perfosfamide

Perfosfamide is a synthetic oxazaphosphorine alkylating agent and a derivative of cyclophosphamide. Unlike its parent compound, perfosfamide is pre-activated and does not require hepatic metabolism by cytochrome P450 enzymes to exert its cytotoxic effects. It spontaneously degrades in aqueous solution to form 4-hydroxycyclophosphamide, which then tautomerizes to aldophosphamide and eventually yields the active cytotoxic metabolite, phosphoramide mustard. This metabolite forms DNA cross-links, primarily at the N-7 position of guanine, leading to DNA strand breakage, inhibition of DNA replication, and apoptosis. Perfosfamide has been primarily utilized in ex vivo settings for purging autologous bone marrow or peripheral blood stem cell grafts to eliminate contaminating malignant cells, such as those in acute myeloid leukemia or non-Hodgkin lymphoma, before re-infusion into the patient.

Brand names

PerfosfamidePergamid

Other names

4-hydroperoxycyclophosphamide4-hydroperoxy-cyclophosphamide