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Updated: Dec 7, 2025

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
Research Status and Outlook of PD-1/PD-L1 Inhibitors for Cancer Therapy
Leilei Ai1, Jian Chen1, Hao Yan1
1Center for Drug Safety Evaluation and Research of Zhejiang University, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, People's Republic of China.
Abstract:
PD-1/PD-L1 inhibitors are a group of immune checkpoint inhibitors as front-line treatment of multiple types of cancer. However, the serious immune-related adverse reactions limited the clinical application of PD-1/PD-L1 monoclonal antibodies, despite the promising curative effects. Therefore, it is urgent to develop novel inhibitors, such as small molecules, peptides or macrocycles, targeting the PD-1/PD-L1 axis to meet the increasing clinical demands. Our review discussed the mechanism of action of PD-1/PD-L1 inhibitors and presented clinical trials of currently approved PD-1/PD-L1 targeted drugs and the incidence of related adverse reactions, helping clinicians pay more attention to them, better formulate their intervention and resolution strategies. At last, some new inhibitors whose patent have been published are listed, which provide development ideas and judgment basis for the efficacy and safety of novel PD-1/PD-L1 inhibitors.
Insights
Novel inhibitors targeting the PD-1/PD-L1 axis are crucial for cancer treatment due to adverse reactions from current antibody therapies. This review explores PD-1/PD-L1 inhibitors, their clinical trials, and emerging alternatives.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- Programmed cell death protein 1 (PD-1)/programmed death-ligand 1 (PD-L1) inhibitors are vital in cancer immunotherapy.
- Current monoclonal antibody therapies show efficacy but are limited by immune-related adverse reactions (irAEs).
Purpose of the Study:
- To review the mechanism of action of PD-1/PD-L1 inhibitors.
- To present clinical trials and adverse reactions of approved PD-1/PD-L1 drugs.
- To highlight novel small molecule, peptide, and macrocycle inhibitors targeting the PD-1/PD-L1 axis.
Main Methods:
- Literature review of PD-1/PD-L1 inhibitors.
- Analysis of clinical trial data for approved PD-1/PD-L1 therapies.
- Survey of recently patented novel PD-1/PD-L1 inhibitors.
Main Results:
- PD-1/PD-L1 inhibitors offer significant therapeutic benefits across various cancers.
- Serious irAEs associated with PD-1/PD-L1 monoclonal antibodies necessitate careful clinical management.
- Emerging small molecules, peptides, and macrocycles present promising alternatives with potential for improved safety profiles.
Conclusions:
- There is an urgent need for novel PD-1/PD-L1 inhibitors to overcome the limitations of current antibody-based treatments.
- Understanding irAEs is critical for optimizing clinical application and management strategies.
- Newly patented inhibitors offer promising avenues for future cancer immunotherapy development.
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