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177Lu-DOTA-EB-FAPI is a novel fibroblast activation protein (FAP)-targeted radiopharmaceutical that combines the therapeutic potential of lutetium-177 with enhanced tumor retention properties. It incorporates Evans Blue (EB) structure which allows reversible binding with serum albumin, significantly improving its pharmacokinetics and pharmacodynamics compared to conventional FAPI radiopharmaceuticals. This modification addresses a major limitation of standard 177Lu-DOTA-FAPI compounds - their short half-life and rapid clearance from the body. The radiopharmaceutical targets fibroblast activation protein (FAP), which is highly expressed in cancer-associated fibroblasts (CAFs) found in the majority of cancer types. Early clinical trials have shown promising results in patients with various end-stage metastatic cancers, particularly in radioiodine-refractory thyroid cancer.
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