Approach


As cyclin-dependent kinases (CDKs) are key regulators of critical biological processes supporting cellular proliferation and growth, there are a number of novel cancer targets worthy of drug development pursuit within this family.

Uncontrolled cellular proliferation is a hallmark of cancer and is commonly driven by dysregulated kinase activity of specific CDK family members. Recent advances in cancer treatment using CDK inhibition have focused on targeting CDK4/6, key mediators of cell cycle progression. While this therapeutic approach has provided significant clinical benefit, many tumors activate other CDK family members to drive uncontrolled proliferation. As a result, primary resistance has limited the broad clinical utility of CDK4/6 inhibitors.

The ARC Therapeutics team has demonstrated success in its profiling strategy and has fine-tuned the process of achieving well-tolerated compounds. The team’s thorough biochemical and biological validation of compounds enhances its ability to target novel CDKs and develop effective and well-tolerated CDK inhibitors.

CDK2 Program


The ARC Therapeutics team is focused on developing a novel, potent and selective inhibitor of CDK2 to treat patients whose tumors are insensitive to CDK4/6 inhibition, either by primary resistance or acquired resistance by prior treatment with a CDK4/6 inhibitor.

CDK2: An Important Therapeutic Target for People with Advanced, Resistant Cancers
CDK2 is a known driver of abnormal cancer cell proliferation and is an important therapeutic target of unmet need.

Historical efforts to target CDK2 have been unsuccessful due to an inability to design or identify potent and selective CDK2 inhibitors. However, the rational design approach the scientific founders used to develop inhibitors selective for CDK4/6 versus CDK2 at G1 Therapeutics led to a keen understanding of key structural features within the CDK2 binding pocket that can be exploited to develop a potent and selective CDK2 inhibitor. This deep understanding and unsurpassed expertise present an incredible opportunity to effectively treat advanced and resistant cancers.

In May 2020, ARC Therapeutics entered into an exclusive license for the IP covering G1 Therapeutics’ preclinical CDK2 inhibitor program. Under the terms of the agreement, G1 Therapeutics received an upfront payment and equity in ARC Therapeutics.