エルデカルシトール 化学特性,用途語,生産方法
用途
活性型ビタミンD誘導体骨折抑制効果を有することが証明された
効能
乾癬治療薬, 骨粗鬆症治療薬, ビタミンD受容体作動薬
商品名
エディロール (中外製薬); エディロール (中外製薬)
説明
Eldecalcitol (Edirol) was approved in January 2011 by the Japanese
Ministry of Health, Labor, and Welfare for the treatment of osteoporosis.
Because of vitamin D’s central role in the bone health, vitamin D and analogs of vitamin D have been used to treat patients diagnosed with osteoporosis.
Eldecalcitol is an analog of the active form of vitamin D, calcitriol, in which the lower cyclohexane ring contains a hydroxypropyl group. The synthesis of eldecalcitol involves the assembly of two units, a fully protected
(3S,4S,5R)-oct-1-en-7-yne-3,4,5-triol and a fused bicyclic system, (R)-6-
((1R,3aR,7aR,E)-4-(bromomethylene)-7a-methyloctahydro-1H-inden-1-
yl)-2-methylheptan-2-ol, through a Diels-Alder reaction to give fully
protected eldecalcitol. The hydroxyl groups are then deprotected to give
the parent molecule. Eldecalcitol binds to the vitaminDreceptor 2.7-fold
more potently than calcitriol, while only weakly inhibiting serum parathyroid hormone.
使用
Eldecalcitol is a derivative of vitamin D3 (V676045) which is the vitamin that mediates intestinal calcium absorbtion, bone calcium metabolism and probably, muscle activity.
定義
ChEBI: A hydroxycalciol that is calcitriol with a 3-hydroxypropoxy group at position 2.
臨床応用
Eldecalcitol is a vitamin D3 analog approved in Japan for the
treatment of osteoporosis. Itwasdiscoveredby Chugai and co-developed
with Taisho. Eldecalcitol, a hormonally active calcitrol analog,
regulates calcium and bone metabolism. The drug was approved on
the basis of results from randomized, double-blinded, parallelgroup,
phase III studies taking place over three years that showed
eldecalcitol to significantly lower incidence of new vertebral fractures
compared to those receiving the comparator drug alfacalcidol. Discovery and SAR studies of vitamin D3 analogs leading
to the identification of eldecalcitol have been reported. In
addition, multiple syntheses, including parallel approaches, have
been reported in publications and patents.
エルデカルシトール 上流と下流の製品情報
原材料
準備製品