ACR-2316 / Acrivon Therap - LARVOL DELTA

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 Meeting 2025 (GlobeNewswire) - "Acrivon Therapeutics, Inc...announced it will 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 taking place April 25-30, 2025 in Chicago."

Clinical • Oncology • Solid Tumor

Detailed mechanistic understanding of ACR-2316, a novel, clinical-stage WEE1/PKMYT1 inhibitor, rationally designed for superior single-agent activity through potent activation of CDK1, CDK2, and PLK1 using Acrivon's machine learning-driven AP3 platform (AACR 2025) - "The unique capabilities of our generative AI-driven AP3 platform used to rationally design ACR-2316 enabled a comprehensive analysis of ACR-2316-regulated CDK1/2-and PLK1-induced pathways underlying its differentiated, potent anticancer activity, as demonstrated in head:head preclinical studies against clinical benchmark inhibitors. ACR-2316 has advanced into the clinic ahead of schedule uniquely enabled by AP3 and is currently in a Phase 1 clinical trial in subjects with AP3-selected advanced solid tumors. Acrivon anticipates reporting initial ACR-2316 clinical Phase 1 data second half of 2025."

Clinical • Machine learning • Oncology • Solid Tumor • CDK1 • CDK2 • PKMYT1 • PLK1

Acrivon Therapeutics Provides Program Updates and Fourth Quarter and Full Year 2024 Financial Results (GlobeNewswire) - "Anticipated Upcoming Milestones: Provide update on registrational intent trial and confirmatory trial design for ACR-368; Report initial clinical data from the Phase 1 clinical study of ACR-2316 in the second half of 2025."

Clinical protocol • P1 data • Solid Tumor

Acrivon stops developing Lilly castoff for ovarian and bladder cancers to switch focus to endometrial (FierceBiotech) - P1b/2b | N=390 | NCT05548296 | Sponsor: Acrivon Therapeutics | "The Watertown, Massachusetts-based biotech had been evaluating the CHK1/2 inhibitor, called prexasertib or ACR-368, in a phase 2b trial of patients with endometrial cancer....Based on an interim data extract, Acrivon was able to show that the OncoSignature 'accurately identified patients whose tumors are sensitive to ACR-368,' with 80% of these individuals seeing their tumor shrink to some extent, according to Acrivon. This cohort saw a confirmed overall response rate of 35%....The company had already made endometrial cancer its top priority but used yesterday's filing to announce that it had now 'officially deprioritized ovarian and bladder cancers' as targets for ACR-368....The clinical resources for these two indications will be redirected to testing ACR-368 in endometrial cancer as well as toward Acrivon’s other clinical-stage candidate, ACR-2316."

P2b data • Pipeline update • Bladder Cancer • Endometrial Cancer • Ovarian Cancer

Acrivon Therapeutics Reports Third Quarter 2024 Financial Results and Business Highlights (GlobeNewswire) - "Provide program updates from our ongoing registrational-intent Phase 2b trial of ACR-368 in patients with gynecological cancers prospectively predicted sensitive to ACR-368 in the first half of 2025; Report initial data from the Phase 1 clinical study of ACR-2316, which is enriched for tumor types predicted to be sensitive to monotherapy through AP3-based indication finding, in the second half of 2025...Research and development expenses were $18.9 million for the quarter ended September 30, 2024 compared to $10.3 million for the same period in 2023. The difference was primarily due to the continued development of ACR-368..."

Commercial • P1 data • Trial status • Gynecologic Cancers • Oncology • Solid Tumor

Rational design of a superior single agent active, potential best-in-class WEE1/PKMYT1 inhibitor using Acrivon Predictive Precision Proteomics (AP3) (EORTC-NCI-AACR 2024) - "WEE1 inhibitors azenosertib and Debio0123, or the PKMYT1 inhibitor lunresertib, had a best response of stable disease at maximum achievable dose... ACR-2316 is a potent, selective dual inhibitor of WEE1 and PKMYT1, uniquely designed using Acrivon's AP3 platform for superior single agent activity through potent activation of CDK1, CDK2, and PLK1, and is on track for IND submission in Q3 2024 and first-in-human dosing in Q4 2024."

Oncology • Ovarian Cancer • Solid Tumor • CASP3 • CDK1 • CDK2 • PKMYT1 • PLK1

Acrivon Therapeutics to Present Data Demonstrating Deployment of its AP3 Platform for Streamlined Drug Discovery and Clinical Development at Two Scientific Conferences - Human Proteome Organization World Congress and EORTC-NCI-AACR Symposium (GlobeNewswire) - "Acrivon Therapeutics, Inc....announced the company will be presenting data on the ability of its AP3 platform to uniquely enable the clinical development of ACR-368 and the discovery and design of ACR-2316 at two upcoming scientific congresses: Human Proteome Organization (HUPO) World Congress taking place from October 20-24, 2024 in Dresden, Germany and EORTC-NCI-AACR (ENA) Symposium taking place from October 23-25, 2024 in Barcelona, Spain."

Clinical data • Oncology • Solid Tumor

Acrivon Therapeutics to Present Data Demonstrating Deployment of its AP3 Platform for Streamlined Drug Discovery and Clinical Development at Two Scientific Conferences - Human Proteome Organization World Congress and EORTC-NCI-AACR Symposium (GlobeNewswire) - "Acrivon Therapeutics, Inc...today announced the company will be presenting data on the ability of its AP3 platform to uniquely enable the clinical development of ACR-368 and the discovery and design of ACR-2316 at two upcoming scientific congresses: Human Proteome Organization (HUPO) World Congress taking place from October 20-24, 2024 in Dresden, Germany and EORTC-NCI-AACR (ENA) Symposium taking place from October 23-25, 2024 in Barcelona, Spain."

P2b data • Preclinical • Oncology • Solid Tumor

Phase 1 Study of ACR-2316 in Specific Advanced Solid Tumors (clinicaltrials.gov) - P1 | N=90 | Recruiting | Sponsor: Acrivon Therapeutics

Metastases • New P1 trial • Oncology • Solid Tumor

Acrivon Therapeutics Announces Initial Patient Dosing in Phase 1 Trial of ACR-2316, a Novel WEE1/PKMYT1 Inhibitor Designed Using AP3 for Superior Single-Agent Activity (GlobeNewswire) - "Acrivon Therapeutics, Inc...today announced that the first patient has been dosed in its Phase 1 clinical trial evaluating ACR-2316, the company’s internally discovered, potent, selective WEE1/PKMYT1 inhibitor, designed by AP3 to overcome the limitations of single-target WEE1 and PKMYT1 inhibitors. ACR-2316 is initially being developed in selected solid tumors identified by AP3...'We look forward to progressing this trial and expect to report initial clinical data in the second half of 2025.'"

P1 data • Trial status • Oncology • Solid Tumor

Acrivon Therapeutics Reports Positive Endometrial Cancer Data from Ongoing ACR-368 Registrational Intent Phase 2 Study at ESMO, Advancement of ACR-2316 into Clinic Ahead of Timelines, and Progress on its AP3 Interactome for Proprietary Data Analysis (GlobeNewswire) - P2 | N=390 | NCT05548296 | Sponsor: Acrivon Therapeutics | "Confirmed overall response rate (ORR) = 62.5% (95% CI, 30.4-86.5) observed in prospectively-selected ACR-368 OncoSignature-positive (BM+) patients with endometrial cancer; Achieved statistically significant segregation of responders in BM+ vs BM- subgroups based on OncoSignature patient selection (p-value = 0.009); ACR-368 endometrial cohort data maturing with all responders still on therapy; mDoR not yet reached (~6 months at time of data-cut); Endometrial cancer now anticipated to be the first tumor type with potential for ACR-368 accelerated regulatory approval; IND clearance and initial sites activated ahead of timelines for ACR-2316 with first-in-human dosing anticipated in Q4 2024."

New P1 trial • P2 data • Endometrial Cancer • Gynecologic Cancers • Oncology • Solid Tumor • Uterine Cancer

Acrivon Therapeutics Reports Second Quarter 2024 Financial Results and Business Highlights (GlobeNewswire) - "Provide pipeline (ACR-368 and ACR-2316), AP3 platform, and corporate updates in 2H 2024, including updated ACR-368 clinical data at the upcoming ESMO conference, where the company will present on September 14, 2024 in the Gynecological Cancers poster session (presentation number P744)....Research and development expenses were $15.0 million for the quarter ended June 30, 2024 compared to $10.5 million for the same period in 2023. The difference was primarily due to the continued development of ACR-368, inclusive of progression of the ongoing clinical trial..."

Clinical data • Commercial • Endometrial Adenocarcinoma • Endometrial Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Acrivon Therapeutics Reports First Quarter 2024 Financial Results and Business Highlights (GlobeNewswire) - "Complete IND-enabling studies for ACR-2316 to support IND submission in 3Q 2024; Initiate a Phase 1 clinical study of ACR-2316 in tumor types predicted sensitive to monotherapy through ongoing AP3-based indication finding in 4Q 2024; Provide pipeline (ACR-368 and ACR-2316), AP3 platform, and corporate updates in 2H 2024; Advance a new potential first-in-class cell cycle program for an undisclosed target towards development candidate nomination in 2025..."

IND • New P1 trial • Pipeline update • Endometrial Cancer • Genito-urinary Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

ACR-2316: A potentially first-in-class, potent, selective WEE1/PKMYT1 inhibitor rationally designed for superior single agent activity through synergistic disruption of cell cycle checkpoints (AACR 2024) - "ACR-2316 is more selective than adavosertib, azenosertib, and lunresertib based on >200 kinases profiled by AP3 and 468 kinases assessed by KINOMEscan...In conclusion, ACR-2316 is a potent, selective dual WEE1/PKMYT1 inhibitor with superior single-agent activity compared to clinical WEE1 or PKMYT1 inhibitors. ACR-2316 is progressing through IND-enabling studies in preparation for clinical monotherapy development."

Oncology • Ovarian Cancer • Solid Tumor • CDK1 • CDK2 • CHEK1 • PKMYT1 • PLK1

Acrivon Therapeutics Presents Data at AACR Annual Meeting Highlighting the Capabilities of Acrivon Predictive Precision Proteomics (AP3) for the Discovery of ACR-2316, a Novel, Selective WEE1/PKMYT1 Inhibitor, and the Identification of Actionable Resistance Mechanisms to ACR-368 (Yahoo Finance) - "Acrivon Therapeutics, Inc...announced data from two posters that the company presented at the American Association for Cancer Research (AACR) Annual Meeting....In a poster...preclinical data showing that ACR-2316 is a potent dual WEE1/PKMYT1 inhibitor with superior anticancer activity were presented. ACR-2316 was highly potent across multiple human tumor cell lines and patient-derived ex vivo tumor models. In proliferation assays across a panel of 19 cancer cell lines, ACR-2316 demonstrated greater potency in all cell lines tested compared to adavosertib and lunresertib (mean IC50 = 70, 252 and 364 nM, respectively)....In the second poster...preclinical studies using five ovarian cancer cell lines that were generated to be durably resistant to ACR-368 were reported."

Preclinical • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor

Acrivon Therapeutics Announces $130 Million Private Placement Financing (GlobeNewswire) - "Acrivon Therapeutics, Inc...announced that it has entered into a securities purchase agreement with certain existing and new accredited investors to issue and sell an aggregate of 8,235,000 shares of its common stock at a price of $8.50 per share, a premium to the closing price on April 8, 2024, and pre-funded warrants to purchase up to an aggregate of 7,060,000 shares of common stock at a purchase price of $8.499 per pre-funded warrant, through a private investment in public equity ('PIPE') financing....Acrivon currently expects to use the net proceeds from the private placement, together with its existing cash, cash equivalents and investments, to fund the continued advancement of its pipeline, including ACR-368, ACR-2316..."

Financing • CNS Tumor • Gastrointestinal Cancer • Genito-urinary Cancer • Gynecologic Cancers • Hematological Malignancies • Leukemia • Oncology • Solid Tumor

Acrivon Therapeutics Reports Fourth Quarter and Full Year 2023 Financial Results and Business Highlights (GlobeNewswire) - "Present more mature clinical data from the ongoing Phase 2 ACR-368 monotherapy single-arm trials and the Phase 1b/2 ACR-368 plus LDG combination single-arm trials during the first half of 2024. Complete IND-enabling studies for ACR-2316 to support IND submission for this novel drug candidate in the fourth quarter of 2024. Initiate Phase 1 monotherapy study in tumor types predicted sensitive to ACR-2316...and subsequent treatment of patients based on OncoSignature-predicted sensitivity in the first half of 2025...Research and development expenses were $15.5 million for the quarter ended December 31, 2023, and $46.0 million for the full year 2023, compared to $5.9 million and $23.9 million, respectively, for the same periods in 2022. The difference was primarily due to the continued development of ACR-368...as well as increased personnel costs to support these development activities and costs associated with our preclinical programs, including ACR-2316."

Commercial • IND • New P1 trial • P1/2 data • P2 data • CNS Tumor • Genito-urinary Cancer • Gynecologic Cancers • Hematological Malignancies • Leukemia • Oncology • Ovarian Cancer • Solid Tumor

Acrivon Therapeutics Reports Third Quarter 2023 Financial Results and Business Highlights (GlobeNewswire) - "Company plans to present more mature clinical data from the ongoing Phase 2 ACR-368 monotherapy single-arm trials and the Phase 1b/2 ACR-368 and LDG combination single-arm trials at a major medical conference during the first half of 2024; Completion of IND-enabling studies for ACR-2316 to support IND submission for this novel drug candidate in the fourth quarter of 2024..."

P1/2 data • P2 data • Preclinical • Endometrial Cancer • Genito-urinary Cancer • Gynecologic Cancers • Oncology • Ovarian Cancer • Solid Tumor • Urothelial Cancer • Uterine Cancer

Acrivon Therapeutics Announces ACR-2316, a Novel Dual WEE1 and PKMYT1 Inhibitor Development Candidate, Designed Using Acrivon’s AP3 Platform to Achieve Potent Single Agent Activity, as Demonstrated in Preclinical Studies (GlobeNewswire) - "Acrivon Therapeutics...announced a novel, internally developed clinical candidate, ACR-2316, a dual WEE1 and PKMYT1 inhibitor. The company plans to prioritize Investigational New Drug (IND) enabling studies for ACR-2316 to be ready for IND submission by the fourth quarter of 2024....ACR-2316 is a novel, internally developed small molecule development candidate, rationally designed through advanced co-crystallography and the AP3 platform to achieve optimal target potency and selectivity delivering potent single agent anti-tumor activity across in vitro and in vivo preclinical studies, compared to benchmark WEE1 and PKMYT1 inhibitors."

IND • New molecule • Preclinical • Oncology