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Aprea Therapeutics Announces First Patient Dosed in ACESOT-1051 Phase 1 Trial Evaluating Oral WEE1 Inhibitor APR-1051
APR-1051 is a highly selective and potentially best-in-class oral WEE1 inhibitor Phase 1 ACESOT-1051 clinical trial is evaluating APR-1051 as monotherapy
About this update from Aprea Therapeutics, Inc.
[{"type":"text","content":"APR-1051 is a highly selective and potentially best-in-class oral WEE1 inhibitor Phase 1 ACESOT-1051 clinical trial is evaluating APR-1051 as monotherapy treatment in patients with significant unmet medical need Dosing of the first patient in the ACESOT-1051 study represents a key advancement in Aprea’s clinical pipeline DOYLESTOWN, Pa., June 17, 2024 (GLOBE NEWSWIRE) -- Aprea Therapeutics, Inc. (Nasdaq: APRE) (“Aprea”, or the “Company”), a clinical-stage biopharmaceutical company focused on precision oncology through synthetic lethality, today announced that the first patient has been dosed in the ACESOT-1051 Phase 1 study evaluating daily oral WEE1 inhibitor APR-1051 as monotherapy in advanced solid tumor patients with unmet medical need. APR-1051 was discovered and preclinically evaluated by Aprea’s team of chemists and scientists. APR-1051 is a potent and highly selective small molecule designed to limit off-target toxicity that may provide good safety and tolerability and has shown a potentially favorable drug exposure in pre-clinical models. APR-1051 targets WEE1 kinase, an enzyme involved in the DNA damage response pathway. Based on preclinical studies, we believe APR-1051 may solve liabilities associated with other WEE1 inhibitors and is differentiated based on: 1) molecular structure; 2) selectivity for WEE1 versus off-target inhibition of the polo-like kinase, or PLK, family of kinases; 3) potentially improved pharmacokinetic (PK) properties; and 4) potential absence of QT prolongation at doses that significantly inhibit WEE1. No head-to-head studies with APR-1051 have been conducted. ACESOT-1051 is a focused biomarker-driven study with advanced/metastatic solid tumors harboring the following cancer-associated gene alterations: Amplification/overexpression of CCNE1 or CCNE2 regardless of tumor type, orDeleterious mutations in FBXW7 or PPP2R1A regardless of tumor type, orColorectal cancer with KRAS-GLY12 and TP53 co-mutation, orUterine serous carcinoma regardless of biomarker status “Dosing of the first patient in the ACESOT-1051 study is an important milestone in our APR-1051 development program and represents a key advancement of our clinical pipeline,” said Oren Gilad, Ph.D., President and Chief Executive Officer of Aprea. “Adding a second clinical program enriches our asset portfolio. We are initially evaluating sin...