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

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.