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PSMA-Targeting Ligands with Optimal Properties for Imaging and Therapy
Inventors: Reinier Hernandez, Anatoly Pinchuk
WARF is seeking commercial partners interested in developing a novel PSMA radionuclide disease-targeting agent for treating metastatic castration-resistant prostate cancer.
We believe this is an especially attractive opportunity for licensing and have invested in the development of this technology through WARF Accelerator by obtaining cGMP grade compound and initial GLP toxicology studies in rats to support a Phase 1 microdose study in humans.
- Our patented compound, ART-101, has better tumor retention (3-fold) and a different excretion pathway (liver) compared to PSMA-617 (Pluvicto, Novartis).
- In targeting cancer cells, the novel agent might be more efficacious and less harmful to the patient than current agents.
- The agent allows for imaging cancer with PET and SPECT medical imaging. It can be prepared to be electrically neutral.
- Dosimetry using 177Lu-ART-101 showed a 10:1 ratio tumor/bone marrow and 8:1 ratio tumor/kidney, respectively, and ~12%ID/g in the tumor at 50 hours post injection.
Researchers at UW–Madison have developed a novel PSMA radionuclide disease-targeting agent, ART-101. This new agent has improved tumor retention, is cleared mostly by the liver (easing the kidney burden) and has shown improved efficacy compared to the same and half-dose of 177Lu-PSMA-617 in mouse model bearing PSMA-positive prostate cancer tumors. The novel agent is extremely versatile and can be composed of various imaging and therapeutical radioactive isotopes.
In addition to treating prostate cancer, ART-101 might be used for the detection and imaging of prostate cancer when used with imaging radioisotopes, which can be done either via PET or SPECT medical imaging. The imaging capability also makes it suitable to be a tool in the staging of cancer and in the evaluation of therapy efficacy. Finally, quantification of the imaging signal strength allows for determining an effective dose for the subsequent delivery of targeted radiation therapy. More importantly, recent studies have found that more than 55% of breast cancers are PSMA-positive, which makes this compound a potentially viable option to treat PSMA-positive breast cancers.
- Treatment of PSMA-positive metastatic castration-resistant prostate cancer via targeted radiation therapy using high energy radioisotopes
- Determining the efficacious dose for targeted radiotherapy imaging and treatment.
For more information, please contact Rafael Diaz at [email protected] or 608-960-9847