[Translation] A randomized, open-label, single-dose, two-period, double-crossover bioequivalence study of tenegliptin hydrobromide tablets in Chinese healthy volunteers: a fasting and fed dose-response study

主要目的：以南京易亨制药有限公司生产的氢溴酸替格列汀片（规格：20 mg）为受试制剂，按生物等效性试验的有关规定，与Mitsubishi Tanabe Pharma Corporation持证的氢溴酸替格列汀片为参比制剂（商品名：泰里安®，规格：20 mg），对比在健康人体内的相对生物利用度，研究两制剂的人体生物等效性。次要目的：观察氢溴酸替格列汀片受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Primary Objective: To investigate the bioequivalence of the test formulation (20 mg) of tenegliptin hydrobromide tablets produced by Nanjing Yiheng Pharmaceutical Co., Ltd.) with the reference formulation (20 mg) of tenegliptin hydrobromide tablets licensed by Mitsubishi Tanabe Pharma Corporation) in healthy volunteers by comparing their relative bioavailability in healthy volunteers. Secondary Objective: To investigate the safety of the test and reference formulations of tenegliptin hydrobromide tablets in healthy volunteers.

Start Date14 Oct 2025

Sponsor / Collaborator

Nanjing Yiheng Pharmaceutical Co., Ltd.

CTR20252533

/ CompletedNot Applicable

氢溴酸替格列汀片在中国健康受试者中单中心、随机、开放、单剂量、两制剂、两周期、两序列、双交叉空腹/餐后状态下生物等效性试验

[Translation] A single-center, randomized, open-label, single-dose, two-formulation, two-period, two-sequence, double-crossover bioequivalence study of tenegliptin hydrobromide tablets in Chinese healthy subjects under fasting/fed conditions

主要研究目的：健康受试者空腹或餐后状态下，单次口服江西施美药业股份有限公司生产的受试制剂氢溴酸替格列汀片（规格：40 mg）或田辺三菱製薬株式会社生产的参比制剂氢溴酸替格列汀片（商品名：Tenelia；规格：40 mg），分别考察空腹或餐后状态下受试制剂与参比制剂在健康受试者体内的药代动力学参数，评价两制剂的生物等效性。次要研究目的：考察受试制剂和参比制剂在健康受试者中的安全性。

[Translation]

Main study purpose: Healthy subjects were given a single oral dose of the test preparation Tenegliptin Hydrobromide Tablets (Specification: 40 mg) produced by Jiangxi Shimei Pharmaceutical Co., Ltd. or the reference preparation Tenegliptin Hydrobromide Tablets (Trade Name: Tenelia; Specification: 40 mg) produced by Tanabe Mitsubishi Pharmaceutical Co., Ltd. in the fasting or postprandial state, to investigate the pharmacokinetic parameters of the test preparation and the reference preparation in healthy subjects, respectively, and to evaluate the bioequivalence of the two preparations. Secondary study purpose: To investigate the safety of the test preparation and the reference preparation in healthy subjects.

Start Date15 Aug 2025

Sponsor / Collaborator

Jiangxi Shimei Pharmaceutical Co., Ltd.

100 Clinical Results associated with Teneligliptin Hydrobromide Hydrate

100 Translational Medicine associated with Teneligliptin Hydrobromide Hydrate

100 Patents (Medical) associated with Teneligliptin Hydrobromide Hydrate

306

Literatures (Medical) associated with Teneligliptin Hydrobromide Hydrate

01 Oct 2026·SPECTROCHIMICA ACTA PART A-MOLECULAR AND BIOMOLECULAR SPECTROSCOPY

DFT, spectroscopic and MD insights into teneligliptin (TLG) adsorption on Cu3 and Cu(111): Implications for SERS sensing and drug-metal interfaces

Article

Author: Al-Otaib, Jamelah S ; Jhaa, Gaurav ; Mary, Y Sheena ; Gamberini, Maria Cristina ; Ismoilov, Mirjalol

Surface-enhanced Raman scattering (SERS) platforms and metal-drug nano-interfaces require a clear, site-resolved understanding of how pharmaceutical molecules bind to small metal clusters and extended metal surfaces. Here, we investigate the interaction of the anti-diabetic drug Teneligliptin (TLG) with a Cu₃ cluster using density functional theory (DFT), complemented by vibrational (Raman/IR) analysis and molecular dynamics (MD) simulations on Cu(111). Geometry optimizations, frequency calculations, and electronic descriptors were obtained at the B3LYP/SDD level (Gaussian16), and adsorption was explored through six binding configurations (TLG1-TLG6) guided by electrostatic/reactive regions of the drug. Adsorption is exothermic for all complexes, with calculated adsorption energies spanning -16.51 to -33.75 kcal mol^-1, indicating strong site dependence; the most stable binding occurs for configurations involving heteroatom-rich motifs (notably TLG4 and TLG3). Cu₃ adsorption substantially perturbs the electronic structure of Teneligliptin, reducing the energy gap relative to the isolated drug (≈ 4.997 eV) and enhancing global reactivity descriptors, consistent with facilitated charge transfer and improved electronic response upon complex formation. Mulliken charge analysis confirms net electron redistribution to the metal moiety across all adsorbed systems. Sensor-relevant kinetics were assessed via recovery time estimates at 400 K, revealing that TLG1 and TLG2 provide the most practical trade-off between adsorption strength and reversibility, whereas the strongest-binding systems exhibit excessively long recovery times. Simulated Raman spectra show adsorption-induced band shifts (including carbonyl/NH downshifts) and the emergence of new low-frequency modes characteristic of metal-molecule coupling, supporting SERS-activity changes upon binding. Finally, MD simulations on Cu(111) indicate stable surface association dominated by dispersive interactions with localized adsorption contacts and partial charge redistribution, consistent with mixed physisorption/weak chemisorption behavior. Overall, the combined DFT-spectroscopic-MD framework clarifies how binding site selection controls stability, electronic tenability, and sensing practically for Teneligliptin at copper-based interfaces.

01 Jul 2026·CURRENT DIABETES REVIEWS

From Diabetes to Dermatology: The Role of Teneligliptin in Bullous Pemphigoid Development

Article

Author: Khan, Yumna ; Hussain, Md. Sadique ; Gupta, Gaurav ; Bisht, Ajay Singh ; Bahl, Gurusha

Bullous pemphigoid (BP) is an autoimmune blistering disease that especially presents in elderly patients, but recently, its incidence has increased in patients treated with inhibitors of dipeptidyl peptidase-4 (DPP-4), among which teneligliptin is widely prescribed as an antidiabetic drug for the treatment of type 2 diabetes mellitus (T2DM). Recent studies describe the association of teneligliptin with the onset of BP, hypothesizing that DPP-4 inhibition could induce immune dysregulation able to trigger autoimmune responses against skin antigens BP180 and BP230. This mini-review discusses the immunomodulatory effects of teneligliptin, immune responses, and chronic inflammation associated with diabetes that predispose patients to BP. It also discusses the clinical implications, such as monitoring for BP in T2DM patients on teneligliptin therapy. Elucidation of this relationship may help in optimizing management strategies by highlighting discontinuation or alternative therapies in the case of a high risk of development of BP.

01 May 2026·FEBS Journal

Deubiquitinase inhibitors: Targeting SARS ‐ CoV ‐2 papain‐like protease with antiviral efficacy in a murine model

Article

Author: Choudhary, Shweta ; Narayan, Rohan ; Verma, Shalja ; Rani, Ruchi ; Sircar, Debabrata ; Sharma, Swati ; Kumar, Pravindra ; Saha, Ankita ; Kumari, Annu ; Tomar, Shailly ; Kaliappan, Abinaya ; Tripathi, Shashank ; Nagaraj, Santhosh Kambaiah ; Nehul, Sanketkumar ; Sharma, Gaurav Kumar

SARS‐CoV‐2 papain‐like protease (PLpro) is a key antiviral target as it plays a dual role in viral replication and modulation of innate immune responses by deubiquitinating or deISGylating host proteins. Therefore, therapeutically targeting PLpro may serve as a two‐pronged approach to mitigate SARS‐CoV‐2 infection. Interestingly, PLpro shares structural and functional similarities with cellular deubiquitinating enzymes (DUBs), and this fact was leveraged in our study to identify DUB inhibitors that target the ubiquitin/ISG15‐binding site and the known substrate‐binding pocket of PLpro. Among the identified compounds, flupenthixol, lithocholic acid, teneligliptin, and linagliptin markedly inhibited the proteolytic activity of purified PLpro and demonstrated potent antiviral effects against SARS‐CoV‐2 infection in a dose‐dependent manner. Treatment with lithocholic acid and linagliptin suppressed the expression of inflammatory mediators, thereby restoring immune responses. Here, crystal structures of SARS‐CoV‐2 PLpro in complex with linagliptin and with lithocholic acid were determined, revealing insights into the mechanism of inhibition and unique interactions within the ubiquitin/ISG15‐binding site (S2 site; Phe69, His73, Asn128, and His175) and the substrate‐binding cleft. Additionally, oral and intraperitoneal treatments with linagliptin increased survival, reduced lung viral load, and ameliorated histopathological damage in a mouse‐adapted model of SARS‐CoV‐2 infection. This study demonstrates for the first time that using DUB inhibitors that target the proteolytic activity of PLpro can simultaneously reinstate the host's immune response against SARS‐CoV‐2, highlighting the potential of this two‐pronged therapeutic approach.

News (Medical) associated with Teneligliptin Hydrobromide Hydrate

20 Oct 2022

·www.pharmaindustrial-india.com

Glenmark launches Teneligliptin + Dapagliflozin Fixed-Dose Combination for adults with Type 2 diabetes

Glenmark Pharmaceuticals became the first to launch Teneligliptin (20mg) + Dapagliflozin (5mg/10mg) fixed-dose combination (FDC) for the treatment of adult patients with type 2 diabetes, especially the ones with comorbidities. Marketed under the brand name Zita D; it contains Teneligliptin (20mg) + Dapagliflozin (5 mg/10 mg), and must be taken once daily under prescription to improve glycemic control & prevent complications in adult patients with type 2 diabetes, especially the ones with comorbidities. Alok Malik, EVP & Business Head, India Formulations, Glenmark Pharmaceuticals, said, “Diabetes is growing in India at an alarming rate, and eight out of every ten diabetic patients suffer from comorbidities. Glenmark being a leader in the diabetes segment in India is proud to bring Zita D, a well researched and affordable fixed-dose combination, which will significantly improve glycemic control in adult patients suffering from uncontrolled Type 2 diabetes, especially the ones with comorbidities.

Drug Approval

07 Sep 2017

·www.daiichisankyo.com

Japan’s First DPP-4 Inhibitor / SGLT2 Inhibitor Combination Drug Launch of CANALIA® Combination Tablets, a type 2 diabetes mellitus treatment agent

PDF (48KB)PDF For Immediate Release Mitsubishi Tanabe Pharma Corporation Daiichi Sankyo Co., Ltd. -Combination of selective DPP-4 inhibitor TENELIA® Tablets and SGLT2 inhibitor CANAGLU® Tablets- Osaka and Tokyo, Japan (September 7, 2017) - Mitsubishi Tanabe Pharma Corporation (hereafter Mitsubishi Tanabe Pharma; Head Office: Chuo-ku, Osaka; President & Representative Director, CEO: Masayuki Mitsuka) and Daiichi Sankyo Co., Ltd. (hereafter Daiichi Sankyo; Head Office: Chuo-ku, Tokyo; Representative Director, President & COO: Sunao Manabe) announced today that both companies would launch CANALIA® Combination Tablets, a type 2 diabetes mellitus treatment agent that combines selective DPP-4 inhibitor TENELIA® Tablets (generic name: teneligliptin) and SGLT2 inhibitor CANAGLU® Tablets (generic name: canagliflozin), in Japan on September 7, 2017, following today’s inclusion of CANALIA® in the National Health Insurance drug price list. Approved for the first time in Japan, CANALIA® Combination Tablets is a combination drug that contains two ingredients, a DPP-4 inhibitor and a SGLT2 inhibitor.Both TENELIA® Tablets and CANAGLU® Tablets are type 2 diabetes mellitus treatment agents originally discovered by Mitsubishi Tanabe Pharma in Japan. CANALIA® Combination Tablets, a combination drug incorporating the above two constituents, is an orally-administered (once daily) agent that lowers blood-glucose levels based on two different mechanisms of action: inhibiting DPP-4 and thereby increasing insulin release according to blood glucose levels; and inhibiting SGLT2 and thereby promoting excretion of glucose into urine. Results of clinical trials conducted in Japanese Type 2 diabetes mellitus patients who have inadequate glycemic control to monotherapy with TENELIA® Tablets or CANAGLU® Tablets demonstrated efficacy, safety and good tolerability. Use of CANALIA® Combination Tablets by patients with type 2 diabetes mellitus whose blood glucose levels are stably controlled by concomitant treatment with TENELIA® Tablets and CANAGLU® Tablets will reduce the number of medicine and improve medication adherence. Use of CANALIA® Combination Tablets by type 2 diabetes mellitus patients who have inadequate glycemic control to monotherapy with TENELIA® Tablets or CANAGLU® Tablets is also expected to result in improved blood glucose control. Currently, marketing of TENELIA® Tabletsis conducted by Daiichi Sankyo, whereas marketing of CANAGLU® Tablets is carried out by Mitsubishi Tanabe Pharma. Marketing of CANALIA® Combination Tablets will be conducted by Daiichi Sankyo, and both companies will co-promote the product, as is the case with TENELIA® Tablets and CANAGLU® Tablets. Mitsubishi Tanabe Pharma and Daiichi Sankyo aim to contribute to the treatment of patients with diabetes by maximizing the product values of the above three agents in the diabetes treatment drug markets as well as by engaging in prompt and appropriate promotion activities through the alliance between both companies. For further information, please contact: Mitsubishi Tanabe Pharma Corporation Corporate Communications Department TEL: +81-6-6205-5211 Daiichi Sankyo Co., Ltd. Corporate Communications Department TEL: +81-3-6225-1126

Drug Approval

03 Jul 2017

·www.daiichisankyo.com

Japan’s First DPP-4 Inhibitor / SGLT2 Inhibitor Combination Drug Application approved in Japan for CANALIA® Combination Tablets, a type 2 diabetes mellitus treatment agent

PDF (41KB)PDF For Immediate Release Mitsubishi Tanabe Pharma Corporation Daiichi Sankyo Co., Ltd. -Combination of selective DPP-4 inhibitor TENELIA® Tablets and SGLT2 inhibitor CANAGLU® Tablets- Osaka and Tokyo, Japan (July 3, 2017) - Mitsubishi Tanabe Pharma Corporation (hereafter Mitsubishi Tanabe Pharma; Head Office: Chuo-ku, Osaka; President & Representative Director, CEO: Masayuki Mitsuka) and Daiichi Sankyo Co., Ltd. (hereafter Daiichi Sankyo; Head Office: Chuo-ku, Tokyo; Representative Director, President & COO: Sunao Manabe) announced today that on July 3, 2017, Mitsubishi Tanabe Pharma received manufacturing and sales approval for CANALIA® Combination Tablets, a type 2 diabetes mellitus treatment agent that combines selective DPP-4 inhibitor TENELIA® Tablets (generic name: teneligliptin) and SGLT2 inhibitor CANAGLU® Tablets (generic name: canagliflozin), from the Japanese Ministry of Health, Labour and Welfare. The approval is for an indication of type 2 diabetes mellitus. Approved for the first time in Japan, CANALIA® Combination Tablets is a combination drug that contains two ingredients, a DPP-4 inhibitor and a SGLT2 inhibitor.Both TENELIA® Tablets and CANAGLU® Tablets are type 2 diabetes mellitus treatment agents originally discovered by Mitsubishi Tanabe Pharma in Japan. CANALIA® Combination Tablets, a combination drug incorporating the above two constituents, is an orally-administered (once daily) agent that lowers blood-glucose levels based on two different mechanisms of action: inhibiting DPP-4 and thereby increasing insulin release according to blood glucose levels; and inhibiting SGLT2 and thereby promoting excretion of glucose into urine. Results of clinical trials conducted in Japanese T2DM patients who have inadequate glycemic control to TENELIA® Tablets or CANAGLU® Tablets demonstrated efficacy, safety and good tolerability. Use of CANALIA® Combination Tablets by patients with type 2 diabetes mellitus whose blood glucose levels are stably controlled by concomitant treatment with TENELIA® Tablets and CANAGLU® Tablets will enhance convenience and improve medication adherence. Use of CANALIA® Combination Tablets by type 2 diabetes mellitus patients who have inadequate glycemic control to monotherapy with TENELIA® Tablets or CANAGLU® Tablets is also expected to result in improved blood glucose control. Currently, marketing of TENELIA® Tabletsis conducted by Daiichi Sankyo, whereas marketing of CANAGLU® Tablets is carried out by Mitsubishi Tanabe Pharma. Marketing of CANALIA® Combination Tablets will be conducted by Daiichi Sankyo, and both companies will co-promote the product, as is the case with TENELIA® Tablets and CANAGLU® Tablets. Mitsubishi Tanabe Pharma and Daiichi Sankyo aim to contribute to the treatment of patients with diabetes by maximizing the product values of the above three agents in the diabetes treatment drug markets as well as by engaging in prompt and appropriate promotion activities through the alliance between both companies. For further information, please contact: Mitsubishi Tanabe Pharma Corporation Corporate Communications Department TEL: +81-6-6205-5211 Daiichi Sankyo Co., Ltd. Corporate Communications Department TEL: +81-3-6225-1126

Drug Approval

100 Deals associated with Teneligliptin Hydrobromide Hydrate

External Link

KEGG	Wiki	ATC	Drug Bank
D09756	Teneligliptin Hydrobromide Hydrate	A10B	DB11950

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	Japan	Tanabe Pharma Corp.	29 Jun 2012

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Diabetes Mellitus	Phase 1	-	Handok, Inc.	01 Jan 2017

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


TOP RENAL (ADA2023)	Not Applicable	Type 2 diabetes mellitus with established diabetic nephropathy	377	Teneligliptin	gfbqcnjbmq(trbolpamgr) = loypuigvwg jyfyvcgrgs (nhcymhmmng )	Positive	20 Jun 2023
NCT02916706 (CTgov)	Phase 3	Diabetes Mellitus, Type 2	254	Teneligliptin 20mg (Teneligliptin 20mg)	xydddrhjmo(lsyinxxmww) = oxshnbhnkv dinacgaoyk (cmgteuqefa, 0.06) View more	-	28 Jan 2022
				Placebo (Placebo)	xydddrhjmo(lsyinxxmww) = oorahvmvkn dinacgaoyk (cmgteuqefa, 0.06) View more
NCT02924064 (CTgov)	Phase 3	Diabetes Mellitus, Type 2	247	Teneligliptin+Metformin (Teneligliptin 20mg + Metformin)	nyataqlatk(yiqfeztbbf) = laqjizklzr fnyjuhnkqb (ezdaxwqpdi, 0.07) View more	-	28 Jan 2022
				Placebo+Metformin (Placebo + Metformin)	nyataqlatk(yiqfeztbbf) = xwtbdqdpof fnyjuhnkqb (ezdaxwqpdi, 0.07) View more
NCT03508323 (EASD2020)	Phase 4	Diabetes Mellitus, Type 2	65	Teneligliptin 20 mg	rmhcvnxdno(tukcmofesc) = wteolaxpuz rzwzqnygci (azrhflfrse ) View more	Positive	24 Sep 2020
NCT02354222 (CTgov)	Phase 3	Diabetes Mellitus, Type 2	154	Teneligliptin+Canagliflozin (Teneligliptin+Canagliflozin)	fprjxkxpuz(vsyxzufitv) = uhqgiwtrrg haxefxknjf (hehsfmaida, 0.08) View more	-	16 Aug 2018
				Placebo+Canagliflozin (Placebo+Canagliflozin)	fprjxkxpuz(vsyxzufitv) = mppsdwqqmo haxefxknjf (hehsfmaida, 0.08) View more
NCT02354222 (Pubmed \| Diabetes Obes Metab) Manual	Phase 3	Diabetes Mellitus, Type 2	-	Canagliflozin+teneligliptin	xepiwurdgv(ieulajluhf): difference = -0.94, P-Value = <0.001	Positive	01 Feb 2018
				Canagliflozin+Placebo
NCT02081599 (Pubmed \| Expert Opin Pharmacother) Manual	Phase 4	Diabetes Mellitus, Type 2	148	teneligliptin	zxpfkghheq(jksxjbcbyk) = wvlbjdjuqg rhebwreekr (karbejhofz, 0.11) View more	Positive	01 Sep 2017
				Placebo	ruuobadevx(paqtljmhhy) = orrjhxicry loogyzpilh (myzxsugmyd )
NCT02354235 (Pubmed \| Diabetes Obes Metab) Manual	Phase 3	Diabetes Mellitus, Type 2	138	canagliflozin as add-on therapy to teneligliptin	rkjvyvncao(ijzzwijcwi): difference = -0.88, P-Value = < 0.001	Positive	01 Jun 2017
				Placebo+teneligliptin
NCT02081599 (CTgov)	Phase 4	Diabetes Mellitus, Type 2	148	Insulin+Teneligliptin (Placebo/Teneli (Teneligliptin) + Insulin)	afbvzcgpxy(bmmgfvclvi) = bejdcipkko dfiknzgxub (bazibffqxs, 0.08) View more	-	05 Jan 2017
				Insulin+Teneligliptin (Teneli (Teneligliptin) /Teneli + Insulin)	afbvzcgpxy(bmmgfvclvi) = dtifmxmjoi dfiknzgxub (bazibffqxs, 0.08) View more
CTRI/2014/01/004315 (EASD2016)	Phase 3	Diabetes Mellitus, Type 2	237	Teneligliptin 20 mg	rflhywemfq(onracmkmrh): difference = 0.555 (95% CI, 0.176 - 0.934), P-Value = 0.0043 View more	Positive	13 Sep 2016
				Placebo

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