Therapeutic potential of targeting LAG-3 in cancer

Immune checkpoint inhibitors targeting negative regulatory checkpoints including programmed death-1 (PD-1) and cytotoxic T-lymphocyte-associated protein 4 have produced significant improvements in progression-free survival (PFS) and overall survival in multiple solid tumors. Lymphocyte activation ge...

Full description

Saved in:
Bibliographic Details
Main Authors: Diwakar Davar, Ana Carrizosa Anderson, Ivan Diaz-Padilla
Format: Article
Language:English
Published: BMJ Publishing Group 2025-07-01
Series:Journal for ImmunoTherapy of Cancer
Online Access:https://jitc.bmj.com/content/13/7/e011652.full
Tags: Add Tag
No Tags, Be the first to tag this record!
_version_ 1850116621243252736
author Diwakar Davar
Ana Carrizosa Anderson
Ivan Diaz-Padilla
author_facet Diwakar Davar
Ana Carrizosa Anderson
Ivan Diaz-Padilla
author_sort Diwakar Davar
collection DOAJ
description Immune checkpoint inhibitors targeting negative regulatory checkpoints including programmed death-1 (PD-1) and cytotoxic T-lymphocyte-associated protein 4 have produced significant improvements in progression-free survival (PFS) and overall survival in multiple solid tumors. Lymphocyte activation gene 3 (LAG-3) is an inhibitory receptor that is highly expressed by exhausted T cells. Dual blockade of LAG-3 and PD-1 with monoclonal antibodies relatlimab and nivolumab has improved PFS in advanced melanoma, leading to Food and Drug Administration approval for this indication. Concurrently, enthusiasm for targeting LAG-3 has been tempered by negative results in multiple indications, although novel approaches including LAG-3-directed bispecifics tebotelimab continue to demonstrate promise. In this review, we discuss the current understanding of LAG-3 in regulating antitumor immunity and the ongoing state of clinical development of LAG-3-directed agents in cancer.
format Article
id doaj-art-6c83ebef901f42569cb2d812758aa866
institution OA Journals
issn 2051-1426
language English
publishDate 2025-07-01
publisher BMJ Publishing Group
record_format Article
series Journal for ImmunoTherapy of Cancer
spelling doaj-art-6c83ebef901f42569cb2d812758aa8662025-08-20T02:36:16ZengBMJ Publishing GroupJournal for ImmunoTherapy of Cancer2051-14262025-07-0113710.1136/jitc-2025-011652Therapeutic potential of targeting LAG-3 in cancerDiwakar Davar0Ana Carrizosa Anderson1Ivan Diaz-Padilla2Department of Medicine, UPMC Hillman Cancer Center, Pittsburgh, Pennsylvania, USAHarvard Medical School, Boston, Massachusetts, USAOncology Global Clinical Development, GSK, Baar, SwitzerlandImmune checkpoint inhibitors targeting negative regulatory checkpoints including programmed death-1 (PD-1) and cytotoxic T-lymphocyte-associated protein 4 have produced significant improvements in progression-free survival (PFS) and overall survival in multiple solid tumors. Lymphocyte activation gene 3 (LAG-3) is an inhibitory receptor that is highly expressed by exhausted T cells. Dual blockade of LAG-3 and PD-1 with monoclonal antibodies relatlimab and nivolumab has improved PFS in advanced melanoma, leading to Food and Drug Administration approval for this indication. Concurrently, enthusiasm for targeting LAG-3 has been tempered by negative results in multiple indications, although novel approaches including LAG-3-directed bispecifics tebotelimab continue to demonstrate promise. In this review, we discuss the current understanding of LAG-3 in regulating antitumor immunity and the ongoing state of clinical development of LAG-3-directed agents in cancer.https://jitc.bmj.com/content/13/7/e011652.full
spellingShingle Diwakar Davar
Ana Carrizosa Anderson
Ivan Diaz-Padilla
Therapeutic potential of targeting LAG-3 in cancer
Journal for ImmunoTherapy of Cancer
title Therapeutic potential of targeting LAG-3 in cancer
title_full Therapeutic potential of targeting LAG-3 in cancer
title_fullStr Therapeutic potential of targeting LAG-3 in cancer
title_full_unstemmed Therapeutic potential of targeting LAG-3 in cancer
title_short Therapeutic potential of targeting LAG-3 in cancer
title_sort therapeutic potential of targeting lag 3 in cancer
url https://jitc.bmj.com/content/13/7/e011652.full
work_keys_str_mv AT diwakardavar therapeuticpotentialoftargetinglag3incancer
AT anacarrizosaanderson therapeuticpotentialoftargetinglag3incancer
AT ivandiazpadilla therapeuticpotentialoftargetinglag3incancer