Cyclin-dependent kinases (CDK) are serine/threonine kinases that act as regulatory enzymes involved in cell proliferation. The dysregulation of CDK activity occurs through overexpression of cyclin E1, a binding partner of CDK2, which is observed in several cancers such as high-grade serous ovarian cancer (HGSOC), bladder cancer, gastric cancer and estrogen receptor-positive breast cancer, among others. Selective inhibition of CDK2 may thus be considered a therapeutic approach to regaining cell cycle control.
More than a decade ago, three scientists were part of a team at G1 Therapeutics Inc. that led to the now-approved CDK4/6 inhibitor Cosela (trilaciclib). The same work also led to findings showing CDK2 as a promising target for cancers that developed resistance to CDK4/6 inhibition.
Incyclix Bio LLC has received FDA approval of an IND application for INX-315, a novel, potent and selective cyclin-dependent kinase 2 (CDK2) inhibitor for advanced or metastatic cancers. The first-in-human phase I/II study will be conducted in patients with estrogen receptor (ER)-positive/HER2-negative breast cancer who have progressed on a CDK4/6 inhibitor regimen and CCNE1-amplified solid tumors that have progressed on standard-of-care treatment.
