Delving into the Latest Updates on Trelagliptin Succinate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Trelagliptin, Trelagliptin succinate (JAN/USAN), 曲格列汀

+ [7]

Target

DPP-4

Mechanism

DPP-4 inhibitors(Dipeptidyl peptidase IV inhibitors)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Diabetes Mellitus, Type 2

Inactive Indication

Kidney Failure, Chronic

Originator Organization

Takeda California, Inc.

Active Organization

Takeda Pharmaceutical Co., Ltd.

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

JP (26 Mar 2015),

Diabetes Mellitus, Type 2

Regulation-

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Structure

Molecular FormulaC18H20FN5O2

InChIKeyIWYJYHUNXVAVAA-OAHLLOKOSA-N

CAS Registry865759-25-7

View All Structures (2)

主要目的：以健康受试者为试验对象，采用随机、开放、两周期、两序列、双交叉试验设计，考察健康受试者空腹及餐后单次口服由江苏万禾制药有限公司生产（MAH：南京万融健诚医药科技有限公司）的琥珀酸曲格列汀片（受试制剂，规格：100mg）与日本武田药品工业株式会社生产的琥珀酸曲格列汀片（参比制剂，Zafatek ®，规格：100mg）后曲格列汀的体内经时过程，估算其相关药代动力学参数及相对生物利用度，评价其空腹及餐后状态下的生物等效性，为受试制剂的生产注册申请提供依据。次要目的：评价琥珀酸曲格列汀片受试制剂和参比制剂（商品名：Zafatek ®）在健康受试者中的安全性.

[Translation]

Main purpose: With healthy subjects as the test subjects, a randomized, open, two-period, two-sequence, double-crossover design was used to investigate the in vivo time course of trelagliptin after a single oral administration of Trelagliptin Succinate Tablets (test preparation, specification: 100 mg) produced by Jiangsu Wanhe Pharmaceutical Co., Ltd. (MAH: Nanjing Wanrong Jiancheng Pharmaceutical Technology Co., Ltd.) and Trelagliptin Succinate Tablets (reference preparation, Zafatek ®, specification: 100 mg) produced by Takeda Pharmaceutical Co., Ltd., Japan, to estimate their relevant pharmacokinetic parameters and relative bioavailability, evaluate their bioequivalence in fasting and postprandial states, and provide a basis for the production registration application of the test preparation. Secondary purpose: To evaluate the safety of the test preparation and reference preparation (trade name: Zafatek ®) of Trelagliptin Succinate Tablets in healthy subjects.

Start Date02 Jan 2024

Sponsor / Collaborator

Jiangsu Wanchuan Medical & Health Industry Group Co., Ltd.

CTRI/2023/01/048826 / Active, not recruitingPhase 3

A randomized, multi-centric, comparative, parallel, open-label, active-controlled, Phase III trial study to demonstrate the non-inferiority of Trelagliptin 100mg once weekly to Vildagliptin 50 mg twice daily in the management of Type-2 Diabetes Mellitus.

Start Date10 Jan 2023

Sponsor / Collaborator

Zuventus Healthcare Ltd.

CTRI/2023/01/048758 / Active, not recruitingNot Applicable

An open label, balanced, randomized, two-treatment, two-sequence, two-period, single-dose, truncated, crossover oral bioequivalence study between the Test Product, Trelagliptin 100 mg Tablets (Zuventus Healthcare Ltd., India) and the Reference Product, Zafatek® (Trelagliptin 100 mg) tablets (Takeda Pharmaceutical Company Limited, Japan) in healthy, adult, human subjects under fasting conditions.

Start Date08 Jan 2023

Sponsor / Collaborator

Zuventus Healthcare Ltd.

100 Clinical Results associated with Trelagliptin Succinate

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100 Translational Medicine associated with Trelagliptin Succinate

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100 Patents (Medical) associated with Trelagliptin Succinate

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60

Literatures (Medical) associated with Trelagliptin Succinate

01 Jul 2024·Diabetology International

Effects of dulaglutide and trelagliptin on beta-cell function in patients with type 2 diabetes: a randomized controlled study: DUET-beta study

Article

Author: Satoh, Shinobu ; Kondo, Yoshinobu ; Terauchi, Yasuo

AimsThis randomized, open-label, parallel-group, controlled trial compared the effects of dulaglutide and trelagliptin on beta-cell function in patients with type 2 diabetes.Materials and methodsFor 24 weeks, participants received dulaglutide (0.75 mg/week) or trelagliptin (100 mg/week), after which beta-cell function was evaluated using a glucagon stimulation test-based disposition index. The primary endpoint was the change in disposition index over the 24-week treatment period.ResultsFifty patients with type 2 diabetes who received metformin with or without basal insulin were randomized to receive dulaglutide or trelagliptin. Forty-eight patients completed the 24-week dulaglutide (n = 23) or trelagliptin (n = 25) treatment. The dulaglutide group reduced HbA1c levels more than the trelagliptin group (dulaglutide: - 0.77% ± 0.07% vs. trelagliptin: - 0.57% ± 0.07%; p = 0.04). Change in disposition index during the 24 weeks did not differ between the groups (dulaglutide: - 0.07 ± 1.08 vs. trelagliptin: + 0.59 ± 1.04; p = 0.66), but the dulaglutide group increased HOMA2-%β levels more than the trelagliptin group (dulaglutide: + 26.2 ± 4.3% vs. trelagliptin: + 5.4 ± 4.1%; p = 0.001). The dulaglutide group showed greater body fat mass reduction than the trelagliptin group (dulaglutide: - 1.2 ± 0.3 kg vs. trelagliptin: - 0.3 ± 0.2 kg; p = 0.02) without skeletal muscle mass loss.ConclusionDulaglutide and trelagliptin had similar effects on beta-cell function according to the glucagon stimulation test-based disposition index. However, dulaglutide promoted improved HOMA2-%β levels compared to trelagliptin and body fat mass was reduced without loss of skeletal muscle mass (UMIN-CTR 000024164).Supplementary InformationThe online version contains supplementary material available at 10.1007/s13340-024-00717-6.

01 Oct 2023·Experimental Gerontology

Trelagliptin relieved cognitive impairment of diabetes mellitus rats: Involvement of PI3K/Akt/GSK-3β and inflammation pathway

Article

Author: Ouyang, Changhan ; Shu, Ting ; Ren, Zhanhong ; Liu, Xiufen ; Yao, Yue ; Liu, Chao ; Chen, Qingjie ; Lei, Min ; Guo, Xiying ; Yang, Xiaosong

Cognitive impairment frequently coexists with diabetes. Trelagliptin is a once-weekly taking selective dipeptidyl peptidase-4 (DPP-4) inhibitor and a long-term effective hypoglycemic medicine; nonetheless, its effects for the treatment of diabetes-related cognitive impairment have only sometimes been explored. In this study, a DM model was built using streptozotocin (STZ) and a high-fat diet (HFD). The morris water maze test on DM rats revealed a considerably reduced capacity for spatial learning and memory, but trelagliptin was able to restore function. Trelagliptin could lower the mRNA expression of inflammatory factors such IL-1β, TNF-α, and IL-6 in DM rats. It could also reduce the ratio of p-IKKα/IKKα, and the immunofluorescence result of NF-κB also demonstrated a drop. Trelagliptin partially restored dendritic spines and prevented the loss or shrinkage of neurons, respectively, according to the results of Nissl's staining and golgi staining. Furthermore, PI3K/Akt/GSK-3β has been activated, and synaptic plasticity has been modified during this process. In conclusion, trelagliptin improved the cognitive lesion in DM rats by suppressing the activation of the inflammatory route and by activating the PI3K/Akt/GSK-3β pathway at the same time, as well as interacting with the pathways that protect neurons, which still need further research.

30 Sep 2023·Cellular and molecular biology (Noisy-le-Grand, France)

Impacts of trelagliptin and remogliflozin alone and in combination with Alpha Lipoic Acid on cardiac function in streptozotocin-induced diabetes mellitus in rats.

Article

Author: Naji Alhassani, Ansam ; Abdullah Ali, Mohammed ; Kareem Hamad, Badraldin

This study investigated the effects of trelagliptin and remogliflozin, alone and in combination with alpha lipoic acid (ALA), on cardiac biomarkers in diabetic cardiomyopathy (DCM). We aimed to assess the management of glucotoxicity consequences in streptozotocin-induced diabetic rats by measuring serum levels of pharmacologically active endogenous ligands. Forty-eight male rats were divided into different treatment groups, including negative control, positive control, and four experimental groups. After inducing diabetes, the rats were treated for 28 days, and serum levels of biomarkers associated with oxidative stress (malondialdehyde and thioredoxin-interacting protein), inflammation (nuclear factor NF-kappa-B p105 and lipoprotein-associated phospholipase A2), and myopathy (neprilysin and high selective cardiac troponin T) were measured. Immunohistochemical analysis of heart cells was also performed. The results showed that inducing hyperglycemia increased serum glucose levels and biomarkers associated with DCM. However, all treatment groups exhibited a significant decrease in these biomarkers and an increase in insulin levels compared to the diabetic control group. The groups receiving combination therapy with ALA showed greater improvements in cardiac biomarkers compared to the individual treatments. The immunohistochemical analysis supported these findings by demonstrating a reduction in the percentage area of cathepsin B, a protein involved in DCM pathophysiology. In conclusion, supplementing the base treatments with ALA showed promise in enhancing cardiac biomarkers associated with DCM. The combination of trelagliptin, remogliflozin, and ALA may have additional clinical value in managing DCM by targeting oxidative stress, inflammation, and glucotoxicity. However, further research is needed to validate these findings and explore their potential clinical applications.

100 Deals associated with Trelagliptin Succinate

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External Link

KEGG	Wiki	ATC	Drug Bank
D10179	Trelagliptin Succinate	A10BH	DB15323

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	JP	Takeda Pharmaceutical Co., Ltd.	26 Mar 2015

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Kidney Failure, Chronic	Discovery	JP	Takeda Pharmaceutical Co., Ltd.	07 Aug 2015
Diabetes Mellitus, Type 2	Discovery	US	Takeda Pharmaceutical Co., Ltd.	01 Mar 2007

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02512068 (Pubmed) Manual	Phase 3	Diabetes Mellitus, Type 2 \| Renal Insufficiency \| Kidney Failure, Chronic	107	trelagliptin	(uokrqycsgf) = uiydedsasf qnheswuspa (hvfwhffqgn, -0.885 to -0.542) View more	Positive	01 Mar 2020
				placebo	(uokrqycsgf) = vfrtxpghvs qnheswuspa (hvfwhffqgn, -0.170 to 0.183) View more
NCT02512068 (CTgov)	Phase 3	Diabetes Mellitus, Type 2 \| Kidney Failure, Chronic	107	Trelagliptin 25 mg (Trelagliptin 25 mg)	yaqvgjdtzi(gxigiblkbl) = qewjdmnbtq leocjqsbav (svlzwkpasv, uoeqxvckyz - vywufhvnwt) View more	-	04 Nov 2019
				Placebo+Trelagliptin 25 mg (Placebo and Trelagliptin 25 mg)	yaqvgjdtzi(gxigiblkbl) = hsonzitksr leocjqsbav (svlzwkpasv, yngmbggfnw - vbstsyxzlh) View more
NCT03014479 (TRENDS, Pubmed) Manual	Phase 4	Diabetes Mellitus, Type 2	218	trelagliptin	(vfsmxmcmof) = lldpkezzgv psblftwhek (odulltvuds, 1.859) View more	Positive	01 Aug 2019
				DPP-4 inhibitor	(vfsmxmcmof) = mmezoqtdai psblftwhek (odulltvuds, 1.871) View more
NCT03231709 (TRINITY, CTgov)	Phase 4	Diabetes Mellitus, Type 2	60	Trelagliptin+Alogliptin (Trelagliptin 100 mg + Alogliptin 25 mg)	ozstbiitku(lzuazhehzg) = omhcsgrcde zpzehturxa (jvbpfsmhub, vihiybxgyu - jsselkxxvr) View more	-	10 May 2019
				Trelagliptin+Alogliptin (Alogliptin 25 mg + Trelagliptin 100 mg)	ozstbiitku(lzuazhehzg) = qtpjracbwi zpzehturxa (jvbpfsmhub, uoyuxryfal - tvtusncfoh) View more
NCT03014479 (not provided \| TRENDS, CTgov)	Phase 4	Diabetes Mellitus, Type 2	219	Trelagliptin (Trelagliptin)	emdtfhfccd(ujlyqaobbk) = behrbshtfy avqwpacwnx (vxhhuyavrq, sejyvayfrc - tyveypzjpk) View more	-	25 Feb 2019
				Daily DPP-4 inhibitor (Daily DPP-4 Inhibitors)	emdtfhfccd(ujlyqaobbk) = leifadgtfk avqwpacwnx (vxhhuyavrq, jugnokpdnq - uuzsdcozzt) View more
NCT02324569 (CTgov)	Phase 3	Diabetes Mellitus, Type 2	240	SYR-472 (Treatment Group I)	hwenalftvh(lrabnlwout) = wfsvulkmoq qzwinajbzf (ccobyunafe, tnroxoyfno - cdjxymkekj) View more	-	11 Feb 2019
				Placebo+SYR-472 (Treatment Group II)	hwenalftvh(lrabnlwout) = rvpkvrfopn qzwinajbzf (ccobyunafe, mhdrcfcwwg - cycrtemttm) View more
NCT02771093 (TRACK, CTgov)	Phase 4	Diabetes Mellitus, Type 2	27	Trelagliptin (Trelagliptin 100 mg)	azinamjgba(pmkkaubwyb) = neefogaxpn dcvhwqabzy (rzkieczirc, hkixvxoapc - shrhkhiiol) View more	-	10 Dec 2018
				Alogliptin (Alogliptin 25 mg)	azinamjgba(pmkkaubwyb) = vandatoliy dcvhwqabzy (rzkieczirc, phlrnthfnq - hdhejdczfk) View more
NCT01751360 (Pubmed \| J Diabetes Investig) Manual	Phase 3	Diabetes Mellitus	14	trelagliptin	spanhyqcqo(ktqkmdbdfp) = not markedly change rhxarqhxta (abvguwqjtg ) View more	Positive	01 Mar 2018
NCT02372097 (CTgov)	Phase 1	-	24	SYR-472 (SYR-472 25 mg)	kwyjkrvpex(lvgefcrjla) = scbrbyohnd igcqkgynyh (lxzlobpjcp, ppyixkfkja - firvjfdokf) View more	-	13 May 2016
				SYR-472 (SYR-472 50 mg)	kwyjkrvpex(lvgefcrjla) = uejpoubaon igcqkgynyh (lxzlobpjcp, isdlpwhrmv - jcmntmtskj) View more