Aprea Therapeutics, Inc. announced that the U.S. Food and Drug Administration has cleared its Investigational New Drug (IND) application (IND 169359) for APR-1051. Based on preclinical studies, APR-1051 is differentiated from other WEE1 inhibitors in its: Molecular structure; No head-to-head studies have been conducted with APR-1051. Based on preclinical studies, APR-1051 is differentiated from other WEE1 inhibitors in its: Molecular structure; Selectivity for WEE1 versus off-target inhibition of the polo-like kinase, or PLK, family of kinases; Potentially superior pharmacokinetic (PK) properties; Potential absence of QT prolongation at doses that significantly inhibit WEE1 APR-1051 was discovered and preclinically evaluated by Aprea?s team of chemists and scientists.

Aprea has conducted extensive pre-clinical studies with APR-1051, which have demonstrated that the molecule has potent anti-tumor activity, along with a favorable pharmacokinetic (PK) profile. Additionally, pre-clinical data show that APR-1051 may demonstrate less toxicity than other WEE1 inhibitors. Clearance of the IND application will allow Aprea to initiate the Phase 1 ACESOT-1051 dose escalation trial to evaluate the safety, tolerability, and preliminary efficacy of APR-1051.

Enrollment of the first patient in this study is expected in the first half of 2024 with an update expected in the fourth quarter of the year.