ACR-368 Data Shows Synergy with Key ADC Payloads
Acrivon Therapeutics announced on March 17, 2026, that its lead drug candidate, ACR-368, demonstrates potent preclinical synergy with Topoisomerase 1 (Topo 1) inhibitors. This is a critical development because Topo 1 inhibitors are the most common payloads used in antibody-drug conjugates (ADCs), a highly valuable class of cancer treatments. ACR-368, a CHK1/2 inhibitor currently in a registrational-intent Phase 2b study, could significantly enhance the effectiveness of these existing and future therapies.
The findings suggest ACR-368 can overcome a key resistance mechanism used by cancer cells against Topo 1 inhibitors. This enhances the potential for ACR-368, which already holds an FDA Fast Track designation for treating endometrial cancer, to become a cornerstone of future combination therapies. The full data will be presented on April 19, 2026, at the American Association for Cancer Research (AACR) Annual Meeting.
Our data show that a key resistance mechanism to Topo1 inhibitors, the most common ADC payload, is the activation of the CHK1/2 DNA damage repair response, which can be overcome by ACR-368 treatment resulting in synergistic tumor cell killing.
— Peter Blume-Jensen, M.D., Ph.D., CEO of Acrivon.
Phase 1 Drug ACR-2316 Achieves Complete Tumor Regression
Further bolstering its pipeline, Acrivon also reported compelling results for ACR-2316, a WEE1/PKMYT1 inhibitor in Phase 1 trials. In preclinical mouse models, combining ACR-2316 with an anti-PD-L1 immune checkpoint inhibitor led to complete and durable tumor regression, including lasting immune memory. This indicates the drug not only kills cancer cells but also primes the immune system to prevent recurrence.
These preclinical results are supported by early human data from the ongoing Phase 1 trial, which has shown a favorable safety profile and initial clinical activity in solid tumors like endometrial cancer and small cell lung cancer. This early success differentiates ACR-2316 from other inhibitors in its class and suggests it may possess a best-in-class profile, significantly increasing its commercial potential ahead of its presentation at the AACR meeting on April 20, 2026.