Clinical Insights Into Novel Immune Checkpoint Inhibitors

Jii Bum Lee, Sang Jun Ha, Hye Ryun Kim

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58 Citations (Scopus)


The success of immune checkpoint inhibitors (ICIs), notably anti-cytotoxic T lymphocyte associated antigen-4 (CTLA-4) as well as inhibitors of CTLA-4, programmed death 1 (PD-1), and programmed death ligand-1 (PD-L1), has revolutionized treatment options for solid tumors. However, the lack of response to treatment, in terms of de novo or acquired resistance, and immune related adverse events (IRAE) remain as hurdles. One mechanisms to overcome the limitations of ICIs is to target other immune checkpoints associated with tumor microenvironment. Immune checkpoints such as lymphocyte activation gene-3 (LAG-3), T cell immunoglobulin and ITIM domain (TIGIT), T cell immunoglobulin and mucin-domain containing-3 (TIM-3), V-domain immunoglobulin suppressor of T cell activation (VISTA), B7 homolog 3 protein (B7-H3), inducible T cell costimulatory (ICOS), and B and T lymphocyte attenuator (BTLA) are feasible and promising options for treating solid tumors, and clinical trials are currently under active investigation. This review aims to summarize the clinical aspects of the immune checkpoints and introduce novel agents targeting these checkpoints.

Original languageEnglish
Article number681320
JournalFrontiers in Pharmacology
Publication statusPublished - 2021 May 6

Bibliographical note

Funding Information:
This work was supported by National Research Foundation of Korea (NRF) grants funded by the Korean Government (MSIT) (NRF-2017M3A9E9072669, 2017M3A9E8029717, NRF-2019M3A9B6065231, 2019M3A9B6065221, 2018R1A2A1A05076997, 2017R1A5A1014560).

Publisher Copyright:
© Copyright © 2021 Lee, Ha and Kim.

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)


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