Enhancement of Oral Drug Absorption - Effect of Lipid and Glycoside Conjugation on the Enzymatic Stability and Intestinal Permeability of IM862

摘要

The dipeptide L-Glu-L-Trp-OH, also known as IM862 or Thymogen~R, is a naturally occurring thymic dipeptide which has been shown to possess immuno-modulating and anti-angiogenic properties [1] and is currently under development for potential treatments of certain cancers and immuno-deficiency disorders. Its intranasal administration in a clinical trial for the treatment of AIDS-related Kaposi's sarcoma showed a large volume of distribution and high bioavailability (71%) [2]. However, due to its highly hydrophilic character, IM862 demonstrates low permeability across the gastro-intestinal track, which makes it not orally available.