Technology Overview

CCT289346 is a highly potent, selective and orally bioavailable inhibitor of spindle assembly checkpoint kinase MPS1. Discovered by scientists at The Institute of Cancer Research, London, it has shown promising early results in a phase I trial.

MPS1 is a key component of the spindle assembly checkpoint (SAC), which ensures proper segregation of the chromosomes during mitosis. Pre-clinical studies led by ICR researchers have shown that inhibition of MPS1 triggers mitosis in tumour cells before the chromosomes are properly aligned along the cellular spindles, leading to gross chromosomal segregation defects.

In combination with the chemotherapy paclitaxel, which has a synergistic mechanism of action, ICR researchers showed that CCT289346 causes robust tumour regression in human xenograft models of triple