Dr Timothy Yap speaks to ecancer about a first-in-human (FIH) phase 1 trial of the oral first-in-class covalent Werner helicase (WRN) inhibitor RO7589831 in patients with microsatellite instable (MSI) and/or mismatch repair deficient (dMMR) advanced solid tumours.

This trial introduces an oral covalent WRN inhibitor targeting advanced solid tumours.

WRN, a crucial helicase enzyme, is essential for DNA repair. Inhibiting WRN results in DNA damage and cell death.

The trial demonstrates early success with manageable side effects and effective absorption, leading to tumour shrinkage and disease stabilisation in MSI patients who have not responded to other treatments.

Ongoing efforts focus on optimising the dose for phase two.