Delving into the Latest Updates on Cetagliptin Phosphate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

森格列汀, 磷酸盛格列汀

+ [3]

Target

DPP-4

Action

inhibitors

Mechanism

DPP-4 inhibitors(Dipeptidyl peptidase IV inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication-

Originator Organization

CGeneTech (Suzhou, China) Co. Ltd.

Active Organization

CGeneTech (Suzhou, China) Co. Ltd.

Nanjing Healthnice Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

China (01 Dec 2024),

Diabetes Mellitus, Type 2

RegulationSpecial Review Project (China)

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Structure/Sequence

Molecular FormulaC18H21F6N4O5P

InChIKeyOZJGFWPPILNFKT-FOKYBFFNSA-N

CAS Registry2243737-33-7

View All Structures (2)

This study aims to evaluate the material balance and biotransformation pathways of [14C] senolagliptin phosphate after a single oral dose in healthy Chinese male volunteers. The overall pharmacokinetic characteristics of senolagliptin phosphate in humans are evaluated to provide a reference for the rational use of the drug.

Start Date07 Jul 2020

Sponsor / Collaborator

CGeneTech (Suzhou, China) Co. Ltd.

CTR20200157

/ CompletedPhase 3

一项多中心、随机、双盲、安慰剂对照评价盛格列汀联合二甲双胍治疗2型糖尿病患者的有效性和安全性临床研究

[Translation] A multicenter, randomized, double-blind, placebo-controlled clinical study to evaluate the efficacy and safety of senagliflozin 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血糖控制不佳的中国成人2型糖尿病患者中，评价磷酸盛格列汀片（50mg和100mg）联合二甲双胍治疗24周的有效性，验证磷酸盛格列汀片联合二甲双胍的疗效优于安慰剂联合二甲双胍。

[Translation]

Primary objective: To evaluate the efficacy of senoside phosphate tablets (50 mg and 100 mg) combined with metformin for 24 weeks in Chinese adult patients with type 2 diabetes who have poor glycemic control on metformin monotherapy, and to verify that the efficacy of senoside phosphate tablets combined with metformin is superior to that of placebo combined with metformin.

Start Date27 Apr 2020

Sponsor / Collaborator

CGeneTech (Suzhou, China) Co. Ltd.

CTR20200172

/ CompletedPhase 3

一项多中心、随机、双盲、安慰剂平行对照评价磷酸盛格列汀片单药治疗2型糖尿病患者的有效性和安全性研究

[Translation] A multicenter, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of senolytic phosphate monotherapy in patients with type 2 diabetes

主要目的：在经饮食和运动治疗后血糖控制不佳的中国成人2型糖尿病患者中，评价磷酸盛格列汀片（50mg、100mg）单药治疗24周的有效性，验证磷酸盛格列汀片的疗效优于安慰剂。

[Translation]

Primary objective: To evaluate the efficacy of 24-week monotherapy with senolagliptin phosphate tablets (50 mg, 100 mg) in Chinese adults with type 2 diabetes who have poor blood sugar control after diet and exercise therapy, and to verify that the efficacy of senolagliptin phosphate tablets is superior to placebo.

Start Date20 Apr 2020

Sponsor / Collaborator

CGeneTech (Suzhou, China) Co. Ltd.

100 Clinical Results associated with Cetagliptin Phosphate

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100 Translational Medicine associated with Cetagliptin Phosphate

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100 Patents (Medical) associated with Cetagliptin Phosphate

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11

Literatures (Medical) associated with Cetagliptin Phosphate

01 Oct 2024·Clinical Pharmacokinetics

Use of a PK/PD Model to Select Cetagliptin Dosages for Patients with Type 2 Diabetes in Phase 3 Trials

Article

Author: Yu, Qiang ; Zhao, Jiahong ; Lu, Jinmiao ; Xie, Daosheng ; Ding, Juping ; Wang, Tong

BACKGROUNDCetagliptin is a novel dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of patients with type 2 diabetes (T2D). Several phase 1 studies have been conducted in China. Modelling and simulation were used to obtain cetagliptin dose for phase 3 trials in T2D patients.METHODSA pharmacokinetic (PK)/pharmacodynamic (PD) model and model-based analysis of the relationship between hemoglobin A1c (HbA1c) and dosage was explored to guide dose selection of cetagliptin for phase 3 trials. The PK/PD data were derived from four phase 1 clinical studies, and sitagliptin 100 mg was employed as a positive control in studies 1, 3, and 4.RESULTSThe PK profiles of cetagliptin were well described by a two-compartment model with first-order absorption, saturated efflux, and first-order elimination. The final PD model was a sigmoid maximum inhibitory efficacy (E_max) model with the Hill coefficient. The final model accurately captured cetagliptin PK/PD, demonstrated by goodness-of-fit plots. Based on weighted average inhibition (WAI), the relationship between HbA1c and dose was well displayed. Cetagliptin 50 mg once daily or above as monotherapy or as add-on therapy appeared more effective in HbA1c reduction than sitagliptin 100 mg. Cetagliptin 50 mg or 100 mg once daily was selected as the dose for phase 3 trials of cetagliptin in T2D patients.CONCLUSIONSThe PK/PD model supports dose selection of cetagliptin for phase 3 trials. A model‑informed approach can be used to replace a dose-finding trial and accelerate cetagliptin's development.

01 Jun 2024·European Journal of Medicinal Chemistry

Synthesis and clinical application of representative small-molecule dipeptidyl Peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes mellitus (T2DM)

Review

Author: Zhao, Li-Jie ; Sun, Jin-Feng ; Shao, Dong-Wei

Diabetes mellitus is a chronic metabolic disorder characterized by high blood glucose levels, which can cause many diseases, including osteoporosis, fractures, arthritis, and foot complications. The inhibitors of dipeptidyl peptidase-4 (DPP-4), an enzyme involved in glucose metabolism regulation, are essential for managing Type 2 Diabetes Mellitus (T2DM). The inhibition of DPP-4 has become a promising treatment approach for T2DM because it can increase levels of active glucagon-like peptide-1 (GLP-1), leading to improved insulin secretion in response to glucose and reduced release of glucagon. The review commences by elucidating the role of DPP-4 in glucose homeostasis and its significance in T2DM pathophysiology. Furthermore, it presents the mechanism of action, preclinical pharmacodynamics, clinical efficacy, and toxicity profiles of small-molecule DPP-4 inhibitors across various clinical stages. This comprehensive review provides valuable insights into the synthesis and clinical application of DPP-4 inhibitors, serving as an invaluable resource for researchers, clinicians, and pharmaceutical professionals interested in diabetes therapeutics and drug development.

01 Dec 2023·Diabetes, Obesity and Metabolism

A randomized, double‐blind, placebo controlled, phase 3 trial to evaluate the efficacy and safety of cetagliptin added to ongoing metformin therapy in patients with uncontrolled type 2 diabetes with metformin monotherapy

Article

Author: Ding, Juping ; Ji, Linong ; Wang, Tong ; Cheng, Zhifeng ; Zhang, Lili ; Xie, Daosheng ; Gao, Leili ; Li, Jifang ; Lu, Jinmiao ; Li, Ping ; Yan, Xiaoguang ; Zhao, Jiahong ; Tian, Junhang ; Yu, Qiang ; Bai, Jie

AbstractAimThis trial was designed to assess the efficacy and safety of cetagliptin added to metformin in Chinese patients with type 2 diabetes who had inadequate glycaemic control with metformin monotherapy.MethodsIn total, 446 patients with type 2 diabetes on metformin monotherapy were randomized to receive the addition of once‐daily cetagliptin 100 mg, cetagliptin 50 mg and placebo in a 2:2:1 ratio for 24‐week double‐blind treatment. At week 24, patients initially randomized to cetagliptin 50 mg and placebo were switched to cetagliptin 100 mg for 28 weeks open‐label treatment. The primary endpoint was the change in haemoglobin A1c (HbA1c) from baseline, and the efficacy analyses were based on an all‐patients‐treated population using an analysis of co‐variance.ResultsAfter 24 weeks, both add‐on therapies led to greater glycaemic control. Reductions in HbA1c from baseline were −1.17 ± 0.794%, −1.23 ± 0.896% in cetagliptin 100 mg and 50 mg plus metformin group, respectively. No difference was observed between the cetagliptin 100 mg and 50 mg plus metformin group. Patients with higher baseline HbA1c levels (≥8.5%) experienced greater reductions in HbA1c. A significantly greater proportion of patients achieved an HbA1c <7.0% with cetagliptin 100 mg (49.4%) and cetagliptin 50 mg (51.1%) plus metformin than metformin monotherapy (14.4%). Both combination therapies also improved the homeostasis model assessment β‐function index and decreased systolic blood pressure. There was no increased risk of adverse effects with combination therapy, and both combination therapies were generally well tolerated.ConclusionsThe addition of cetagliptin once daily to metformin was more efficacious and well tolerated than metformin monotherapy in Chinese patients with type 2 diabetes who had inadequate glycaemic control with metformin monotherapy.

100 Deals associated with Cetagliptin Phosphate

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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	China	CGeneTech (Suzhou, China) Co. Ltd.	01 Dec 2024

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	NDA/BLA	China	Nanjing Healthnice Pharmaceutical Co., Ltd.	02 Feb 2023

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CTR20200172 (NEWS) Manual	Phase 3	Diabetes Mellitus, Type 2	-	磷酸森格列汀片 50mg	(udidlpsybv) = jhbnexvfgh lpxbejrwfp (tujzgavgpy )	Positive	03 Dec 2024
CTR20200172 (NEWS) Manual	Phase 3	Diabetes Mellitus, Type 2	-	磷酸森格列汀片 100mg	(udidlpsybv) = ncqhlyogzn lpxbejrwfp (tujzgavgpy )	Positive	03 Dec 2024
CTR20200157 \| CTR20200172 (Corporate Publications) Manual	Phase 3	Diabetes Mellitus, Type 2	1,000	盛格列汀	(csmorpaqco) = 盛格列汀片50mg剂量组（低剂量组）第24周末糖化血红蛋白（HbA1c）降低值达到主要临床终点，显著优于对照组 nkzcgplzzb (dtkcjulcvb ) View more	Positive	17 Oct 2022