Novel radiopharmaceutical pair detects and treats melanoma, shows potential for broad application in solid tumors

Novel radiopharmaceutical pair detects and treats melanoma; study shows potential for broad application in solid tumors

A newly developed small-molecular radiopharmaceutical pair has successfully visualized and treated melanoma in a preclinical study, according to new research presented at the Society of Nuclear Medicine and Molecular Imaging 2022 Annual Meeting. Targeting a receptor that is aberrantly overproduced in many human solid tumors, this theranostic (therapy + diagnostic) approach shows promise for non-invasive diagnosis and treatment of patients with various forms of cancer.

Metabotropic glutamate receptor 1 (GRM1) is aberrantly overproduced in a wide variety of human solid tumors, including melanoma. However, it is not found in normal surrounding organs. As such, GRM1 has been identified as a widely applicable target for theranostics for cancers.

In the study, researchers designed and developed a novel small-molecular radiopharmaceutical pair, [11C]1 and [211At]1, to target the GRM1. The theranostic potential of the pair was then explored in GRM1 melanoma-bearing mice. In vivo PET imaging with [11C]1 was performed to visualize the melanoma, and an ex vivo biodistribution study was conducted to determine the uptake and clearance of the radiopharmaceutical. After imaging, mice were treated with [211At]1 and monitored for tumor growth and adverse side effects.

PET imaging with [11C]1 clearly visualized the tumors with good tumor-to-background contrast and with rapid clearance from normal organs after injection. In the therapeutic studies, [211At]1 successfully prevented tumor growth with only a single treatment. No decrease in body weight, liver or kidney damage, or other side effects were observed.

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