Metformin DR (metformin delayed-release) is Elcelyx’s lead product candidate, currently in Phase 2b development as a potential agent uniquely suited for patients who cannot currently use metformin owing to contraindications or poor tolerability.
Elcelyx retains full worldwide rights to the Metformin DR program.
About Metformin DR
Metformin DR (a delayed-release formulation of metformin) has been designed to release metformin primarily in the distal small intestine and restrict metformin to the bowel, in contrast to currently available metformin products that target high systemic exposure. Metformin DR development is based in the recent findings that metformin exerts its glucose lowering activity principally by action at the intestinal L cell, rather than via systemic exposure as had been previously thought. This is consistent with the L cell being the primary source of several glucose-regulating and satiety-regulating hormones including glucagon-like peptide-1 (GLP-1) and peptide YY (PYY).
Metformin DR uses an enteric-coating technology to accomplish once-daily, targeted delivery to the region of the gut where the density of L cells is high. Delaying release of metformin to the distal intestine reduces bioavailability while still achieving efficacy. Metformin DR once-daily administration in patients with type 2 diabetes resulted in comparable glucose lowering to Metformin XR with a 40% lower dose and substantially lower systemic exposure. This reduction in systemic exposure may allow for metformin use in type 2 diabetes patients with moderate to severe renal impairment, a population that is presently contraindicated for metformin use. Because metformin is not “wasted” to the circulation, lower doses can be used and bypassing the upper GI should lead to improved tolerability, without the need for dose titration upon initiation of therapy.