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Updated: Aug 15, 2025

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
Advances in pharmacokinetics and pharmacodynamics of PD-1/PD-L1 inhibitors
Ting Yan1, Lun Yu2, Dangang Shangguan1
1Department of Pharmacy, Hunan Cancer Hospital, the Affiliated Cancer Hospital of Xiangya School of Medicine, Central South University, Changsha 410011, China.
Abstract:
Immune checkpoint inhibitors (ICIs) are a group of drugs designed to improve the therapeutic effects on various types of malignant tumors. Irrespective of monotherapy or combinational therapies as first-line and later-line therapy, ICIs have achieved benefits for various tumors. Programmed cell death protein-1 (PD-1) / ligand 1 (PD-L1) is an immune checkpoint that suppresses antitumor immunity, especially in the tumor microenvironment (TME). PD-1/PD-L1 immune checkpoint inhibitors block tumor-related downregulation of the immune system, thereby enhancing antitumor immunity. In comparison with traditional small-molecule drugs, ICIs exhibit pharmacokinetic characteristics owing to their high molecular weight. Furthermore, different types of ICIs exhibit different pharmacodynamic characteristics. Hence, ICIs have been approved for different indications by the Food and Drug Administration (FDA) and National Medical Products Administration (NMPA). This review summarizes pharmacokinetic and pharmacodynamic studies of PD-1/ PD-L1 inhibitors to provide a reference for rational clinical application.
Insights
Immune checkpoint inhibitors (ICIs), particularly targeting PD-1/PD-L1, enhance antitumor immunity. This review details their pharmacokinetics and pharmacodynamics for optimal clinical use in cancer therapy.
Area of Science:
- Oncology
- Immunology
- Pharmacology
Background:
- Immune checkpoint inhibitors (ICIs) are crucial in cancer therapy, improving outcomes across various malignancies.
- The programmed cell death protein-1 (PD-1) / ligand 1 (PD-L1) pathway is a key target for enhancing antitumor immunity within the tumor microenvironment (TME).
Purpose of the Study:
- To review pharmacokinetic and pharmacodynamic properties of PD-1/PD-L1 inhibitors.
- To provide a reference for the rational clinical application of these immunotherapies.
Main Methods:
- Literature review of pharmacokinetic and pharmacodynamic studies on PD-1/PD-L1 inhibitors.
- Analysis of drug characteristics, including molecular weight and specific pharmacodynamic profiles.
Main Results:
- ICIs, including PD-1/PD-L1 inhibitors, demonstrate significant benefits in monotherapy and combination therapies.
- Distinct pharmacokinetic and pharmacodynamic profiles exist among different ICIs.
- Regulatory approvals by FDA and NMPA highlight the efficacy of ICIs for various indications.
Conclusions:
- Understanding the pharmacokinetics and pharmacodynamics of PD-1/PD-L1 inhibitors is essential for effective clinical application.
- This review serves as a guide for optimizing the use of these immunotherapies in cancer treatment.
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