Department of Medicine, Section of Endocrinology, Yale School of Medicine, New Haven, CT, USA.
Englewood Hospital and Medical Center, Englewood, NJ, USA.
Calcif Tissue Int. 2018 Jun;102(6):666-670. doi: 10.1007/s00223-017-0382-0. Epub 2018 Jan 30.
Previous work has demonstrated that a single subcutaneous dose of salmon calcitonin leads to a transient decline in circulating levels of FGF23 in patients with X-linked hypophosphatemia (XLH). Since the calcitonin receptor is expressed on osteocytes, this raises the possibility that interdicting signals through that receptor could modulate circulating levels of FGF23 in XLH. In the present study, 21 subjects with XLH were randomly assigned to receive either placebo nasal spray or 400 IU of nasal salmon calcitonin daily for three months. On the first and last day of the study, serial measurements of FGF23, 1,25-dihydroxyvitamin D, and TmP/GFR were made over 27 h. At the beginning of Visit 2 (the first day of month 2) and the beginning of Visit 3 (the first day of month 3), single, first-morning, fasting measurements of these same parameters were made before the next administered dose of study drug. Following the initial or final dose of study drug, there were no differences in area under the curve, based on treatment assignment, for the three principal outcome variables. Similarly, there were no differences in the fasting measures taken at the beginning of Visit 2 or Visit 3 compared to the fasting values on either day 2 of Visit 1 or the fasting values on day 2 of Visit 4. There were also no significant changes over time in serum phosphorus, serum calcium, circulating levels of PTH, CTx, or P1NP. The reasons why nasal salmon calcitonin did not recapitulate the findings with subcutaneously administered drug may relate to the kinetics of drug delivery, the bioavailability of drug or peak drug dose achieved. It remains possible, however, that other means of altering calcitonin receptor signaling may still provide an opportunity for regulating FGF23 production.
先前的工作已经表明,单次皮下给予鲑鱼降钙素会导致 X 连锁低磷血症(XLH)患者循环中 FGF23 水平短暂下降。由于降钙素受体在骨细胞上表达,这就提出了一种可能性,即通过该受体阻断信号可能会调节 XLH 患者循环中 FGF23 的水平。在本研究中,21 名 XLH 患者被随机分配接受安慰剂鼻喷剂或每天 400IU 鲑鱼降钙素鼻喷剂,持续 3 个月。在研究的第 1 天和最后 1 天,在 27 小时内连续测量 FGF23、1,25-二羟维生素 D 和 TmP/GFR。在第 2 次就诊(第 2 个月的第 1 天)和第 3 次就诊(第 3 个月的第 1 天)开始时,在接受下一次研究药物剂量之前,测量这些相同参数的单次空腹清晨测量值。在接受初始或最终研究药物剂量后,基于治疗分配,三个主要结局变量的曲线下面积没有差异。同样,在第 2 次就诊或第 3 次就诊开始时的空腹测量值与第 1 次就诊第 2 天的空腹值或第 4 次就诊第 2 天的空腹值相比没有差异。血清磷、血清钙、循环 PTH、CTX 或 P1NP 水平也没有随时间发生显著变化。鼻用鲑鱼降钙素未能重现皮下给予药物的发现,其原因可能与药物输送的动力学、药物的生物利用度或达到的药物峰值剂量有关。然而,改变降钙素受体信号的其他方法仍有可能为调节 FGF23 的产生提供机会。