[Translation] A single-center, open-label, single-dose clinical trial to investigate the absorption, metabolism, and excretion of 50 mg/80 μCi [14C] janagliptin suspension in healthy Chinese male subjects

研究[14C]-加格列净在健康受试者全血和血浆中总放射性的药代动力学；定量分析健康受试者口服[14C]-加格列净后排泄物的总放射性，获得人体内物质平衡数据，评估加格列净在人体内的主要排泄途径；测定健康受试者口服[14C]-加格列净后血浆、尿液和粪便中的放射性代谢物谱，鉴定主要代谢产物，评估加格列净在人体内的主要代谢途径。

[Translation]

To study the pharmacokinetics of total radioactivity of [14C]-janagliflozin in whole blood and plasma of healthy subjects; to quantitatively analyze the total radioactivity excreted in the excreta of healthy subjects after oral administration of [14C]-janagliflozin, obtain material balance data in the human body, and evaluate the main excretion pathway of janagliflozin in the human body; to measure the radioactive metabolite profile in plasma, urine and feces of healthy subjects after oral administration of [14C]-janagliflozin, identify the main metabolites, and evaluate the main metabolic pathways of janagliflozin in the human body.

Start Date01 Jul 2020

Sponsor / Collaborator

Beijing Sihuan Pharmaceutical Co. Ltd.

[+1]

CTR20192721 / CompletedPhase 1

加格列净片在肾功能正常及轻、中度肾功能损害的中国2型糖尿病患者中的药动学/药效学和安全性的I期研究

[Translation] Phase I study of the pharmacokinetics/pharmacodynamics and safety of janagliflozin tablets in Chinese patients with type 2 diabetes mellitus with normal renal function and mild to moderate renal impairment

主要目的:1、评价加格列净片在肾功能正常及轻、中度肾功能损害的2型糖尿病患者中的药代动力学特征，为加格列净在肾功能损害患者中的临床应用提供依据。次要目的：1、评价加格列净片在肾功能正常及轻、中度肾功能损害的2型糖尿病患者中的药效学特征；2、观察加格列净片在肾功能正常及轻、中度肾功能损害的2型糖尿病患者中的安全性。

[Translation]

Main objectives: 1. To evaluate the pharmacokinetic characteristics of janagliflozin tablets in patients with type 2 diabetes mellitus with normal renal function and mild to moderate renal impairment, and to provide a basis for the clinical application of janagliflozin in patients with renal impairment. Secondary objectives: 1. To evaluate the pharmacodynamic characteristics of janagliflozin tablets in patients with type 2 diabetes mellitus with normal renal function and mild to moderate renal impairment; 2. To observe the safety of janagliflozin tablets in patients with type 2 diabetes mellitus with normal renal function and mild to moderate renal impairment.

Start Date12 Mar 2020

Sponsor / Collaborator

Beijing Sihuan Pharmaceutical Co. Ltd.

[+1]

CTR20190513 / CompletedPhase 3

一项多中心、随机、双盲、安慰剂对照评价加格列净联合二甲双胍治疗2型糖尿病患者有效性和安全性的临床研究

[Translation] A multicenter, randomized, double-blind, placebo-controlled clinical study to evaluate the efficacy and safety of janagliflozin combined with metformin in the treatment of patients with type 2 diabetes

主要目的：在二甲双胍单药治疗效果不佳的中国2型糖尿病成人患者中：评价加格列净片联合二甲双胍治疗24周的有效性；验证在联合二甲双胍治疗时，加格列净片疗效优于安慰剂。次要目的：在二甲双胍单药治疗效果不佳的中国2型糖尿病成人患者中：评价加格列净片联合二甲双胍治疗52周的有效性；评价加格列净片联合二甲双胍治疗的安全性。

[Translation]

Primary objective: To evaluate the efficacy of janagliflozin combined with metformin for 24 weeks in Chinese adult patients with type 2 diabetes who have not responded well to metformin monotherapy; to verify that janagliflozin is superior to placebo when combined with metformin. Secondary objective: To evaluate the efficacy of janagliflozin combined with metformin for 52 weeks in Chinese adult patients with type 2 diabetes who have not responded well to metformin monotherapy; to evaluate the safety of janagliflozin combined with metformin.

Start Date27 May 2019

Sponsor / Collaborator

Beijing Sihuan Pharmaceutical Co. Ltd.

[+1]

100 Clinical Results associated with Janagliflozin

100 Translational Medicine associated with Janagliflozin

100 Patents (Medical) associated with Janagliflozin

Literatures (Medical) associated with Janagliflozin

01 Aug 2023·Clinical pharmacokinetics

Pharmacokinetics, Pharmacodynamics and Safety of Janagliflozin in Chinese Type 2 Diabetes Mellitus Patients with Renal Impairment.

Article

Author: Mi, Nianrong ; He, Kun ; Zhang, Wenyu ; Lou, Kai ; Sun, Jingfang ; Zhao, Zhirui ; Cheng, Hong ; Pang, Shuguang ; Dong, Xiaolin ; Zhao, Hengli ; Wen, Qing ; Hu, Xinyu

BACKGROUNDJanagliflozin is a novel sodium-glucose cotransport-2 inhibitor. Despite its remarkable effect in glycemic control, no systematic research has evaluated the effect of renal impairment (RI) on its pharmacokinetics and pharmacodynamics.METHODSHere, patients with T2DM (n = 30) were divided into normal renal function (eGFR ≥ 90 mL/min/1.73 m²), mild RI (eGFR between 60 and 89 mL/min/1.73 m²), moderate RI-I (eGFR between 45 and 59 mL/min/1.73 m²), and moderate RI-II (eGFR between 30 and 44 mL/min/1.73 m²) groups. They were administered 50 mg janagliflozin orally, and plasma and urine samples were collected for the determination of janagliflozin concentration.RESULTSFollowing oral administration, janagliflozin was rapidly absorbed, with the time to C_max of 2-6 h for janagliflozin and 3-6 h for its metabolite XZP-5185. Plasma exposure levels were similar for janagliflozin in T2DM patients with or without RI but decreased for the metabolite XZP-5185 in T2DM patients with eGFR between 45 and 89 mL/min/1.73 m². Janagliflozin significantly promoted the excretion of urinary glucose, even in patients with reduced eGFR. Janagliflozin was well tolerated in patients with T2DM with or without RI, and no serious adverse events (SAEs) occurred during this trial.CONCLUSIONSThe exposure levels of janagliflozin in T2DM patients were slightly increased with worsening of RI (i.e., 11% increase in the AUC in patients with moderate RI compared with the normal renal function group). Despite worsening of renal function, janagliflozin exerted a significant pharmacologic effect and was well tolerated, even in patients with moderate RI, implying a promising role in the treatment of patients with in T2DM.REGISTRATIONChina Drug Trial register ( http://www.chinadrugtrials.org.cn/I ) identifier no.: CTR20192721.

01 May 2023·Diabetes, Obesity and Metabolism

Efficacy and safety of janagliflozin monotherapy in Chinese patients with type 2 diabetes mellitus inadequately controlled on diet and exercise: A multicentre, randomized, double‐blind, placebo‐controlled, Phase 3 trial

Article

Author: Liu, Jie ; Cheng, Zhifeng ; Ji, Linong ; Hao, Qingshun ; Guo, Yushan ; Pang, Shuguang ; Zhang, Zhinong ; Bian, Fang ; Wang, Kun ; Song, Weihong ; Jiang, Xiaozhen ; Liu, Meiying ; Chen, Xiaowen ; Su, Xiuhai ; Ning, Tao ; Li, Yulan ; Sun, Jingfang

AbstractAimsTo evaluate the efficacy and safety of janagliflozin, a selective renal sodium‐glucose cotransporter‐2 inhibitor, as monotherapy in drug‐naive Chinese patients with type 2 diabetes mellitus (T2DM).Materials and methodsThis Phase 3 trial included a 24‐week, multicentre, randomized, double‐blind, placebo‐controlled period, followed by a 28‐week extension period. A total of 432 patients with glycated haemoglobin (HbA1c) levels ≥7.0% (53 mmol/mol) and ≤10.5% (91 mmol/mol) were randomized (1:1:1) to receive once‐daily placebo, 25 mg or 50 mg janagliflozin. After 24 weeks, patients on placebo were switched and re‐randomized (1:1) to 25 mg or 50 mg janagliflozin, whereas patients on janagliflozin maintained the initial therapy. The primary endpoint was change from baseline in HbA1c after 24 weeks.ResultsAt Week 24, the placebo‐adjusted least squares mean changes in HbA1c were −0.80% (95% confidence interval [CI] −0.98% to −0.62%)/−8.7 mmol/mol (95% CI −10.7 mmol/mol to −6.8 mmol/mol) and −0.88% (95% CI −1.06% to −0.70%)/−9.6 mmol/mol (95% CI −11.6 mmol/mol to −7.7 mmol/mol), respectively (P < 0.001 for both). A higher proportion of patients achieved HbA1c <7.0% (53 mmol/mol) with janagliflozin 25 mg and janagliflozin 50 mg compared with placebo (47.2%, 49.3%, and 23.5%, respectively). Both janagliflozin doses significantly decreased fasting plasma glucose, 2‐hour postprandial glucose, body weight and systolic blood pressure, as well as increased high‐density lipoprotein (HDL) cholesterol and insulin sensitivity compared with placebo (P < 0.05 for all). The trends in improvement of these variables were sustained during the 28‐week extension period. Overall incidences of adverse events were 67.8%, 71.5% and 60.7% with janagliflozin 25 mg, janagliflozin 50 mg and placebo, respectively. The incidence of urinary tract infections and genital fungal infections was low. No severe hypoglycaemia or ketoacidosis occurred.ConclusionsJanagliflozin 25 mg and 50 mg monotherapy once‐daily effectively improved glycaemic control, reduced body weight and blood pressure, improved HDL cholesterol and insulin sensitivity, and was generally well tolerated.

01 Mar 2023·Diabetes, Obesity and Metabolism

Efficacy and safety of janagliflozin as add‐on therapy to metformin in Chinese patients with type 2 diabetes inadequately controlled with metformin alone: A multicentre, randomized, double‐blind, placebo‐controlled, phase 3 trial

Article

Author: Tan, Xingrong ; Xu, Fangjiang ; Su, Benli ; Song, Weihong ; Wang, Kun ; Gao, Leili ; Ye, Jun ; Su, Xiuhai ; Guo, Yushan ; Li, Jiarui ; Chen, Xiaowen ; Pang, Shuguang ; Chen, Lili ; Wang, Yuan ; Liao, Lin ; Ji, Linong ; Sun, Jingfang ; Cheng, Zhifeng

AbstractAimTo evaluate the efficacy and safety of janagliflozin in Chinese patients with type 2 diabetes (T2D) inadequately controlled with metformin monotherapy.Materials and methodsThis multicentre phase 3 trial included a 24‐week, randomized, double‐blind, placebo‐controlled period, followed by a 28‐week extension period. Patients (N = 421) with HbA1c of 7.0% or higher and 10.5% or less were randomized (1:1:1) to receive once‐daily placebo, janagliflozin 25 or 50 mg. After the 24‐week treatment period, patients on placebo were re‐randomized (1:1) to janagliflozin 25 or 50 mg for the additional 28‐week treatment, whereas patients on janagliflozin maintained the same therapy. The primary endpoint was the change from baseline in HbA1c to week 24.ResultsAt week 24, the placebo‐adjusted least squares mean changes of HbA1c were –0.58% and –0.58% with janagliflozin 25 and 50 mg, respectively (P < .0001 for both). The proportion of patients achieving HbA1c less than 7.0% was higher with janagliflozin 25 and 50 mg compared with placebo (41.8%, 41.7% and 28.0%, respectively). Both janagliflozin doses provided significant reductions in fasting plasma glucose, 2‐hour postprandial glucose, body weight and systolic blood pressure, and improvements in high‐density lipoprotein cholesterol and insulin sensitivity compared with placebo (P < .05 for all). The trends in improvement of these variables were retained during the 28‐week extension period. No severe hypoglycaemia occurred throughout the whole 52‐week treatment.ConclusionsJanagliflozin 25 or 50 mg once‐daily added to metformin therapy significantly improved glycaemic control, reduced body weight and systolic blood pressure, improved high‐density lipoprotein cholesterol and insulin sensitivity, and was generally well‐tolerated by Chinese T2D patients who had poor glycaemic control with metformin monotherapy.

100 Deals associated with Janagliflozin

External Link

KEGG	Wiki	ATC	Drug Bank
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R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	16 Jan 2024

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	NDA/BLA	CN	Beijing Sihuan Pharmaceutical Co. Ltd.	28 Feb 2022

Clinical Result

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Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03811548 (Pubmed) Manual	Phase 3	Diabetes Mellitus, Type 2	432	Janagliflozin 25mg	(tmdrnyjtxd) = kswicafcdk ynftcbmily (rbsicglnvf, -0.98 to -0.62) Met View more	Positive	20 Jan 2023
				Janagliflozin 50mg	(tmdrnyjtxd) = fvwixxqnqo ynftcbmily (rbsicglnvf, -1.06 to -0.70) Met View more

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