Target intelligence / Profile preview

Lymphocyte activation gene 3 receptor (LAG-3)

Target
LAG-3
Molecular classification
Receptor, Immune checkpoint receptor, Cell surface protein
01

Overview

Lymphocyte activation gene 3 receptor (**LAG‑3**, also known as **CD223**) is an immune checkpoint receptor expressed on activated T cells and some other immune cells. It functions primarily as an inhibitory regulator of the immune response by delivering negative signals upon binding to its ligands—most notably MHC class II molecules and FGL1—thereby suppressing T cell proliferation, cytokine secretion, and cytotoxic activity. This mechanism helps maintain self-tolerance but can be exploited by tumors to evade the immune system. As a result, LAG‑3 has become a major therapeutic target in cancer immunotherapy; both antagonists that block its function to boost anti-tumor immunity and agonists that enhance its inhibitory effect for autoimmune diseases are under active development. Drugs targeting this pathway include relatlimab (an antagonist antibody), IMP321/eftilagimod alpha (a soluble fusion protein), and GSK2831781 (an agonist antibody). The safety profile is similar to other checkpoint inhibitors with risks related to overactivation or suppression of the immune system depending on the therapeutic approach.[1][2]

Other names
CD223LAG3Lymphocyte activating 3 proteinFDC (less common)
02

Mechanism of action

Antagonist antibodies block inhibitory signaling to enhance anti-tumor immunity by reactivating effector T cells and inhibiting regulatory T cell suppression.

03

Biological functions

Immune response regulationInhibition of T cell activation and proliferationMaintenance of immune tolerance (via regulatory T cells)Negative regulation of dendritic cell activation
04

Disease associations

Cancer (immune evasion, target for immunotherapy)Autoimmune disease (regulation and potential therapeutic target)
05

Safety considerations

Immune-related adverse events typical of checkpoint inhibition therapies such as autoimmunity or excessive immune activation may occur. Combination with other checkpoint inhibitors can increase risk
06

Interacting drugs

Relatlimab (anti-LAG3 monoclonal antibody, clinical trials for cancer)

2 more in the full profile.

07

Biomarkers

LAG3 expression on tumor-infiltrating lymphocytes is being explored as a biomarker for patient selection in immunotherapy clinical trials; however, no universally established companion diagnostic exists yet

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