Targeted Synergy

Targeted Synergy has the potential to enhance therapeutic index, which is one of the most important challenges to the successful development of an oncology drug. First, Targeted Synergy drugs are active only in the hypoxic regions of tumours, increasing efficacy without undesired side effects on normal tissues. Second, Targeted Synergy drugs are more active than conventional agents because they combine the induction of DNA damage with the inhibition of DNA repair by cancer cells. Together, these properties make Targeted Synergy a ‘next-generation’ approach for the development of safe yet powerful anti-cancer drugs.

The diagram below describes the concepts behind Targeted Synergy.  The solid tumour (red) contains regions of hypoxia (blue).  Targeted Synergy inhibitors exploit the hypoxic regions of solid tumours by delivering two separate and synergistic activities with a single drug molecule: 1, hypoxia induced DNA damage and 2, inhibition of DNA repair (shown in the inset).

The Sentinel drug molecule (blue sphere) is a single entity that has been engineered to have dual activity; inhibition of DNA repair and hypoxia induced DNA damage.  

Our approach is differentiated from others by delivering two separate activities through the action of one drug molecule.  We have a well developed Targeted Synergy pipeline, with proof of concept achieved for two well validated DNA repair enzymes, Poly (ADP-ribose) Polymerase 1 (PARP1) & Checkpoint Kinase 1 (Chk1).

For more information please contact us.