Acrivon Therapeutics, Inc. has commenced a Phase 1 clinical trial for ACR-2316, a novel therapeutic agent targeting WEE1 and PKMYT1, in patients with selected solid tumors. The first patient has been dosed, marking a significant milestone in the development of this potential cancer treatment.
ACR-2316: A Novel WEE1/PKMYT1 Inhibitor
ACR-2316 is designed to overcome the limitations of single-target WEE1 and PKMYT1 inhibitors. The drug was discovered and advanced to Phase 1 trials within 15 months, a timeline facilitated by Acrivon's AP3 (Acrivon Predictive Precision Proteomics) platform. Preclinical data suggests that ACR-2316 can induce complete tumor regression and pro-apoptotic tumor cell death through potent activation of CDK1, CDK2, and PLK1.
Phase 1 Trial Design and Objectives
The Phase 1 monotherapy trial aims to evaluate the safety and tolerability of ACR-2316. Additional objectives include determining the maximum tolerated dose (MTD) and the recommended Phase 2 monotherapy dose. The trial will also characterize the pharmacokinetic profile of ACR-2316 and provide a preliminary evaluation of its anti-tumor activity. Dose optimization will be guided by drug target engagement, aligning with the FDA's Project Optimus.
AP3 Platform and Precision Medicine Approach
Acrivon's AP3 platform plays a crucial role in the development of ACR-2316. The platform leverages machine learning to integrate phosphoproteomic drug profiling data, providing actionable insights for streamlined drug discovery. According to Peter Blume-Jensen, M.D., Ph.D., chief executive officer, president, and founder of Acrivon, the AP3 Interactome enables the rapid advancement of drug candidates like ACR-2316.
Anticipated Clinical Data
Initial clinical data from the Phase 1 dose optimization trial is expected in the second half of 2025. The trial is designed to assess the safety and tolerability of ACR-2316, as well as to determine the optimal dosage for further clinical development. Acrivon is also conducting AP3-based indication finding and OncoSignature development to identify patients most likely to benefit from ACR-2316.
