Ensem Therapeutics Showcases Promising CDK2 Inhibitor Data

Ensem Therapeutics Advances Innovative Oncology Solutions

Ensem Therapeutics, Inc. (ENSEM) is taking significant strides in the oncology space with its unique approach to drug discovery. Utilizing the Kinetic Ensemble® platform, the company focuses on creating small molecule precision medicines tailored to treat various cancers effectively.

ETX-197/BG-68501: The Potential Game Changer

At the renowned annual San Antonio Breast Cancer Symposium, Ensem Therapeutics will unveil preclinical data on its promising drug candidate, ETX-197/BG-68501. This selective oral CDK2 inhibitor demonstrates a differentiated profile that could pave the way for better patient outcomes in cancers relying on CDK2.

Understanding CDK2 Vulnerabilities

CDK2 has emerged as a critical vulnerability for numerous cancer types, particularly those where Cyclin E (CCNE) is overexpressed or where the Retinoblastoma 1 gene (RB1) is either mutated or lost. Currently, there remains a notable absence of approved drugs explicitly targeting CDK2, making ETX-197/BG-68501 an exciting prospect.

Advantages of ETX-197/BG-68501

This innovative candidate, designed via the Kinetic Ensemble platform, showcases significant binding affinity for CDK2. Its unique mechanism leads to enhanced potency and selectivity, surpassing the performance of existing CDK2 inhibitors. ETX-197/BG-68501 stands out as it exhibits 100-fold higher selectivity for CDK2 compared to its kinases and shows promise against a wide array of 385 other kinases, suggesting excellent tolerability during clinical usage.

Preclinical Results and Efficacy

In studies involving mouse xenografts with CCNE-amplified ovarian cancer, ETX-197/BG-68501 not only maintained effective target engagement but also achieved notable tumor growth inhibition while demonstrating excellent tolerance levels in subjects. The drug showed single-agent effectiveness in breast cancer models that developed resistance to the traditional CDK4/CDK6 inhibitors, proving its capabilities in overcoming treatment challenges.

Broader Applications Beyond Breast Cancer

The anti-cancer potential of ETX-197/BG-68501 extends to various tumor models, including small cell lung and ovarian cancers. These findings suggest that its clinical applications may encompass a wide range of malignancies.

Statement from Leadership

Shengfang Jin, CEO and Co-Founder of ENSEM, expresses confidence in the results garnered thus far. "Inhibiting CDK2 while achieving selectivity over other family members is traditionally challenging, yet our promising data indicates that our Kinetic Ensemble platform is revolutionizing approaches to tackle intricate drug targets." She also emphasized that BeiGene is currently conducting a Phase 1a/1b clinical study—a vital step in assessing the safety and overall effectiveness of ETX-197/BG-68501.

Poster Presentation at the Symposium

The details surrounding ETX-197/BG-68501's presentation are as follows:

• Title: ETX-197/BG-68501, a potential best-in-class potent, selective oral small molecule CDK2 inhibitor, has anti-tumor activity in cancer models with Cyclin E amplification or deficiency in the Retinoblastoma 1 gene.
• Poster ID: P4-12-29
• Sessions: Poster Session
• Date/Time: Thursday, December 12, from 5:30 to 7 p.m. CT
• Location: Halls 2-3

About Ensem Therapeutics

Ensem Therapeutics operates at the forefront of oncological innovation with its Kinetic Ensemble platform, integrating cutting-edge methodologies like AI deep learning and advanced computational techniques. The company is focused on identifying challenging drug targets, emphasizing the discovery of small molecules that unlock significant therapeutic potential.

Frequently Asked Questions

What is the main focus of Ensem Therapeutics?

Ensem Therapeutics specializes in drug discovery and development for oncology, utilizing a unique platform to create precision medicines.

What is ETX-197/BG-68501?

ETX-197/BG-68501 is a selective oral CDK2 inhibitor with promising preclinical data indicating its potential to treat various cancers.

How does ETX-197/BG-68501 work?

The drug is designed to bind effectively to the CDK2 ATP pocket, enhancing the inhibitor's potency and selectivity over existing treatments.

When will the data on ETX-197/BG-68501 be presented?

The preclinical data will be showcased at the upcoming San Antonio Breast Cancer Symposium.

What future plans does Ensem Therapeutics have?

Ensem aims to further assess ETX-197/BG-68501's clinical potential through ongoing studies and enhance its drug discovery capabilities.

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