Department of Endocrinology, Hematology and Gerontology, Chiba University Hospital, Chiba, Japan.
Department of Diabetes, Metabolism and Endocrinology, Chiba University Hospital, Chiba, Japan.
Diabetes Obes Metab. 2020 Jul;22(7):1102-1110. doi: 10.1111/dom.14006. Epub 2020 Mar 12.
LIK066 (licogliflozin) is a dual sodium glucose co-transporter 1/2 inhibitor with potential benefits in weight loss. This study evaluated the efficacy, tolerability and safety of licogliflozin in Japanese adults with obesity.
This study was a randomized, double-blind, placebo-controlled, dose-finding study to evaluate the effect of licogliflozin (2.5, 10, 25 and 50 mg once daily) in 126 Japanese patients with obesity. The primary objective was to examine the dose-response relationship of licogliflozin treatment in body weight reduction relative to placebo at 12 weeks. The secondary objectives included assessment of responder rates, change in parameters related to complications, visceral and subcutaneous fat area, and safety during 12 weeks of treatment.
The placebo-subtracted least square mean percentage change in body weight from baseline at week 12 was -1.99 (95% confidence interval -2.92, -0.21), -3.00 (-4.15, -1.70), -3.54 (-4.54, -2.26) and - 3.91% (-5.01, -2.77) in licogliflozin 2.5, 10, 25 and 50 mg once-daily dose groups, respectively. The proportion of responders with ≥3% reduction in body weight in the licogliflozin 2.5, 10, 25 and 50 mg once-daily dose groups were 15.8%, 55.6%, 50.0% and 56.7%, respectively, versus placebo [7.1%; P ≤0.002 for all except the 2.5 mg once-daily group (P = 0.39)]. Dose-dependent reductions were observed significantly in haemoglobin A1c, uric acid, fasting plasma glucose and potentially in the waist circumference, diastolic blood pressure and visceral fat area.
Dual inhibition of SGLT1/2 with licogliflozin treatment induced a dose-dependent reduction in body weight in Japanese patients with obesity. Treatment with licogliflozin was safe and well tolerated in this study. The study is registered with ClinicalTrials.gov (NCT03320941).
LIK066（licogliflozin）是一种钠-葡萄糖共转运蛋白 1/2 双重抑制剂，具有减肥的潜在益处。本研究评估了 licogliflozin 对肥胖的日本成年人的疗效、耐受性和安全性。
这是一项随机、双盲、安慰剂对照、剂量探索研究，旨在评估 licogliflozin（每日一次 2.5、10、25 和 50mg）治疗 126 例肥胖日本患者的效果。主要目的是检查 licogliflozin 治疗相对于安慰剂在 12 周时体重减轻的剂量反应关系。次要目标包括评估应答率、与并发症相关参数、内脏和皮下脂肪面积的变化，以及治疗 12 周期间的安全性。
安慰剂校正后，第 12 周时体重相对于基线的最小平方均数百分比变化分别为-1.99%（95%置信区间-2.92，-0.21）、-3.00%（-4.15，-1.70）、-3.54%（-4.54，-2.26）和-3.91%（-5.01，-2.77），分别为 licogliflozin 2.5、10、25 和 50mg 每日一次剂量组。体重下降≥3%的应答者比例分别为 licogliflozin 2.5、10、25 和 50mg 每日一次剂量组为 15.8%、55.6%、50.0%和 56.7%，安慰剂组为 7.1%[除 2.5mg 每日一次组外（P=0.39），所有组 P≤0.002]。观察到血红蛋白 A1c、尿酸、空腹血糖以及腰围、舒张压和内脏脂肪面积显著剂量依赖性降低。
SGLT1/2 的双重抑制作用导致肥胖的日本患者体重呈剂量依赖性下降。在这项研究中，licogliflozin 的治疗是安全且耐受良好的。该研究在 ClinicalTrials.gov（NCT03320941）注册。
