Purpose

SUVN-1105 is a novel formulation of abiraterone acetate which was developed to demonstrate improved bioavailability, compared to Zytiga and Yonsa, and to reduce the dose and eliminate the food effect. A Phase 1 study was conducted to assess the bioequivalence, food effect, and comparative pharmacokinetics of SUVN-1105 to Zytiga in healthy male subjects.

Methods

The study comprised of 2 segments. Segment 1 was a single-center, 4-period crossover, open-label, fixed treatment sequence, single-dose study to evaluate the safety and pharmacokinetics of SUVN-1105 (N = 12 subjects per period). Segment 2 was a single-center, open-label, single-dose, randomized, 4-period, 4-treatment, 4-sequence crossover study to evaluate bioequivalence and comparative pharmacokinetics of SUVN-1105 against Zytiga (N = 44) under overnight fasted, modified fasted, and fed conditions.

Results

Abiraterone exposures appeared to increase proportionately with SUVN-1105 dose (200 mg vs. 250 mg) in Segment 1. In Segment 2, abiraterone exposures of 250 mg SUVN-1105 in the fasted or fed conditions were higher than those of Zytiga 1000 mg in the overnight fasted conditions. Abiraterone exposures of 250 mg SUVN-1105 decreased in the fed conditions (64% and 29% decrease in C_max and AUC, respectively) compared to overnight fasted conditions.

Conclusions

The abiraterone exposures of 250 mg SUVN-1105 in the fasted or fed conditions fall within the abiraterone exposures of 1000 mg Zytiga in fasted and modified fasted conditions. Single doses of SUVN-1105 were safe and well-tolerated in healthy males both in the fasted and fed conditions.

中文翻译：

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SUVN-1105（一种新型醋酸阿比特龙颗粒制剂）与 Zytiga 在健康男性受试者中的生物等效性、食物效应和比较药代动力学

目的

SUVN-1105 是醋酸阿比特龙的一种新型制剂，与 Zytiga 和 Yonsa 相比，其开发的目的是证明其生物利用度有所提高，并减少剂量并消除食物影响。进行了一项 1 期研究，以评估健康男性受试者中 SUVN-1105 与 Zytiga 的生物等效性、食物效应和药代动力学比较。

方法

该研究由 2 个部分组成。第 1 部分是一项单中心、4 期交叉、开放标签、固定治疗顺序、单剂量研究，旨在评估 SUVN-1105 的安全性和药代动力学（ 每期N = 12 名受试者）。第 2 部分是一项单中心、开放标签、单剂量、随机、4 个周期、4 个治疗、4 个序列交叉研究，旨在评估 SUVN-1105 与 Zytiga（N  = 44）在隔夜条件下的生物等效性和比较药代动力学禁食、修改禁食和进食条件。

结果

在第 1 部分中，阿比特龙暴露量似乎与 SUVN-1105 剂量（200 mg 与 250 mg）成比例增加。在第 2 部分中，空腹或进食条件下 250 mg SUVN-1105 的阿比特龙暴露量高于在空腹或进食条件下 Zytiga 1000 mg 的暴露量。过夜禁食条件。与隔夜禁食条件相比，进食条件下 250 mg SUVN-1105 的阿比特龙暴露量降低（C _max和 AUC 分别降低 64% 和 29% ）。

结论

在禁食或进食条件下250 mg SUVN-1105的阿比特龙暴露落入在禁食和改良禁食条件下1000 mg Zytiga的阿比特龙暴露范围内。单剂量 SUVN-1105 对于健康男性在禁食和进食条件下都是安全且耐受性良好的。