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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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Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts
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225Ac-H4py4pa for Targeted Alpha Therapy.

Lily Li1,2, Julie Rousseau3, María de Guadalupe Jaraquemada-Peláez1

  • 1Medicinal Inorganic Chemistry Group, Department of Chemistry, University of British Columbia, 2036 Main Mall, Vancouver, British Columbia V6T 1Z1, Canada.

Bioconjugate Chemistry
|March 29, 2020
PubMed
Summary

A new chelator, H4py4pa, shows high affinity for Actinium-225 for targeted alpha therapy (TAT). Conjugated to Trastuzumab, it demonstrates excellent in vivo stability and tumor specificity, outperforming DOTA-based conjugates.

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Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction
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Area of Science:

  • Radiochemistry and Nuclear Medicine
  • Bioconjugation Chemistry
  • Cancer Therapeutics

Background:

  • Targeted alpha therapy (TAT) offers a promising approach for cancer treatment.
  • Development of novel chelators is crucial for stable radiometal complexation in TAT.
  • Monoclonal antibodies like Trastuzumab are vital for targeted delivery to HER2+ cancers.

Purpose of the Study:

  • To synthesize and characterize a new undecadendate chelator, H4py4pa, and its bifunctional analog.
  • To evaluate the chelator's affinity and stability with Actinium-225 (225Ac) for TAT.
  • To conjugate the bifunctional chelator to Trastuzumab and assess its in vivo performance for HER2+ cancer targeting.

Main Methods:

  • Synthesis and characterization of H4py4pa and H4py4pa-phenyl-NCS.
  • Radiolabeling studies with 225Ac under optimized conditions (ambient temperature, pH 7).
  • Bioconjugation of H4py4pa-phenyl-NCS to Trastuzumab via a phenyl-NCS linker.
  • In vitro serum stability assays and in vivo biodistribution studies in animal models.
  • Comparison with DOTA-benzyl-Trastuzumab conjugate.

Main Results:

  • H4py4pa demonstrated quantitative radiolabeling yield with 225Ac at ambient conditions.
  • The 225Ac-H4py4pa complex exhibited high stability in mouse serum for at least 9 days.
  • Density functional theory (DFT) calculations and lanthanum (La3+) complexation confirmed high symmetry and stability of the [La(py4pa)]- complex.
  • The H4py4pa-Trastuzumab conjugate showed excellent in vivo stability and tumor specificity, comparable to DOTA-benzyl-Trastuzumab.
  • The bifunctional py4pa precursor allows facile bioconjugation through nucleophilic substitution.

Conclusions:

  • H4py4pa is a highly effective chelator for 225Ac, suitable for TAT.
  • The H4py4pa-Trastuzumab conjugate exhibits promising characteristics for HER2+ cancer targeted therapy.
  • The chelator's design offers versatility for developing novel radiopharmaceuticals.