Synonyms: Melflufen | Pepaxti® | Pepaxto® | Prodrug J 1 | Prodrug J-1
melphalan flufenamide is an approved drug (FDA (2021), EMA (2022))
Compound class:
Synthetic organic
Comment: Melphalan flufenamide is a peptide-conjugated prodrug of the cytotoxic DNA alkylating drug melphalan [3]. It is highly lipophilic and is rapidly transported into cells where it is quickly hydrolysed by aminopeptidases that are overexpressed by some cancer cells. Melphalan flufenamide is being evaluated as a treatment for multiple myeloma [2,5-6].
The IUPAC Condensed peptide sequence for melphalan flufenamide is H-Phe(Unk)-Phe(4-F)-OEt. |
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Bioactivity Comments |
Melphalan flufenamide's anti-tumour activity is identical to that of melphalan, but is it more selective for tumour cells that overexpress aminopeptidases that the parent drug [3]. |