RM2

RM2 is a synthetic peptide-based antagonist of the gastrin-releasing peptide receptor (GRPR), also known as bombesin receptor 2 (BB2)[1][2][4][6][8]. RM2 is used as a radiolabeled imaging agent (with gallium-68, “68Ga-RM2”) for PET imaging, and as a radiotherapeutic when labeled with lutetium-177 (“177Lu-RM2”)[1][2][4][6][7][8]. It selectively binds to GRPR, which is highly expressed on the cell surface of several cancers including prostate and breast cancer, enabling both the detection (diagnostics) and targeted treatment (therapy) of tumors via theranostic approaches. After binding to GRPR, the radiolabeled RM2 is internalized by cancer cells; in the therapeutic form, the radionuclide delivers cytotoxic radiation to the target cell[2][4][7]. RM2-based diagnostics and therapeutics are under clinical investigation, particularly for recurrent prostate cancer and estrogen receptor-positive breast cancer, as well as selected other GRPR-positive malignancies[3][5][6][7].

Other names

Bombesin receptor antagonist RM2gallium Ga 68-labeled RM2lutetium-177 RM2lutetium177 RM2lutetium 177 RM2