白蛋白结合修饰剂

 In pharmaceuticals, pharmacokinetics is one of the important factors for drug efficacy. Pharmacokinetics of drugs and contrast agents is optimized by introducing fatty acids and Diphenylcyclohexane derivatives which have affinity with human serum albumin. Recently, several insulin drugs having a regulated half-life in blood by modification with fatty acids such as myristic acid or palmitic acid have been developed and approved. These reagents are expected to be available for optimization of pharmacokinetics with peptides generally having a short half-life in blood.

Topics

• Diphenylcyclohexane Derivatives for Optimization of Pharmacokinetics in Blood

Related Categories

• Albumin Binding Agents
• Drug Delivery Systems (DDS)
• PEGylation

References

• Fatty acid binding to plasma albumin
  • A. A. Spector, J. Lipid Res. 1975, 16, 165.
• Soluble, fatty acid acylated insulins bind to albumin and show protracted action in pigs
  • J. Markussen, S. Havelund, P. Kurtzhals, A. S. Andersen, J. Halstrøm, E. Hasselager, U. D. Larsen, U. Ribel, L. Schäffer, K. VadI. Jonassen, Diabetologia 1996, 39, 281.
• Phosphate Ester Serum Albumin Affinity Tags Greatly Improve Peptide Half-Life In Vivo
  • K. Zobel, M. F. T. Koehler, M. H. Beresini, L. D. Caris, D. Comb, Bioorg. Med. Chem. Lett. 2003, 13, 1513.

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