lunresertib + Debio 0123

The combination of **lunresertib** and **Debio 0123** represents a first-in-class, dual targeted therapy researched for the treatment of solid tumors. Lunresertib is a selective, potent, orally bioavailable small molecule inhibitor of PKMYT1, which regulates the cell cycle by phosphorylating CDK1 at threonine 14. Debio 0123 is an orally bioavailable, brain-penetrant, highly selective inhibitor of WEE1 kinase, which also regulates CDK1 by phosphorylating it at tyrosine 15. Simultaneous inhibition of PKMYT1 and WEE1 cripples the cell’s checkpoint control mechanisms, promotes uncontrolled cell cycle progression, accumulation of DNA damage, mitotic catastrophe, and apoptosis of cancer cells. The combination is being studied in a Phase 1/1b arm (MYTHIC trial, NCT04855656) with the goal of leveraging the synthetic lethality and synergistic anti-tumor effects observed in preclinical models, particularly in ovarian and breast cancer. Lunresertib was developed by Repare Therapeutics and Debio 0123 by Debiopharm, both clinical-stage precision oncology companies focused on targeted therapies for cancer patients with high unmet need[1][3][5][9][10].

Other names

RP-6306 + Debio0123lunresertib + Debio0123