Adis, a Wolters Kluwer Business, Auckland, New Zealand.
Drugs. 2011 Sep 10;71(13):1755-70. doi: 10.2165/11206790-000000000-00000.
Eldecalcitol (1α,25OH-2β-(3-hydroxypropyloxy)vitamin D(3); ED-71; Edirol®) is an orally administered analogue of active vitamin D (calcitriol) that is available in Japan for the treatment of osteoporosis. Two randomized, double-blind, multicentre trials were conducted in patients with osteoporosis. In a placebo-controlled, dose-ranging trial, eldecalcitol significantly reduced serum bone-specific alkaline phosphatase (BALP) and serum osteocalcin, markers of bone formation, more than placebo. Eldecalcitol at a 1.0 μg/day dosage, but not at lower dosages, also significantly reduced urinary type I collagen N-telopeptide (NTX), a marker of bone resorption, more than placebo. In a comparison with alfacalcidol (a prodrug of calcitriol), eldecalcitol produced significantly greater reductions in serum BALP and urinary NTX, and had a positive effect on CT markers of femoral biomechanical properties. In the comparison with alfacalcidol, eldecalcitol 0.75 μg/day significantly reduced the 3-year incidence of vertebral fractures, with an absolute risk reduction of 4.1% over this period, representing a relative risk reduction of 26%. There was no significant difference in the rate of non-vertebral fractures. In both trials, eldecalcitol treatment was also associated with an increase in bone mineral density, whereas patients who received the comparators generally had a reduction in bone mineral density. Increases in blood calcium (to >2.6 mmol/L) and urinary calcium (to >0.1 mmol/L glomerular filtrate) were the most clinically important treatment-emergent adverse events. In the placebo-controlled, dose-ranging trial, 23% and 25% of patients in the eldecalcitol 1 μg/day group had increased blood and urinary calcium compared with 7% and 7%, 6% [corrected] and 9%, and 0% and 1.9% in the eldecalcitol 0.5 and 0.75 μg/day, and placebo groups, respectively. In the comparison with alfacalcidol, 21.0% and 13.5% of eldecalcitol 0.75 μg/day and alfacalcidol 1.0 μg/day recipients had increased blood calcium, whereas hypercalcaemia (defined as a serum calcium >2.9 mmol/L) occurred in 0.4% and urolithiasis in 1.3% of eldecalcitol recipients over 36 months of treatment. Eldecalcitol is an efficacious treatment for patients with osteoporosis that should be further investigated in head-to-head trials with other recommended first-line pharmacological treatments.
依降钙素（1α，25[OH]（2）-2β-（3-羟丙氧基）维生素 D（3）；ED-71；Edirol®）是一种口服活性维生素 D（骨化三醇）类似物，在日本可用于治疗骨质疏松症。两项随机、双盲、多中心试验在骨质疏松症患者中进行。在安慰剂对照、剂量范围试验中，依降钙素显著降低了血清骨特异性碱性磷酸酶（BALP）和血清骨钙素，这是骨形成的标志物，比安慰剂更有效。依降钙素 1.0μg/天的剂量，而不是较低的剂量，也显著降低了尿Ⅰ型胶原 N-末端肽（NTX），这是骨吸收的标志物，比安慰剂更有效。与骨化三醇前体药物阿尔法骨化醇相比，依降钙素显著降低了血清 BALP 和尿 NTX，对股骨生物力学特性的 CT 标志物有积极影响。与阿尔法骨化醇相比，依降钙素 0.75μg/天显著降低了 3 年椎体骨折的发生率，在此期间绝对风险降低了 4.1%，相对风险降低了 26%。非椎体骨折的发生率没有显著差异。在这两项试验中，依降钙素治疗也与骨密度的增加有关，而接受对照治疗的患者通常骨密度降低。血钙（>2.6mmol/L）和尿钙（>0.1mmol/L 肾小球滤过率）的增加是最具临床意义的治疗相关不良事件。在安慰剂对照、剂量范围试验中，与安慰剂组相比，依降钙素 1μg/天组有 23%和 25%的患者出现血钙升高，而依降钙素 0.5μg/天和 0.75μg/天组分别有 7%和 7%、6%[校正]和 9%以及 0%和 1.9%。与阿尔法骨化醇相比，依降钙素 0.75μg/天和阿尔法骨化醇 1.0μg/天组各有 21.0%和 13.5%的患者出现血钙升高，而在 36 个月的治疗过程中，依降钙素组有 0.4%的患者发生高钙血症（定义为血清钙>2.9mmol/L），有 1.3%的患者发生尿路结石。依降钙素是一种有效的骨质疏松症治疗药物，应在与其他推荐的一线药物治疗的头对头试验中进一步研究。
