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KSP-0914 is an orally bioavailable small molecule antagonist of the thyroid-stimulating hormone receptor (TSHR), currently under development by Kissei Pharmaceutical for the treatment of Graves' disease. In Graves' disease, autoantibodies (thyroid-stimulating immunoglobulins) bind to and activate the TSH receptor, leading to excessive production of thyroid hormones and hyperthyroidism. KSP-0914 is designed to block these autoantibodies from binding to and activating the receptor, thereby normalizing thyroid function. The compound has completed Phase 1 clinical trials, including dose-escalation studies in both Japanese and Caucasian healthy volunteers.
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