CX-4945 + gemcitabine + cisplatin

CX-4945 + gemcitabine + cisplatin is a investigational combination regimen comprising: - **CX-4945 (silmitasertib)**, a first-in-class, orally available, small molecule that selectively inhibits casein kinase 2 (CK2), an enzyme implicated in cancer cell survival, oncogenic signaling, and cell cycle regulation. CX-4945 also inhibits other CMGC kinase family members, notably DYRK1A and GSK3β, binding their ATP pockets and modulating related signaling pathways. - **Gemcitabine**, a nucleoside analog and antimetabolite chemotherapeutic, primarily inhibiting DNA synthesis by targeting ribonucleotide reductase and DNA polymerase, leading to DNA damage and apoptosis. - **Cisplatin**, a platinum-based DNA cross-linking agent that induces DNA damage, inhibits replication, and triggers apoptosis in rapidly dividing cells. The triple combination is under clinical investigation (notably for **cholangiocarcinoma**) due to its capacity for synergistic anti-tumor activity; CX-4945 potentiates the cytotoxicity of gemcitabine and cisplatin by inhibiting DNA repair pathways and further disrupting cancer cell proliferation and survival[2].

Other names

CX-4945 + gemcitabine + cisplatin