Abstract
Debio 0123 is an investigational, orally bioavailable, highly selective, adenosine triphosphate (ATP)-competitive inhibitor of the WEE1 tyrosine kinase. WEE1 is a key regulator of cell cycle progression that influences entry into mitosis by modulating activity of cyclin-dependent kinase 1 (CDK1, also referred to as cell division cycle 2 [CDC2]). Inhibition of WEE1 presents an opportunity as a therapeutic strategy in cancer, either as monotherapy or in combination with other therapies1, by inducing a reduction of phosphorylated CDC2 (pCDC2) and driving cancer cells into mitotic catastrophe and apoptosis.
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