The Apo E mimetics were developed through the intimate knowledge of the structure and function of the receptor and lipid binding domains of the apolipoproteins.
Scientists at the University of Alabama, Birmingham, designed and synthesized small peptides that incorporate the receptor binding (polar) and lipid binding (non-polar) domains of apolipoprotein E. The peptides insert into lipid rich lipoproteins and directs them to the receptors on the liver. The lipoproteins are then internalized and degraded through existing pathways, dramatically decreasing blood cholesterol levels.
The base peptide, AEM-28, is 28 amino acids in length, and inserts into LDL as well as VLDL remnants, clearing these cholesterol rich lipoproteins from the blood, even in the absence of the LDL receptor. Modification and derivatization of AEM-28 has resulted in the Chimeric Apo E Mimetic Peptide (CHAMP) technology, creating a suite of Apo E mimetic peptides with enhanced efficacy and diverse functionality.
LipimetiX filed new composition of matter patents for the CHAMP technology in 2014 and full US and PCT applications in 2015. The most potent CHAMP is AEM-28-14. The figures below display a dose response curve for the cholesterol lowering effect of a single injection of AEM-28-14 into Apo E null mice. These rapid and profound cholesterol reductions at a 50 ugdose (2 mg/kg) are unique and unprecedented.>> Learn more about atherosclerosis