Scholarlink

<p>Enavogliflozin is a recently developed novel sodium‒glucose cotransporter-2 inhibitor that is used to treat type 2 diabetes mellitus. During clinical development, a 0.3&#xa0;mg daily dose regimen was effective at lowering the blood glucose level, whereas a 0.1&#xa0;mg dose formulation was used in the early clinical phase. This study aimed to evaluate the pharmacokinetic (PK) properties of a low-strength formulation of 0.1&#xa0;mg of enavogliflozin and two high-strength formulations of 0.3&#xa0;mg of enavogliflozin. Two clinical trials designed as randomized, open-label, single-dose, two-way crossover studies were conducted in healthy Korean subjects. In Study A, the subjects received either three tablets of 0.1&#xa0;mg enavogliflozin or one tablet of 0.3&#xa0;mg enavogliflozin according to their assigned sequence. In Study B, the subjects received a single dose of 0.3&#xa0;mg of enavogliflozin in one of two different formulations. Blood samples were collected for up to 72&#xa0;h to assess the PK of enavogliflozin. The maximum concentration (C<sub>max</sub>) and area under the concentration‒time curve from 0 to the last measurable time (AUC<sub>last</sub>) were calculated to determine bioequivalence. Safety and tolerability were evaluated throughout the studies. In Study A, 42 subjects were enrolled, 38 of whom completed the study, whereas in Study B, 43 subjects were included, 37 of whom completed the study. The geometric mean ratio (GMR) (90% confidence interval, 90% CI) of 0.3&#xa0;mg of enavogliflozin (Formulation A) to 0.1&#xa0;mg of enavogliflozin for the C<sub>max</sub> and AUC<sub>last</sub> were 1.02 (0.98–1.07) and 0.99 (0.95–1.02), respectively. The GMRs (90% CIs) of 0.3&#xa0;mg of enavogliflozin (Formulation B) to 0.3&#xa0;mg of enavogliflozin (Formulation A) for the corresponding parameters were 0.96 (0.91–1.02) and 1.00 (0.95–1.04), respectively, which met the conventional bioequivalence criteria. The most common adverse events were headache and diarrhea in both studies. This study demonstrated that three tablets of 0.1&#xa0;mg enavogliflozin had PK characteristics similar to those of one tablet of 0.3&#xa0;mg enavogliflozin. Furthermore, the two high-strength formulations showed bioequivalence and were well tolerated.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Evaluation of formulation on the pharmacokinetics, safety, and tolerability of enavogliflozin in healthy Korean adults

  • 期刊论文

  • 发表日期：

    2025年12月27日

查看全文
  • Soyoung Lee,
  • Jae Jin Nah,
  • Wonsuk Shin,
  • Anhye Kim,
  • Hyounggyoon Yoo

摘要

Enavogliflozin is a recently developed novel sodium‒glucose cotransporter-2 inhibitor that is used to treat type 2 diabetes mellitus. During clinical development, a 0.3 mg daily dose regimen was effective at lowering the blood glucose level, whereas a 0.1 mg dose formulation was used in the early clinical phase. This study aimed to evaluate the pharmacokinetic (PK) properties of a low-strength formulation of 0.1 mg of enavogliflozin and two high-strength formulations of 0.3 mg of enavogliflozin. Two clinical trials designed as randomized, open-label, single-dose, two-way crossover studies were conducted in healthy Korean subjects. In Study A, the subjects received either three tablets of 0.1 mg enavogliflozin or one tablet of 0.3 mg enavogliflozin according to their assigned sequence. In Study B, the subjects received a single dose of 0.3 mg of enavogliflozin in one of two different formulations. Blood samples were collected for up to 72 h to assess the PK of enavogliflozin. The maximum concentration (Cmax) and area under the concentration‒time curve from 0 to the last measurable time (AUClast) were calculated to determine bioequivalence. Safety and tolerability were evaluated throughout the studies. In Study A, 42 subjects were enrolled, 38 of whom completed the study, whereas in Study B, 43 subjects were included, 37 of whom completed the study. The geometric mean ratio (GMR) (90% confidence interval, 90% CI) of 0.3 mg of enavogliflozin (Formulation A) to 0.1 mg of enavogliflozin for the Cmax and AUClast were 1.02 (0.98–1.07) and 0.99 (0.95–1.02), respectively. The GMRs (90% CIs) of 0.3 mg of enavogliflozin (Formulation B) to 0.3 mg of enavogliflozin (Formulation A) for the corresponding parameters were 0.96 (0.91–1.02) and 1.00 (0.95–1.04), respectively, which met the conventional bioequivalence criteria. The most common adverse events were headache and diarrhea in both studies. This study demonstrated that three tablets of 0.1 mg enavogliflozin had PK characteristics similar to those of one tablet of 0.3 mg enavogliflozin. Furthermore, the two high-strength formulations showed bioequivalence and were well tolerated.