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Related Concept Videos

Targeted Cancer Therapies02:57

Targeted Cancer Therapies

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The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
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Optimization Processes of Clinical Chelation-Based Radiopharmaceuticals for Pathway-Directed Targeted Radionuclide

Katsumi Tomiyoshi1, Lydia J Wilson2, Firas Mourtada2

  • 1Shonan Research Institute of Innovative Medicine, Shonan Kamakura General Hospital, Kamakura 247-8533, Japan.

Pharmaceutics
|November 27, 2024
PubMed
Summary

Targeted radionuclide therapy (TRT) offers precision medicine for cancer, improving tumor control and patient survival. Advances in radiopharmaceuticals, dosimetry, and imaging enhance TRT efficacy and safety.

Keywords:
177Lu225Acchelationdosimetryimagingtheranostics

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Area of Science:

  • Nuclear medicine
  • Radiopharmaceutical chemistry
  • Oncology

Background:

  • Targeted radionuclide therapy (TRT) is revolutionizing precision medicine by enhancing tumor control and patient survival.
  • Theranostic-paired TRT, combined with correlative analyses, shows significant potential for managing malignant diseases.
  • Chelation chemistry is fundamental for developing effective theranostic radiopharmaceuticals for TRT.

Purpose of the Study:

  • To review the latest advancements in chelation-based theranostic radiopharmaceuticals for TRT.
  • To discuss improvements in micro-dosimetry for refining dose-response evaluations.
  • To highlight the role of SPECT/CT technologies and cytogenetic analyses in TRT.

Main Methods:

  • Review of current diagnostic (e.g., 68Ga, 99mTc) and therapeutic (e.g., 177Lu, 225Ac) radionuclides for TRT.
  • Analysis of chelation chemistry challenges, including radionuclide production and daughter radionuclide toxicity.
  • Exploration of micro-dosimetry modeling and SPECT/CT technologies for treatment monitoring.

Main Results:

  • 177Lu and 225Ac are promising for beta and alpha TRT, respectively, due to favorable properties for clinical use.
  • Challenges remain in optimizing radionuclide production, ensuring chelation stability, and refining micro-dosimetry.
  • Current TRT delivery relies on empirical activity levels, leading to variable outcomes and toxicities.

Conclusions:

  • Optimizing chelation chemistry and micro-dosimetry is crucial for advancing theranostic radiopharmaceuticals.
  • Enhanced imaging and correlative analyses are essential for personalized TRT and improved patient outcomes.
  • Further research is needed to overcome challenges in radionuclide production and minimize treatment-related toxicities.