Acrivon Therapeutics to Reveal the Molecular Mechanisms Driving Strong Single-Agent Activity of ACR-2316, its AP3-Enabled Clinical Stage WEE1/PKMYT1 Inhibitor, at the AACR Annual Meeting 2025

Core Insights - Acrivon Therapeutics is advancing its clinical-stage asset ACR-2316, a selective WEE1/PKMYT1 inhibitor, which has shown superior anti-cancer activity in preclinical studies and is currently in a Phase 1 clinical trial with promising early results [1][2][3] Group 1: Clinical Development - ACR-2316 has completed three dose-escalation cohorts in its Phase 1 trial ahead of schedule, with solid tumor shrinkage observed at dose level three [1][2] - The trial has shown no safety concerns or dose-limiting toxicities (DLTs) at dose levels 1, 2, and 3, with dose level 4 currently enrolling [2] - Initial clinical activity of approximately 25% RECIST tumor shrinkage has been noted, along with a reduction of metastatic lesions in the chest, abdomen, and pelvis at dose level three [2] Group 2: Mechanism of Action - ACR-2316 was designed using Acrivon's AP3 platform to activate CDK1, CDK2, and PLK1 pathways, aiming to induce pro-apoptotic tumor cell death and achieve superior single-agent activity [3][7] - The drug's mechanism is intended to overcome limitations associated with single-target WEE1 and PKMYT1 inhibitors, demonstrating a favorable therapeutic index in preclinical studies [3][7] Group 3: Research and Technology - Acrivon utilizes its proprietary Acrivon Predictive Precision Proteomics (AP3) platform for drug discovery, which measures compound-specific effects on tumor cell protein signaling networks [5][6] - The AP3 platform enables the identification of patients most likely to benefit from Acrivon's drug candidates through OncoSignature companion diagnostics [6][7] - Acrivon is also developing ACR-368, a selective small molecule inhibitor targeting CHK1 and CHK2, which is in a potentially registrational Phase 2 trial for endometrial cancer [6][7]