Misakian Aaron L, Ariel Danit, Sullivan Erika A, Singh Gagandeep, Loeb Danielle, Strickland Tyler, Iwamoto Sean J, Rothman Micol S, Botzheim Bren, Liang Jane W, Kelley Carly, Hamnvik Ole-Petter R
Division of Pediatric Endocrinology, Department of Pediatrics, University of Virginia School of Medicine, Charlottesville, Virginia.
Division of Endocrinology, Gerontology and Metabolism, Department of Medicine, Stanford University School of Medicine, Stanford, California.
Endocr Pract. 2025 Nov;31(11):1462-1469. doi: 10.1016/j.eprac.2025.07.002. Epub 2025 Jul 8.
To evaluate the association between injectable estradiol and serum total testosterone (TT) concentrations and determine additional associations between covariates (age, intramuscular vs subcutaneous administration, ester [cypionate vs valerate], injection timing relative to laboratory draw, antiandrogen use, and progestogen use) and TT concentration.
Cross-sectional retrospective multisite study including adult transgender and gender-diverse patients without a history of gonadectomy or concurrent gonadotropin-releasing hormone agonist use prescribed weekly injectable estradiol at a stable dose for >75 days between 2019 and 2023 with confirmed timing of estradiol and TT concentrations relative to last injection. Those who reached guideline-recommended TT suppression (<50 ng/dL) were compared with those who did not. A weighted linear mixed model evaluated relationship between TT concentration and covariates.
Of the 357 patients included, the median estradiol dose, estradiol concentration, and TT concentration were 4 mg (interquartile range [IQR], 3-6 mg), 232 pg/mL (IQR, 134-371 pg/mL), and 17 ng/dL (IQR, 10-33 ng/dL), respectively. There was no significant difference in TT concentration or proportion reaching TT suppression between patients using estradiol monotherapy and estradiol with an antiandrogen(s) and/or a progestogen. In the weighted linear mixed model, higher estradiol concentration, fewer days since injection, and progestogen use were associated with a lower TT concentration.
Injectable estradiol, even as monotherapy, was effective at TT suppression in 82.6% of patients and comparable with combination therapy with an antiandrogen(s) or progestogen. Progestogen use was independently associated with a lower TT concentration, whereas spironolactone had no significant effect.
评估注射用雌二醇与血清总睾酮（TT）浓度之间的关联，并确定协变量（年龄、肌肉注射与皮下注射、酯类[环戊丙酸酯与戊酸酯]、相对于实验室采血的注射时间、抗雄激素使用情况以及孕激素使用情况）与TT浓度之间的其他关联。
横断面回顾性多中心研究，纳入成年跨性别和性别多样化患者，这些患者无性腺切除术病史或未同时使用促性腺激素释放激素激动剂，于2019年至2023年期间以稳定剂量每周注射一次注射用雌二醇，持续>75天，并确定了雌二醇和TT浓度相对于最后一次注射的时间。将达到指南推荐的TT抑制水平（<50 ng/dL）的患者与未达到该水平的患者进行比较。采用加权线性混合模型评估TT浓度与协变量之间的关系。
纳入的357例患者中，雌二醇剂量中位数、雌二醇浓度和TT浓度分别为4 mg（四分位间距[IQR]，3 - 6 mg）、232 pg/mL（IQR，134 - 371 pg/mL）和17 ng/dL（IQR，10 - 33 ng/dL）。使用雌二醇单药治疗的患者与使用雌二醇联合抗雄激素和/或孕激素的患者在TT浓度或达到TT抑制的比例方面无显著差异。在加权线性混合模型中，较高的雌二醇浓度、注射后天数较少以及使用孕激素与较低的TT浓度相关。
注射用雌二醇即使作为单药治疗，在82.6%的患者中对TT抑制有效，且与抗雄激素或孕激素联合治疗效果相当。使用孕激素与较低的TT浓度独立相关，而螺内酯无显著影响。
