NCI Drug Dictionary
The search textbox has an autosuggest feature. When you enter three or more characters, a list of up to 10 suggestions will popup under the textbox. Use the arrow keys to move through the suggestions. To select a suggestion, hit the enter key. Using the escape key closes the listbox and puts you back at the textbox. The radio buttons allow you to toggle between having all search items start with or contain the text you entered in the search box.
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 or closed clinical trials using this agent. (NCI Thesaurus)
|Synonyms:||L-melphalanyl-p-L-fluorophenylalanine ethyl ester |