HESylation - Introduction
Innovative formulation and drug delivery play a crucial part in optimising drug characteristics, such as pharmacodynamics, side effect profiles or water solubility. However, there is an increasing medical need to improve drug characteristics further – for existing therapeutics as well as for new pharmaceuticals.
Fresenius Kabi has developed a new drug delivery technology with superior properties: the HESylation technology. HESylation utilises hydroxyethyl starch (“HES”) derivatives linked to drug substances in order to modify the drug characteristics. This modification enables the prolongation of the circulation half-life by increasing the stability of the molecule, as well as by reducing renal clearance, resulting in an increased biological activity. Furthermore, HESylation potentially alters the immunogenicity or allergenicity. By varying different parameters, such as the molecular weight of HES, a wide range of HES drug conjugates can be customized.
HESylation is based on the extensive expertise in the field of hydroxyethyl starch (“HES”) that Fresenius Kabi has gathered as the world’s largest producer of HES. HES is a modified natural polymer derived from waxy maize starch and can be metabolized by the body’s enzymes. HES solutions are usually administered to substitute deficient blood volume and to improve the rheological properties of the blood.
At present, the most important application for HESylation is in the area of biopharmaceuticals, i.e. to address protein drug delivery issues. However, there is a strong potential for HESylation to improve the profile of other classes of therapeutics, e.g. small molecule drugs.
Fresenius Kabi has a broad portfolio of patents and patent applications covering coupling chemistry, special linkers and HESylated drugs on a target-by-target basis.