desethyl-melflufen

Desethyl-melflufen is an **active metabolite of melphalan flufenamide (melflufen)**, a first-in-class peptide-drug conjugate developed as an anticancer agent. Melflufen is designed to target aminopeptidases and rapidly release alkylating agents specifically within tumor cells, leading to cytotoxic effects. **Desethyl-melflufen possesses alkylating potential equal to melflufen and melphalan**, exerting cytotoxicity primarily via DNA damage, induction of apoptosis, and antiangiogenic effects. These properties contribute to potent antitumor activity, particularly in multiple myeloma cells resistant to other therapies, including in settings where p53 is impaired. Desethyl-melflufen is not used clinically as an isolated drug, but is an important metabolite responsible for the pharmacological activity of melflufen in the body[1].