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Updated: Jul 16, 2026

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Deciphering LAG-3: unveiling molecular mechanisms and clinical advancements
Alejandra Martínez-Pérez1,2,3, Rocío Granda-Díaz1,2,3, Candelaria Aguilar-García1,2,3
1Department of Functional Biology, Immunology, Universidad de Oviedo, Oviedo, Spain.
Abstract:
Treatment based on immune checkpoint blockade has revolutionized cancer therapy. Despite the remarkable success achieved and the preclinical development of multiple checkpoint inhibitors targeting other checkpoints, only antibodies targeting the PD-1/PD-L1 axis and CTLA-4 have been approved for patient treatment, especially in solid tumors. Currently, with the approval of relatlimab, a LAG-3 blocking antibody, a third player, has been used in the fight against cancer. The endorsement of relatlimab marks a significant milestone in cancer immunotherapy, opening new avenues for combination therapies and enhancing treatment outcomes. However, the complex biology of LAG-3 may hinder its full development as a therapeutic alternative. In this review, we provide in-depth insight into the biology of LAG-3 and its current and future development in cancer treatment.
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