主要原理是使用高專一性的單株抗體直接結合到腫瘤細胞特有的蛋白質或是細胞激素，影響腫瘤細胞的生長、引起免疫系統反應或是其他功能。已經發展的藥物有針對乳癌的曲妥珠單抗和針對白血病的吉妥單抗在臨床使用。治療某些白血病和淋巴瘤則需要使用高劑�

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