Dr. Jean-Claude Bertrand, Associate Professor of Medicine/Medicinal Chemistry, Royal Victoria Hospital/McGill University Health Centre, Montreal, Quebec

Project Title: “Brain penetrability and in vivo potency of novel multi-targeted combi-drugs”

Research Summary

Glioblastoma multiforme (GBM) is the most aggressive form of primary brain tumours. Forty to fifty percent of primary central nervous system tumours are gliomas and, of these, 50% are GBMs. Grade IV gliomas grow rapidly, invading the brain causing death within 3 months if no appropriate treatment is administered. In order to induce significant cell killing in these aggressive tumours, drugs capable of blocking targets are required. Our laboratory has now designed and synthesized such type of drugs directed at proteins termed EGFR, EGFRvIII, Src that drive tumour progression and reduce tumour sensitivity to chemotherapeutic drugs.

In order to block the progression of these aggressive tumours, novel type of multitargeted molecules are urgently needed. Our laboratory has now designed and synthesize such type of molecules termed “combi-molecules”. The purpose of this proposal is to study their ability to penetrate into the brain and to strike the tumours at multiple targets (e.g. EGFR, EGFRvIII, Src) that shield them against the effects of chemotherapeutic drugs.