PC-DAC™:Exendin-4

PC-DAC™:Exendin-4 (CJC-1134-PC)

Current approaches in the treatment of type 2 diabetes focus on alleviating the target tissue deficiencies. Treatments can reduce hepatic glucose production, increase peripheral insulin sensitivity, or enhance insulin secretion. Most patients with type 2 diabetes require some combination of treatments, and ultimately might need to include insulin as part of their regimen. Exendin-4 is a glucagon-like peptide-1 (GLP-1) homolog and an agonist for the GLP-1 receptor. It lowers the blood glucose levels through a distinct mechanism complementary to the mechanisms of action of currently available anti-diabetic drugs. By decreasing glucagon and increasing insulin secretion in a glucose-dependent manner, Exendin-4 may stimulate β-cell proliferation, restore β-cell sensitivity to glucose, delay gastric emptying, and increase peripheral sensitivity to glucose. Despite these effects, the clinical application of Exendin-4 is limited by its relatively short half-life in plasma (<1 hour). CJC-1134-PC, the modified Exendin-4 analogue conjugated to recombinant human albumin, is based on ConjuChem's PC-DACTM technology. This preformed conjugate, besides having a much longer half-life than its natural counterpart is only slightly less potent. Based on the combined preclinical data, ConjuChem has moved forward with the development of CJC-1134-PC for the treatment of type 2 diabetes. Data from a phase I/II single escalating dose clinical study demonstrated an excellent tolerability profile and positive efficacy on glucose reduction supporting once-a-week dosing. The product is a highly soluble small volume liquid formulation injected subcutaneously utilizing a very small gauge (29 to 31) needle.