LAG-3 antagonists for cancer treatment: an updated patent review (2020-2025)

Martín Pérez-Santos1, Gerardo Landeta1, Maricruz Anaya-Ruiz2

  • 1Dirección de Innovación y Transferencia de Conocimiento, Benemérita Universidad Autónoma de Puebla, Puebla, México.

Abstract

Insights

The patent landscape reveals that monospecific antibodies are the leading LAG-3 antagonists, with several new drugs like encelimab and miptenalimab emerging. This highlights ongoing advancements in targeting Lymphocyte-activation gene 3 (LAG-3) for cancer therapy.

Area of Science:

  • Immunology
  • Oncology
  • Intellectual Property Law

Background:

  • Lymphocyte-activation gene 3 (LAG-3) is overexpressed on tumor-infiltrating CD4+ and CD8+ cells.
  • LAG-3 inhibits T-cell activation and the production of crucial cytokines like IL-2 and IFN-γ.

Purpose of the Study:

  • To generate a comprehensive patent landscape analysis of Lymphocyte-activation gene 3 (LAG-3) antagonists.
  • To categorize and identify emerging therapeutic strategies targeting LAG-3.

Main Methods:

  • A systematic search of patent databases including USPTO, EPO, WIPO, JPO, SIPO, and KIPO.
  • Categorization of LAG-3 antagonists into monospecific antibodies, multispecific antibodies, peptides, and small molecules.

Main Results:

  • Monospecific anti-LAG-3 antibodies represent the dominant class of antagonists.
  • Several new monospecific (encelimab, miptenalimab) and bispecific antibodies (e.g., tobemstomig, IBI323) have been patented.
  • The patent landscape also includes LAG-3 binding peptides and small molecules.

Conclusions:

  • Monospecific antibodies remain the primary focus for LAG-3 antagonism development.
  • The identified antibodies and other therapeutics show significant potential for novel cancer treatments targeting the tumor microenvironment.

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