WATERTOWN, Mass., August 5, 2026 — Leads & Copy — Acrivon Therapeutics, Inc., a clinical-stage biotechnology company, announced that its investigational drug ACR-2316 has advanced into the randomized dose expansion portion of its ongoing Phase 1/2 study. This progression is supported by a favorable safety profile and observed clinical activity, including tumor shrinkage and partial responses with durable clinical benefit in multiple patients. Acrivon has selected 120 mg and 160 mg doses, administered orally once daily on a three-days-on, four-days-off weekly schedule, for further dose optimization and final dose selection.
The company is advancing ACR-2316 based on its differentiated safety profile and promising clinical activity. The selected oral weekly regimen was established alongside another weekly regimen, while a bi-weekly regimen was evaluated but deprioritized. A total of 35 subjects received ACR-2316 across six dose levels, ranging from 30 to 240 mg once daily, in the two weekly oral dosing schedules.
Tumor shrinkage with long-lasting clinical benefit was observed across multiple tumor types, including partial responses in lung cancer and endometrial cancer, among subjects treated with ACR-2316 at 120 mg once daily or higher in the weekly schedules. In seven efficacy-evaluable subjects with small cell lung cancer (SCLC), squamous non-small cell lung cancer (sqNSCLC), and lung adenocarcinoma (adNSCLC)—tumor types predicted by Acrivon’s AP3 platform to be sensitive and not previously shown to be sensitive to single-agent WEE1 or PKMYT1 inhibitors—a disease control rate of 86% was observed, including two partial responses and four stable diseases.
Durable clinical benefit has been observed in three heavily pretreated lung cancer subjects who remain on treatment for over a year. In the selected three-days-on, four-days-off regimen, the 120 mg and 160 mg once daily doses were well-tolerated, with a favorable safety profile. No Grade 4 treatment-related adverse events were reported, and Grade 3 treatment-related adverse events were primarily limited to transient, mechanism-based hematologic events, predominantly neutropenia. These findings support the further evaluation of ACR-2316 in the selected regimen through a randomized dose expansion study in AP3-informed tumor types.
The dose expansion phase will evaluate ACR-2316 in subjects with SCLC, sqNSCLC, and adNSCLC, as well as endometrial cancer, cervical cancer, and esophago-gastric junction carcinoma. These patients will have AP3-identified biomarker signatures associated with pathway vulnerability, including loss or mutation of TP53 or FBXW7, or overexpression or amplification of CCNE1 or CCNB1, or HPV+ in the case of cervical cancer. The expansion study will use a three-days-on, four-days-off weekly administration schedule and will include stratification by lung cancer versus non-lung cancer tumor types, with a 1:1 randomization within each group to either the 120 mg or 160 mg once daily dose level. These two doses are candidate doses for final recommended Phase 2 dose selection.
The ACR-2316 dose escalation and expansion study adheres to the principles of the FDA’s Project Optimus, which emphasizes dose selection based on the totality of efficacy, safety, tolerability, pharmacokinetic, and pharmacodynamic data, and specifically stipulates randomized evaluation of multiple doses rather than routine selection of the maximum tolerated dose. Acrivon anticipates providing further updates as the study progresses.
Acrivon Therapeutics is a clinical-stage biopharmaceutical company focused on discovering and developing precision medicines using its proprietary Generative Phosphoproteomics AP3 platform. This platform enables the interpretation and quantification of compound-specific, drug-regulated pathway activity levels within intact cells in an unbiased manner, generating proprietary data and providing rapid, actionable insights. The AP3 platform includes tools such as the AP3 Data Portal, AP3 Kinase Substrate Relationship Predictor, and AP3 Interactome, which facilitate the design of differentiated compounds with desirable pathway effects through intracellular protein network analyses and streamlined clinical development.
The company is also advancing its lead program, ACR-368 (prexassertib), a selective small molecule inhibitor targeting CHK1 and CHK2, in a potentially registrational Phase 2 trial for endometrial cancer. The FDA has granted Fast Track designation for the investigation of ACR-368 as a monotherapy and a Breakthrough Device designation for the ACR-368 OncoSignature assay for patient identification. In addition to ACR-2316 and ACR-368, Acrivon is in early IND-enabling studies for several potential first-in-class development candidates targeting CDK11.
Source: Acrivon Therapeutics, Inc.
