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177Lu-ACT-101 is a targeted radiopharmaceutical therapeutic being developed by Alpha Cancer Technologies for the treatment of various cancers. It consists of ACT-101, a recombinant, non-glycosylated form of human alpha-fetoprotein (AFP), labeled with the beta-emitting radioisotope lutetium-177 (177Lu). The drug targets the alpha-fetoprotein receptor (AFPR), which is highly expressed on over 80% of cancer cells—including colorectal, ovarian, breast, prostate, and lung cancers—but is minimally present on healthy adult tissues. Upon binding to the AFPR, the radiopharmaceutical is internalized, delivering localized ionizing radiation directly to the tumor cells to induce DNA damage and cell death while sparing normal tissues. It is part of a theranostic platform that includes a corresponding diagnostic imaging agent, 89Zr-ACT-101.
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