Peptides Fatty Acids Conjugation

To improve peptide pharmacokinetics, conjugating the peptide to lipids is a favored approach. Peptides-Fatty acids conjugation is obtained by fatty acid modification of the main chain structure or contralateral chain group of polypeptide drugs. Type of fatty acid includes: Caprylic acid (C8), Capric acid (C10), Lauric acid (C12), Myristic acid (C14), Palmitic acid (C16) or Stearic acid (C18) etc. Peptides-Fatty acids conjugation drugs can improve the liposolubility, intestinal mucosal permeability and absorption efficiency. It prolongs the half-life in the circulation significantly. Fatty acid conjugated peptides can also be used for a number of different applications, for example, Detemir (Levemir) is a new insulin analogue developed by Northrop. After the removal of human insulin B30 Thr, a myristic acid side chain was attached to B29 Lys, which could release the drug slowly and achieve the effect of long-term hypoglycemia.