LAG-3 Emerging As Next Generation Immune Checkpoint Inhibitor Immunotherapy

Release Date: 06-Feb-2023

Global LAG-3 Inhibitor Market, Drug Sales, Price and Clinical Trials Insight 2028 Report highlights:



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In the last few decades, many different immunotherapies have reformed cancer therapeutics landscape. However, the quest for exploring the potential of different cancer antigens as targets never stopped, as a result of which many new protein targets have been identified. The LAG-3 is one such protein which has been getting a lot of attention in the last few years and the recent approval of the first LAG-3 inhibitor has only fueled the research and developmental activities. The commercial performance of this LAG-3 inhibitor points towards a promising future for LAG-3 inhibitors and many pharmaceutical companies are working to exploit this new-found protein.


The lymphocyte-activation gene 3, commonly known as the LAG-3, is another immune checkpoint whose role has been identified in prevalent diseases including cancer and autoimmune diseases, which has helped bring it into the limelight for drug development. At present, only one LAG-3 inhibitor has been granted marketing approval. Opdualag, which is a fix-dose cocktail containing nivolumab and relatlimab-rmbw, was developed by Bristol Myers’ Squibb and was granted regulatory approval in the US and EU months apart in 2022. While nivolumab (Opdivo) is a blockbuster PD-1 inhibitor developed and marketed by Bristol Myers’ Squibb, relatlimab-rmbw (Relatlimab) is a novel LAG-3 inhibitor which was first developed by Ono Pharmaceutical and later licensed to Bristol Myers’ Squibb.


Opdualag was granted approval by the FDA in March 2022 and its sales have been increasing every quarter. Its sales in the first quarter amounted to only US$ 6 Million but increased drastically to US$ 252 Million by the end of 2022. Sales climbed by 24% from the third to the fourth quarter, going from US$ 84 Million to US$ 104 million, demonstrating the market's overall expansion and success for a novel drug. The successful commercial stint it pulled off in its first year itself has encouraged research and the development of more LAG-3 targeted drugs which utilize a variety of modalities such as antibodies, small molecule inhibitors and also fusion proteins. 


As per our report findings, Fianlimab developed by Regeneron is the most LAG-3 targeting drug in the pipeline. The drug is being evaluated in a phase III clinical study in patients with melanoma and in a phase I trial in combination with a PD-1 inhibitor for solid tumors. Some other drugs in the pipeline include FS118, Sym022, TSR-033 and LBL-007 which are being developed by pharmaceutical companies around the world including Avacta, Bristol Myers’ Squibb, Novartis, Immutep, F-Star Therapeutics and Merck.


Efti (eftilagimod alpha) is a particular drug candidate that has been getting attention for its unique mechanism of action compared to other drugs in the pipeline. It is an antigen-presenting cell activator made from the soluble version of LAG-3 and aimed to increase immune response to tumors. Efti has been developed by Immutep and in addition to evaluating the drug in monotherapies, Immutep has also partnered with Merck to assess its asset in combination with Avelumab, a PD-1 inhibitor made under collaboration between Merck and Pfizer. This INSIGHT-005 will be jointly funded by both companies and will be carried out at the Institute of Clinical Cancer Research, Krankenhaus Nordwest in Germany. Recently, Efti was also granted the Fast Track Designation by the FDA in combination with Keytruda for treating patients with late stage NSCLC.


It is evident that several notable drugs are in the pipeline which also demonstrates how far cancer therapeutic research has come from using systematic conventional therapies to developing drugs targeting the LAG-3, a protein which was not being considered as a viable target until recently. The clinical pipeline had been growing modestly but with the approval and success of Opdualag, inhibition of the LAG-3 has emerged as a potential therapeutic approach for not only drug makers but also patients who have been unresponsive to previous treatments. The combination therapy of PD-1 and LAG-3 inhibition has generated a lot of interested in the recent years and it is anticipated that with the growing interest in LAG-3 inhibition, novel combinations and innovating LAG-3 targeting approaches will be heard of in the coming years.



Neeraj Chawla

Kuick research

Research Head


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