预约演示

更新于：2025-09-05

Pioglitazone Hydrochloride

盐酸吡格列酮

更新于：2025-09-05

概要

基本信息

药物类型

小分子化药

别名

(±)-5-((4-(2-(5-ethyl-2-pyridinyl)ethoxy)phenyl)methyl)-2,4-thiazolidinedione、5-{4-[2-(5-ethylpyridin-2-yl)ethoxy]benzyl}-1,3-thiazolidine-2,4-dione、pioglitazone

+ [39]

靶点

PPARγ

作用方式

激动剂

作用机制

PPARγ激动剂(过氧化物酶体增长因子活化受体γ激动剂)

治疗领域

内分泌与代谢疾病

在研适应症

2型糖尿病

非在研适应症

腹痛阿尔茨海默症心绞痛+ [31]

原研机构

Takeda Pharmaceutical Co., Ltd.

在研机构

Takeda Pharmaceuticals U.S.A., Inc.

Celltrion, Inc.

CHEPLAPHARM Arzneimittel GmbH

+ [8]

非在研机构

Vaia S.A.Takeda Pharma A/S

Merck Sharp & Dohme Corp.

+ [5]

权益机构

Celltrion, Inc.

Celltrion Healthcare Co., Ltd.

Eli Lilly & Co.

+ [3]

最高研发阶段批准上市

首次获批日期

美国 (1999-07-15),

2型糖尿病

最高研发阶段(中国)批准上市

特殊审评孤儿药 (美国)、孤儿药 (欧盟)

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结构/序列

分子式C19H21ClN2O3S

InChIKeyGHUUBYQTCDQWRA-UHFFFAOYSA-N

CAS号112529-15-4

关联

562

项与盐酸吡格列酮相关的临床试验

NCT07053319

/ Recruiting临床1期IIT

Protocol lV: SGLT2 Inhibitors, Pioglitazone and Ketone Production in Type 2 Diabetes Mellitus

To examine whether the empagliflozin-induced stimulation of EGP, lipolysis, and ketone production in T2D individuals can be blocked by pioglitazone (which has direct hepatic and adipose tissue effects).

开始日期2026-02-01

申办/合作机构

University of Texas Health Science Center At San Antonio

[+1]

NCT07056699

/ Not yet recruiting临床3期IIT

Protocol V: San Antonio Site Sub Study: Can Pioglitazone Block SGLT2 Inhibitor-induced Stimulation of Lipolysis, Ketone Production and Liver Glucose Production in Type I Diabetic Patients

Participants are being asked to be in a research study. Scientists do research to answer important questions which might help change or improve treatment of participants disease in the future.
In patients with Type 1 Diabetes (T1D), Dapagliflozin a Selective Glucose Transporter 2 Inhibitor (SGLT2i) is known to increase production of glucose in the liver, increase breakdown of fats (lipolysis), and increase production of ketones (ketogenesis). Ketones are chemicals produced by the liver when the body breaks down fat for energy instead of glucose. When the level of ketones in the body becomes too high, a condition called ketoacidosis develops. In this study, the study team will investigate whether adding pioglitazone (a medication commonly used to treat type 2 diabetes), can reduce the Dapagliflozin - induced liver glucose production, fat break down (lipolysis) and ketone body production (ketogenesis) in patients with Type 1 Diabetes (T1D).

开始日期2025-10-15

申办/合作机构

University of Texas Health Science Center At San Antonio

[+1]

NCT06922656

/ Not yet recruiting临床4期IIT

Can the Addition of Pioglitazone to SGLT2 Inhibitor in Type 1 Diabetic Patients Amplify the Decrease in HbA1c and Prevent the Increase in Plasma Ketone Concentration?

Previous data from our clinical trial has demonstrated that the combination of dapagliflozin plus pioglitazone cause robust decrease in the plasma glucose concentration without significant increase in plasma ketone concentration in subjects with T1DM receiving multiple insulin injections or insulin pump. Although patients receiving insulin therapy with pump have participated in the study, none has insulin delivered in automated pump (780 pump) which automatically adjusts the rate of insulin infusion based upon the measured plasma glucose concentration. Although automated insulin pumps have been introduced to practice only last year, they are gaining popularity in the care of T1DM patients worldwide. The aim of this amendment is to demonstrate the efficacy (decrease in HbA1c) and safety (no significant increase in plasma ketone concentration) of combination of dapagliflozin plus pioglitazone in T1DM patients receiving insulin therapy with automated insulin pump.

开始日期2025-09-15

申办/合作机构

Dasman Diabetes Institute

100 项与盐酸吡格列酮相关的临床结果

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100 项与盐酸吡格列酮相关的转化医学

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100 项与盐酸吡格列酮相关的专利（医药）

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7,019

项与盐酸吡格列酮相关的文献（医药）

2025-12-31·ANNALS OF MEDICINE

PPAR-mediated reduction of lipid accumulation in hepatocytes involves the autophagy-lysosome-mitochondrion axis

Article

作者: Cetti, Federica ; Ossoli, Alice ; Gomaraschi, Monica ; Da Dalt, Lorenzo ; Garavaglia, Carola ; Norata, Giuseppe Danilo

BACKGROUND AND AIM:

Lipid accumulation in hepatocytes is reduced by the activation of the peroxisome proliferator-activated receptor (PPAR) α, which is associated with increased lysosomal acid lipase (LAL) activity, transcription factor EB (TFEB) expression, and mitochondrial β-oxidation.Aim of the study was to assess whether the three isoforms of PPAR, i.e. α, δ and γ, share the same ability to reduce lipid accumulation in hepatocytes and to clarify the involvement of autophagy activation, lysosomal hydrolysis, and mitochondrial β-oxidation in lipid clearance induced by PPARs.

METHODS:

HepG2 cells were treated with oleate/palmitate (O/P) to induce lipid accumulation and exposed to the PPARα agonist fenofibric acid, the γ agonist pioglitazone, the δ agonist seladelpar, or the dual α/γ agonist saroglitazar.

RESULTS:

The treatment of HepG2 cells with fenofibric acid, pioglitazone, seladelpar, or saroglitazar halved lipid accumulation induced by O/P. PPAR agonists increased TFEB, p62, and LC3 expression and rescued LAL impairment induced by O/P. Moreover, PPAR agonists significantly increased mitochondrial mass and the expression of genes involved in mitochondrial dynamics and fatty acid catabolism. Interestingly, PPAR agonists lost their ability to reduce lipid accumulation when autophagic flux, LAL activity, or fatty acid transport in the mitochondria were blocked by specific inhibitors.

CONCLUSION:

All PPAR agonists were able to promote the clearance of lipids in cells loaded with long-chain fatty acids. The key role of acid hydrolysis to generate fatty acids, which can be then catabolized in the mitochondria, and the ability of the PPAR system to sustain each phase of this clearing process were elucidated.

2025-12-01·INFLAMMATION RESEARCH

Peroxisome proliferator-activated receptor gamma prevents activation of RBL-2H3 cells by inhibiting FcεRI-mediated signal transduction

Article

作者: Xie, Yuhang ; Wang, Weihua ; Ruan, Suyu ; Zhang, Yu ; Rui, Xiaoqing ; Zhou, Jianjun

BACKGROUND:

Mast cells are essential contributors to the pathophysiology of allergic diseases. Peroxisome proliferator-activated receptor gamma (PPAR-γ) has recently been identified as being involved in the anti-inflammatory response by inhibiting mast cell activation.

METHOD:

In this study, the PPAR-γ agonist pioglitazone (PIO) was employed to evaluate the effects of PPAR-γ on the degranulation and production of pro-inflammatory mediators in RBL-2H3 cells. Meanwhile, differentially expressed genes (DEGs) were characterised in mast cells exposed to PIO, and pathway enrichment analysis were conducted. Furthermore, we conducted validation to confirm the involvement of PPAR-γ signaling pathways in the FcεRI-mediated signal transduction in mast cells.

RESULTS:

Administration of PIO significantly reduced the release of β-hexosaminidase and the mRNA expression levels of pro-inflammatory cytokines induced by the cross-linking of FcεRIs expressed on the surface of RBL-2H3 cells. A total of 24 DEGs were identified between RBL-2H3 cells treated with and without PIO, and there were 15 up-regulated and 9 down-regulated. GO and KEGG analyses revealed that the immune system, signal transduction, infectious disease, and signaling molecules and interactions were the most enriched annotations. According to PPI network analysis, most DEGs interacted with PPAR-γ. PPAR-γ agonist could activate PPAR-γ and NRF2 signaling pathways in resting RBL-2H3 cells. The protein expression levels of PPAR-γ, Cpt1a, and Acsl4 were greatly upregulated in activated RBL-2H3 cells mediated by FcεRI aggregation. Moreover, the suppressive effects of PPAR-γ agonist on degranulation and phosphorylation levels of FcεRI-mediated signaling molecules in RBL-2H3 cells were PPAR-γ-dependent.

CONCLUSION:

These data demonstrate that PPAR-γ inhibits FcεRI-mediated mast cell activation by modulating intracellular-specific signal transduction in a PPAR-γ-dependent manner.

2025-12-01·JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Computational investigation to identify multi-targeted anti-hyperglycemic potential of substituted 2-Mercaptobenzimidazole derivatives and synthesis of new α-glucosidase inhibitors

Article

作者: Ahmed, Madiha ; Zargaham, Muhammad Kazim ; Waseem, Tanya ; Rajput, Tausif Ahmed ; Nadeem, Humaira ; Amin, Adnan

One of the most widespread diseases recognized all over the world is diabetes, accounting for 1.5 million deaths each year. Recent studies have demonstrated benzimidazole derivatives as potential antidiabetic agents. Hence, the present study is focused on designing new derivatives of 2-mercaptobenzimidazole by C-S cross-coupling reaction and are subjected to computational screening to identify the most promising candidate. Molecular docking and MM-GBSA calculations were performed to ascertain the binding potential with different antidiabetic targets, including α-glucosidase, PPaR-γ, DPP-4, and AMPK. We observed somewhat moderate binding interactions of the synthesized compound against the α-glucosidase. Since binding affinities can be improved using synthetic chemistry approaches, synthesis of analogues (A-18a-c) by designing hybrids at sites such as the acidic functionality of A-18 was done. The analogue A-18a, with p-fluorobenzyl substitution, exhibited enhanced binding affinity (-4.339 Kcal/mol) with the α-glucosidase compared to the parent compound (-3.827 Kcal/mol). The synthesized analogues were also subjected to an in-vitro α-glucosidase inhibitory assay. Among them, A-18a exhibited the most significant inhibitory potential, with an IC₅₀ value of 0.521 ± 0.01 µM as compared to the standard drug Acarbose (IC₅₀ 21.0 ± 0.5 µM). This aligns with the computational study findings, where A-18a exhibited stronger binding interactions within the active site of the enzyme. Hence, a promising analogue of the designed compound was synthesized through a computationally guided approach as an anti-hyperglycaemic agent. Additionally, most of the designed compounds showed significantly greater binding affinity with PPaR-γ as compared to the standard pioglitazone. A-18 was successfully synthesized by S-arylation reaction using CuI in 89% yield and was subjected to MD-simulation against PPaR-γ, which revealed stable binding throughout the 200 ns run. Future studies will focus on exploring the activity of the designed drugs against PPaR-γ through in-vitro and in-vivo assays.

212

项与盐酸吡格列酮相关的新闻（医药）

2025-09-05

·药通社

恒瑞年轻副总，辞职赴任CEO！

9月2日，海森生物发布消息称，刘文军担任公司首席执行官(CEO)，其将全面执掌海森生物战略规划与运营管理体系。海森生物CEO刘文军公开资料显示，刘文军乃是恒瑞前高管，其在恒瑞任职期间为公司创造了诸多亮眼的成绩，包括开拓降尿酸药非布司他院外市场、负责恒瑞用于成人2型糖尿病患者血糖控制的原研重点产品“恒格列净”的市场开发、负责恒瑞组织架构调整后的代谢疼痛产品线等。 2024年，年仅35岁的刘文军被任命为综合产品事业部副总经理，依旧主管代谢疼痛产品线，但仅任新职位一年，其于今年8月突然宣布辞职，并且去向未知。如今，刘文军的新“东家”有了着落。海森生物网站显示，集研发、生产和商业推广，覆盖全产业链的海森生物是一家创新型生物医药企业，成立于2020年，由亚洲一家专注于医疗健康行业的资产管理公司——康桥资本、合肥产投集团与合肥市肥东县共同投资组建。2023年4月，海森生物获得来自康桥资本和阿布扎比主权财富基金穆巴达拉投资公司等机构新一轮的融资，用于未来的收购和创新产品管线的业务发展。目前，公司的业务覆盖中国大陆、瑞士及泛亚太8个国家和地区，产品聚焦于慢性病和急重症治疗领域。 ↓ 扫码加入药通社交流群 ↓ 近年来，该公司为丰富其产品管线，对外收购、合作动作频频。例如，2020年12月，海森生物以3.2亿美元收购了武田制药在中国区心血管和代谢领域处方药业务，将后者包括沙坦类降压药美阿沙坦钾片(易达比)、坎地沙坦酯片(必洛斯)、伏格列波糖片(倍欣)、盐酸吡格列酮片(艾可拓)以及用于急重症的盐酸乌拉地尔注射液(亚宁定)等产品收入囊中。 2023年5月，海森生物子公司宣布与罗氏达成合作，将独家拥有注射用头孢曲松钠(罗氏芬)在中国大陆的专有权。同年9月，海森生物和LIB Therapeutics Inc.联合宣布就海森生物在大中华区(包括中国大陆和港澳台地区)开发及商业化Lerodalcibep达成许可协议。Lerodalcibep融合蛋白是由LIB Therapeutics开发的第三代长效PCSK9抑制剂，每月一针皮下注射，对解决当前临床降脂治疗中未被满足的需求具有潜力，有望助力更多高脂血症患者实现血脂控制达标，目前正处于III期临床开发阶段。 2024年6月28日，海森生物又宣布正式完成对韩国生物制药企业Celltrion旗下14种品牌产品在亚太多个国家和地区商业权益的收购，并拥有这些产品在包括韩国*、新加坡、泰国、澳大利亚、中国香港等8个国家及地区的药品上市许可持有人(MAH)权益。随着刘文军的加入，业内认为这是海森生物强化领导团队、加速业务拓展的重要信号。未来，刘文军能否助力海森生物再创佳绩，值得持续关注。 ↓⭐关注药通社，洞见行业趋势↓ 投稿/企业合作/内容沟通：药通社总编—华籍美人（Ww_150525） *添加请注明备注及来意

2025-08-29

·EINPresswire

July - September 2021 | Potential Signals of Serious Risks/New Safety Information Identified by the FDA Adverse Event Reporting System (FAERS)

Ajovy (fremanezumab-vfrm) Emgality (galcanezumab-gnlm) Nurtec ODT (rimegepant) Ubrelvy (ubrogepant) Vyepti (eptinezumab-jjmr) Hypertension The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2025 to include information about the risk of hypertension. Example: Ajovy labeling Apriso (mesalamine) Asacol (mesalamine) Asacol HD (mesalamine) Azulfidine (sulfasalazine) Azulfidine EN-Tabs (sulfasalazine) Canasa (mesalamine) Colazal (balsalazide disodium) Delzicol (mesalamine) Dipentum (osalazine sodium) Giazo (balsalazide disodium) Lialda (mesalamine) Rowasa (mesalamine) Pentasa (mesalamine) Severe cutaneous adverse reactions The Warnings and Precautions section of the labeling was updated November 2021 to include severe cutaneous adverse reactions. Example: Delzicol labeling Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Pancreatitis FDA determined that no action is necessary at the time based on available information. Avastin (bevacizumab) Mvasi (bevacizumab-awwb) Zirabev (bevacizumab-bvzr) Anaphylactic shock The "Warnings and Precautions" section of the labeling was updated between September 2022 and February 2023 to include anaphylactoid/anaphylactic reactions. Example: Avastin labeling Ayvakit (avapritinib) Photosensitivity reaction The "Warnings and Precautions", "Adverse Reactions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in March 2023 to include information about photosensitivity. Ayvakit labeling Azacitidine Onureg (azacitidine) Vidaza (azacitidine) Generic products containing azacitidine Pericarditis The "Adverse Reactions" section of the labeling was updated between September 2022 and June 2023 to include pericarditis. Example: Vidaza labeling FDA determined that no action is necessary at the time based on available information for Onureg. Bavencio (avelumab) Imfinzi (durvalumab) Libtayo (cemiplimab-rwlc) Keytruda (pembrolizumab) Opdivo (nivolumab) Tecentriq (atezolizumab) Yervoy (ipilimumab) Tumour lysis syndrome FDA determined that no action is necessary at the time based on available information. Cymbalta (duloxetine hydrochloride) Drizalma Sprinkle (duloxetine hydrochloride) Generic products containing duloxetine hydrochloride Anosmia, Hyposmia This issue is posted as two individual newly identified safety signal (NISS) entries in the January-March 2022 quarter, to reflect the focus on the potential signals of anosmia and hyposmia, separately. Darzalex (daratumumab) Darzalex Faspro (daratumumab and hyaluronidase-fihj) Blood stem cell transplant failure FDA determined that no action is necessary at the time based on available information. Dipeptidyl peptidase-4 (DPP-4) inhibitors Glyxambi (empagliflozin and linagliptin) Janumet (metformin hydrochloride and sitagliptin phosphate) Janumet XR (metformin hydrochloride and sitagliptin phosphate) Jentadueto (linagliptin and metformin hydrochloride) Jentadueto XR (linagliptin and metformin hydrochloride) Kazano (alogliptin and metformin hydrochloride) Kombiglyze XR (metformin hydrochloride and saxagliptin) Nesina (alogliptin) Onglyza (saxagliptin) Oseni (alogliptin and pioglitazone) Steglujan (ertugliflozin and sitagliptin) Tradjenta (linagliptin) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Qtern (saxagliptin and dapagliflozin) Generic products containing dipeptidyl peptidase-4 inhibitors Tubulointerstitial nephritis The "Adverse Reactions" section of the labeling was updated between March 2022 and June 2022 for products containing alogliptin and sitagliptin to include tubulointerstitial nephritis. Example: Janumet labeling FDA determined that no action is necessary for products containing linagliptin and saxagliptin at the time based on available information. *An administrative error resulted in the omission of Januvia from the list of product names after the initial quarterly report was posted. Dupixent (dupilumab) Angioedema The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include angioedema. Dupixent labeling Glucagon-like peptide-1 (GLP-1) analogues Adlyxin (lixisenatide) Bydureon (exenatide) Bydureon BCise (exenatide) Byetta (exenatide) Ozempic (semaglutide) Rybelsus (semaglutide) Saxenda (liraglutide) Soliqua 100/33 (insulin glargine and lixisenatide injection) Trulicity (dulaglutide) Victoza (liraglutide) Wegovy (semaglutide) Xultophy 100/3.6 (insulin degludec and liraglutide injection) Generic products containing glucagon-like peptide-1 analogues Gallbladder related disorders The "Warnings and Precautions", "Adverse Reactions", and "Patient Counseling Information" sections of the GLP-1 analogues labeling were updated between March 2022 and June 2022 to include information about acute gallbladder disease. Example: Adlyxin labeling FDA has determined that the last approved labeling for Saxenda and Wegovy is adequately labeled for acute gallbladder disease, and that no further regulatory action is needed at this time. Gonadotropin releasing hormone (GnRH) analogues Fensolvi (leuprolide acetate) Lupron Depot-PED (leuprolide acetate) Supprelin LA (histrelin acetate) Synarel (nafarelin acetate) Triptodur (triptorelin) Idiopathic intracranial hypertension The "Warnings", "Precautions", and "Adverse Reactions" sections of the labeling were updated in April 2022 to include idiopathic intracranial hypertension. Example: Fensolvi labeling Jakafi (ruxolitinib phosphate) Herpes simplex virus (HSV) reactivation and/or disseminated HSV The "Dosage and Administration", "Warnings and Precautions", and "Adverse Reactions" sections of the labeling were updated in January 2023 to include information about herpes simplex and herpes zoster infections. Jakafi labeling Ibrance (palbociclib) Kisqali (ribociclib) Kisqali Femara Co-Pack (letrozole and ribociclib) Embolic and thrombotic events, venous The "Adverse Reactions" section of the Ibrance labeling was updated in December 2024 to include venous thromboembolism. Ibrance labeling FDA determined that no action is necessary at the time for Kisqali and Kisqali Femara Co-Pack based on available information. Ocrevus (ocrelizumab) Myocardial infarction FDA determined that no action is necessary at the time based on available information. Potassium Chloride Product preparation error The “Warnings” section of the labeling was updated in December 2022 to include information about fatal cardiac adverse reactions with intravenous administration of undiluted potassium chloride. Praxbind (idarucizumab) Wrong dose errors The carton labeling and "Dosage and Administration" sections of the labeling were revised in February 2022 to clarify the number of vials included in each carton and the recommended dosing. Praxbind labeling Qbrexza (glycopyrronium tosylate) Accidental exposure to product The container label, carton labeling, "Dosage and Administration", "Warnings and Precautions", "Patient Counseling Information", and "Patient Information" sections of the labeling were updated in October 2022 to include information about accidental exposure. Qbrexza labeling Qbrexza (glycopyrronium tosylate) Urinary retention The “Warnings and Precautions”, “Adverse Reactions”, and “Patient Counseling Information” sections of the labeling were updated in October 2022 to include information about new or worsening urinary retention. Qbrexza labeling Sodium-glucose cotransporter-2 (SGLT-2) inhibitors Farxiga (dapagliflozin) Glyxambi (empagliflozin and linagliptin) Invokamet (canagliflozin and metformin hydrochloride) Invokamet XR (canagliflozin and metformin hydrochloride) Invokana (canagliflozin) Jardiance (empagliflozin) Qtern (saxagliptin and dapagliflozin) Steglatro (ertugliflozin) Steglujan (ertugliflozin and sitagliptin) Segluromet (ertugliflozin and metformin hydrochloride) Synjardy (empagliflozin and metformin hydrochloride) Synjardy XR (empagliflozin and metformin hydrochloride) Trijardy XR (empagliflozin, linagliptin and metformin hydrochloride) Xigduo XR (dapagliflozin and metformin) Generic products containing sodium-glucose cotransporter-2 (SGLT-2) inhibitors Tubulointerstitial nephritis FDA determined that no action is necessary at the time based on available information. Somatostatin Receptor Imaging Agents Detectnet (copper Cu-64 dotatate injection) Gallium Dotatoc (GA 68) Octreoscan (Indium In 111 Pentetreotide) Netspot (Gallium GA 68 Dotatate) Hypersensitivity The "Warnings and Precautions" and "Adverse Reactions" sections of the labeling were updated in December 2021 to include hypersensitivity reactions. Example: Netspot labeling Stromectol (ivermectin) Generic products containing ivermectin Off label use FDA determined that no action is necessary at the time based on available information. Stromectol (ivermectin) Generic products containing ivermectin Neurotoxicity The "Warnings", "Adverse Reactions", and "Overdosage" sections of the labeling were updated in March 2022 to include neurotoxicity. Example: Stromectol labeling Sunosi (solriamfetol hydrochloride) Hypersensitivity FDA determined that no action is necessary at the time based on available information. Vivitrol (naltrexone) Incorrect route of product administration The container label (vial), carton labeling, "Dosage and Administration", "Warnings and Precautions", and "Description", sections of the labeling were revised in September 2022 to emphasize the appropriate route and site of administration. Vivitrol labeling Xcopri (cenobamate) Psychiatric disorders The "Adverse Reactions" section of the labeling was updated in June 2022 to include psychiatric disorders. Xcopri labeling Legal Disclaimer: EIN Presswire provides this news content "as is" without warranty of any kind. We do not accept any responsibility or liability for the accuracy, content, images, videos, licenses, completeness, legality, or reliability of the information contained in this article. If you have any complaints or copyright issues related to this article, kindly contact the author above.

上市批准

2025-08-08

·国际糖尿病idiabetes

早期强化，追本溯源——二甲双胍在早期糖尿病治疗中的地位

点击“蓝字”关注我们编者按防治关口前移已成为2型糖尿病（T2DM）管理的普遍共识。如何更有效地管理早期T2DM患者，是当前临床关注的重点。在刚刚结束的第二十八次全军内分泌代谢病学术大会上，西北大学附属西安国际医学中心医院姬秋和教授围绕新诊断T2DM管理中的早期强化控糖价值进行了学术分享。姬教授的报告围绕临床治疗需求展开，首先阐述了当前面临的挑战；随后，从疾病发病机制角度进行深入剖析，追本溯源；最后，重点探讨了经典降糖药二甲双胍在早期强化控糖策略中的应用价值与基石地位。本刊特此整理报道核心内容，旨在帮助读者及时了解相关进展。治疗需求：早期强化控糖是新诊断T2DM患者的核心治疗策略我国糖尿病流行病学数据显示，新诊断T2DM患者占比高达54%，但其血糖控制现状严峻，HbA1c≥7.0%者达63.2%，且随访1年后仍有31.5%未达标[1,2]。大型队列研究证实，新诊断T2DM患者确诊后1年内HbA1c水平越高，未来13年发生微血管与大血管并发症及死亡的风险显著增加[3]，凸显早期强化血糖管理的紧迫性。该领域里程碑研究——英国前瞻性糖尿病研究（UKPDS）为此提供了关键证据。UKPDS 88显示，T2DM确诊后立即治疗使HbA1c降低1%，可在10~15年后显著降低全因死亡风险18.8%和心肌梗死风险19.7%。然而，若延迟至确诊后5或10年才实现相同HbA1c降幅，则上述风险获益显著缩小[4]。UKPDS 35进一步表明，HbA1c每降低1%，多种并发症风险可显著降低12%~43%（图1）[5]。这些结果共同强调，对新诊断T2DM患者尽早实施严格控糖至关重要，且HbA1c目标越严格，远期并发症风险降低越显著。图1. 新诊T2DM患者强化控糖，HbA1c控制越严格，并发症风险越低 2024年CDS指南[6]亦建议对新诊断T2DM患者设定更严格的降糖目标。指南强调HbA1c目标需个体化，但对年龄较轻、病程较短或是新诊断患者、预期寿命较长、无并发症、未合并心血管疾病的T2DM患者，在安全前提下，可设定强化目标（HbA1c≤6.5%甚至正常）。因此，早期强化控糖是新诊断T2DM患者管理的核心策略，能最大程度降低远期并发症风险，在制定具体方案前需明确其高血糖的主要原因。追本溯源：肝糖输出增加是新诊断T2DM患者血糖升高的主要原因肝脏是维持人体血糖稳态的重要器官。空腹状态下，其肝糖输出（包括糖异生和肝糖原分解）提供了人体约90%的血糖来源；餐后状态时，肝脏处理约1/3由肠道吸收的葡萄糖[7]。 T2DM患者肝糖输出显著增加，且在新诊断阶段即已出现。相较于非糖尿病者，其增加主要源于糖异生率升高，而非糖原分解率变化[8]。空腹血糖水平与肝糖输出呈正相关，T2DM患者的空腹肝糖输出比非糖尿病者约增加1倍，同样主要归因于糖异生增加[9]。肝糖输出异常不仅影响空腹血糖，也与餐后血糖密切相关。研究显示，口服葡萄糖后，T2DM患者肝糖输出的抑制程度（较服糖前仅降低20.3%）远低于非糖尿病对照（降低45.9%），表明其餐后肝糖输出抑制不足。此时T2DM患者平均动脉血糖浓度高达14.6 mmol/L，其中近50%由肝糖输出贡献[10]。因此，肝糖输出增加是T2DM患者空腹及餐后高血糖的重要成因。高血糖本身又会加剧肝脏胰岛素抵抗，形成“胰岛素抵抗-肝糖输出增加-血糖升高”的恶性循环[9,11-15]。在此循环中，肝糖输出增加是重要环节和血糖升高的主要根源（图2）。因此，抑制肝糖输出成为早期强化控糖策略的关键。图2. 在“胰岛素抵抗-肝糖输出增加-血糖升高”的恶性循环中，肝糖输出增加尤为关键降糖基石：二甲双胍抑制肝糖输出，直击病因，强效降糖近年来，降糖新药层出不穷，而二甲双胍因其独特的降糖机制、直击病因，强效降糖，始终是国内外指南一致推荐的T2DM血糖管理的基础用药。 1、独特机制：直击病因，打破恶性循环二甲双胍通过OCT1转运进入细胞，主要作用于抑制线粒体和溶酶体功能，从而直接激活AMPK通路[16,17]。在肝脏中，AMPK激活可阻碍糖异生关键酶PEPCK/G6Pase的转录并下调PEPCK水平[18]，显著减少肝糖输出。此外，二甲双胍还能增加胰岛素与其受体的结合，激活PI3K-AKT通路，协同抑制肝糖输出。AMPK的激活不仅提高了肝脏和外周组织的胰岛素敏感性，有效改善胰岛素抵抗，还促进这些组织对葡萄糖的摄取及糖原合成。同时，血糖降低本身也有助于改善胰岛素抵抗，打破“胰岛素抵抗-肝糖输出增加-血糖升高”恶性循环（图3）。图3. 二甲双胍直接激活AMPK，抑制肝糖输出，改善胰岛素抵抗，打破恶性循环 2、坚实循证：强效降糖，基石地位，多重获益强效抑制肝糖输出一项针对10例非肥胖、血糖控制不佳T2DM患者的随机双盲交叉研究显示，在治疗最后1天进行高胰岛素正葡萄糖钳夹试验时，二甲双胍组较安慰剂组显著降低空腹肝糖输出达62%[19,20]。显著改善胰岛素抵抗 MARCH研究亚组分析证实，新诊断T2DM患者使用二甲双胍治疗48周后，胰岛素抵抗指数——HOMA-IR（评估全身胰岛素抵抗）和HIRI（评估肝脏胰岛素抵抗）均显著下降，且基线肝脏胰岛素抵抗严重者改善更明显[21]。研究还显示，相较于钠-葡萄糖共转运蛋白2抑制剂（SGLT2i）或胰高糖素样肽-1受体激动剂（GLP-1RA）单药治疗，二者分别联合二甲双胍均能进一步改善胰岛素抵抗[22,23]。此外，二甲双胍联合西格列汀、阿卡波糖、吡格列酮或甘精胰岛素治疗12~24周，相比单用相应药物，空腹胰岛素水平及HOMA-IR的降幅均更大[24-27]。持久强效降糖 DeFronzo教授牵头的随机双盲平行对照研究表明，新诊断T2DM患者使用二甲双胍治疗29周，较安慰剂显著降低空腹血糖3.2 mmol/L和餐后血糖4.0 mmol/L；治疗9周即可降低HbA1c 1.0%，治疗半年后HbA1c降幅稳定在1.8%[28]。重要的是，二甲双胍的降糖疗效不受患者体重指数（BMI）[29]和胰岛功能状态[30]的影响，表现出广泛的适用性和有效性。得益于其独特机制，二甲双胍降糖强效且不增加低血糖风险[6,31]。剂量研究证实，2000 mg/d为二甲双胍最佳降糖剂量，可显著降低HbA1c达2.0%，且此剂量下的胃肠道反应与低剂量相比无显著差异（图4）[32]。图4. 二甲双胍强效降糖，足量（2000 mg/d）可降低HbA1c达2.0% 明确靶器官保护 UKPDS研究长达42年的随访数据显示，与常规治疗相比，二甲双胍治疗显著降低T2DM患者的心肌梗死风险31%和全因死亡风险20%（图5），且此获益持续存在[33]。图5. UKPDS 91：早期应用二甲双胍显著降低心肌梗死及死亡风险指南一致推荐基石地位综合多项权威指南，二甲双胍在T2DM治疗中的基石地位得到明确和重申。2025年IDF指南[34]推荐二甲双胍仍为T2DM患者的一线基石用药（图6），指出其单药治疗具有良好的全球可及性、疗效、安全性（包括低血糖风险低）、成本效益以及长期心血管获益；在联合治疗中，二甲双胍被视为基石。该指南同时指出，研究证据支持早期使用SGLT2i和GLP-1RA，通常与二甲双胍联用，以改善血糖控制不佳的不良结局及心肾结局，但这些新型降糖药作为一线单药治疗的证据尚有限。2024年CDS指南[6]同样强调二甲双胍是控制高血糖的基础用药。我国《国家基层糖尿病防治管理指南（2022）》[35]将其列为首选药物，要求若无禁忌且耐受，应全程保留在治疗方案中。《二甲双胍临床应用专家共识（2023年版）》[36]进一步细化其定位：对于无心肾保护强适应症需优先使用GLP-1RA或SGLT2i的患者，二甲双胍应作为首选一线药物并全程保留；对于优先使用GLP-1RA或/和SGLT2i的患者，二甲双胍则是首选的联合用药。图6. 2025年IDF糖尿病指南：二甲双胍仍是T2DM患者的一线基石用药结语早期强化控糖是新诊断T2DM患者的核心治疗策略，可显著降低远期并发症风险。从病理机制看，肝糖输出增加是新诊断T2DM患者早期病理特征，也是其空腹及餐后血糖升高的主要原因。抑制肝糖输出是打破“胰岛素抵抗-肝糖输出增加-血糖升高”这一恶性循环的关键突破点，因而成为早期强化控糖方案中的关键环节。二甲双胍通过直接激活AMPK，抑制肝糖输出，有效降低血糖并改善胰岛素抵抗，从而降低远期并发症风险，被各大权威指南一致推荐为T2DM治疗的基础用药。参考文献（上下滑动可查看） 1. Li Y, et al. BMJ. 2020; 369: m997. 2. Cai X, et al. J Diabetes Investig . 2020; 11(1): 151-161. 3. Laiteerapong N, et al. Diabetes Care. 2019; 42(3): 416-426. 4. Lind M, et al.Diabetes Care. 2021; 44(10): 2231-2237. 5. Stratton IM, et al. BMJ. 2000; 321(7258): 405-412. 6. 中华医学会糖尿病学分会. 中华糖尿病杂志. 2025; 17(1): 16-139. 7. Warner S, et al. Front Endocrinol (Lausanne). 2020; 11: 567. 8. Chung ST, et al. Diabetologia. 2015; 58(3): 596-603. 9. Consoli A, et al. Diabetes.1989; 38(5): 550-557. 10. Mitrakou A, et al. Diabetes. 1990; 39(11): 1381-1390. 11. Tripathy D, et al. J Clin Endocrinol Metab. 2019; 104(7): 2842-2850. 12. Onyango AN. Heliyon.2022; 8(12): e12294. 13. Barroso E, et al. Trends Endocrinol Metab. 2024; 35(12): 1062-1077. 14. Firth R, et al. J Clin Invest.1986; 77(5): 1525-1532. 15. Shannon C, et al. J Clin Endocrinol Metab. 2022; 107(8): e3177-e3185. 16. Bailey CJ, et al. Nat Rev Endocrinol. 2012; 8(8): 449-450. 17. Ma T, et al. Nature. 2022; 603(7899): 159-165. 18. Dutta S, et al. Drug Des Devel Ther. 2023; 17: 1907-1932. 19. Marena S, et al. Diabete Metab. 1994; 20(1): 15-19. 20. Phielix E, et al. Trends Pharmacol Sci. 2011; 32(10): 607-616. 21. Cui R, et al. Diabetes Res Clin Pract . 2024; 214: 111788. 22. Cheng L, et al. Sci Rep. 2021; 11(1): 24263. 23. 周瑞凤, 等. 临床荟萃. 2017; 32(11): 965-968. 24. Goldstein BJ, et al. Diabetes Care. 2007; 30(8): 1979-1987. 25. 庞宁, 等. 中国药房. 2017; 28(27): 3774-3777. 26. Perez A, et al. Curr Med Res Opin. 2009; 25(12): 2915-2923. 27. 董付青. 中国医药指南. 2023; 21(10): 42-45. 28. DeFronzo RA, et al. N Engl J Med. 1995; 333(9): 541-549. 29. Ji L, et al. PLoS One. 2013; 8(2): e57222. 30. Fu J, et al. Endocr J. 2019; 66(5): 443-450. 31. ADA. Diabetes Care. 2025; 48(Suppl_1): S181-S206. 32. Garber AJ, et al. Am J Med. 1997; 103(6): 491-497. 33. Adler AI, et al. Lancet. 2024; 404(10448): 145-155. 34. IDF Global Clinical Practice Recommendations for Managing Type 2 Diabetes 2025. Idf.org 35. 中华医学会糖尿病学分会, 等. 中华内科杂志. 2022; 61(3): 249-262. 36. 《二甲双胍临床应用专家共识》更新专家组. 中华内科杂志. 2023; 62(6): 619-630. 声明：本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。最新《国际糖尿病》读者专属微信交流群建好了，快快加入吧！扫描左边《国际糖尿病》小助手二维码（微信号：guojitnb），回复“国际糖尿病读者”，ta会尽快拉您入群滴！（来源：《国际糖尿病》编辑部）版权声明版权属《国际糖尿病》所有。欢迎个人转发分享。其他任何媒体、网站未经授权，禁止转载。

临床研究

100 项与盐酸吡格列酮相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00945	盐酸吡格列酮	A10BG03	DB01132

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
2型糖尿病	美国	Takeda Pharmaceuticals U.S.A., Inc.	1999-07-15

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
神经性听力损失	临床3期	捷克	Strekin AG	2018-02-24
神经性听力损失	临床3期	德国	Strekin AG	2018-02-24
神经性听力损失	临床3期	瑞士	Strekin AG	2018-02-24
阿尔茨海默症	临床3期	美国	Takeda Pharmaceutical Co., Ltd.	2013-08-01
阿尔茨海默症	临床3期	澳大利亚	Takeda Pharmaceutical Co., Ltd.	2013-08-01
阿尔茨海默症	临床3期	德国	Takeda Pharmaceutical Co., Ltd.	2013-08-01
阿尔茨海默症	临床3期	瑞士	Takeda Pharmaceutical Co., Ltd.	2013-08-01
阿尔茨海默症	临床3期	英国	Takeda Pharmaceutical Co., Ltd.	2013-08-01
轻度认知障碍	临床3期	美国	Takeda Pharmaceutical Co., Ltd.	2013-08-01
轻度认知障碍	临床3期	澳大利亚	Takeda Pharmaceutical Co., Ltd.	2013-08-01

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临床结果

适应症

分期

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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


NCT05107765 (CTgov)	临床1/2期	酒精使用障碍	67	Placebo (Placebo)	選窪遞鑰餘獵選壓膚廠(廠膚壓鬱築鏇淵艱繭衊) = 網鏇壓餘積襯顧蓋網遞製獵憲憲鹽艱襯膚糧鏇 (鏇齋齋製艱餘衊餘網淵, 11.426) 更多	-	2025-08-27
				Pioglitazone (Pioglitazone)	選窪遞鑰餘獵選壓膚廠(廠膚壓鬱築鏇淵艱繭衊) = 鑰築淵鏇網觸範積壓糧製獵憲憲鹽艱襯膚糧鏇 (鏇齋齋製艱餘衊餘網淵, 11.885) 更多
NCT04300127 (PIOGAS, CTgov)	早期临床1期	胃轻瘫	14	Pioglitazone 30 mg	鹹衊選餘製廠顧壓壓鑰(蓋鏇繭簾窪鑰範窪鑰築) = 襯蓋鑰繭遞鹹獵鑰獵觸膚醖積夢蓋網餘選壓醖 (醖願鬱糧齋築糧積壓夢, 0.9) 更多	-	2025-04-30
NCT00179400 (CTgov)	临床4期	2型糖尿病	26	Pioglitazone (2000-200 Study 10-day Pioglitazone)	憲壓醖壓衊鏇廠築憲壓(遞觸廠襯膚廠醖鑰鹹鑰) = 淵製鹽願鏇觸糧遞廠艱鑰鑰選艱範糧壓壓構鑰 (窪觸構簾蓋構糧範顧製, 0.19) 更多	-	2025-03-03
				placebo+pioglitazone (2000-200 Study 10-day Placebo)	憲壓醖壓衊鏇廠築憲壓(遞觸廠襯膚廠醖鑰鹹鑰) = 積憲窪鏇顧膚範鏇築鬱鑰鑰選艱範糧壓壓構鑰 (窪觸構簾蓋構糧範顧製, 0.20) 更多
NCT01107717 (EDICT, Pubmed \| BMJ Open Diabetes Res Care)	临床4期	糖尿病追加	55	Metformin/Exenatide/Pioglitazone	鏇憲製遞窪顧願獵繭夢(鬱鹹膚選鹹網鬱顧膚鏇) = 衊觸願襯齋壓築艱糧觸願齋築鏇範網餘鹹壓艱 (鏇簾築積鏇獵廠網簾構 )	积极	2025-03-01
				Metformin/Glipizide/Insulin Glargine	鏇憲製遞窪顧願獵繭夢(鬱鹹膚選鹹網鬱顧膚鏇) = 鑰選觸蓋壓醖鑰觸鏇築願齋築鏇範網餘鹹壓艱 (鏇簾築積鏇獵廠網簾構 )
NCT04604223 (Pubmed \| Front Immunol) 人工标引	临床4期	新型冠状病毒感染 \| 2型糖尿病	350	Pioglitazone	範襯鏇糧餘鹽醖廠觸遞(廠選積簾觸憲觸衊艱膚) = no significant difference in the CRP reduction was observed between the two groups 顧遞膚鬱襯鏇廠襯餘艱 (製膚糧網網醖憲壓淵鹽 ) 更多	不佳	2024-09-06
				Placebo
NCT01107717 (EDICT \| EDICT study, CTgov)	临床4期	2型糖尿病	318	exenatide+pioglitazone+metformin (Triple Therapy)	觸範獵醖壓壓繭夢窪遞(遞選顧醖夢窪願窪鹹憲) = 醖構範餘構鬱蓋製獵獵範廠憲繭衊製衊蓋鹹衊 (顧襯鬱糧襯願願壓憲廠, 0.1) 更多	-	2024-09-05
				glargine+metformin+glyburide (Conventional Therapy)	觸範獵醖壓壓繭夢窪遞(遞選顧醖夢窪願窪鹹憲) = 窪膚鹽淵憲襯顧鬱糧膚範廠憲繭衊製衊蓋鹹衊 (顧襯鬱糧襯願願壓憲廠, 0.1) 更多
NCT04885712 (Pubmed \| Clin Ther) 人工标引	临床3期	2型糖尿病追加	366	Pioglitazone 15 mg	獵獵鏇衊遞鹽選壓襯鏇(網餘鑰積壓鬱淵糧製鏇) = 壓淵鑰顧壓蓋築壓淵觸廠夢蓋鏇鏇膚襯廠顧選 (窪範廠艱糧鬱廠夢選餘 )	积极	2024-07-01
				Pioglitazone 30 mg	獵獵鏇衊遞鹽選壓襯鏇(網餘鑰積壓鬱淵糧製鏇) = 簾鹹積膚憲繭夢憲鬱繭廠夢蓋鏇鏇膚襯廠顧選 (窪範廠艱糧鬱廠夢選餘 )
ISRCTN45546616 \| ISRCTN29234515 \| ISRCTN11062950 (ISRCTN11062950;ISRCTN29234515;ISRCTN45546616, Pubmed)	临床3期	多囊卵巢综合征 HOTAIR rs1443512 genotype	65	pioglitazone	獵醖顧顧簾衊糧積憲鏇(淵觸鬱網構餘範鹹簾簾) = 餘鏇網積襯餘選積獵憲廠淵鑰簾糧齋積願鏇製 (餘獵鏇壓憲壓顧觸鏇鏇 ) 更多	-	2024-04-01
NCT05226897 (Pubmed) 人工标引	临床3期	2型糖尿病	249	YYC405+Metformin+Dapagliflozin	構繭鹹製鑰獵遞願繭鏇(簾積衊衊範齋繭鬱築鏇) = Pioglitazone administration resulted in a significant reduction in HbA1c levels (from 7.80% ± 0.72% to 7.27% ± 0.82%) compared with placebo (from 7.79% ± 0.76% to 7.69% ± 0.86%, corrected mean difference: -0.42% ± 0.08%; p < 0.01). 窪壓膚觸艱襯憲選觸構 (鏇壓選蓋壓觸壓膚膚觸 )	积极	2024-02-29
				Placebo+Metformin+Dapagliflozin
NCT05101135 (Pubmed)	-	2型糖尿病	250	Pioglitazone Hydrochloride+二甲双胍+达格列净	簾鹹願獵鹹簾窪顧繭糧(窪廠範構鑰範築衊繭襯) = 衊蓋築膚獵構獵願襯蓋製鏇糧衊簾繭顧襯構鑰 (窪鑰鹽選衊鹹齋壓衊鏇 ) 更多	积极	2024-02-02
				Placebo+二甲双胍+达格列净	簾鹹願獵鹹簾窪顧繭糧(窪廠範構鑰範築衊繭襯) = 夢觸積衊網淵膚糧簾製製鏇糧衊簾繭顧襯構鑰 (窪鑰鹽選衊鹹齋壓衊鏇 ) 更多