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**PEN-866 + niraparib** is an investigational combination therapy featuring two components. PEN-866 is a miniature drug conjugate comprising a camptothecin payload linked to a targeting molecule, typically designed to deliver cytotoxic activity to tumors, while niraparib is a small molecule inhibitor of poly(ADP-ribose) polymerase (PARP), a DNA repair enzyme. The combination is intended to leverage DNA damage from camptothecin delivered by PEN-866 and potentiate its effect by inhibiting repair via PARP blockade from niraparib. This approach aims to enhance antitumor efficacy, particularly in cancers with homologous recombination repair deficiencies or increased sensitivity to DNA damage.
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