canfosfamide

Canfosfamide is a small molecule, investigational antineoplastic agent developed for the treatment of various solid tumors, most notably chemotherapy-resistant ovarian cancer. It is a modified glutathione analogue and nitrogen mustard prodrug that is selectively activated by the enzyme glutathione S-transferase P1-1 (GST P1-1), which is overexpressed in many human cancers. Upon activation by GST P1-1, canfosfamide splits into two fragments: a glutathione analog fragment and an active cytotoxic phosphorodiamidate alkylating metabolite. The cytotoxic fragment forms covalent linkages with nucleophilic centers in tumor cell DNA, RNA, and proteins, leading to cellular stress responses and apoptosis. This mechanism exploits elevated GST P1-1 activity in cancer cells for selective toxicity[1][2][5][6][7]. Canfosfamide was primarily developed by Telik and has been evaluated in clinical trials for ovarian cancer (including platinum-resistant/refractory cases), non-small cell lung cancer, lymphomas, multiple myeloma, breast cancer, and colorectal cancer[4]. Clinical development was ultimately suspended or discontinued due to lack of significant improvement over standard therapies.

Brand names

Telcyta

Other names

canfosfamide hydrochloridecanfosfamida