On August 5, 2026 Acrivon Therapeutics, Inc. ("Acrivon" or "Acrivon Therapeutics") (Nasdaq: ACRV), a clinical stage biotechnology company discovering and developing precision medicines utilizing its proprietary Generative Phosphoproteomics AP3 (Acrivon Predictive Precision Proteomics) platform deployed for rational drug design and predictive clinical development, reported that ACR-2316 has advanced into the randomized dose expansion portion of its ongoing Phase 1/2 study. The advancement is supported by the differentiated favorable safety profile and clinical activity observed during dose escalation, including tumor shrinkage and partial responses (PRs) with durable clinical benefit in multiple subjects. Acrivon has selected 120 mg and 160 mg administered orally once daily (QD) on a 3d on/4d off weekly schedule for further dose optimization and final dose selection.

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"Advancing ACR-2316 into dose expansion is an important milestone for Acrivon, and the exciting initial clinical activity observed represents further clinical validation of our AP3 platform," said Peter Blume-Jensen, M.D., Ph.D., chief executive officer, president and co-founder of Acrivon. "We rationally designed ACR-2316 using AP3 to overcome the resistance mechanisms that limit efficacy of single-target WEE1 and PKMYT1 inhibition, hence enabling potent tumor cell death. We are highly encouraged by the durable single-agent activity, including tumor shrinkage and PRs, and clinical benefit observed for more than a year in multiple heavily pretreated subjects with lung cancer. These data support our belief that ACR-2316 has the potential to become an important therapy across multiple high unmet need patient populations."

"ACR-2316 has demonstrated a favorable safety profile in dose escalation, with adverse events limited primarily to transient, mechanism-based hematological events, mainly neutropenia, and a notable absence of non-hematological adverse events," said Mansoor Raza Mirza, M.D., chief medical officer of Acrivon. "This promising differentiated safety profile and initial clinical activity support its rapid advancement into a randomized expansion phase, to establish the dose with the optimal benefit-risk profile to carry into subsequent development."

ACR-2316 Dose Escalation Data and Observations To Date

Two weekly (3d on / 4d off QD and 2d on / 5d off QD) oral dosing regimens have been established, while a bi-weekly (3d on / 11d off QD) oral dosing regimen was evaluated, but deprioritized.
A total of 35 subjects received ACR-2316 across 6 dose levels ranging from 30 to 240 mg QD in the two weekly oral dosing schedules.
Amongst the subjects treated with ACR-2316 at ≥120 mg QD in the weekly schedules, tumor shrinkage with long-lasting clinical benefit were observed across multiple tumor types, including PRs in lung cancer and endometrial cancer.
In the 7 efficacy-evaluable subjects (median 3 prior lines of systemic therapy) with SCLC, sqNSCLC, and adNSCLC, AP3-predicted tumor types not previously shown to be sensitive to clinical single agent WEE1 or PKMYT1 inhibitors, a disease control rate of 86% (2 PRs, 4 SD, and 1 PD) was observed.
Ongoing durable clinical benefit observed in 3 heavily pretreated lung cancer subjects remaining on treatment for over one year.
In the selected 3d on / 4d off dosing regimen, the 120 mg QD and 160 mg QD doses were well tolerated, with a favorable, differentiated safety profile; no grade ≥4 treatment-related adverse events (TRAEs) were reported, and grade 3 TRAEs were limited to primarily transient, mechanism-based hematologic events, predominantly neutropenia.
These observations support further evaluation of ACR-2316 in the selected 3d on / 4d off QD regimen in a randomized dose expansion study of AP3-informed tumor types.

The dose expansion will evaluate ACR-2316 in subjects with SCLC, sqNSCLC and adNSCLC, as well as endometrial cancer, cervical cancer, and esophago-gastric junction carcinoma, all with 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 utilizes a 3d on / 4d off weekly administration schedule and will include stratification by lung cancer versus non-lung cancer tumor types, with 1:1 randomization within each group to the 120 mg QD or 160 mg QD dose level. The two selected 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 emphasize dose selection based on the totality of efficacy, safety, tolerability, pharmacokinetic and pharmacodynamic data, and specifically stipulate randomized evaluation of multiple doses rather than routine selection of the maximum tolerated dose. Acrivon expects to provide further updates as the study progresses.

(Press release, Acrivon Therapeutics, AUG 5, 2026, View Source [SID1234669759])