Pepaxti® (melphalan flufenamide, also called melflufen) is a lipophilic peptide conjugated alkylating drug that rapidly and selectively is delivering cytotoxic agents into tumor cells. The drug is composed of a di-peptide and an alkylating moiety. The lipophilicity allows a faster cellular uptake whereas the peptide hydrolysis mediated by aminopeptidases, results in accumulation of alkylating moieties in cancer cells. This results in an improved efficacy without an increased toxicity compared to melphalan. Pepaxti inhibits proliferation and induces apoptosis of hematopoietic and solid tumor cells. It shows synergistic cytotoxicity in combination with dexamethasone in melphalan resistant and non-resistant multiple myeloma cell lines.? Pepaxti has been granted marketing authorization in EU and EEA-countries and is indicated in combination with dexamethasone, for the treatment of adult patients with multiple myeloma who have received at least three prior lines of therapy, whose disease is refractory to at least one proteasome inhibitor, one immunomodulatory agent, and one anti-CD38 monoclonal antibody, and who have demonstrated disease progression on or after the last therapies. For patients with a prior autologous stem cell transplantation, the time to progression should be at least 3 years from transplantation. Pepaxti® is the trademark for melphalan flufenamide in Europe, the trademark in the US is Pepaxto®.
About anti-CD38 mAbs
Anti–CD38 monoclonal antibodies (mAbs) are targeting the CD38 antigen on plasma cells in multiple myeloma. The treatments have a distinct mode of action and have an immunomodulatory effect provided by the depletion of CD 38 immunosuppressive immune cell populations. The products can be used as monotherapy or in combination therapy, in the relapsed setting as well as in earlier lines of therapy. The monotherapy of anti-CD38 monoclonal antibodies with steroid support as studied in the LIGHTHOUSE study currently represents 30-40 % of anti-CD38 prescription in the US in RRMM (1+prior line of therapy). European use of anti-CD38 monoclonal antibody therapy is similar (Source IntrinsiQ IMATS, 2021).
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