Delving into the Latest Updates on Retagliptin Phosphate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

瑞格列汀, 瑞泽唐

Target

DPP-4

Mechanism

DPP-4 inhibitors(Dipeptidyl peptidase IV inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2Diabetes Mellitus, Noninsulin-Dependent, 2Diabetes Mellitus

Inactive Indication

Renal Insufficiency

Originator Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Active Organization

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

CN (27 Jun 2023),

Diabetes Mellitus, Type 2

RegulationSpecial Review Project (CN)

Login to view timeline

Structure

Molecular FormulaC19H18F6N4O3

InChIKeyWIIAMRXFUJLYEF-SNVBAGLBSA-N

CAS Registry1174122-54-3

View All Structures (2)

Primary study objective: To evaluate and compare the pharmacokinetics of SP2086 in subjects with mild to moderate hepatic impairment and subjects with normal hepatic function; Secondary study objective: To evaluate the safety of SP2086 in subjects with mild to moderate hepatic impairment and subjects with normal hepatic function

Start Date20 Sep 2023

Sponsor / Collaborator

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

NCT06035406 / Not yet recruitingPhase 1

Pharmacokinetics and Safety of SP2086 in Subjects With Mild and Moderate Liver Impairment and Normal Liver Function.

This study used a single-dose, open design to compare the pharmacokinetics of subjects with mild and moderate liver impairment and subjects with normal liver function.

Start Date01 Sep 2023

Sponsor / Collaborator

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

NCT05682495 / CompletedPhase 1

A Bioequivalence Study of HR20031 Tablet in Healthy Subjects

The purpose of this study is to assess the bioequivalence between HR20031 FDC tablet and co-administration of SHR3824 tablets, SP2086 tablets and metformin XR tablets.

Start Date31 Jan 2023

Sponsor / Collaborator

Shandong Suncadia Medicine Co., Ltd.Startup

100 Clinical Results associated with Retagliptin Phosphate

Login to view more data

100 Translational Medicine associated with Retagliptin Phosphate

Login to view more data

100 Patents (Medical) associated with Retagliptin Phosphate

Login to view more data

6

Literatures (Medical) associated with Retagliptin Phosphate

01 Jul 2024·Diabetes, Obesity and Metabolism

Retagliptin as add‐on therapy to metformin in Chinese patients with type 2 diabetes inadequately controlled with metformin: A multicentre, randomized, double‐blind, placebo‐controlled, phase 3 trial

Article

Author: Liu, Li ; Qin, Jie ; Yu, Dongni ; Liu, Cong ; Zhang, Yawei ; Chen, Mingwei ; Guo, Lixin ; Dai, Wei ; Zong, Yicen ; Li, Shuangqing ; Tian, Fengsheng ; Jiang, Chengxia

AbstractAimTo evaluate the efficacy and safety of retagliptin in Chinese patients with type 2 diabetes (T2D) inadequately controlled with metformin.Materials and MethodsThis multicentre, phase 3 trial consisted of a 16‐week, randomized, double‐blind, placebo‐controlled period, where patients with HbA1c levels between 7.5% and 11.0% were randomized to receive either once‐daily (QD) retagliptin 100 mg (n = 87) or placebo (n = 87), both as an add‐on to metformin. The primary endpoint was the change in HbA1c from baseline to week 16.ResultsAt week 16, the least squares mean change in HbA1c from baseline, compared with placebo, was −0.82% (95% CI, −1.05% to −0.58%) for the retagliptin 100 mg QD group (P < .0001) per treatment policy estimand. Significantly higher proportions of patients in the retagliptin 100 mg QD group achieved HbA1c levels of less than 6.5% (11.5%) and less than 7.0% (26.4%) compared with those receiving placebo (0% and 4.6%; P = .0016 and P < .0001, respectively) at week 16. Retagliptin 100 mg QD also lowered fasting plasma glucose and 2‐hour postprandial plasma glucose levels. The incidence of adverse events (AEs) during the treatment period was similar between the two groups. However, slightly higher proportions of increased lipase and increased amylase in the retagliptin 100 mg QD group were observed. No patients discontinued treatment permanently because of AEs, and no episodes of severe hypoglycaemia were reported.ConclusionsRetagliptin 100 mg QD as an add‐on therapy to metformin offers a new therapeutic option for treating Chinese patients with T2D inadequately controlled by metformin alone, and is generally well tolerated.

01 Jul 2024·Diabetes, Obesity and Metabolism

Combination of retagliptin and henagliflozin as add‐on therapy to metformin in patients with type 2 diabetes inadequately controlled with metformin: A multicentre, randomized, double‐blind, active‐controlled, phase 3 trial

Article

Author: Wang, Quanren ; Zhang, Danli ; Zhang, Lihui ; Jiang, Chengxia ; Ye, Zi ; Gu, Qin ; Chen, Mingwei ; Peng, Liang ; Xu, Jing ; Wang, Yao ; Sun, Xiaodong ; Lin, Xiang ; Song, Weihong ; Dong, Xiaolin ; Lu, WeiPing ; Dai, Wei ; Fu, Yanqin ; Bi, Yan ; Yang, Wenying ; Pan, Tianrong

AbstractAimThis study assessed the efficacy and safety of co‐administering retagliptin and henagliflozin versus individual agents at corresponding doses in patients with type 2 diabetes mellitus who were inadequately controlled with metformin.MethodsThis multicentre, phase 3 trial consisted of a 24‐week, randomized, double‐blind, active‐controlled period. Patients with glycated haemoglobin (HbA1c) levels between 7.5% and 10.5% were randomized to receive once‐daily retagliptin 100 mg (R100; n = 155), henagliflozin 5 mg (H5; n = 156), henagliflozin 10 mg (H10; n = 156), co‐administered R100/H5 (n = 155), or R100/H10 (n = 156). The primary endpoint was the change in HbA1c from baseline to week 24.ResultsBased on the primary estimand, the least squares mean reductions in HbA1c at week 24 were significantly greater in the R100/H5 (−1.51%) and R100/H10 (−1.54%) groups compared with those receiving the corresponding doses of individual agents (−0.98% for R100, −0.86% for H5 and −0.95% for H10, respectively; p < .0001 for all pairwise comparisons). Achievement of HbA1c <7.0% at week 24 was observed in 27.1% of patients in the R100 group, 21.2% in the H5 group, 24.4% in the H10 group, 57.4% in the R100/H5 group and 56.4% in the R100/H10 group. Reductions in fasting plasma glucose and 2‐h postprandial glucose were also more pronounced in the co‐administration groups compared with the individual agents at corresponding doses. Decreases in body weight and systolic blood pressure were greater in the groups containing henagliflozin than in the R100 group. The incidence rates of adverse events were similar across all treatment groups, with no reported episodes of severe hypoglycaemia.ConclusionsFor patients with type 2 diabetes mellitus inadequately controlled by metformin monotherapy, the co‐administration of retagliptin and henagliflozin yielded more effective glycaemic control through 24 weeks compared with the individual agents at their corresponding doses.

01 Jan 2022·Journal of Separation Science

High‐throughput bioanalysis of sitagliptin in plasma using direct analysis in real time mass spectrometry and its application in the pharmacokinetic study thereof

Article

Author: Shan, Yuqin ; Zhang, Linge ; Gu, Jingkai ; Zhang, Yuyao ; Meng, Xiangjun ; Liu, Yingze ; Sun, Dong

AbstractSitagliptin is a dipeptidyl peptidase‐IV inhibitor for the treatment of type 2 diabetes mellitus. In the present study, a sensitive and high‐throughput quantitative method based on the direct analysis in real time tandem mass spectrometry has been developed and validated for the bioanalysis of sitagliptin in rat plasma without chromatographic separation. Sitagliptin and its internal standard retagliptin were detected in positive ion mode by multiple reaction monitoring transitions at m/z 408.2→235.0 and 465.2→260.1, respectively. The method includes a simple solid‐phase extraction sample preparation procedure, through which appropriate and reproducible analytical results within the linear concentration range of 20–2000 ng/mL have been achieved. The intra‐ and interday precisions were <10.6% and the accuracies were ranging from −8.17 to 2.60%. This method has been successfully applied to the pharmacokinetic study of sitagliptin after single intravenous administration in rats. This approach shows considerable promise of direct analysis in real time tandem mass spectrometry method in the high‐throughput bioanalysis.

100 Deals associated with Retagliptin Phosphate

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14898

R&D Status

Approved

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	27 Jun 2023

Developing

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Noninsulin-Dependent, 2	Phase 3	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	06 Dec 2021
Diabetes Mellitus	Phase 1	-	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	01 Sep 2023
Renal Insufficiency	Preclinical	CN	Jiangsu Hengrui Pharmaceuticals Co., Ltd.	26 Jun 2014

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CTR20131399 (SP2086-301, Corporate Publications) Manual	Phase 3	Diabetes Mellitus, Type 2	340	磷酸瑞格列汀 50 mg	-	Positive	01 Jul 2023
				磷酸瑞格列汀 100 mg
CTR20160943 (SP2086-303, Corporate Publications) Manual	Phase 3	Diabetes Mellitus, Type 2	321	磷酸瑞格列汀+盐酸二甲双胍	(vflmpiutle): Difference(%) = -0.62, P-Value = <0.0001	Positive	01 Jul 2023
				Placebo