Delving into the Latest Updates on Alogliptin Benzoate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

ALOGLIPTIN, Alogliptin benzoate (JAN/USAN), 阿格列汀

+ [6]

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

Acute Coronary Syndrome

Originator Organization

Takeda Pharmaceutical Co., Ltd.

Active Organization

Takeda Canada, Inc.

Huadong Medicine Co., Ltd.Takeda Pharmaceuticals U.S.A., Inc.

+ [4]

Inactive Organization-

License Organization

Celltrion, Inc.

Celltrion Healthcare Co., Ltd.

Takeda Pharmaceutical Co., Ltd.

+ [4]

Drug Highest PhaseApproved

First Approval Date

Japan (06 Apr 2010),

Diabetes Mellitus, Type 2

Regulation-

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Structure/Sequence

Molecular FormulaC25H27N5O4

InChIKeyKEJICOXJTRHYAK-XFULWGLBSA-N

CAS Registry850649-62-6

A Multicenter, Randomized, Double-Blind, Placebo-Controlled, Phase 3 Clinical Trial and Open-Label Extension Study to Evaluate the Efficacy and Safety of Add-On Therapy With Empagliflozin for Patients With Inadequately Controlled Type 2 DiabetesMellitus in the Combination Treatment With Metformin and Alogliptin

Phase 3 study to assess the Efficacy and Safety of CT-L02-301 in Type 2 Diabetes Patients with Insufficient Glycemic Control with Metformin and Alogliptin Combination Therapy.

Start Date18 Jul 2025

Sponsor / Collaborator

Celltrion, Inc.

CTR20250730

/ CompletedNot Applicable

苯甲酸阿格列汀片（25mg）在中国健康受试者中空腹给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验

[Translation] A randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence study of alogliptin benzoate tablets (25 mg) in Chinese healthy subjects under fasting conditions

主要研究目的：按有关生物等效性试验的规定，选择Takeda Pharmaceutical Company Limited为持证商的苯甲酸阿格列汀片（商品名：尼欣那，规格：25mg）为参比制剂，对石家庄四药有限公司生产并提供的受试制剂苯甲酸阿格列汀片（规格：25mg）进行空腹给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在空腹给药条件下的生物等效性。次要研究目的：观察健康受试者口服受试制剂苯甲酸阿格列汀片（规格：25mg）和参比制剂苯甲酸阿格列汀片（商品名：尼欣那，规格：25mg）的安全性。

[Translation]

Main purpose of study: According to the relevant provisions of bioequivalence test, Takeda Pharmaceutical Company Limited was selected as the reference preparation for alogliptin benzoate tablets (trade name: Nisina, specification: 25mg), and the test preparation alogliptin benzoate tablets (specification: 25mg) produced and provided by Shijiazhuang Siyao Co., Ltd. was used for fasting human bioequivalence test, to compare whether the absorption rate and degree of the drug in the test preparation were within the acceptable range with the reference preparation, and to evaluate the bioequivalence of the two preparations under fasting conditions. Secondary purpose of study: To observe the safety of oral administration of the test preparation alogliptin benzoate tablets (specification: 25mg) and the reference preparation alogliptin benzoate tablets (trade name: Nisina, specification: 25mg) in healthy subjects.

Start Date24 Mar 2025

Sponsor / Collaborator

Shijiazhuang No. 4 Pharmaceutical Co., Ltd.

CTR20250729

/ CompletedNot Applicable

苯甲酸阿格列汀片（25mg）在中国健康受试者中餐后给药条件下随机、开放、单剂量、两序列、两周期、双交叉生物等效性试验

[Translation] A randomized, open-label, single-dose, two-sequence, two-period, double-crossover bioequivalence study of alogliptin benzoate tablets (25 mg) in Chinese healthy volunteers after meal administration

主要研究目的：按有关生物等效性试验的规定，选择Takeda Pharmaceutical Company Limited为持证商的苯甲酸阿格列汀片（商品名：尼欣那，规格：25mg）为参比制剂，对石家庄四药有限公司生产并提供的受试制剂苯甲酸阿格列汀片（规格：25mg）进行餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在餐后给药条件下的生物等效性。次要研究目的：观察健康受试者口服受试制剂苯甲酸阿格列汀片（规格：25mg）和参比制剂苯甲酸阿格列汀片（商品名：尼欣那，规格：25mg）的安全性。

[Translation]

Main purpose of study: According to the relevant provisions of bioequivalence test, Takeda Pharmaceutical Company Limited was selected as the reference preparation for alogliptin benzoate tablets (trade name: Nisina, specification: 25mg), and the test preparation alogliptin benzoate tablets (specification: 25mg) produced and provided by Shijiazhuang Siyao Co., Ltd. was used for human bioequivalence test after meal administration. The difference between the absorption rate and absorption extent of the drug in the test preparation and the reference preparation was compared to see whether it was within an acceptable range, and to evaluate the bioequivalence of the two preparations under the condition of postprandial administration. Secondary purpose of study: To observe the safety of oral administration of the test preparation alogliptin benzoate tablets (specification: 25mg) and the reference preparation alogliptin benzoate tablets (trade name: Nisina, specification: 25mg) to healthy subjects.

Start Date23 Mar 2025

Sponsor / Collaborator

Shijiazhuang No. 4 Pharmaceutical Co., Ltd.

100 Clinical Results associated with Alogliptin Benzoate

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100 Translational Medicine associated with Alogliptin Benzoate

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100 Patents (Medical) associated with Alogliptin Benzoate

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1,071

Literatures (Medical) associated with Alogliptin Benzoate

01 Dec 2025·American journal of medicine open

The Association of SGLT2i vs DPP4i on Fracture: A Cohort Study in Veterans with Diabetes

Article

Author: Hackstadt, Amber ; Griffin, Katherine ; Javid, Amir ; Hung, Adriana ; Roumie, Christianne L ; Snyder, Kathryn ; Greevy, Robert

Background:

Increased bone turnover is associated with use of SGLT2i. Patients with diabetes experience adverse effects on bone metabolism. Our aim was to evaluate if SGLT2i was associated with fractures vs DPP4i as add-on therapy to diabetes regimens.

Methods:

We assembled a retrospective cohort of Veterans with diabetes combining Veterans Administration, Medicare, and National Death Index databases. Using an active comparator new user design, patients starting on SGLT2i or DPP4i were followed from prescription fill until a fracture event, death, stopping medication, loss of follow-up, or study end. Fractures included: face/skull, spine, ribs, long bones, hand/feet/digits, or hip. Fractures were identified based on a validated algorithm with positive predictive value 91.3% (86.8, 94.4). Cox models compared the association of fractures between SGLT2i and DPP4i in a propensity score-weighted cohort that balanced 70+ covariates including comorbidities, vital signs, labs, vitamin D levels, smoking, and medications.

Results:

The unweighted sample included 115,124 SGLT2i episodes (104,086 Veterans; 94% empagliflozin; 4% canagliflozin; 2% dapagliflozin) and 213,095 DPP4i episodes (173,724 Veterans; 45% saxagliptin; 15% sitagliptin; 34% alogliptin; 6% Linagliptin). After propensity score calculation and matched weighting, the cohort included 76,072 SGLT2i and 75,833 DPP4i episodes. Median age was 69.3 years and diabetes duration 9.7 (6.1, 14.0) years. In the matched weighted analyses, there were 1431 and 1564 fractures among SGLT2i and DPP4i users, respectively. There were no clinical differences in fractures per 1000 person-years: 18.2 (17.4, 19.1) vs 19.8 (19.0, 20.6). The adjusted hazard ratio (adjusted hazard ratio 0.93 [0.87, 0.99]) excluded increased risk of fractures (adjusted hazard ratio > 1) in SGLT2i users.

Conclusions:

SGLT2i use as add-on treatment for diabetes was not associated with increased fracture outcomes compared to DPP4i.

09 Jul 2025·Current Reviews in Clinical and Experimental Pharmacology

Dipeptidyl Peptidase-4 Inhibitors and the Risk of Fractures in Type 2 Diabetes Mellitus Patients: A Bayesian Network Meta-Analysis

Article

Author: Azharuddin, Mohammad ; Vohora, Divya ; Adil, Mohammad ; Ansari, Shamsuzzaman ; Sharma, Manju ; Ahmad, Tufail

Background/Objective::

Type 2 diabetes mellitus (T2DM) increases the risk of fractures and its effects on bone health. The impact of dipeptidyl peptidase-4 inhibitors (DPP-4i) on bone fracture risk is unclear. We performed a network meta-analysis (NMA) to assess the impact of DPP-4i on fracture risk in patients with T2DM.

Methods::

A comprehensive systematic literature search was conducted on PubMed/Medline, Cochrane Library, and ClinicalTrials.gov until June 2024 to identify RCTs reporting fracture events with DPP-4i among T2DM patients. A Bayesian NMA has been performed to calculate the odds ratio (OR) and 95% credible intervals (CrI). Surface under the cumulative ranking analysis (SUCRA) was utilized to assess the rank probability of DPP-4i.

Results::

A total of 85 RCTs were identified, including 89,965 T2DM patients with 1,083 fracture events. In the direct meta-analysis, DPP-4i did not elevate fracture risk compared to placebo or other oral anti-diabetics (OADs) (OR (95%CI): 1.04 (0.91-1.18); p=0.57 and 1.18 (0.79-1.74); p=0.96, respectively). Alogliptin and sitagliptin indicated a non-significant trend towards reducing fracture risk compared to placebo (OR (95%CI): 0.59 (0.31-1.15); p=0.12) and OADs (OR (95%CI): 0.73 (0.41-1.30); p=0.28), respectively. In the NMA, alogliptin significantly reduced fracture risk compared to linagliptin and SGLT2i (OR (95%CrI): 0.41 (0.16-0.93) and 0.16 (0.017-0.83), respectively). Conversely, linagliptin increased fracture risk compared to sulfonylurea (OR (95%CrI): 2.3 (1.1-5.2)). According to SUCRA, alogliptin (84%) ranked as the preferred treatment for reducing fracture risk in T2DM patients.

Conclusion::

Overall, DPP-4i was not associated with an increased risk of fractures in patients with T2DM. However, alogliptin demonstrated a reduced risk of fractures when compared to both linagliptin and SGLT2i. Further long-term clinical studies are needed to confirm the present findings.

24 Jun 2025·ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

Desulfurizative Fluorination of N‐CF₃ Thioformamides for the Efficient Synthesis of N(CF₃)(CF₂H) Amines with Enhanced Stability

Article

Author: Schoenebeck, Franziska ; Liu, Linhao ; Wycich, Gina ; Ponce‐de‐León, Jaime

Abstract:

With poor metabolic stability being a major cause of failure in drug development, there is a pressing need for strategic molecular modifications to optimize for desired properties and function. N‐substitution has emerged as a powerful approach, with N‐CF3 amines previously demonstrating enhanced lipophilicity and reduced susceptibility to oxidation, albeit inherent instability to hydrolysis. This report discloses the further evolution of this motif—the introduction of an additional N‐difluoromethyl unit, resulting in an extraordinary 2000‐fold increase in stability. We present the first general synthetic strategy for accessing N(CF3)(CF2H) amines. The method relies on an operationally simple desulfurization–fluorination strategy of N‐CF3 thioformamides and is characterized by broad functional group tolerance.

15

News (Medical) associated with Alogliptin Benzoate

23 May 2025

·pharma.economictimes.indiatimes.com

GLP-1 diabetes drugs like Ozempic may modestly reduce cancer risks

London: Widely used GLP-1 drugs for type 2 diabetes such as Novo Nordisk 's Ozempic may modestly reduce the risk of obesity-related cancers, especially colorectal cancer , according to data released on Thursday ahead of a major medical meeting. Among more than 85,000 people with type 2 diabetes and obesity treated between 2013 and 2023 and followed for an average of nearly four years, 2,501 obesity-related cancers developed in those taking GLP-1 diabetes drugs , compared with 2,671 such cancers in those treating their diabetes with drugs from a class known as DPP-4 inhibitors . After accounting for individual risk factors, those taking GLP-1 drugs had a 7 per cent lower risk of developing an obesity-related cancer and an 8 per cent lower risk of death from any cause compared to those who took a DPP-4 inhibitor, a brief summary of data to be presented at the upcoming American Society of Clinical Oncology meeting in Chicago showed. The effect was only statistically significant in women, researchers said. Other GLP-1 drugs for improving blood glucose control taken by patients in the study include Eli Lilly's Trulicity and Novo's Victoza and Rybelsus, among others. These drugs deliver a lower dose of their main ingredient compared to GLP-1 drugs designed to induce weight loss. DPP-4 inhibitors include Merck & Co's Januvia and Nesina from Takeda Pharmaceuticals. While a modestly reduced risk for 14 obesity-related cancers was evident with GLP-1 drugs, the suggestion of a protective effect was particularly strong for colorectal malignancies. There were 16 per cent fewer colon cancer cases and 28 per cent fewer rectal cancer cases in the group prescribed GLP-1 receptor agonists. Observational studies like this cannot prove that the GLP-1 drugs caused lower cancer rates. "These data are reassuring, but more studies are required to prove causation," lead study author Lucas Mavromatis, a medical student at the NYU Grossman School of Medicine in New York, said in a statement. (Reporting by Nancy Lapid; Editing by Bill Berkrot)

ASCOClinical Result

23 May 2025

·pharma.economictimes.indiatimes.com

GLP-1 diabetes drugs like Ozempic may modestly reduce cancer risks

London: Widely used GLP-1 drugs for type 2 diabetes such as Novo Nordisk 's Ozempic may modestly reduce the risk of obesity-related cancers, especially colorectal cancer , according to data released on Thursday ahead of a major medical meeting. Among more than 85,000 people with type 2 diabetes and obesity treated between 2013 and 2023 and followed for an average of nearly four years, 2,501 obesity-related cancers developed in those taking GLP-1 diabetes drugs , compared with 2,671 such cancers in those treating their diabetes with drugs from a class known as DPP-4 inhibitors . After accounting for individual risk factors, those taking GLP-1 drugs had a 7 per cent lower risk of developing an obesity-related cancer and an 8 per cent lower risk of death from any cause compared to those who took a DPP-4 inhibitor, a brief summary of data to be presented at the upcoming American Society of Clinical Oncology meeting in Chicago showed. The effect was only statistically significant in women, researchers said. Other GLP-1 drugs for improving blood glucose control taken by patients in the study include Eli Lilly's Trulicity and Novo's Victoza and Rybelsus, among others. These drugs deliver a lower dose of their main ingredient compared to GLP-1 drugs designed to induce weight loss. DPP-4 inhibitors include Merck & Co's Januvia and Nesina from Takeda Pharmaceuticals. While a modestly reduced risk for 14 obesity-related cancers was evident with GLP-1 drugs, the suggestion of a protective effect was particularly strong for colorectal malignancies. There were 16 per cent fewer colon cancer cases and 28 per cent fewer rectal cancer cases in the group prescribed GLP-1 receptor agonists. Observational studies like this cannot prove that the GLP-1 drugs caused lower cancer rates. "These data are reassuring, but more studies are required to prove causation," lead study author Lucas Mavromatis, a medical student at the NYU Grossman School of Medicine in New York, said in a statement. (Reporting by Nancy Lapid; Editing by Bill Berkrot)

ASCOClinical Result

14 Feb 2024

·endpts.com

Appeals court sides with AstraZeneca, BMS, McKesson in saxagliptin heart failure case

A Sixth Circuit appeals court this week upheld a decision in favor of AstraZeneca, Bristol Myers Squibb and McKesson in a case alleging that diabetes products containing saxagliptin can cause heart failure. Saxagliptin is the key ingredient in the discontinued type 2 diabetes treatments Onglyza and Kombiglyze. It’s a dipeptidyl peptidase-4 (DPP-4) inhibitor, designed to help lower blood sugar along with diet and exercise. But in 2016, an FDA safety review found that saxagliptin and another DPP-4 inhibitor called alogliptin may increase patients’ risk of heart failure. You’ll get access to free articles each month, plus you can customize what newsletters get delivered to your inbox each week, including breaking news.

Patent Infringement

100 Deals associated with Alogliptin Benzoate

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External Link

KEGG	Wiki	ATC	Drug Bank
D06553	Alogliptin Benzoate	A10BH04	DB06203

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Japan	Teijin Pharma Ltd.	06 Apr 2010
Diabetes Mellitus, Type 2	Japan	Takeda Pharmaceutical Co., Ltd.	06 Apr 2010

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Acute Coronary Syndrome	Phase 3	United States	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Japan	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Argentina	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Australia	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Austria	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Belgium	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Brazil	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Bulgaria	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Canada	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009
Acute Coronary Syndrome	Phase 3	Chile	Takeda Pharmaceutical Co., Ltd.	01 Sep 2009

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02856113 (2015-000208-25, Pubmed \| Diabetes Ther)	Phase 3	Diabetes Mellitus, Type 2	152	Alogliptin 25 mg QD	swdpjgdzix(qqlfmlqebm) = tspgymydiv hnabavgzdg (nhznghvrrz, -0.63 to 0.83)	Negative	04 Mar 2025
1340-P (ADA2024)	Not Applicable	Diabetes Mellitus	-	SGLT2i	bjauagjxyx(noibcrkqjk) = ebctjidsff vcrbihvsgi (swempesyeo, 16.6 - 19.7)	Positive	14 Jun 2024
				DPP4i	bjauagjxyx(noibcrkqjk) = ndygujeidk vcrbihvsgi (swempesyeo, 19.1 - 21.4)
NCT05782192 (Pubmed)	Phase 3	Diabetes Mellitus, Type 2	-	Fotagliptin	sgnukqdryj(ztyrdxdbuo) = hpjhbmuvrt ocoigfyily (etojffeflp ) View more	Positive	09 Oct 2023
				Alogliptin	sgnukqdryj(ztyrdxdbuo) = wsllhznnuc ocoigfyily (etojffeflp ) View more
NCT02856113 (2015-000208-25, CTgov)	Phase 3	Diabetes Mellitus, Type 2	152	Placebo (Placebo)	lgekqtfhfb(enobqbgxvp) = rdvjkrxuvx ciyavredrk (wfnhjzhpwi, 0.2809) View more	-	19 Oct 2022
				Alogliptin Benzoate (Alogliptin 25 mg)	lgekqtfhfb(enobqbgxvp) = irxvxgxzrt ciyavredrk (wfnhjzhpwi, 0.2879) View more
NCT03794336 (ACADEMIC, Pubmed \| Diabetes Obes Metab) Manual	Phase 4	Diabetes Mellitus, Type 2 \| Coronary Disease	1,088	aspirin+alogliptin	kihrkqujgj(vepbvcibhq) = wzargrjcys nfwawbeone (jlvolrvmiu, 0.4) View more	Positive	03 Feb 2022
				aspirin+acarbose	kihrkqujgj(vepbvcibhq) = mzktqfgazt nfwawbeone (jlvolrvmiu, 0.5) View more
NCT03794336 (EASD2021)	Phase 4	Cardiovascular Diseases \| Diabetes Mellitus, Type 2 \| Coronary Disease	-	Alogliptin 25 mg q.d.	gvderynnuz(evfmwytxtt) = Significantly lesser GI adverse events were observed with alogliptin than acarbose (8.9% vs 33.6%, P <0.0001) qltdtmmxca (kwakyeyjsg ) View more	Positive	29 Sep 2021
				Acarbose 100 mg t.i.d.
NCT03231709 (TRINITY, CTgov)	Phase 4	Diabetes Mellitus, Type 2	60	Trelagliptin+Alogliptin (Trelagliptin 100 mg + Alogliptin 25 mg)	cnprorclat = ymogkzodss zqamgjoozx (kwaqdhffqq, gcoeimtmon - hdzpbltumi) View more	-	10 May 2019
				Trelagliptin+Alogliptin (Alogliptin 25 mg + Trelagliptin 100 mg)	cnprorclat = fdbqfqcwma zqamgjoozx (kwaqdhffqq, wrizsjldmp - catfnziwnp) View more
NCT02771093 (TRACK, CTgov)	Phase 4	Diabetes Mellitus, Type 2	27	Trelagliptin (Trelagliptin 100 mg)	aurhshkonc(isiijultzs) = alfyorycig uiidgyvusz (owralqhjea, bqrqophcqs - mggyhcalab) View more	-	10 Dec 2018
				Alogliptin (Alogliptin 25 mg)	aurhshkonc(isiijultzs) = ifozskqogc uiidgyvusz (owralqhjea, dkcqtlxoqe - wevukcqbyy) View more
NCT00968708 (EXAMINE, Pubmed \| Am J Med)	Phase 3	Diabetes Mellitus, Type 2	1,398	Alogliptin	apfdtyyfus(pmpvkqkgot) = Reported rates of hypoglycemia were 8.8% for alogliptin and 6.7% for placebo jnwensjiwz (xeqaxwwibn )	-	01 Jul 2018
				Placebo