Related Experiment Video
Updated: Feb 28, 2026
![Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F68356.jpg&w=3840&q=50)
10:33
Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
1.2K
First-in-Human Evaluation of [68Ga]Ga-HTK03149, a PSMA-Targeted Tracer for PET Imaging in Prostate Cancer
Guillaume Chaussé1, Xinchi Hou1, Carlos Uribe1,2
1Molecular Imaging and Therapy, BC Cancer, Vancouver, British Columbia, Canada; and.
Summary
The novel PET radiopharmaceutical [68Ga]Ga-HTK03149 shows safety and favorable biodistribution for prostate cancer imaging. This PSMA-targeted agent demonstrates high tumor uptake and improved lesion contrast, supporting its use in theranostics.
Area of Science:
- Nuclear Medicine
- Radiopharmaceutical Science
- Oncology
Background:
- Prostate-specific membrane antigen (PSMA) is a key target for prostate cancer diagnostics and therapeutics.
- [68Ga]Ga-HTK03149 is a novel PSMA inhibitor designed with a 2-aminoadipic acid moiety to enhance biodistribution.
- First-in-human studies are crucial for evaluating new radiotracers.
Purpose of the Study:
- To assess the safety, biodistribution, and dosimetry of [68Ga]Ga-HTK03149 in men with recurrent prostate cancer.
- To explore organ uptake patterns for potential theranostic applications.
- To evaluate the impact of forced diuresis on radiation dose to the bladder.
Main Methods:
- Ten men with biochemical recurrence of prostate cancer underwent dynamic and static PET/CT scans after [68Ga]Ga-HTK03149 injection.
- Organ absorbed doses were calculated using OLINDA/EXM software.
- Forced diuresis was administered in a subset of participants to assess its effect on bladder dose.
Main Results:
- [68Ga]Ga-HTK03149 was well-tolerated with no adverse events or significant changes in vital signs or lab parameters.
- The radiotracer exhibited rapid clearance from blood and soft tissues, with notable uptake in salivary and lacrimal glands, liver, spleen, kidneys, and small intestine.
- Kidneys received the highest absorbed dose (0.107 ± 0.020 mGy/MBq), while forced diuresis significantly reduced bladder wall dose (0.029 ± 0.0097 mGy/MBq).
- Lesions demonstrated high uptake (SUVmax 9.52 at 2h) and improved tumor-to-background ratios (20.42 at 2h), indicating excellent lesion conspicuity.
Conclusions:
- [68Ga]Ga-HTK03149 is a safe PSMA-targeted PET radiopharmaceutical with comparable biodistribution and dosimetry to existing agents.
- Its high tumor uptake and enhanced delayed lesion contrast support its further clinical evaluation for prostate cancer imaging.
- The agent holds promise for future theranostic applications in prostate cancer management.
More Related Videos
Related Concept Videos
01:29Positron Emission Tomography
7.8K
Positron emission tomography (PET) is a medical imaging technique involving radiopharmaceuticals — substances that emit short-lived radiation. Although the first PET scanner was introduced in 1961, it took 15 more years before radiopharmaceuticals were combined with the technique and revolutionized its potential.
One of the main requirements of a PET scan is a positron-emitting radioisotope, which is produced in a cyclotron and then attached to a substance used by the part of the body...
One of the main requirements of a PET scan is a positron-emitting radioisotope, which is produced in a cyclotron and then attached to a substance used by the part of the body...
7.8K
01:25Imaging Studies II: Positron Emission Tomography and Scintigraphy
678
Positron Emission Tomography (PET) is a medical imaging technique that provides crucial insights into the body's physiological functions at a molecular level. It is an indispensable resource for diagnosing, staging, and monitoring various illnesses, notably cancer, neurological disorders, and cardiovascular conditions.
Fundamental Principles of PET
Fundamental Principles of PET
678