Poster presented at the DDR Inhibitors Summit 2024 in Boston, USA
Luke Piggott, Noemie Luong, Frederic Massiere, Anne Bellon, Annett Kunze, Sandrine Micallef, Esteban Rodrigo Imedio
Debiopharm International SA, Chemin Messidor 5-7, CH-1002 Lausanne, Switzerland
Summary
Debio 0123 is an investigational, orally-available, selective ATP-competitive WEE1 inhibitor. Its main characteristics are an IC50 on WEE1 in the low nanomolar range, high selectivity, in particular lacking PLK1 and PLK2 inhibition, and good efficacy in animal models in several tumor types, as monotherapy or in combination with DNA damaging agents, such as etoposide and carboplatin.
Debio 0123 is currently being tested in two clinical studies, as monotherapy and in combination with carboplatin, in patients with advanced solid tumors. At the highest doses tested so far, a consistent pharmacodynamic effect on the downstream marker pCDC2 has been observed, suggesting target engagement.