Effects of bazedoxifene/conjugated estrogens on reproductive endocrinology and reproductive tract ultrasonographic appearance in premenopausal women: a preliminary study

Abstract

Bazedoxifene (BZA) paired with conjugated estrogens (CE) is the first tissue selective estrogen receptor complex (TSEC) approved by the United States Food and Drug Administration for the treatment of menopausal symptoms. Clinical trials in menopausal women and in premenopausal murine models of endometriosis have demonstrated safety and efficacy, however, the impact of BZA/CE on premenopausal women is not known. Here we report a case series study in premenopausal women assessing effects of BZA/CE on reproductive hormones, and uterine/ovarian ultrasonographic appearance. After one monitoring cycle, five subjects underwent daily administration of BZA/CE (20 mg/0.45 mg) for 12 weeks, and were followed for 4 weeks after treatment. Uterine/ovarian morphology was assessed with ultrasound, and endocrinologic function with ovulation prediction kits and serum assessment of reproductive hormones throughout the menstrual cycle. All subjects demonstrated an LH surge on the medication; interestingly there was a significant decrease in luteinizing hormone level during treatment compared to posttreatment values. BZA/CE was well-tolerated in premenopausal women and did not induce clinically relevant reproductive hormone changes, endometrial alterations, or abnormal ovarian folliculogenesis.

摘要

Bazedoxifene (BZA)联合结合雌激素(CE)是美国食品和药物管理局批准的用于治疗绝经期症状的第一种具有组织选择性的雌激素受体复合物(TSEC)。绝经期妇女和患有子宫内膜异位症的绝经前小鼠模型的临床试验已证明其安全性和有效性, 然而, BZA/CE对绝经前妇女的影响尚不清楚。在这里, 我们报告了一个绝经前妇女的病例系列研究, 评估BZA/CE对生殖激素和子宫/卵巢超声表现的影响。在一个监测周期后, 5名受试者每日服用BZA/CE (20mg/0.45mg) 12周, 并且在治疗后随访4周。通过超声检查子宫/卵巢形态, 通过排卵预测试剂盒检查内分泌功能, 并对整个月经周期的生殖激素进行血清评估。所有受试者均表现为用药后的LH峰;有趣的是, 与治疗后相比, 治疗期间黄体生成素水平显著下降。BZA/CE在绝经前妇女中耐受性良好, 并且没有引起临床相关的生殖激素变化、子宫内膜改变或异常卵泡形成。

The Chinese abstracts are translated by Prof. Dr. Xiangyan Ruan and her team: Beijing Obstetrics and Gynecology Hospital, Capital Medical University, Beijing 100026, China.

Keywords:

• Bazedoxifene
• conjugated estrogens
• premenopausal
• reproductive tract
• selective estrogen receptor modulators

Disclosure statement

This was an investigator-initiated study, supported by Pfizer, Inc. Pfizer had no role in the design, execution, analysis/interpretation, or reporting of the study.

Additional information

Funding

This work was supported by Pfizer, Inc., Grant WI195105 (to HST).