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124I-PU-H71 is an investigational radiopharmaceutical developed by Memorial Sloan Kettering Cancer Center for positron emission tomography (PET) imaging. It consists of the small molecule PU-H71, a purine-scaffold inhibitor of Heat shock protein 90 (HSP90), radiolabeled with the positron emitter iodine-124. The agent specifically binds to the ATP-binding site of HSP90 when it is incorporated into the "epichaperome," a stress-induced protein network found in many cancer cells. By visualizing the expression and activity of the epichaperome, 124I-PU-H71 serves as a companion diagnostic to identify patients likely to respond to HSP90 inhibitors and to determine optimal therapeutic dosing. It has been evaluated in various cancers, including solid tumors, lymphomas, and plasma cell dyscrasias.
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