NCI Drug Dictionary

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The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

melphalan-flufenamide prodrug
A melphalan prodrug in which the alkylating agent melphalan is bound to flufenamide, with potential antineoplastic and anti-angiogenic activities. Upon administration, the dipeptide bond in the melphalan-flufenamide compound is hydrolyzed by peptidases, which are overexpressed by certain cancer cells. This results in the specific release and accumulation of the active metabolite melphalan in cancer cells. Melphalan alkylates DNA at the N7 position of guanine residues and induces DNA intra- and inter-strand cross-linkages. This results in the inhibition of DNA and RNA synthesis and the induction of apoptosis, thereby inhibiting tumor cell proliferation. The administration of the melphalan-flufenamide prodrug allows for enhanced efficacy and reduced toxicity compared to melphalan alone. Check for active clinical trials using this agent. (NCI Thesaurus)
Synonyms:L-melphalanyl-p-L-fluorophenylalanine ethyl ester
Code name:J1