karenitecin + cyclophosphamide

karenitecin + cyclophosphamide is a combination chemotherapy regimen consisting of the novel camptothecin derivative karenitecin (also known as BNP1350) and the cytotoxic alkylating agent cyclophosphamide. Karenitecin is a highly lipophilic 7-alkylsilane derivative of camptothecin that functions as a topoisomerase I inhibitor; it stabilizes the covalent complex between the enzyme and DNA, leading to irreversible DNA strand breaks and apoptosis during the S-phase of the cell cycle. Cyclophosphamide is a nitrogen mustard prodrug that is metabolically activated to form DNA-alkylating metabolites, which create interstrand and intrastrand cross-links, further inhibiting DNA replication. This combination has been primarily investigated in Phase 1 clinical trials sponsored by the Baylor College of Medicine, specifically targeting pediatric patients with refractory or recurrent solid tumors and adult patients with recurrent malignant gliomas.

Other names

Karenitecin and cyclophosphamide