Debio 0123, a highly selective WEE1 inhibitor, combined with carboplatin and etoposide in patients with small cell lung cancer that progressed after platinum-based therapy: a phase 1 dose escalation and expansion study

Valentina Gambardella1, Alejandro Navarro2*, Jose Maria Lopez-Picazo3, Prantesh Jain4, Gonzalo Fernandez5, Maria de Miguel6, Jon Zugazagoitia7, Sirish Gadgeel8, Sajjad Bhatti9, Anna Vilalta Lacarra3, Eduardo Castanon5, Pedro Rocha2, Sandrine Micallef10, Rikke Frederiksen10, Luke Piggott10, Anne Bellon10,Esteban Rodrigo Imedio10, Luis Paz-Ares7

1  Hospital Clinico Universitario de Valencia, Valencia, Spain
2 Hospital Universitario Vall d’Hebron, Barcelona, Spain
3 Clinica Universidad de Navarra, Pamplona, Spain
4 Roswell Park Cancer Institute, Buffalo, Cancer Institute, Buffalo, NY, USA
5 Clinica Universidad de Navarra, Madrid, Spain
6 Hospital Universitario HM Sanchinarro, Madrid, Spain
7 Hospital Universitario 12 de Octubre, Madrid, Spain
8 Henry Ford Health System, Detroit, MI, USA
9 University of Arkansas for Medical Sciences, Little Rock, AR, USA
10 Debiopharm International SA, Chemin Messidor 5-7, CP 435, 1001 Lausanne, Switzerland

*Affiliation at the time of start of the study

Background

Debio 0123 is an oral, brain-penetrant, highly selective WEE1 inhibitor. WEE1 inhibition leads to S phase and G2/M cell cycle abrogation, allowing mitosis without DNA repair, leading to mitotic catastrophe and cell death. Debio 0123 is in clinical development, as monotherapy or in combination, in solid tumors, and has shown manageable safety profile with early signals of antitumor activity. SCLC is an aggressive disease with poor prognosis carrying a high mutational burden and genomic instability. Preclinically, Debio 0123 has shown to significantly improve antitumor activity of CP and ETOP, in SCLC models. These data support clinical investigation of Debio 0123 combined with CP and ETOP in SCLC.