NCIt definition : The hydrochloride salt form of melphalan flufenamide, a peptide-drug conjugate composed
of a peptide conjugated, via an aminopeptidase-targeting linkage, to the alkylating
agent melphalan, with potential antineoplastic and anti-angiogenic activities. Upon
administration, the highly lipophilic melphalan flufenamide penetrates cell membranes
and enters cells. In aminopeptidase-positive tumor cells, melphalan flufenamide is
hydrolyzed by peptidases to release the hydrophilic alkylating agent melphalan. This
results in the specific release and accumulation of melphalan in aminopeptidase-positive
tumor 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.
Peptidases are overexpressed by certain cancer cells. The administration of melphalan
flufenamide allows for enhanced efficacy and reduced toxicity compared to melphalan.;
UNII : 3412470A0V;
InChIKey : ZCMWSKHHXLCVHI-VROPFNGYSA-N;
CAS number : 380449-54-7; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 380449-54-7
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