Monitoring the Response of PD-L1 Expression to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Nonsmall-Cell Lung Cancer Xenografts by Immuno-PET Imaging

Mol Pharm. 2019 Aug 5;16(8):3469-3476. doi: 10.1021/acs.molpharmaceut.9b00307. Epub 2019 Jul 8.

Abstract

Accumulating evidence has suggested that the tumor microenvironment of nonsmall-cell lung cancer (NSCLC) may be impacted by chemotherapy, radiotherapy, or epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs). PD-L1 is an important biomarker in the tumor microenvironment that can predict patient response to immunotherapies. Therefore, it is highly desirable to achieve a real-time, noninvasive assessment of PD-L1 expression, which can provide critical information for recruiting patients as well as monitoring therapeutic efficacy. We herein studied the EGFR-TKI-induced effects on PD-L1 levels in NSCLC tumor models using immuno-PET imaging with 89Zr-Df-KN035, an imaging tracer previously established by our group. A549 human NSCLC xenografts were established in BALB/c nude mice and treated with different doses of an EGFR-TKI gefitinib. PET imaging with 89Zr-Df-KN035 was performed before and after the treatment to evaluate PD-L1 expression, which was further verified by immunohistochemical staining. Our results demonstrate that 89Zr-Df-KN035 can specifically evaluate PD-L1 levels in NSCLC tumor models. Compared to the untreated control, the high dose of gefitinib inhibited tumor growth and lowered the tumor uptake of 89Zr-Df-KN035. In comparison, the low dose of gefitinib did not affect tumor growth, although the extensive tumor necrosis also led to the lower uptake of 89Zr-Df-KN035. In conclusion, our results demonstrate that immuno-PET imaging with 89Zr-Df-KN035 is a promising tool to noninvasively monitor PD-L1 expression in NSCLC treated with EGFR-TKIs and can be used to optimize treatment plans for immunotherapy.

Keywords: EGFR-TKIs; NSCLC; PD-L1; PET imaging.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • A549 Cells
  • Animals
  • B7-H1 Antigen / analysis*
  • B7-H1 Antigen / immunology
  • B7-H1 Antigen / metabolism
  • Carcinoma, Non-Small-Cell Lung / diagnostic imaging
  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Non-Small-Cell Lung / pathology
  • Dose-Response Relationship, Drug
  • Down-Regulation / drug effects
  • Drug Monitoring / methods*
  • Drug Resistance, Neoplasm
  • ErbB Receptors / antagonists & inhibitors
  • Gefitinib / pharmacology
  • Gefitinib / therapeutic use
  • Humans
  • Immunotherapy / methods
  • Lung Neoplasms / diagnostic imaging
  • Lung Neoplasms / drug therapy*
  • Lung Neoplasms / pathology
  • Mice
  • Mice, Nude
  • Molecular Imaging / methods
  • Positron-Emission Tomography / methods
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use
  • Radioactive Tracers
  • Radioisotopes / administration & dosage
  • Tumor Microenvironment / drug effects
  • Xenograft Model Antitumor Assays
  • Zirconium / administration & dosage

Substances

  • B7-H1 Antigen
  • CD274 protein, human
  • Protein Kinase Inhibitors
  • Radioactive Tracers
  • Radioisotopes
  • Zirconium
  • EGFR protein, human
  • ErbB Receptors
  • Zirconium-89
  • Gefitinib