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E7449 + temozolomide is a **combination therapy** under clinical investigation for cancer treatment, comprising E7449—a small molecule dual inhibitor of poly(ADP-ribose) polymerase 1/2 (PARP1/2) and tankyrase 1/2 (TNKS1/2), and temozolomide, an oral alkylating chemotherapy agent. E7449 inhibits DNA repair mechanisms and disrupts Wnt/β-catenin signaling, thereby enhancing the cytotoxicity of DNA-damaging agents like temozolomide. The combination synergistically potentiates antitumor activity, demonstrated in preclinical melanoma models and evaluated in Phase 1/2 studies for advanced solid tumors and melanoma[3][5]. E7449 is developed by Eisai; temozolomide is off-patent and produced by multiple manufacturers.
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