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Emerging PET Imaging Agents and Targeted Radioligand Therapy: A Review of Clinical Applications and Trials

Maierdan Palihati1, Jeeban Paul Das2, Randy Yeh2

  • 1Department of Radiology, Columbia University Irving Medical Center, 622 W 168th St., New York, NY 10032, USA.

Tomography (Ann Arbor, Mich.)
|August 27, 2025
PubMed

Insights

Emerging targeted radioligand therapies show promise for imaging multiple cancers, potentially surpassing 18F-FDG PET scans. These advanced agents offer new theranostic options for various tumor types and stages.

Area of Science:

  • Oncology
  • Nuclear Medicine
  • Radiopharmaceutical Development

Background:

  • Targeted radioligand therapy (RLT) is a rapidly advancing anticancer treatment modality.
  • Current RLT focuses on somatostatin receptors and prostate-specific membrane antigen (PSMA), but new agents are emerging for other targets.
  • Advanced radioconjugation and molecular targeting are driving the development of novel theranostic combinations.

Purpose of the Study:

  • To review recent data on emerging molecularly targeted positron emission tomography (PET) imaging agents.
  • To highlight the clinical applications and potential of these novel agents, including companion radiotherapeutics.
  • To provide a primer for radiologists on understanding new PET agents, their regulatory status, challenges, and future opportunities.

Main Methods:

  • Review of recent clinical trial data for emerging targeted PET imaging agents.
  • Inclusion of exemplar clinical images for agents targeting fibroblast activation protein (FAP), hypoxia markers, gastrin-releasing peptide receptors (GRPrs), and integrins.
  • Assessment of potential superiority over 18F-fluorodeoxyglucose (18F-FDG) based on early clinical findings.

Main Results:

  • Several novel radiopharmaceuticals targeting FAP, hypoxia, GRPrs, and integrins show potential for imaging multiple cancer types.
  • Early clinical trials suggest some agents may outperform 18F-FDG in PET imaging.
  • These agents are progressing to clinical trials and may significantly impact PET imaging and cancer treatment.

Conclusions:

  • Emerging targeted PET imaging agents offer new theranostic possibilities across various cancers.
  • These novel radiopharmaceuticals have the potential to become superior alternatives to 18F-FDG for PET imaging.
  • Understanding these agents is crucial for radiologists and nuclear medicine clinicians to leverage their full therapeutic and diagnostic potential.
Keywords:
clinical trialsfibroblast activation protein (FAP)gastrin-releasing peptide receptors (GRPrs)hypoxiaintegrinsradiopharmaceuticals

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