预约演示

更新于：2026-07-25

Sitagliptin

西格列汀

更新于：2026-07-25

概要

基本信息

药物类型

小分子化药

别名

DIABIT-IS X、RT-001、RT001

+ [2]

靶点

DPP-4

作用方式

抑制剂

作用机制

DPP-4抑制剂(二肽基肽酶IV抑制剂)

治疗领域

内分泌与代谢疾病神经系统疾病遗传病与畸形+ [2]

在研适应症

2型糖尿病杜氏肌营养不良症瘢痕

非在研适应症-

原研机构

Zydus Lifesciences Ltd.

在研机构

中国人民解放军总医院

Zydus Lifesciences Ltd.

Azurity Pharmaceuticals, Inc.

+ [1]

非在研机构

Merck Sharp & Dohme SA

Merck Sharp & Dohme GmbH

Merck Sharp & Dohme Corp.

+ [2]

权益机构

Libytec Pharmaceutical SA

Cosmos Health, Inc.

Cana Laboratories

最高研发阶段批准上市

首次获批日期

美国 (2023-10-18),

2型糖尿病

最高研发阶段(中国)临床前

特殊审评孤儿药 (美国)

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结构/序列

分子式C16H15F6N5O

InChIKeyMFFMDFFZMYYVKS-SECBINFHSA-N

CAS号486460-32-6

关联

项与西格列汀相关的临床试验

CTRI/2024/12/077770

/ Not yet recruitingN/A

An open label, randomized, balanced, two treatment, two sequence, two-period, cross-over, single-dose, oral bioequivalence study of Sitagliptin tablets 100 mg, Gliclazide Sustained Release Tablets 60 mg and Metformin Hydrochloride Sustained Release Tablets 500 mg (T) Manufactured by Eris Lifesciences Ltd., India with ALSITA® -M 100 (Sitagliptin 100 mg and Metformin Hydrochloride Extended Release Tablets 500 mg) (R1) Manufactured by Alkem Health Science., India and Diamicron® XR 60 mg (Gliclazide Extended Release Tablet 60 mg) (R2) Manufactured by Serdia Pharmaceuticals (India) Pvt, Ltd., India in normalhealthy, adult human male subjects under fasting condition. - NIL

开始日期2024-12-16

申办/合作机构

Eris Lifesciences Ltd.

NCT06659744

/ CompletedN/AIIT

Emulation of Effects of Injectable Semaglutide on Cardiovascular Outcomes in Individuals With Type 2 Diabetes: SUSTAIN6 Trial

Investigators are building an empirical evidence base for real world data through large-scale emulation of randomized controlled trials. The investigators' goal is to understand for what types of clinical questions real world data analyses can be conducted with confidence and how to implement such studies.

开始日期2024-10-24

申办/合作机构

The Brigham & Women's Hospital, Inc.

NCT06659679

/ CompletedN/AIIT

Emulation of the Effects of Oral Semaglutide on Cardiovascular Outcomes in Individuals With Type 2 Diabetes: PIONEER6 Trial

开始日期2024-10-24

申办/合作机构

The Brigham & Women's Hospital, Inc.

100 项与西格列汀相关的临床结果

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100 项与西格列汀相关的转化医学

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100 项与西格列汀相关的专利（医药）

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4,006

项与西格列汀相关的文献（医药）

2026-07-07·LANGMUIR

Coimmobilized Pyridoxal 5′-Phosphate and Aminotransferase in a Hydrogen-Bonded Organic Framework for Sustainable Synthesis of Sitagliptin

Article

作者: Sun, Yan ; Zhang, Siyao ; Yu, Linling ; Liu, Si

Aminotransferases (ATAs), essential enzymes for the synthesis of chiral amine drugs, play a crucial role in the synthesis of sitagliptin. The catalytic process of ATAs relies on the effective synergistic action of the cofactor pyridoxal 5'-phosphate (PLP). However, practical applications face challenges such as the poor stability of ATAs and the inefficient recovery of the expensive cofactor PLP. To address these issues, this study proposes a high-efficiency and stable catalytic nanoreactor, ATA&PLP@PAH-BioHOF-1, fabricated by polyelectrolyte poly(allylamine hydrochloride) (PAH)-mediated coencapsulation of both ATA and PLP in a hydrogen-bonded organic framework, BioHOF-1, for the synthesis of sitagliptin. This immobilization system overcomes the limitations of traditional single immobilization methods that were unable to simultaneously maintain enzyme activity and sustainably reuse the cofactor. The system exhibits excellent loading capacity and catalytic performance, achieving a sitagliptin yield of over 95% within 4 h. Additionally, the system demonstrates outstanding stability, retaining 78.3% of its initial sitagliptin yield (95%) after 18 consecutive catalytic cycles (4 h each), with a total PLP turnover number of 175. This study has thus provided an efficient nanoreactor system for the sustainable production of sitagliptin with in situ PLP recycling.

2026-07-01·DIABETES OBESITY & METABOLISM

Sitagliptin, Metformin and Glimepiride Fixed‐Dose Combination Compared to Co‐Administration of Metformin and High‐Dose Glimepiride in Indian Patients With Type 2 Diabetes: A Randomised, Double‐Blind, Double‐Dummy, Phase 3 Clinical Study

Article

作者: Singh, Manish Kumar ; Sahoo, Abhay Kumar ; Patil, Sandesh Sahebarao ; Patel, Piyush ; Gowda, Ambanna ; Gangwani, Dinesh ; Mehta, Suyog ; Agarwal, Vikas ; Joglekar, Sadhna ; Shaikh, Raisa ; Rao, A. Gopal ; Saha, Shruti ; Rai, Pradeep Kumar ; Ghadge, Pravin ; Duraisamy, Ramesh ; K. N., Satish Babu ; Patil, Dipak ; Gofne, Sandip Krishnrao ; Sahay, Rakesh ; Palawat, Arvind ; C., Ambrish ; Shukla, Jitendra ; Lakhwani, Lalit

ABSTRACT:

Aims:

This study assessed the efficacy and safety of a triple fixed‐dose combination (FDC) of sitagliptin, metformin, and glimepiride versus co‐administered metformin and glimepiride in Indian patients with uncontrolled Type 2 diabetes (T2D).

Materials and Methods:

In this Phase 3, randomised, double‐blind, double‐dummy study, adult patients with T2D and glycated haemoglobin (HbA 1c ) of 8%–11%, despite treatment with metformin and glimepiride, were randomised 1:1 to triple FDC of sitagliptin 50 mg, metformin 1000 mg and glimepiride 1 mg (SITA + MET + GLIM group) or metformin 1000 mg and glimepiride 2 mg (Co‐administration group) for 16 weeks. Patients assigned to the SITA + MET + GLIM group could continue treatment for a 12‐week open‐label period. The primary endpoint was the change in HbA 1c from baseline to Week 16.

Results:

Overall, 190 patients were randomised to the SITA + MET + GLIM group and 202 to the Co‐administration group. The least squares mean (standard error) change from baseline in HbA 1c at Week 16 was −1.79 (0.07%) in the SITA + MET + GLIM group and −1.27 (0.06%) in the co‐administration group (estimated treatment difference −0.51; 95% confidence interval [CI] −0.69 to −0.33; p < 0.0001). The proportion of patients with HbA 1c below 7% at Week 16 was 32.1% in the SITA + MET + GLIM group and 12.6% in the Co‐administration group ( p < 0.0001). Adverse events occurred in 25 patients (13.2%) in the SITA + MET + GLIM group and 30 patients (14.9%) in the Co‐administration group.

Conclusions:

The triple FDC was superior to co‐administered metformin and high‐dose glimepiride for achieving glycaemic control and was well tolerated in Indian patients with T2D.

Trial Registration:

Clinical Trials Registry–India identifier: CTRI/2021/11/038169 (registered on 22 November 2021); URL: https://www.ctri.nic.in/Clinicaltrials/pmaindet2.php?EncHid=NjI1Mjk=&Enc=&userName=

2026-07-01·BIOORGANIC CHEMISTRY

Click inspired new series of pyridazine-triazole-persulfonimide derivatives as DPP-4 inhibitors with exploratory HepG2 phenotypic screening

Article

作者: Kumar, Vipin ; Devan, Aswathy R ; Nath, Lekshmi R ; Tewari, Ashish Kumar ; Nidhar, Manisha ; Sura, Sooraj ; Gupta, Gaurav ; Rekha, A ; Chandramoorthy, Harish C ; Alqahtani, Abdulah Jarboa

A click-enabled pyridazine-1,2,3-triazole sulfonimide platform yielded two libraries: persulfonimides (7a-7f) and aryl sulfonamides (8a-8d). All synthesized compounds were characterized by ¹H and ¹³C NMR spectroscopy and mass spectrometry. In a fluorometric DPP-4 assay at fixed concentrations, inhibition increased with dose, with the most favorable profiles observed for 7d and 7f and the highest activity at 100 nM for 8c (91.31%) versus sitagliptin. In HepG2 cells. 7f reduced viability to 53% at 50 μM, while 8c showed a dose-dependent effect. Sorafenib was more potent (37.45% viability at 10 μM). AO/EB dual staining confirmed apoptosis induction (7f, 100 μM: 66 ± 5.6%; 8c, 100 μM: 42 ± 3.4%), with sorafenib producing (5 μM; 77 ± 3.06%) apoptosis. Docking supported plausible accommodation of top ligands in the DPP-4 cleft, and QikProp suggested favorable permeability with solubility liabilities for some analogues. Overall, pyridazine-triazole sulfonimides emerge as robust DPP-4 inhibitor chemotypes in fixed-dose screening, while the HepG2 effects are exploratory and justify further target-engagement studies.

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项与西格列汀相关的新闻（医药）

2026-07-24

·梅斯医学

脱发增加68%！BMJ万人研究：风靡一时的减肥针又双叒出问题了？

成年人两大烦恼：身材越来越差，头发越来越少。被“班味”不断腌入味，当代年轻人惊恐地发现，身体越来越“脆”、体型日趋圆润、头顶也愈发光亮了！这就是成熟的代价吗？有点过于可怕了！于是，在健康deadline和外界颜值评价的极限逼迫下，一批人拿起了“科技的武器”，誓死要从匆匆忙忙连滚带爬的生活中抢回自我！包括但不限于：用于改善状态的维生素、用于减肥的司美格鲁肽、用于防脱的生姜洗发水…… 但！最近发表在国际高水平期刊BMJ上的一篇研究无情地击碎了一部分人的希望：还在用司美减肥呢？你头发要没啦[1]！脱发率增加68%，看完头顶凉凉的我变“强”了也变秃了？因为这是一项囊括了数万人数据的大型对比性研究，来自宾夕法尼亚大学的研究者们并没有局限于司美格鲁肽这一款药物，而是综合研究了司美所属的所有GLP-1受体激动剂，它们和司美一样，或多或少都有一些减肥的效果；同时，因为GLP-1受体激动剂的主要受众还不是减肥人群，而是2型糖尿病患者，为公平起见，研究者将研究对象设置为糖尿病患者，并将对照组设置为另两类糖尿病药物：SGLT-2抑制剂（如卡格列净等）和DPP-4抑制剂（如西格列汀等）。结果是立竿见影的。在与SGLT-2抑制剂组的对比研究中，GLP-1受体激动剂表现出了6.91‰的脱发率，而SGLT-2抑制剂组只有5.04‰；在与DPP-4抑制剂组的对比研究中，GLP-1受体激动剂表现出了6.53‰的脱发率，而SGLT-2抑制剂组只有3.89‰。也就是说，和SGLT-2抑制剂相比，GLP-1受体激动剂能将脱发率提升37%，而与DPP-4抑制剂相比，则提升了68%！图注：使用年限越长，GLP-1受体激动剂的脱发“优势”越明显更可怕的是，这种“担惊受怕哪一天就秃了”的担忧都不用持续很久，因为从开始用GLP-1受体激动剂到出现脱发，一共也才平均1.71~1.81年，坚持用21个月，瘦没瘦不知道，但可能已经秃了！每个“减肥困难户”都想尝试的GLP-1受体激动剂，为啥会导致脱发？看完数据心都死了，但为什么会这样？按理说，GLP-1受体激动剂能通过减重和改善能量代谢让人变得更健康，难道是需要付出头发作为代价？在研究的最后，本文研究者们提出了几种可能的原因：首先，快速或显著的体重减轻是休止期脱发（即，大量毛囊提前进入静止并与毛发脱离以“节能维稳”的状态）的重要诱因，而很多人使用GLP-1受体激动剂，不就是为了“快速或显著的体重减轻”嘛！毕竟它能够延缓胃排空、抑制食欲、增加饱腹感等。图注：GLP-1受体激动剂作用效果[2] 当因为GLP-1受体激动剂的介入，热量摄入减少、一些微量营养素缺乏，毛囊就会觉得，“完了，这具身体遭遇饥荒了，那我也得省着点”，于是毛发生长周期就会被扰乱，进而导致休止期脱发。其次，GLP-1信号通路的改变还可能对激素或免疫造成影响，从而间接影响毛发生长、导致脱发。那对照组的SGLT-2抑制剂和DPP-4抑制剂呢？它们一个是促进尿液排糖的，一个是增强肠促胰素作用的[3]，都不会像GLP-1受体激动剂那样产生激烈的减重效果或扰乱激素和免疫，因此也不会导致严重的脱发，其中DPP-4抑制剂对体重的影响更小，对脱发的影响也就更小。图注：SGLT-2抑制剂和DPP-4抑制剂的抗糖尿病机制成年人的困境：头发、身材我都想要，该怎么办？到这里，其实已经很明朗了，司美可能导致的脱发，其实就是想在减重这件事上“走捷径”的后果！那既不想超重也不想脱发，正确的方法是什么？要么放平心态，休止期其实是毛发生长周期中正常的一环，休止期脱发也并非永久性，当停止用药，脱发的情况就会得到缓解，头发也会慢慢长回来；要么就改变方法！不去追求所谓“速成”的减肥方式，减重的同时保持营养的摄入，再加上运动锻炼、调整作息，头发、身材、健康“全得”，其实一点也不难。参考文献： [1] TANG H, ZHANG B, LU Y, et al. Risk of hair loss associated with glucagon-like peptide-1 receptor agonists in adults with type 2 diabetes: target trial emulation[J]. BMJ, 2026, 394: e100077. [2] Kalinkova M, Kadiyska T, Handjieva-Darlenska T. Pharmacogenetics of Glucagon-like-peptide-1 receptor in diabetes management[J]. Pharmacia, 2023, 70: 383-390. [3] AMERICAN DIABETES ASSOCIATION PROFESSIONAL PRACTICE COMMITTEE. 9. Pharmacologic Approaches to Glycemic Treatment: Standards of Care in Diabetes—2025[J]. Diabetes Care, 2024, 48(Suppl 1): S181-S206. 来源 | 梅斯消化新前沿编辑 | VOX

2026-07-24

·PRNewswire

Par Health Launches First and Only Generic Version of Janumet® XR (sitagliptin and metformin HCl extended-release) Tablets in the United States

First-to-Market Generic Entry Underscores Par Health's Commitment to Expanding Access to High-Quality, Affordable Medicines ST. LOUIS, July 24, 2026 /PRNewswire/ -- Par Health, Inc. ("Par Health" or the "Company"), a global pharmaceutical company and manufacturer of essential medicines, today announced the launch of its generic version of Merck's Janumet® XR (sitagliptin and metformin HCl extended-release) tablets for oral use, following final approval from the U.S. Food and Drug Administration (FDA) of its Abbreviated New Drug Application. Par Health's sitagliptin metformin XR is the first and currently the only FDA-approved generic of Janumet® XR available in the U.S. According to IQVIA data, Janumet® XR had estimated annual U.S. sales of approximately $269.9 million for the 12 months ended May 2026. "We are proud to introduce this first-to-market generic, helping expand access to more affordable treatment options for patients," said Jake Longenecker, Executive Vice President and Chief Commercial Officer, Generics. "This milestone strengthens our generics portfolio and reflects our continued focus on delivering quality, low-cost medicines for patients and healthcare providers." Click for Full Prescribing Information including Boxed Warning. Janumet® XR is a registered trademark of Merck Sharp & Dohme LLC. Cautionary Note Regarding Forward-Looking Statements This press release contains forward-looking statements, including, but not limited to, statements regarding the Company's business priorities, strategic objectives, product development and commercialization, expected market position, and growth. These statements are based on current expectations, assumptions, and projections of management and are subject to significant risks and uncertainties. Actual results may differ materially from those expressed or implied in the forward-looking statements due to a variety of factors, many of which are outside the Company's control. These factors include, but are not limited to: the Company's ability to successfully commercialize its products, including its generic version of Janumet® XR; competition within the pharmaceutical industry; the timing and impact of regulatory actions and approvals by the U.S. Food and Drug Administration and other authorities; the Company's ability to maintain compliance with applicable regulatory requirements at its manufacturing facilities; the Company's ability to sustain sales and profits on products over time; reliance on third-party manufacturers, suppliers, and service providers; supply chain disruptions; market acceptance, pricing pressures, and reimbursement dynamics; and general economic, industry, and market conditions. Readers are cautioned not to place undue reliance on these forward-looking statements, which speak only as of the date of this release. The Company undertakes no obligation to update or revise any forward-looking statements to reflect new information, future events, or otherwise, except as required by applicable law. About Par Health Par Health is a pharmaceutical company focused on Elevating the Essentials™. We develop, manufacture, and deliver high-quality generic medicines, active pharmaceutical ingredients (APIs) and sterile injectable products across a broad range of therapeutic areas, dosage forms and delivery technologies. With a vertically integrated, U.S.-advantaged manufacturing network and global workforce, we are committed to reliability, integrity and operational excellence – because we believe great healthcare is built on getting the essentials right. To learn more, please visit parhealth.com and connect with us on LinkedIn. Contacts Investors Stacie Phillips, Corporate Controller and Head of Investor Relations [email protected] Media Gena Holthaus, Senior Director, Corporate Brand and Communications [email protected] SOURCE Par Health 21% more press release views with Request a Demo

上市批准

2026-07-23

·JPharmAnal

点击蓝字，关注我们贵州医科大学钱星凯、马红红团队与上海中医药大学邹立伟团队综述——DPP-IV检测技术及其抑制剂筛选研究进展 Cite: H. Ma, X. Li, X. Qian, et al., Techniques for the determination of dipeptidyl peptidase IV and screening of its inhibitors, J. Pharm. Anal. 16 (2026), 101499. DOI: https://doi.org/10.1016/j.jpha.2025.101499 长按扫码阅读全文 JPA 文章推荐 01 研究背景和研究意义二肽基肽酶-IV（DPP-IV），又称CD26，是丝氨酸水解酶家族的重要成员。DPP-IV通过快速降解胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP），在血糖稳态调控中发挥关键的负调节作用。自2006年首个DPP-IV抑制剂西格列汀获美国食品药品监督管理局（FDA）批准上市以来，DPP-IV已成为治疗2型糖尿病的重要药物靶点。然而，现有DPP-IV抑制剂仍面临临床响应率有限（约40%的糖尿病患者经西格列汀治疗无法实现血糖控制）、潜在不良反应（如急性胰腺炎、肝毒性等）以及对肠道微生物来源DPP-IV抑制效果不佳等多重挑战。此外，DPP-IV还广泛参与肿瘤、心血管疾病、免疫炎症等多种病理生理过程。近年来，随着微生物来源的DPP-IV被证实为2型糖尿病管理的重要治疗靶点，DPP-IV重新成为研究焦点。鉴于DPP-IV抑制剂在代谢调节、神经保护、抗肿瘤等非糖尿病领域展现出显著潜力，未来开发更安全、更有效，尤其对宿主DPP-IV具有高度选择性的抑制剂仍是药物开发的重点方向。因此，系统梳理DPP-IV检测方法及抑制剂筛选策略，对于揭示DPP-IV相关疾病的分子机制、开发新一代高效安全的DPP-IV靶向药物具有重要意义。 02 图文摘要 03 文章亮点系统比较了DPP-IV在信使RNA（mRNA）、蛋白质和功能三个层面的检测方法，并重点突出了基于药物及光学探针在功能测定中的优越性能。从结构（肽类/非肽类）、作用机制（竞争性/非竞争性/不可逆性）、来源（天然/合成）及靶点特异性（选择性/非选择性）等多个维度对DPP-IV抑制剂进行了系统分析。基于肠道微生物组的新型DPP-IV抑制剂筛选策略，鉴定了影响宿主代谢的微生物来源DPP-IV，并通过高通量平台获得了选择性天然生物碱类抑制剂。通过对合成类及天然DPP-IV抑制剂的系统构效关系（SAR）分析，从传统药物中鉴定出活性化合物，为新型抑制剂的研发提供了指导。 04 文章简介 DPP-IV作为一种重要的丝氨酸水解酶，通过代谢多种内源性激素、趋化因子和生长因子，在炎症反应、氧化应激、血管功能及胰岛素抵抗等过程中发挥关键调控作用（图1）。本文首先系统回顾了DPP-IV的生物学功能、催化机制及其内源性和外源性底物，指出DPP-IV介导的蛋白水解加工是调控生理过程的基本机制之一。在检测方法方面，本文全面比较了DPP-IV在基因水平（如单核苷酸多态性分析）、蛋白水平（如Western blot、免疫组化、质谱等）以及功能水平（内源性底物检测、药物底物检测及光学底物检测）的检测方法。文章特别强调，基于荧光和生物发光探针的检测方法因其快速、便捷、灵敏和特异性高等优势而应用最为广泛。其中，研究团队首次将萘二胺用作DPP-IV探针的荧光基团（OS-11），具有高灵敏度、高荧光量子产率和良好选择性的特点；后续开发的近红外半菁探针（OS-16）可实现深层组织成像（图2）。在抑制剂筛选方面，文章从重组人DPP-IV（rhDPP-IV）、肠道细菌来源DPP-IV（microbial DPP-IV）及复杂生物体系（如人血浆/血清）等多个层面系统阐述了DPP-IV靶向药物的筛选模型（图3）。特别值得关注的是，研究发现microbial DPP-IV可进入宿主肠外组织和血浆，降解GLP-1从而导致糖耐量受损，而临床DPP-IV抑制剂对microbial DPP-IV的抑制作用较弱，这可能是部分患者临床响应率低的重要原因。研究通过构建Bacteroides thetaiotaomicron DPP-IV（btDPP-IV）高通量筛选平台，发现了天然生物碱Dau及其衍生物Dau-d4可选择性抑制btDPP-IV，并改善糖耐量与肥胖小鼠的葡萄糖稳态（图4）。此外，研究还验证了人血清/血浆DPP-IV可作为糖尿病生物标志物及药物筛选酶源，并通过该体系筛选出蒽醌类等新型DPP-IV抑制剂（图5）。文章进一步归纳了已上市DPP-IV抑制剂的结构分类、作用机制、药理学参数及不良反应，涵盖吡咯烷类、黄嘌呤类、苯乙胺类等代表性药物（图6）。在天然产物来源抑制剂方面，文章系统综述了中药提取物、黄酮类、多酚类、生物碱类及蛋白水解肽等DPP-IV抑制剂的筛选进展，并介绍了基于“谱效结合”的中药活性成分发现策略（图7）。最后，文章指出当前DPP-IV活性检测方法仍面临酶选择性不确定、人工底物与内源性肽代谢相关性不明确等挑战，并展望了未来应优先优化酶特异性、建立更清晰的肽代谢关联以及开发近红外/红外探针以推动临床转化的发展方向。 05 图文导读图1 二肽基肽酶-IV（DPP-IV）活性升高破坏全身葡萄糖稳态。DPP-IV活性升高可催化肠促胰素激素胰高血糖素样肽-1（GLP-1）和葡萄糖依赖性促胰岛素多肽（GIP）的蛋白水解切割，导致其失活，进而损害胰腺β细胞的葡萄糖依赖性胰岛素分泌，同时减弱对α细胞胰高血糖素释放的抑制作用，最终导致血糖水平升高。图2 基于二肽基肽酶-IV（DPP-IV）抑制剂的底物探针设计策略。将荧光基团连接至与DPP-IV紧密结合的两种抑制剂阿格列汀和利格列汀，获得新型荧光探针，可用于活细胞中DPP-IV的特异性识别和成像。图3 二肽基肽酶-IV（DPP-IV）抑制剂的多层次、多维度筛选模型。系统涵盖了重组人DPP-IV（rhDPP-IV）、肠道细菌来源DPP-IV、组织/细胞模型、类器官芯片及整体动物模型等多层次筛选体系。图4 微生物来源二肽基肽酶-IV（DPP-IV）对宿主糖代谢的影响及选择性抑制策略。肠道微生物来源的DPP-IV可转运至宿主肠黏膜组织和循环系统，加速胰高血糖素样肽-1（GLP-1）降解，降低血浆胰岛素水平，加剧糖耐量受损。人源靶向DPP-IV抑制剂（如西格列汀）对微生物DPP-IV的抑制效果有限。新型选择性抑制剂Dau-d4可特异性靶向微生物DPP-IV，显著抑制GLP-1水解，维持胰岛素分泌稳态，改善糖耐量受损。图5 血清或血浆二肽基肽酶-IV（DPP-IV）的生物学应用。（A）人静脉血来源的血浆DPP-IV与血清DPP-IV。（B、C）血清DPP-IV酶活性作为糖尿病生物标志物：以血清为酶源检测糖尿病患者与非糖尿病患者（B）、有糖尿病家族史与无家族史者（C）的DPP-IV酶活性。（D、E）沙格列汀和维格列汀对血清DPP-IV与重组人DPP-IV（rhDPP-IV）抑制效果的比较。（F）以人血浆为酶源筛选蒽醌类DPP-IV抑制剂。（G）蒽醌类化合物与人血浆DPP-IV的构效关系（SAR）。（H）化合物29（西格列汀）、AQ13和AQ7对人肾近端小管上皮细胞（RTPECs）DPP-IV活性的抑制。s-DPP-IV：可溶性DPP-IV；m-DPP-IV：膜结合型DPP-IV；BAN：丁基-4-氨基-1,8-萘二甲酰亚胺；GP-BAN：Gly-Pro-丁基-4-氨基-1,8-萘二甲酰亚胺（甘氨酰-脯氨酰-丁基-4-氨基-1,8-萘二甲酰亚胺）。图6 代表性已上市二肽基肽酶-IV（DPP-IV）抑制剂。汇总了结构多样的已上市DPP-IV抑制剂，包括研发企业、半数抑制浓度（IC₅₀）及给药频率等药理学数据。图7 基于“谱效结合”的中药活性成分发现策略。将现代高分辨率色谱分离分析技术与酶学体系相结合，从天然药物资源中分离分析化学成分，通过多元相关分析和量效曲线拟合，鉴定具有显著二肽基肽酶IV（DPP-IV）抑制活性的关键成分。（A）从中药粗提物中筛选具有抑制潜力的活性组分。（B）组分分离与收集的液相制备。（C）馏分中组分的确认。（D）抑制效果评价。（E）抑制机制研究。（F）通过分子对接进行体外验证。作者简介通讯作者钱星凯，贵州医科大学基础医学院药理学系、贵州医科大学组织工程与干细胞实验中心和转化医学研究中心副教授、博士生导师。主要研究方向：药物代谢酶结构与功能、天然产物活性成分筛选。邹立伟，上海中医药大学交叉科学研究院研究员。主要研究方向：药物代谢酶功能评价新方法开发与应用、中药功效物质分发现与成药性优化、中药-药物相互作用。第一作者马红红，贵州医科大学基础医学院药理学系副教授。主要研究方向：DPP-IV酶活性检测方法及抑制剂筛选。李小东，上海中医药大学交叉科学研究院博士研究生。主要研究方向：药物代谢酶与天然产物相互作用。近期阅读推荐 Journal of Pharmaceutical Analysis 2026年第6期 Journal of Pharmaceutical Analysis 2026年第5期期刊简介 Journal of Pharmaceutical Analysis（JPA,《药物分析学报（英文）》）创刊于2011年，由教育部主管，西安交通大学主办，是国内第一本有关药物分析的专业英文学术期刊，JPA 始终秉承服务国家重大战略需求、建设世界一流科技期刊的办刊宗旨，重点报道药物发现与药品全生命周期质量控制的新理论、新技术、新方法，临床精准用药，以及药物与生物、人工智能等交叉领域的技术方法方面的最新研究成果，为全球药物研发和药品质量控制提供高水平的国际学术交流平台，持续推动药物分析学科以及药学领域的快速发展。 JPA目前已组建一支以主编贺浪冲教授为核心的国际化的学术团队和专业的编辑出版团队，已实现编委国际化、稿源国际化、同行评议国际化、读者国际化和出版国际化。已被SCIE、PubMed、Scopus、DOAJ、中国科学引文数据库（CSCD）及中国科技论文与引文数据库（中国科技核心期刊）等多种重要国际和国内数据库和评价体系定为刊源。JPA连续8年入选“中国最具国际影响力学术期刊”。2019年入选“中国科技期刊卓越行动计划”重点期刊，2024年入选“中国科技期刊卓越行动计划二期”英文领军期刊。2025年影响因子 11.2，位于全球药理学和药学类学术期刊第15位（15/356），继续稳居于Q1区前列。2026年新锐期刊分区表1区，Top期刊。收稿范围药物分析新技术、新方法，分析药理学，药物代谢与递送，中药与天然药物，生物传感，可视化分析，生物功能分析，生物技术药物，药物分析装备，人工智能应用收稿栏目原创论文、综述、快报、展望、观点、新闻、社评等期刊官网 https://www.journals.elsevier.com/journal-of-pharmaceutical-analysis 投稿网址 https://www.editorialmanager.com/jpa/Default.aspx 供稿 | 钱星凯、马红红编辑 | 李蕾校对 | 朱丹丹审核 | 王梦杰、马维娜阅读原文了解更多

100 项与西格列汀相关的药物交易

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适应症	国家/地区	公司	日期
2型糖尿病	美国	Zydus Lifesciences Ltd.	2023-10-18

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适应症	最高研发状态	国家/地区	公司	日期
杜氏肌营养不良症	临床前	美国	Revio Therapeutics LLP	2026-01-24
瘢痕	临床前	中国	中国人民解放军总医院	2025-10-21

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT06115460 (Pubmed \| Diabetologia)	临床3期	1型糖尿病 \| 糖尿病肾病追加 SDF-1 levels	46	Sitagliptin 50 mg	餘構鏇簾築餘艱憲鬱鹹(夢繭淵襯衊願範鏇憲壓) = 選窪壓窪積淵夢淵齋鑰艱鹽膚壓範鹹觸鏇艱簾 (範獵簾膚網糧觸夢蓋範 ) 更多	积极	2024-09-14
				sitagliptin (AHCL only)	餘構鏇簾築餘艱憲鬱鹹(夢繭淵襯衊願範鏇憲壓) = 鏇範糧繭積獵範製鑰繭艱鹽膚壓範鹹觸鏇艱簾 (範獵簾膚網糧觸夢蓋範 )
1340-P (ADA2024)	N/A	糖尿病	-	SGLT2i	築築襯齋鏇鬱鏇網鹽齋(廠醖鏇構網鑰範蓋鏇選) = 製夢構鑰願構願鑰衊餘餘壓餘膚蓋鬱網憲構艱 (觸繭簾繭繭襯壓鹹膚淵, 16.6 ~ 19.7)	积极	2024-06-14
				DPP4i	築築襯齋鏇鬱鏇網鹽齋(廠醖鏇構網鑰範蓋鏇選) = 築壓艱鏇積顧選淵構窪餘壓餘膚蓋鬱網憲構艱 (觸繭簾繭繭襯壓鹹膚淵, 19.1 ~ 21.4)
FDA 人工标引	N/A	2型糖尿病	701	Sitagliptin 100 mg + Metformin	顧廠餘醖鏇構糧廠壓簾(醖窪鹽鹹淵鹽顧餘衊衊) = 廠糧鑰鏇繭鹽糧簾鹽醖齋蓋鬱簾鏇壓廠築窪簾 (遞鏇餘繭艱獵鬱鏇鹽鏇 ) 更多	积极	2023-11-03
				Placebo + Metformin	顧廠餘醖鏇構糧廠壓簾(醖窪鹽鹹淵鹽顧餘衊衊) = 窪窪齋簾簾艱鬱窪鹹憲齋蓋鬱簾鏇壓廠築窪簾 (遞鏇餘繭艱獵鬱鏇鹽鏇 ) 更多
FDA 人工标引	N/A	2型糖尿病	1,091	Placebo	範願鬱積餘窪鬱鑰壓網(衊憲鹽網鏇觸襯憲鑰蓋) = 醖積觸衊範獵壓鏇糧簾選製顧顧艱憲蓋壓糧鑰 (鬱蓋齋淵壓壓繭夢蓋蓋 ) 更多	积极	2023-11-03
				Sitagliptin 100 mg	範願鬱積餘窪鬱鑰壓網(衊憲鹽網鏇觸襯憲鑰蓋) = 糧鑰衊積遞鏇夢廠構窪選製顧顧艱憲蓋壓糧鑰 (鬱蓋齋淵壓壓繭夢蓋蓋 ) 更多
NCT01760447 (MK-0431A-170 \| MK-0431A-289, Pubmed \| Pediatr Diabetes) 人工标引	临床3期	2型糖尿病	220	Metformin+Insulin+Sitagliptin	鏇衊壓製夢鹽積鏇膚網(憲餘觸艱網艱築淵憲壓) = 蓋鬱憲鏇醖觸願襯艱鹹顧獵獵觸鹹鹽鬱鹹膚鏇 (艱鹹網顧壓衊遞繭醖壓, -0.94 ~ -0.22) 更多	不佳	2021-11-14
				Metformin+Insulin+Placebo	鏇衊壓製夢鹽積鏇膚網(憲餘觸艱網艱築淵憲壓) = 鑰艱積鑰構觸遞鹽鏇顧顧獵獵觸鹹鹽鬱鹹膚鏇 (艱鹹網顧壓衊遞繭醖壓, -0.43 ~ 0.26) 更多
NCT00790205 (TECOS, Pubmed \| Diabetes Care)	临床3期	2型糖尿病 \| 动脉粥样硬化	-	Sitagliptin	窪繭膚糧糧鹹窪齋窪獵(夢築壓製壓糧繭製襯壓) = 觸遞衊顧艱鬱壓願構鏇鹽淵艱築壓廠憲願鑰淵 (製築淵鬱膚蓋衊網襯簾 ) 更多	-	2017-12-01
				Placebo	築製觸窪積鹽網餘積艱(選選廠膚廠構鏇築壓遞) = 憲簾鬱襯獵鑰膚壓鹽鬱選蓋繭廠遞積壓鬱襯遞 (構構餘蓋窪鏇窪築鑰顧 )
NCT01183104 (START-J, CTgov)	N/A	2型糖尿病	305	Sitagliptin (Sitagliptin)	網餘艱廠壓構壓齋憲齋(鬱範願艱壓選範廠網繭) = 製齋網顧膚鏇齋鏇鹽願簾夢襯醖衊簾餘鹹繭窪 (艱選窪範廠廠餘襯構鹹, 選觸築鏇繭願糧糧艱窪 ~ 壓醖鏇夢淵齋壓繭窪獵) 更多	-	2017-04-14
				Glimepiride (Glimepiride)	網餘艱廠壓構壓齋憲齋(鬱範願艱壓選範廠網繭) = 鏇艱醖鑰觸糧艱淵醖餘簾夢襯醖衊簾餘鹹繭窪 (艱選窪範廠廠餘襯構鹹, 構夢觸窪壓衊膚製蓋淵 ~ 範餘夢鹽憲淵膚窪簾淵) 更多
NCT00993187 (Pubmed \| J Diabetes)	临床4期	2型糖尿病	292	Sitagliptin/metformin fixed-dose combination	窪觸廠積窪構製衊夢糧(蓋糧積構鑰襯鏇選願窪) = 簾壓鹽選選鑰積簾獵簾願窪觸膚窪網鬱襯鬱襯 (壓鏇淵製襯糧糧齋觸顧 ) 更多	积极	2017-04-01
				Glimepiride	窪觸廠積窪構製衊夢糧(蓋糧積構鑰襯鏇選願窪) = 範壓鹹壓壓醖獵廠簾餘願窪觸膚窪網鬱襯鬱襯 (壓鏇淵製襯糧糧齋觸顧 ) 更多
NCT00790205 (0431-082 \| TECOS, Pubmed \| Diabetes Care)	临床3期	-	14,671	Sitagliptin	鹹構齋觸積餘糧膚鏇衊(憲築襯蓋壓衊鬱壓遞廠) = 糧鹹憲觸蓋構窪窪鹽網窪獵壓襯夢顧糧鏇廠網 (繭鏇淵鬱夢網繭艱壓醖 )	-	2017-04-01
				Placebo	鹹構齋觸積餘糧膚鏇衊(憲築襯蓋壓衊鬱壓遞廠) = 鹹構築夢鏇衊餘糧積觸窪獵壓襯夢顧糧鏇廠網 (繭鏇淵鬱夢網繭艱壓醖 )
NCT00790205 (0431-082 \| TECOS, Pubmed \| Diabetes Care)	临床3期	-	14,671	Sitagliptin	蓋簾夢醖獵衊構積艱艱(觸鑰積選鹹壓選鬱繭襯): hazard ratio = 0.66 (95% CI, 0.28 ~ 1.51), P-Value = 0.32 更多	-	2017-02-01
				Placebo