[Translation] A multicenter, randomized, double-blind, placebo-controlled, dose-finding clinical trial to preliminarily evaluate the efficacy and safety of oral GW117 tablets in the treatment of depression

探索口服GW117片治疗抑郁症的最佳给药剂量，初步评价疗效和安全性，为Ⅲ期临床试验方案的研究设计和给药方案的确定提供依据。

[Translation]

To explore the optimal dosage of oral GW117 tablets for the treatment of depression, preliminarily evaluate the efficacy and safety, and provide a basis for the research design and dosing regimen of the Phase III clinical trial.

Start Date07 Jul 2022

Sponsor / Collaborator

Nanjing Guangwei Medical Technology Co., Ltd.

[+1]

CTR20221750 / CompletedPhase 1

中国健康受试者舌下含服GW117口崩片的随机、双盲、安慰剂对照、剂量递增的I期临床试验

[Translation] A randomized, double-blind, placebo-controlled, dose-escalation phase I clinical trial of sublingual GW117 orodisintegrating tablets in healthy Chinese subjects

研究健康受试者单次舌下含服不同剂量GW117口崩片的耐受性及药代动力学，研究健康受试者多次舌下含服不同剂量GW117口崩片的耐受性及药代动力学，为后期临床试验提供依据。

[Translation]

To study the tolerance and pharmacokinetics of a single sublingual administration of different doses of GW117 orodisintegrating tablets in healthy subjects, and to study the tolerance and pharmacokinetics of multiple sublingual administration of different doses of GW117 orodisintegrating tablets in healthy subjects, so as to provide a basis for later clinical trials.

Start Date12 Jul 2021

Sponsor / Collaborator

Beijing Guangwei Pharma Technology Co., Ltd.

ChiCTR2100043858 / RecruitingPhase 1IIT

The tolerance, pharmacokinetics, and dietary effects of oral GW117 tablets to Healthy Chinese Subjects

Start Date15 Mar 2021

Sponsor / Collaborator

Chinese People's Liberation Army General Hospital

100 Clinical Results associated with GW-117

100 Translational Medicine associated with GW-117

100 Patents (Medical) associated with GW-117

Literatures (Medical) associated with GW-117

01 Feb 2024·European Journal of Pharmacology

Mechanism of GW117 antidepressant action: melatonin receptor-mediated regulation of sleep rhythm

Article

Author: Ji, Hong-Xian ; Tiliwaerde, Murezati ; Zhang, Ting-Ting ; Yang, Ya-Qi ; Gu, Wei ; Gao, Na-Na ; Jin, Zeng-Liang

Alterations in circadian sleep patterns constitute a salient manifestation in major depressive disorder. GW117, an emergent antidepressant, functions as an agonist for melatonin 1 and melatonin 2 (MT1/MT2) receptors, in tandem with antagonism of the serotonin (5-HT) 2C receptor. The present investigation is dedicated to elucidating the role and underlying mechanisms by which GW117 ameliorates circadian sleep disruptions. Utilizing an adapted chronic unpredictable mild stress protocol, we induced a depressive-like phenotype and perturbed circadian rhythms in rodent models. Our methodological approach integrated quantitative polymerase chain reaction (qPCR) in real-time, enzyme-linked immunosorbent assay (ELISA), and immunoblotting techniques to probe alterations in the expression of core circadian genes and homeostatic sleep markers. The impact of GW117 was assessed across various dosages (10, 20, and 40 mg/kg) on these molecular signatures. In a parallel examination, we evaluated the influence of GW117 (administered at 15, 40, and 60 mg/kg) on the sleep patterns of healthy mice. The results showed that GW117 significantly improved sleep-wake circadian rhythms, altered sleep architecture, and shortened sleep latency. Furthermore, GW117 increased the expression of several clock genes in the hypothalamus of chronic unpredictable mild stress model rats and normal mice. It also regulated circadian biomarkers, including melatonin and cortisol. Based on our findings, we propose that the beneficial effects of GW117 on sleep rhythms may be due to the melatonin system-mediated activation of the Wnt/β-catenin signaling pathway.

01 Apr 2023·Journal of Applied Toxicology

28‐day repeated dose toxicity and toxicokinetics study on new melatonergic antidepressant GW117 in beagle dogs

Article

Author: Zhang, Daizhou ; Ying, Yong ; Gu, Wei ; Liu, Xiaoyu ; Liu, Tianbin ; Cao, Chong ; Chen, Kai ; Zhang, Yanhua ; Gao, Mei ; Yang, Guiwen

AbstractGW117 is new melatonergic antidepressant being developed to show better antidepressant action than agomelatine. The purpose of this study was to evaluate the toxicity and to determine potential target organs after oral (gavage) administration of the test article GW117 for 28 days and to assess the reversibility after a 4‐week recovery phase in beagle dogs. Toxicokinetics was also evaluated. Four groups were designed in this study, including the vehicle control group and the GW117 50, 150 and 500 mg/kg/day groups, with 5 dogs/sex/group. Body weight, hematology, clinical chemistry, gross necropsy, organ weight, histopathology, and other indicators were examined. Results showed that animals dosed at ≥150 mg/kg/day showed gastrointestinal reactions (watery feces and dark green/red brown feces), with a dose–response relationship in the incidence and severity grade. Female dogs at 500 mg/kg/day had an increase in organ weight and ratios of the liver at the end of the dosing phase. Histopathology examination showed that some animals at 500 mg/kg/day, especially female animals, had minimal centrilobular hepatocyte hypertrophy in the liver, which reversed after 28‐day recovery. With the exception of the above, no GW117‐related abnormality was noted. Meanwhile, there were no sexual differences in drug exposure and accumulation after the first and last dosing. The no observed adverse effect dose level (NOAEL) was 150 mg/kg/day, under which mean Cmax and AUC0 → t were 583.5 and 2767.0 ng/ml*h for females and 663.2 and 4046.3 ng/ml*h for males on Day 28.

01 Mar 2023·Heliyon

Acute toxicity and genotoxicity studies on new melatonergic antidepressant GW117

Article

Author: Zhang, Daizhou ; Liu, Tianbin ; Cao, Chong ; Tang, Liansheng ; Sun, Haiji ; Gao, Mei ; Gu, Wei ; Zheng, Zhiyong ; Ma, Hui

GW117, a novel derivate compound of agomelatine that acts as both a 5-HT2C receptor antagonist and a MT1/MT2 receptor agonist, likely underlines the potent antidepressant action with less hepatotoxicity than agomelatine. We evaluated the acute toxicity of GW117, and the genotoxicity of GW117 using bacterial reverse mutation test, mammalian chromosomal aberration test in Chinese hamster lung cells (CHL) and mouse bone marrow micronucleus test. The acute toxicity test results showed that maximum tolerated dose (MTD) of GW117 was 2000 mg/kg, under which mean C_max and AUC_0→t was 10,782 ng/mL and 81,046 ng/mL × h, respectively. The result of bacterial reverse mutation test showed that the number of bacterial colonies in each dose group of GW117 did not increase significantly compared with that in the solvent control group with or without S9 metabolic activation system. In vitro chromosome aberration test of CHL cells, the chromosome aberration rate of each dose group of GW117 did not increase with or without S9 metabolic activation system. In mouse micronucleus test, the highest dose was 2000 mg/kg, the micronucleus rate did not increase significantly. Under the conditions of this study, the MTD of a single GW117 administration was 2000 mg/kg, there was no genotoxicity effect of GW117.

100 Deals associated with GW-117

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Indication	Highest Phase	Country/Location	Organization	Date
Depressive Disorder	Phase 2	CN	Beijing Guangwei Pharma Technology Co., Ltd.	07 Jul 2022

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