Project title: Preclinical Toxicity and Therapy Study of 225Ac-crown-TATE

Paul Schaffer, PhD University of British Columbia

Paul Schaffer, PhD
  • Status: Active
  • Year(s): 2021
  • Grant Type: Pilot
  • Research Type: Basic
  • Primary Tumor Site: Gastrointestinal
  • Area of Inquiry: Targeted Radionuclide Therapy


Schaffer and his team will study a new chelate, or compound, that holds the radionuclinde called Ac-225. They are testing whether Ac-225-crown-TATE compound can safely and effectively treat tumors and prolong the survival of tumor-bearing models.

What question will the researchers try to answer?

Targeted radionuclide therapy involves developing tumor-specific drugs that can carry particle-emitting radioactive isotopes to tumors. The accumulation of these radiopharmaceuticals that contain toxic radionuclides will cause targeted cell death while sparing surrounding healthy tissue. Actinium-225 (Ac-225) is an alpha-emitting isotope that is showing significant clinical response in some advanced, untreatable cancers. A major hurdle in developing Ac-radiopharmaceuticals includes finding ways of attaching Ac-225 to drug carrier molecules. Dr. Schaffer’s research aims to demonstrate that a novel actinium chelate, or compound, can incorporate the radioisotope into molecules targeted toward the somatostatin receptor – an important cellular marker in some neuroendocrine tumors.

Why is this important?

Actinium is unstable, so drugs made with this isotope cannot be stockpiled. Dr. Schaffer and his team will demonstrate a chelate designed to incorporate the isotope under mild conditions, allowing pharmacists to easily produce and administer the radiopharmaceutical in a hospital setting. This project will also demonstrate the efficacy of the radiopharmaceutical for treating somatostatin-positive tumors.

What will researchers do?

Dr. Schaffer’s team will establish the radiopharmaceutical synthesis protocol and perform biodistribution studies to establish the toxicity and therapeutic response of somatostatin-positive neuroendocrine tumors. 

How might this improve the treatment of NETs?

Synthesizing actinium-labeled radiopharmaceuticals will enable the treatment of advanced, metastatic disease for which no other treatment options exist. 

What is the next step?

They will begin by synthesizing the drug precursors and label them with actinium produced at TRIUMF in Vancouver, Canada. Tumor-bearing models will receive escalating doses of the radiopharmaceutical to establish dose tolerance and tumor response. 


Additional Details

  • City: Vancouver
  • State: British Columbia
  • Country: Canada
  • Grant Duration: 1 year


NETRF funds laboratory research to understand the development of neuroendocrine tumors and translational research to explore new concepts in treatment. Research grant descriptions and research updates from NETRF are not intended to serve as medical advice. It can take years for research discoveries to be fully validated and approved for patient care. Always consult your health care providers about your treatment options.

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