[¹⁷⁷Lu]Lu-FAPI Radioligand Therapy: Emerging Horizons and Clinical Promise in Solid Tumors: A Comprehensive Review

Area of Science:

• Oncology
• Radiopharmaceutical Therapy
• Molecular Imaging

Background:

• Fibroblast Activation Protein (FAP) is highly expressed in cancer-associated fibroblasts (CAFs) across various solid malignancies.
• [177Lu]Lu-FAPI is a novel radioligand targeting FAP, offering a potential therapeutic strategy for difficult-to-treat cancers.

Purpose of the Study:

• To critically review the current clinical evidence on [177Lu]Lu-FAPI radioligand therapy (RLT).
• To outline available formulations, therapeutic efficacy, safety, advancements, challenges, and emerging applications of [177Lu]Lu-FAPI in oncology.

Main Methods:

• Comprehensive synthesis of existing clinical data on [177Lu]Lu-FAPI RLT.
• Analysis of preliminary studies and ongoing clinical trials exploring its therapeutic potential.

Main Results:

• [177Lu]Lu-FAPI demonstrates considerable promise as an effective and safe theranostic agent.
• It shows particular advantages in combination therapy approaches for various tumor types.
• Preliminary evidence suggests potential in treating difficult-to-treat solid malignancies.

Conclusions:

• Larger, well-controlled studies are essential to establish long-term efficacy and safety.
• [177Lu]Lu-FAPI is emerging as a valuable tool in oncological care and personalized medicine.
• Further investigation is needed to optimize its clinical integration and patient outcomes.