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m-sarcolysine is an alkylating agent with antineoplastic (anticancer) activity. It is a nitrogen mustard derivative structurally related to melphalan and is known as the para-isomer of melphalan (“sarcolysin” typically refers to the meta-isomer, m-sarcolysine)[1][3]. Like other alkylating agents, m-sarcolysine exerts its cytotoxic effect by crosslinking DNA strands, thereby inhibiting DNA replication and cellular proliferation, ultimately leading to cell death[1][3]. The agent has been explored both as a free drug and as part of peptide-drug conjugates for improved uptake and efficacy in cancer cells[3]. It has shown activity in preclinical and clinical studies involving hematological malignancies such as chronic lymphocytic leukemia. m-Sarcolysine is distinct from L-sarcolysin (melphalan) in its mechanism and pharmacokinetic profile, notably lacking cross-resistance to melphalan in certain cell types[3].
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