Targeted drug delivery: a major challenge

A major challenge in the drug delivery field is to enhance transport of (bio)therapeutics across biological barriers. First and foremost the blood-brain barrier (BBB), composed of a unique highly selective vascular/endothelial system, remains a major hurdle for the development of Central Nervous System (CNS) drugs as it prevents the vast majority of (bio)therapeutics from penetrating into the nervous tissue. This leads to low efficacy and high attrition rates for CNS drug developers and remains a major industrial challenge of the 21st century.

Another challenge is to improve therapeutic or diagnostic benefits while minimizing both dose-levels and off-target effects of newly developed molecules. Growth drivers molecules for pharmaceutical industry such as theragnostic agents and ASOs can be trapped in liver and kidneys, which will hamper their distribution to intended cells and tissues. Targeted drug delivery to tissues of interest should enable administration of minimal drug doses with maximal treatment efficacy.

A solution: the VECTrans® Technology Platform

Vect-Horus has developed its “VECTrans®” breakthrough technology platform with the objective of making the ‘undruggable’ druggable by overcoming challenges of the BBB, and more generally biological barriers. VECTrans® is based on the specific design and optimization of ‘molecular vectors’ that, once conjugated to a payload, enable its delivery to target cells in the body. In other words, Vect-Horus’ core expertise relies on modifying pharmacokinetic (PK) and distribution profile of therapeutic or imaging candidates.

Specifically, the vectors developed by the Company target and take advantage of endogenous cell-surface receptors naturally involved in “Receptor-Mediated Transport” (RMT). This targeted delivery approach combines the advantages of not relying on invasive administration routes, and is believed to be the most effective and safest physiological pathway for the transport of macromolecules across cellular barriers.

The VECTrans® technology exploits specific receptors selected for their high uptake/endocytosis and constitutive recycling capacity, thereby allowing significant intracellular transport and accumulation of therapeutic or imaging agents. Once the vector moiety of a vector-payload complex is locked onto the appropriate receptor at the surface of BBB endothelial cells, cancer cells or any target cell type expressing such receptors, the vector-payload complex undergoes rapid internalisation and subsequent intra/transcellular trafficking. This ultimately leads to payload delivery into cells and across the BBB into the brain via transport and transcytosis processes respectively.

Thus, Vect-Horus’ VECTrans® technology enables the development of vector-therapeutic or -imaging agent complex for the diagnosis or treatment of CNS diseases, including neurodegenerative diseases, or pathological conditions, including genetic disorders or cancers.

IP & Publications

6 PATENT FAMILIES

3 international patent applications for vectors

  • Peptide derivatives and use thereof as carriers for molecules in the form of conjugates (Application WO 2010/046588).
  • Peptide derivatives, preparation thereof and uses thereof (Application WO 2011/131896).
  • Compositions and methods for drug delivery (Application WO 2014/060601).

1 international patent application for a vectorised neuroprotective agent

  • Activated neurotensin molecules and the uses thereof (Application WO 2015/107182).

1 international patent application for uses of vectors in cancer imaging and radiotherapy

  • Compositions and methods for cancer imaging and radiotherapy (Application WO 2018/138372).

1 international patent applications for new vectors

  • Receptor-binding molecules, conjugates thereof and their uses (Application WO2020)

REVIEWS AND SCIENTIFIC PUBLICATIONS