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Identifying PD-1/PD-L1 Inhibitors with Surface Plasmon Resonance Technology
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Identification of an Inhaled Pulmonary Selective PDGFR Inhibitor with Sustained Target Engagement.

Glenn Marsboom1, Tianbao Lu2, Zhigang Hong1

  • 1Pulmonary Hypertension Therapeutic Area, Research & Development, Johnson & Johnson Innovative Medicine, Spring House, Pennsylvania, USA.

Journal of Aerosol Medicine and Pulmonary Drug Delivery
|May 8, 2026
PubMed
Summary
This summary is machine-generated.

Researchers developed a novel inhaled platelet-derived growth factor receptor (PDGFR) inhibitor for pulmonary diseases. This optimized compound demonstrates extended lung retention, minimizing systemic exposure and offering a new therapeutic strategy.

Keywords:
inhaled drug deliverylung retentionnebulizationpulmonary disease

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Published on: July 17, 2020

Area of Science:

  • Pulmonary pharmacology
  • Drug discovery
  • Receptor tyrosine kinase (RTK) inhibition

Background:

  • Inhaled corticosteroids, bronchodilators, antivirals, and antibiotics are established treatments for pulmonary diseases.
  • Receptor tyrosine kinases (RTKs) play a crucial role in pulmonary diseases, yet no inhaled RTK inhibitors are approved.
  • This study focuses on developing an inhaled platelet-derived growth factor receptor (PDGFR) inhibitor for lung conditions.

Purpose of the Study:

  • To identify, optimize, and derisk an inhaled PDGFR inhibitor with sustained lung activity.
  • To establish a roadmap for developing inhaled RTK inhibitors for pulmonary diseases.
  • To minimize systemic effects by enhancing lung retention.

Main Methods:

  • Utilized stable isotopes for in vivo receptor turnover modeling.
  • Generated high-resolution crystal structures for structure-based drug design.
  • Identified physicochemical parameters for lung retention and developed a cell painting assay to eliminate non-specific compounds.

Main Results:

  • Optimized nebulized delivery for deep lung administration.
  • Achieved >90% PDGFR inhibition for at least 6 hours post-nebulization in rats at a 1 mg/kg dose.
  • Modeled projected human dosage for the developed inhibitor.

Conclusions:

  • The developed inhaled PDGFR inhibitor shows promise for treating pulmonary diseases.
  • The methodology for creating a potent inhaled compound with extended lung retention can be applied to other RTK drug discovery efforts.
  • This approach facilitates targeted lung delivery, minimizing systemic side effects.