SR-16234, a Novel Selective Estrogen Receptor Modulator for Pain Symptoms with Endometriosis: An Open-label Clinical Trial
SR-16234, a Novel Selective Estrogen Receptor Modulator for Pain Symptoms with Endometriosis: An Open-label Clinical Trial
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DOI：
10.33160/yam.2017.12.003
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发表时间：
2017-12-01
影响因子：
1
通讯作者：
Taniguchi, Fuminori
中科院分区：
文献类型：
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作者：
Harada, Tasuku;Ohta, Ikuko;Taniguchi, Fuminori
背景SR-16234是一种选择性雌激素受体调节剂（SERM），其结构与已批准的SERM不同，已报告具有雌激素受体（ER）拮抗活性和强亲和力，对ER β受体具有弱的部分激动活性。SR-16234对大鼠和小鼠子宫内膜异位症模型中移植的子宫内膜囊肿显示出强抑制作用。在这项临床试验中，SR-16234的有效性和安全性进行了评估，在子宫内膜异位症patients.Methods这项试验是一个开放标签的单臂临床试验。10例子宫内膜异位症和子宫腺肌病相关痛经和盆腔疼痛患者入组本试验，接受40 mg SR-16234每日一次给药，持续12周。主要终点是骨盆疼痛的视觉模拟评分（VAS）。次要终点包括痛经评分、盆腔疼痛评分、客观观察结果口服SR-16234 40 mg 12周后，盆腔疼痛VAS、盆腔疼痛总评分、子宫内膜厚度和血清CA 125浓度在统计学上显著降低，结论本试验首次提示选择性雌激素受体调节剂可用于治疗子宫内膜异位症相关疼痛。
Background SR-16234 is a selective estrogen receptor modulator (SERM) structurally different from approved SERM and has been reported to have estrogen receptor (ER) a antagonistic activity and strong affinity with a weak partial agonistic activity to ER beta receptor. SR-16234 showed strong inhibitory effects on transplanted endometrial cysts in the endometriosis model of rat and mouse. In this clinical trial, efficacy and safety of SR-16234 have been evaluated in endometriosis patients.Methods This trial was an open-label single arm clinical trial. Ten patients with dysmenorrhea and pelvic pain associated with endometriosis and adenomyosis were enrolled in this trial, and received 40 mg of SR-16234 once daily for 12 weeks. The primary endpoint was the visual analogue scale (VAS) of pelvic pain. The secondary endpoints included dysmenorrhea score, pelvic pain score, objective observations (stiffness of Douglas' pouch, limitation of uterine movement, size of ovarian chocolate cysts, thickness of endometrium, and serum CA125 concentration) and safety.Results After oral administration of SR-16234 40 mg for 12 weeks, there were statistically significant decreases in pelvic pain VAS, total pelvic pain score, total dysmenorrhea score, stiffness of Douglas' pouch, limitation of uterine movement compared with the baseline values.Conclusion The present trial suggested that a selective estrogen receptor modulator could be used for treatment of pain associated with endometriosis for the first time.