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Updated: Apr 17, 2026

Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
Published on: May 2, 2025
Pembrolizumab: PD-1 inhibition as a therapeutic strategy in cancer
1Division of Medical Oncology, Department of Medicine, University of Colorado School of Medicine, Aurora, Colorado, USA.
Abstract:
Programmed cell death protein 1 (PD-1) and its ligands, programmed cell death 1 ligand 1 (PD-L1) and 2 (PD-L2) play an important role in regulating immune response through various mechanisms. This inhibitory action is thought to assist in immune evasion by cancer cells as PD-1, PD-L1 and PD-L2 have been found to be abnormally expressed by tumor cells and lymphocytes in the tumor microenvironment. Preclinical studies described PD-1 blockade resulting in tumor growth suppression and even decreased metastasis. This has led to the development of pembrolizumab (MK-3475), a highly selective, humanized monoclonal IgG4-kappa isotype antibody against PD-1. Early clinical trials have shown high tumor response rates and long duration of effect in previously treated advanced melanoma resulting in accelerated FDA approval for the drug in this situation. Pembrolizumab has also had success in non-small cell lung cancer and is being tested in multiple other tumor types. This review will discuss the development, preclinical data, pharmacokinetics and clinical efficacy to date of pembrolizumab.
Insights
Pembrolizumab, an antibody targeting Programmed Cell Death 1 (PD-1), shows significant promise in cancer treatment by blocking immune evasion. Clinical trials demonstrate high response rates and durable effects, particularly in advanced melanoma.
Area of Science:
- Immunology
- Oncology
- Pharmacology
Background:
- Programmed cell death protein 1 (PD-1) and its ligands (PD-L1, PD-L2) regulate immune responses.
- Abnormal expression of PD-1/PD-L1/PD-L2 in the tumor microenvironment facilitates cancer immune evasion.
- Preclinical studies indicated PD-1 blockade suppresses tumor growth and metastasis.
Purpose of the Study:
- To review the development of pembrolizumab, a humanized monoclonal antibody against PD-1.
- To discuss preclinical data, pharmacokinetics, and clinical efficacy of pembrolizumab.
- To highlight pembrolizumab's role in cancer immunotherapy.
Main Methods:
- Review of preclinical studies on PD-1 blockade.
- Analysis of early clinical trial data for pembrolizumab (MK-3475).
- Examination of pharmacokinetic and efficacy data in cancer patients.
Main Results:
- Pembrolizumab demonstrated high tumor response rates and long duration of effect in advanced melanoma.
- Accelerated FDA approval was granted for pembrolizumab in advanced melanoma.
- Successful outcomes observed in non-small cell lung cancer, with ongoing trials in other tumor types.
Conclusions:
- Pembrolizumab represents a significant advancement in cancer immunotherapy by targeting the PD-1 pathway.
- The drug has shown considerable clinical efficacy across various cancer types.
- Further investigation into pembrolizumab's therapeutic potential is warranted.
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