UCN-01 + irinotecan

UCN-01 + irinotecan is an investigational combination therapy consisting of UCN-01 (7-hydroxystaurosporine), a broad-spectrum serine-threonine kinase inhibitor, and irinotecan, a topoisomerase I inhibitor. UCN-01 acts primarily as a non-selective checkpoint kinase 1 (Chk1) inhibitor, disrupting cell cycle checkpoints and enhancing the cytotoxic effects of DNA-damaging agents like irinotecan. Irinotecan inhibits topoisomerase I, leading to DNA damage during replication. The combination has been studied in advanced solid tumors, particularly metastatic triple negative breast cancer (TNBC) and colorectal cancer models, based on preclinical evidence that Chk1 inhibition sensitizes tumor cells—especially those with TP53 mutations—to chemotherapy-induced DNA damage. Clinical trials have shown limited but notable activity in heavily pretreated TNBC patients; however, inconsistent pharmacokinetics of UCN-01 may limit efficacy[1][6][7].

Brand names

Camptosar

Other names

7-hydroxystaurosporine + irinotecan