Acrivon Therapeutics, Inc. announced a novel, internally developed clinical candidate, ACR-2316, a dual WEE1 and PKMYT1 inhibitor. The company plans to prioritize Investigational New Drug (IND) enabling studies for ACR-2316 to be ready for IND submission by the fourth quarter of 2024. Based on the emerging favorable preclinical profile of ACR-2316, the company has entered into IND-enabling studies.

The compound is designed for high selectivity towards WEE1 and PKMYT1, exhibiting single-digit nM IC50 potency in a carefully predetermined ratio to ensure strong single agent anti-tumor activity, as demonstrated in tumor-bearing rodent models and other preclinical analyses. Using AP3 for unbiased quantitative high-resolution measurement of the effects of ACR-2316 on the human tumor cell phosphoproteome, this compound has been further optimized for potent induction of mitotic catastrophe, which is key to its strong single agent activity in preclinical models and potentially favorable clinical profile for monotherapy development.