Melflufen has been successful in overcoming resistance to standard chemotherapeutics as well as novel agents, such as proteasome inhibitors and immunomodulatory drugs. The high lipophilicity of melflufen facilitates rapid entry into myeloma cells. Furthermore, its alkylating activity is initiated by aminopeptidases, which are often overexpressed by myeloma cells, making the agent particularly selective. As a result, melflufen is better tolerated, with fewer off-target effects than its predecessor, melphalan.
Here, Paul Richardson discusses the major findings from preclinical studies and topline data from ongoing clinical trials evaluating melflufen for the treatment of multiple myeloma.