Our proprietary Esterase Sensitive Motif™ (ESM™) platform is a unique and validated technology platform for delivering active drugs into macrophages with exquisite specificity resulting in better pharmacology, efficacy and safety for best-in-class drugs against validated targets and biology as well as novel, first-in-class targets.
The technology is based on the utility of a drug-amino acid ester conjugate that is selectively hydrolysed by human carboxylesterase-1 (hCE-1) leading accumulation of charged, pharmacologically active drug within the myelomonocytic cells; monocytes, macrophages and dendritic cells expressing hCE-1.
The benefits of selective drug accumulation in macrophages include:
- Improved levels of potency
- Longer duration of action resulting from the increased cell residence time of the active drug.
Importantly the pharmacodynamic effect of the active drug is observed only in hCE-1 positive cells, while the function of other important immune cells such as lymphocytes and granulocytes as well as epithelial and stromal cell etc are spared by the macrophage selective delivery of ESM™ molecules. Accordingly, maximal efficacy is observed in the absence of systemic drug providing improved PK/PD relationships and tolerability compared to conventional small molecules.