Galecto Biotech AB, Ole Maaløes Vej 3, DK-2200, Copenhagen, Denmark.
QPS Netherlands BV, Groningen, The Netherlands.
Cancer Chemother Pharmacol. 2024 Nov;94(5):707-720. doi: 10.1007/s00280-024-04710-3. Epub 2024 Aug 21.
Overexpression of galectin-3, a β-galactoside-binding lectin, is associated with fibrotic diseases and cancer. Selvigaltin is an oral galectin-3 inhibitor, previously administered as a 50 mg capsule. This study aimed to evaluate the relative bioavailability and food effect of selvigaltin as a 100 mg tablet in healthy volunteers.
In this single-dose, randomized, three-period, crossover study (GALBA-1; NCT05747573), participants received selvigaltin as a 100 mg tablet (under fasted and fed conditions) or as two 50 mg capsules (under fasted conditions). Primary endpoints included plasma and urine pharmacokinetic (PK) parameters. Secondary endpoints were safety and tolerability.
Of the 13 enrolled participants, 12 completed the study. Under fasted conditions, geometric mean maximum observed plasma concentration (C) and systemic exposure (AUC) of selvigaltin were 161.0% and 84.0% higher, respectively, after administration of a tablet vs. capsules. Under fed vs. fasted conditions, geometric mean C of the selvigaltin tablet was 20.0% lower, whereas AUC was unaffected. Geometric mean percentage of total dose of selvigaltin excreted in urine over 0─96 h was 30.3% and 35.9% for the tablet under fasted and fed conditions, respectively, and 14.5% for the capsules. No treatment-emergent severe or serious adverse events or study discontinuations due to a treatment-emergent adverse event were reported.
The tablet formulation of selvigaltin displayed higher bioavailability vs. the capsule formulation, with minimal effect of food on PK. Selvigaltin was well-tolerated during all treatments. These findings warrant further clinical development of the tablet formulation of selvigaltin without specific food restrictions.
NCT05747573; February 28, 2023.
半乳糖凝集素-3（一种β-半乳糖苷结合凝集素）的过表达与纤维化疾病和癌症有关。Selvigaltin 是一种口服半乳糖凝集素-3 抑制剂，此前以 50mg 胶囊形式给药。本研究旨在评估健康志愿者中单剂量、随机、三周期、交叉设计（GALBA-1；NCT05747573）下 Selvigaltin 100mg 片剂相对于 50mg 胶囊的相对生物利用度和食物效应。
本研究纳入 13 名参与者，均接受 Selvigaltin 100mg 片剂（空腹和进食状态下）或 2 粒 50mg 胶囊（空腹状态下）治疗。主要终点包括血浆和尿液药代动力学（PK）参数。次要终点为安全性和耐受性。
13 名纳入的参与者中，12 名完成了研究。空腹条件下，片剂相对于胶囊的 Selvigaltin 最大观测血浆浓度（C）和全身暴露（AUC）的几何均数分别高 161.0%和 84.0%。与空腹相比，进食条件下 Selvigaltin 片剂的 C 几何均数降低 20.0%，AUC 不受影响。0-96h 尿液中 Selvigaltin 总剂量的几何平均排泄率分别为片剂空腹和进食条件下的 30.3%和 35.9%，胶囊为 14.5%。未报告与治疗相关的严重或严重不良事件或因治疗相关不良事件导致的研究中止。
Selvigaltin 片剂制剂的生物利用度高于胶囊制剂，食物对 PK 的影响最小。所有治疗中 Selvigaltin 均具有良好的耐受性。这些发现支持在没有特定食物限制的情况下进一步开发 Selvigaltin 片剂制剂。
NCT05747573；2023 年 2 月 28 日。
