팔레칼시트리올

팔레칼시트리올 화학적 특성, 용도, 생산

• 개요

  Falecalcitriol, previously known as flocalcitrol, was launched by several codevelopers in Japan for the treatment of secondary hyperthyroidism (SHPT). This hexafluorinated analog of 1α,25-dihydroxyvitamin D3 (calcitriol), the hormonally active form of vitamin D3, can be obtained by several different synthetic routes from a conveniently protected cholestenol, a key step being an aldol reaction with hexafluoroacetone. Falecalcitriol is several times more active than 1,25(OH)₂D₃ in regulating the proliferation of parathyroid cells and parathyroid hormone (PTH) synthesis that are believed to be mediated through binding to VDR, a nuclear receptor for vitamin D; furthermore, it was proposed that a bioactive 23S-hydroxylated metabolite, resistant to further metabolism, contributes to the retention of an active compound for longer in cells and so, to significantly lengthen the duration of action. In a comparative clinical study conducted in hemodialysis patients with moderate to severe SHPT, falecalcitriol was found to be more active than alfacalcidol in suppressing parathyroid hormone without triggering hypercalcemia.

• 용도

  Hexafluorinated analog of Calcitriol (C144500). A more potent therapeutic agent for secondary hyperparathyroidism.

• 위험도

  A poison by ingestion.

팔레칼시트리올 공급 업체

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