The Lundquist Institute and Harbor-UCLA Medical Center, Torrance, CA, US.
University of Connecticut School of Medicine, Farmington, CT, US.
J Clin Endocrinol Metab. 2020 Aug 1;105(8):2515-31. doi: 10.1210/clinem/dgaa238.
A novel formulation of oral testosterone (T) undecanoate (TU) was evaluated in a phase 3 clinical trial.
Determine efficacy, short-term safety, and alignment of new oral TU formulation with current US approval standards for T replacement therapy.
Randomized, active-controlled, open-label study.
Academic and private clinical practice sites; enrolled patients were clinically hypogonadal men 18 to 65 years old.
Patients were randomized 3:1 to oral TU, as prescribed (JATENZO®; n = 166) or a topical T product once daily (Axiron®; n = 56) for 3 to 4 months. Dose titration was based on average T levels (Cavg) calculated from serial pharmacokinetic (PK) samples. T was assayed by liquid chromatography-mass spectrometry/mass spectrometry. Patients had 2 dose adjustment opportunities prior to final PK visit. Safety was assessed by standard clinical measures, including ambulatory blood pressure (BP).
87% of patients in both groups achieved mean T Cavg in the eugonadal range. Sodium fluoride-ethylenediamine tetra-acetate plasma T Cavg (mean ± standard deviation) for the oral TU group was 403 ± 128 ng/dL (14 ± 4 nmol/L); serum T equivalent, ~489 ± 155 ng/dL (17 ± 5 nmol/L); and topical T, 391 ± 140 ng/dL (14 ± 5 nmol/L). Modeling/simulation of T PK data demonstrated that dose titration based on a single blood sample 4 to 6 h after oral TU dose yielded efficacy (93%) equivalent to Cavg-based titration (87%). Safety profiles were similar in both groups, but oral TU was associated with a mean increase in systolic BP of 3 to 5 mm Hg.
A new oral TU formulation effectively restored T to mid-eugonadal levels in hypogonadal patients.
一种新型口服睾酮（T）十一酸酯（TU）制剂在 3 期临床试验中进行了评估。
确定疗效、短期安全性，以及新的口服 TU 制剂与目前美国 T 替代治疗批准标准的一致性。
随机、活性对照、开放性研究。
学术和私人临床实践场所；入组患者为临床性腺功能减退的 18 至 65 岁男性。
患者随机分为 3:1 组，分别接受口服 TU 治疗（JATENZO®；n = 166）或每日一次的外用 T 产品治疗（Axiron®；n = 56），疗程为 3 至 4 个月。剂量调整基于从连续药代动力学（PK）样本计算的平均 T 水平（Cavg）。T 通过液相色谱-质谱/质谱法进行检测。在最后一次 PK 就诊前，患者有 2 次剂量调整机会。安全性通过标准临床指标评估，包括动态血压（BP）。
两组患者的平均 T Cavg 均有 87%达到性腺功能正常范围。口服 TU 组氟化物-乙二胺四乙酸钠血浆 T Cavg（平均值 ± 标准差）为 403 ± 128 ng/dL（14 ± 4 nmol/L）；血清 T 当量为 489 ± 155 ng/dL（17 ± 5 nmol/L）；外用 T 为 391 ± 140 ng/dL（14 ± 5 nmol/L）。T PK 数据的建模/模拟表明，基于口服 TU 剂量后 4 至 6 小时的单次血样进行剂量调整可达到 93%的疗效（与基于 Cavg 的剂量调整等效）。两组的安全性谱相似，但口服 TU 与收缩压平均升高 3 至 5 mmHg 相关。
一种新型口服 TU 制剂可有效将 T 恢复至性腺功能减退患者的中性腺水平。
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