pipeline

Cylene Pipeline of Small Molecule Targeted Agents

The Protein Kinase CK2 is essential for cancer cell survival, is up-regulated in many different cancers and is a key driver of multiple oncogenic pathways, so as a cancer target it is ideally suited for exploitation in combination drug therapy.  Cylene’s leadership in exploiting CK2 pathways enables the design and development of highly selective and potent small molecule drugs that can be utilized in rational combination therapies to substantially boost the antitumor efficacy of other cancer drugs for improved treatment outcomes. CX-4945 is the first clinical stage CK2 inhibitor and has demonstrated favorable safety, pharmacokinetic characteristics and pharmacodynamic responses in the Phase I clinical theatre. CX-4945 is now poised to advance into clinical trials in which it is rationally combined with other cancer drugs and in specific cancer indications.

The RNA Polymerase I program discovers and develops selective inhibitors of the newly validated RNA Polymerase I (POL I) cancer target that activate the p53 protein via a non-genotoxic mechanism.  The p53 protein normally functions as a tumor suppressor by causing cancer cells to self-destruct.  By targeting POL I to activate p53, Cylene’s first-in-class agents safely trigger the body’s natural cancer fighting capability to selectively kill tumor cells. Hematologic malignancies are particularly sensitive to activated p53, and these cancers will be the first to be treated in the clinical setting.

PIM kinases (embodied by the family of PIM-1, -2 and -3) stimulate excessive proliferation in numerous types of cancer and represent validated drug targets in many hematologic cancers and select solid tumors. Cylene’s pam-PIM Kinase Program has created multiple, proprietary chemical series which inhibition of all three PIM kinases isoforms in the low nM to pM range, and can do so selectively without affecting other kinase enzymes.