ArticleJournal for immunotherapy of cancer2026
Fluorination augments tumor engagement and antitumor immunity of a D-peptide-based radiotheranostic agent for combinatorial immune checkpoint blockade therapy.
Article in Journal for immunotherapy of cancer, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
backgroundProgrammed death-ligand 1 (PD-L1)-targeted radiopharmaceutical therapy (RPT) combined with immune checkpoint blockade (ICB) represents a promising combinatorial treatment because of the "magic" bystander and abscopal effects of RPT. However, the overall efficacy of this combinatorial approach is often constrained by limited tumor retention and insufficient accumulation of existing radiopharmaceuticals. D-peptides, with their superior metabolic stability, offer a promising modality to overcome these limitations. We previously reported [
methodsHerein, fluorine modification-directed rational design was used to optimize DPA's target engagement and retention, thereby boosting its immune-activating potential in RPT. Following two rounds of screening, a series of fluorinated D-peptides was synthesized. Their in vivo performance was assessed by positron emission tomography (PET)/CT imaging in tumor-bearing mice and subsequently in patients with cancer. The therapeutic efficacy of the corresponding
results[
conclusionThis study highlights the potential of fluorinated D-peptide radiopharmaceuticals as powerful PD-L1 targeting radiotheranostics, enabling more effective systemic antitumor efficacy in RPT and ICB combination therapy.
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