dosing regimens of SAR236553/REGN727.

Patients receiving SAR236553/REGN727 for 12 weeks achieved a mean LDL-C reduction from baseline of 28.9% to 67.9%, compared to 10.7% in patients receiving placebo.

Metabolic and Atherosclerosis Research Center, US, director and principal investigator of the study Evan Stein said the data suggested that SAR236553/REGN727 may provide a new option to lower LDL-cholesterol and finally reach LDL-C goals for the difficult-to-treat patients.

Regeneron chief scientific officer and Regeneron Laboratories president George Yancopoulos said the data, along with recently presented data in patients with hypercholesterolemia, further support the company’s belief that blocking PCSK9 with its antibody has the potential to offer a mechanism for lowering LDL-cholesterol in a broad range of patients.

Based on discussions with the US and European regulatory authorities, the companies plan to begin a global Phase 3 program with SAR236553/REGN727 in June 2012.