Kang Choon Lee
SungKyunKwan University, South Korea
Title: Smart high molecular PEGylated exendin-4 as a noble long-acting type 2 diabetic therapy
Biography
Biography: Kang Choon Lee
Abstract
Exendin-4, a GLP-1 receptor agonists is viewed as potent therapeutic peptide for type 2 diabetes. Yet due to the short circulating half-life, high doses of the drug must be administered frequently which gives rise to concentration-dependent adverse effects. The high molecular PEGylated Exendin-4 was created by site specifically attaching a novel polyethylene glycol (PEG) molecule to Exendin-4. The PK in rats, dogs and monkeys and the PD in diabetic mice models are compared. Unlike existing PEGylation technology or other half-life extension technologies that often significantly reduce the biological activities of peptide drugs, modification of Exendin-4 with smart PEGylation approach enables a very long biological half-life (t1/2: 88 hr in cynomolgus monkeys) combined with retention of Exendin-4’s potency, resulting in a long duration of action with potentially reduced adverse effects in humans. In turn, this can lead to weekly and monthly dosing frequencies with low adverse effects and overall provide higher patient compliance.
