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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

Key Takeaway: Acrivon Therapeutics has announced the development of ACR-2316, a novel dual inhibitor targeting WEE1 and PKMYT1, utilizing the company's AP3 platform for precision oncology. The compound has shown compelling anti-tumor activity during preclinical studies and is designed to overcome resistance mechanisms associated with existing inhibitors. Acrivon plans to submit an Investigational New Drug application by the fourth quarter of 2024 to commence monotherapy development tailored to patients predicted to respond to the drug. The focus on preclinical optimization illustrates the potential for ACR-2316 to address unmet needs in solid tumor treatments.

Market Sentiment Analysis

POSITIVE FACTORS

  • ACR-2316 demonstrates potent anti-tumor activity in preclinical studies.
  • The drug is designed with AP3 platform, enhancing its selectivity and potency.
  • The upcoming IND submission for ACR-2316 indicates proactiveness in advancing its development.

Full Press Release Details

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
Acrivon s Predictive Precision Proteomics (AP3) platform is a proprietary, broadly applicable, next-generation precision oncology
platform at the forefront of the next wave of biology-driven drug discovery, in addition to its previously demonstrated utility in clinical development for treating patients based on predicted drug sensitivity
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
The AP3 platform has uniquely enabled the rapid generation of this novel dual
inhibitor optimized to potentially overcome resistance mechanisms induced by WEE1 and PKMYT1 single inhibitors, and other mechanism-based liabilities
The company is prioritizing advancement of this molecule, with planned IND submission by the fourth quarter of 2024, to initiate clinical
monotherapy development in tumor types predicted responsive to ACR-2316 through prior AP3-derived OncoSignature indication finding and subsequent treatment of patients
based on OncoSignature-predicted sensitivity
WATERTOWN, Massachusetts, September 5, 2023 Acrivon Therapeutics, Inc.
( Acrivon or Acrivon Therapeutics ) (Nasdaq: ACRV), a clinical stage biopharmaceutical company developing precision oncology medicines that it matches to patients whose tumors are predicted to be sensitive to each specific
medicine by utilizing its proprietary proteomics-based patient responder identification platform, today 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.
The rapid generation and optimized design of ACR-2316 further demonstrates the broad utility of the AP3 platform
in drug discovery, in addition to its applications in clinical development, said Kristina Masson, Ph.D., M.B.A., co-founder, executive vice president, and site head of Acrivon AB, Acrivon
Therapeutics wholly-owned drug discovery and phosphoproteomics subsidiary in Medicon Village, Lund, Sweden. This dual inhibitor development candidate is yet another powerful validation of our
AI-enabled AP3 platform, which has been instrumental for the identification of this compound, optimized for strong single agent activity compared to existing WEE1 and PKMYT1 inhibitors.
Previously, we have shown how AP3 can be used to develop drug-tailored predictive OncoSignature tests
for effective identification of patients likely to respond to a given therapy, as we have done for our clinical stage CHK1/2 inhibitor, ACR-368, said Peter Blume-Jensen, M.D., Ph.D., chief executive
officer, president, and founder of Acrivon Therapeutics. We now believe that we have shown how AP3 can be used to go beyond the limitations of traditional drug discovery methods by enabling biological pathway-based rational design of
development candidates with optimal target selectivity profile and potency, with ACR-2316 being the first example. This novel dual WEE1/PKMYT1 inhibitor has the potential to address significant unmet needs
across many solid tumor types based on its compelling preclinical profile, with the potential for monotherapy development in tumors predicted to be sensitive to ACR-2316 using our OncoSignature patient
Based on the emerging favorable preclinical profile of ACR-2316, the company has
entered into IND-enabling studies. The compound is designed for high selectivity towards WEE1 and PKMYT1, exhibiting single-digit nM IC50 potency in a
carefully predetermined ratio to ensure strong single agent anti-tumor activity, as demonstrated in tumor-bearing rodent models and other preclinical analyses. Using AP3 for unbiased quantitative high-resolution measurement of the effects of ACR-2316 on the human tumor cell phosphoproteome, this compound has been further optimized for potent induction of mitotic catastrophe, which is key to its strong single agent activity in preclinical models and
potentially favorable clinical profile for monotherapy development.
The preclinical data we have generated thus far is consistent with potential
clinical advantages and possible differentiation compared to current single inhibitors of WEE1 and PKMYT1, both critically important cell cycle regulators with demonstrated clinical activity, said Erick Gamelin, M.D., Ph.D., chief medical
officer of Acrivon. We are particularly encouraged by its compelling target selectivity and preclinical potency profile. With ACR-2316, we have demonstrated that the company s data-driven,
streamlined AP3 approach can generate molecules with desirable preclinical properties tailored for clinical monotherapy development.
information regarding ACR-2316 can be found in the company s updated corporate presentation, which can be found on the company s website using this link.
About Acrivon Therapeutics
is a clinical stage biopharmaceutical company developing precision oncology medicines that it matches to patients whose tumors are predicted to be sensitive to each specific medicine by utilizing Acrivon s proprietary proteomics-based patient
responder identification platform, Acrivon Predictive Precision Proteomics, or AP3. The AP3 platform enables the creation of drug-specific proprietary OncoSignature companion diagnostics that are used to identify the patients most likely to benefit
from Acrivon s drug candidates. Acrivon is currently advancing its lead candidate, ACR-368, a selective small molecule inhibitor targeting CHK1 and CHK2 in a potentially registrational Phase 2 trial
across multiple tumor types. The company has received fast track designation from the Food and Drug Administration, or FDA, for the investigation of ACR-368 as monotherapy based on OncoSignature-predicted
sensitivity in patients with platinum-resistant ovarian or endometrial cancer. Acrivon s ACR-368 OncoSignature test, which has not yet obtained regulatory approval, has been extensively evaluated in
preclinical studies, including in two separate, blinded, prospectively-designed studies on pretreatment tumor biopsies collected from past third-party Phase 2 trials in patients with ovarian cancer treated
with ACR-368. In addition to ACR-368, Acrivon is also leveraging its proprietary AP3 precision medicine platform
for developing its internally-discovered preclinical stage pipeline programs, consisting of its development candidate, ACR-2316, a selective, dual WEE1/PKMYT1 inhibitor, and additional programs targeting these
two critical nodes in the DNA Damage Response, or DDR, pathways.
Forward-Looking Statements
This press release includes certain disclosures that contain forward-looking statements within the meaning of the Private Securities
Litigation Reform Act of 1995 about us and our industry that involve substantial risks and uncertainties. All statements other than statements of historical facts contained in this press release, including statements regarding our future results of
operations or financial condition, business strategy and plans and objectives of management for future operations, are forward-looking statements. In some cases, you can identify forward-looking statements because they contain words such as
anticipate, believe, contemplate, continue, could, estimate, expect, intend, may, plan, potential,
possible, predict, project, should, target, will, or would or the negative of these words or other similar terms or expressions. Forward-looking statements are based
on Acrivon s current expectations and are subject to inherent uncertainties, risks and assumptions that are difficult to predict. Factors that could cause actual results to differ include, but are not limited to, risks and uncertainties that
are described more fully in the section titled Risk Factors in our reports filed with the Securities and Exchange Commission. Forward-looking statements contained in this press release are made as of this date, and Acrivon undertakes no
duty to update such information except as required under applicable law.
Investor and Media Contacts:
Adam D. Levy, Ph.D., M.B.A

Frequently Asked Questions

What is ACR-2316 developed by Acrivon Therapeutics?

ACR-2316 is a dual WEE1 and PKMYT1 inhibitor designed for anti-tumor activity.

What platform was used to develop ACR-2316?

ACR-2316 was developed using Acrivon's Predictive Precision Proteomics (AP3) platform.

When does Acrivon plan to submit the IND for ACR-2316?

The IND submission for ACR-2316 is planned for the fourth quarter of 2024.

What is the potential of ACR-2316 in cancer treatment?

ACR-2316 may address unmet needs in solid tumors predicted to respond to it.

How does ACR-2316 compare to current inhibitors?

ACR-2316 aims for enhanced selectivity and anti-tumor potency versus existing inhibitors.

Last updated: Sep 5, 2023