On December 21, 2021 Precision Molecular, Inc. (PMI), a clinical-stage company developing targeted radiopharmaceuticals and theranostics for patients with cancer, reported it has executed a licensing agreement with Johns Hopkins University for exclusive rights to an astatine-211-labeled inhibitor of prostate-specific membrane antigen (PSMA) which is typically elevated in prostate cancer cells (Press release, Precision Molecular, DEC 21, 2021, View Source [SID1234597549]). PMI is developing this astatine-211-labeled inhibitor of PSMA as PMI21 and expects to initiate clinical trials in the first half of next year. Martin Pomper, M.D., Ph.D., director of nuclear medicine and molecular imaging at Johns Hopkins and Michael Zalutsky, Ph.D., professor of radiology, at the Duke University School of Medicine are co-inventors of the astatine-211-labeled targeted alpha therapy.

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Radiopharmaceuticals consist of a radionuclide and a targeting molecule that delivers a sufficient level of radiation to disease sites. Radionuclides used for oncology applications must emit radiation with a relatively short path length to maximize impact on cancer cells while minimizing effects on healthy tissue; two main types of radiation used in targeted radionuclide therapy are alpha particles and beta particles.

"When designing radiopharmaceuticals, the choice of radionuclide has important implications related to efficacy and toxicity," said Dr. Zalutsky, senior advisor to PMI. "Astatine-211 emits a single alpha particle which has more energy and travels a shorter distance than other forms of radiation, offering the potential to kill cancer cells while limiting damage to surrounding tissue. In contrast, beta particles emitted by other radionuclides can travel further which increases the risk of irradiating normal tissue. Astatine-211 also offers an advantage over other alpha emitters such as actinium-225 which emits four alpha particles. These particles can break the bonds that hold the radionuclide to its targeting molecule, releasing the radioactivity and potentially causing off-target toxicity."

PMI21 is designed to target PSMA which is present at a low level in normal prostate tissue, but markedly elevated in prostate cancer cells. The vast majority of PSMA exists on the surface of prostate cells making it highly accessible for both diagnostic imaging and drug delivery.

"The PSMA-binding and astatine labeling functions of PMI21 have been optimized in combination," said Seulki Lee, Ph.D., Chief Executive Officer of PMI. "It has been engineered for high tumor uptake and rapid clearance from normal tissues to minimize toxicity which has been a challenge with some other PSMA-targeted radiotherapies. We believe this compound has the potential to offer major advantages to what is currently in development, and we look forward to advancing PMI21 into clinical trials."