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Recombinant human TSH superagonists are engineered analogs of human thyroid-stimulating hormone (TSH) designed to have significantly increased potency and/or duration of action compared to native or standard recombinant hTSH. These molecules act as agonists at the thyrotropin receptor (TSHR), stimulating thyroidal iodide uptake and enhancing radioactive iodine uptake in thyroid tissue. Superagonists such as TR1401 and TR1402 have been shown in preclinical studies to stimulate thyroidal iodide and FDG uptake much more potently than wild-type hTSH[3][8]. The modifications typically involve introducing additional positively charged amino acids into the alpha subunit, increasing receptor binding affinity and bioactivity by 100- to 1000-fold over native hTSH[6][8]. These agents are being developed primarily for use in diagnostic imaging and radioiodine therapy preparation for patients with differentiated thyroid cancer, especially those who have undergone thyroidectomy. They may also offer improved convenience due to longer half-life formulations that reduce dosing frequency[4][7]. The main developer is Trophogen.
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