Approaches for development of LAG-3 inhibitors and the promise they hold as anticancer agents

Introduction: LAG-3 is considered to be the third point of immunological control in relation to clinical trials that address Cancer treatment, only behind PD-1 and CTLA-4, due to its role as a suppressor of the immune response and enhancer of differentiation of Treg cells.

Areas covered: The authors focus on emphasizing the strategy of development of LAG-3 inhibitors to develop Anticancer therapeutics, especially from the perspective of designing new monoclonal and bispecific Antibodies against LAG-3. This article also covers details of patents and clinical trials of LAG-3 inhibitors reported in the literature. In addition, we highlight as future research challenges the design and development of Peptides and small molecules as inhibitors of LAG-3 function.

Expert opinion: Three approaches have been used for the development of LAG-3 inhibitors, and they include inhibitory LAG-3 binding Peptides and antagonist monoclonal and multispecific Antibodies. These approaches include more than 100 clinical trials of 21 molecules that bind to LAG-3 and block its binding to MHC II. However, these approaches do not cover the design and development of Peptides and small molecules that could inhibit the function of LAG-3, for which it is necessary to develop new alternatives that cover this gap.

LAG-3; antibodies; cancer; clinical trials; inhibitors; patents.