Acrivon Therapeutics reports progress in Phase 1 trial of ACR-2316.

Acrivon Therapeutics announced the completion of three dose-escalation cohorts in its Phase 1 trial of ACR-2316. Solid tumor shrinkage has already been observed at dose level three, which is well below the projected recommended Phase 2 dose. The company will present data from AP3 Generative Phosphoproteomic analyses of ACR-2316-regulated CDK1-, CDK2-, and PLK1-induced pathways.

Title: Acrivon Therapeutics Advances Phase 1 Trial of ACR-2316, Demonstrates Early Clinical Activity

Acrivon Therapeutics, Inc. (Nasdaq: ACRV) has announced the successful completion of three dose-escalation cohorts in its Phase 1 trial of ACR-2316, a novel WEE1/PKMYT1 inhibitor. The company reported solid tumor shrinkage at dose level three, which is well below the projected recommended Phase 2 dose. This promising result was observed in patients with high unmet need solid tumor types predicted to be sensitive to ACR-2316.

The trial, which is enrolling patients with specific high unmet need solid tumor types, has shown drug target engagement already at dose levels 1 and 2, with evidence of dose proportionality. Notably, initial clinical activity, including ~25% RECIST tumor shrinkage and reduction of metastatic lesions, was observed at dose level three.

Acrivon plans to present data from AP3 Generative Phosphoproteomic analyses of ACR-2316-regulated CDK1-, CDK2-, and PLK1-induced pathways at the American Association for Cancer Research (AACR) Annual Meeting in Chicago, April 25-30, 2025. The presentation will highlight how the company's AP3 platform uncovered the mechanisms underlying ACR-2316's superior preclinical potency and single-agent activity.

The company's chief executive officer, Peter Blume-Jensen, M.D., Ph.D., expressed excitement about the early clinical observations, including the initial activity of ACR-2316. He emphasized that the drug was rationally designed through AP3-based SAR to induce desirable anti-tumor pathway effects and overcome the limitations of single-target WEE1 and PKMYT1 inhibitors.

Acrivon Therapeutics is leveraging its proprietary AP3 precision medicine platform to develop precision oncology medicines. The company is also advancing its lead candidate, ACR-368, a selective small molecule inhibitor targeting CHK1 and CHK2, in a potentially registrational Phase 2 trial for endometrial cancer.

References

[1] https://www.globenewswire.com/news-release/2025/04/25/3068264/0/en/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-Mee.html