Research & Development

Seliciclib (CYC202)

Seliciclib is a novel, orally-available inhibitor of CDK2/E, CDK2/A, CDK7 and CDK9 - enzymes that are central to the process of cell division and cell cycle control and play pivotal roles in cancer cell growth and DNA damage repair. Inhibition of CDKs 2 and 9 may also correct aberrant cell cycle control in certain non-malignant diseases of proliferation. Seliciclib exerts an anti-proliferative effect via several key mechanisms:

  • selective downregulation of proliferative and survival proteins and upregulation of p53, leading to growth arrest or apoptosis;
  • decreasing phosphorylation of Rb and modulating E2F transcriptional activity leading to growth arrest or apoptosis;
  • inhibiting HR and NHEJ DNA repair pathways, resulting in synergy with DNA damaging agents; and
  • in sequence with chemotherapy, overcoming cell cycle related drug resistance.

Seliciclib is being evaluated in an all-oral Phase 1/2 combination study with our sapacitabine in patients with BRCA mutations.

Learn more about seliciclib (PDF)

Research & Development