Sapacitabine + seliciclib

Sapacitabine + seliciclib is an investigational oral combination therapy being studied primarily for the treatment of advanced solid tumors and BRCA-deficient cancers. Sapacitabine is a nucleoside analog prodrug that, once metabolized to its active form (CNDAC), incorporates into DNA and induces single-strand breaks, which upon further replication can lead to double-strand breaks and cell death. This mechanism exploits deficiencies in homologous recombination repair pathways, such as those seen in BRCA-mutated cancers. Seliciclib (also known as roscovitine or CYC202) is a small molecule cyclin-dependent kinase (CDK) inhibitor targeting CDK2, CDK7, and CDK9; it impairs cell cycle progression and diminishes DNA repair machinery by inhibiting key kinases involved in cell division. The combination has shown synergistic antitumor activity in preclinical models by both inducing DNA damage (sapacitabine) and impairing the cancer cells' ability to repair this damage (seliciclib). Both drugs are developed by Cyclacel Pharmaceuticals[1][4][5][6].

Other names

sapacitabine + roscovitine