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 Incyclix Bio 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 these compounds enhances its ability to target novel CDKs and develop effective and well-tolerated CDK inhibitors.

CDK2 Program

Incyclix Bio 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 due to prior treatment with a CDK4/6 inhibitor.

CDK2: An Important Therapeutic Target for People with Advanced, Resistant Cancers.
Incyclix Bio’s lead compound, INX-315, is a novel, potent and selective CDK2 with compelling pre-clinical efficacy and safety data. 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. Incyclix is leveraging a keen understanding of key structural features within the CDK2 binding pocket to develop a potent and selective CDK2 inhibitor. Incyclix Bio’s scientific founders honed a rational design approach while at G1 Therapeutics that enabled the development of inhibitors selective for CDK4/6 and provided insight into other CDK family characteristics. This deep understanding and unsurpassed expertise present a a unique vantage point from which to advance novel CDK2 and other CDK family inhibitors to effectively treat advanced and resistant cancers.

In May 2020, Incyclix Bio entered into an exclusive license for the IP covering G1 Therapeutics’ preclinical CDK2 inhibitor program.