Non-viral vectorisation for the targeted delivery of therapeutic and diagnostic agents

Introduction

The technology offers the possibility to conjugate rapidly and efficiently molecules for disease/tissue/receptor targeting with therapeutic and/or diagnostic agents. More precisely, the technology is based on the use of a cyclopeptide scaffold that exposes two sides, which can be functionalised selectively. This feature opens up the possibility to link, in a structurally controlled manner, therapeutics and/or diagnostic agents to the appropriate targeting ligand. As part of this design, the platform contains multiple attachment points on each side. Multivalency benefits , e.g. clustering effects resulting from multiple ligand-receptor interactions, can therefore be thoroughly exploited as a result of this technology.

Highly encouraging results have already been obtained in vivo in the diagnosis and imaging of malignant tumours when molecules targeting tumour neo-angiogenesis together with molecules bearing imaging capabilities were conjugated to this scaffold. In addition, multivalency of the targeting ligand (RGD) was highly beneficial with regards to anti-angiogenic effect and significant reduction of tumour growth was observed.

It is believed that this multivalent type of interaction further increases cellular uptake of the conjugated drug, thereby enhancing its efficacy, whilst simultaneously minimising potential side effects. As the technology is based on a highly modular approach, we are seeking partners who are expert in the selective targeting of ligands or are able to provide promising contrast agents for imaging and/or diagnosis.