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NPSP795 is a selective **calcilytic** agent, functioning as a calcium-sensing receptor (**CaSR**) antagonist that reduces the receptor's sensitivity to extracellular calcium, thereby increasing parathyroid hormone (**PTH**) secretion and plasma calcium levels. Developed initially by NPS Pharmaceuticals (later acquired by Takeda), it targets **autosomal dominant hypocalcemia type 1 (ADH1)**, a rare genetic disorder caused by gain-of-function mutations in the CaSR gene, leading to hypocalcemia, low PTH, and hypercalciuria. Preclinical studies in mouse models demonstrated dose-dependent PTH elevation and hypocalcemia correction, while a Phase IIa trial evaluated its intravenous safety, PTH stimulation, calcium modulation, and renal effects in ADH1 patients.[1][2][5]
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