预约演示
更新于：2026-10-28
Dorzagliatin
多格列艾汀
更新于：2026-10-28
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 中国 (2022-09-30), |
最高研发阶段(中国)批准上市 |
特殊审评特殊审批 (中国) |
登录后查看时间轴
结构/序列
分子式C22H27ClN4O5 |
InChIKeyHMUMWSORCUWQJO-QAPCUYQASA-N |
CAS号1191995-00-2 |
关联
31
项与 多格列艾汀 相关的临床试验NCT07786571
A Prospective, Randomized, Active-Controlled, Multicenter Clinical Study on Improving Blood Glucose Homeostasis With Dorzagliatin Tablets in the Treatment of Type 2 Diabetes Mellitus Patients With Moderate to Severe Chronic Renal Insufficiency
NCT06995651
Pharmacokinetic and Pharmacodynamic Effects of Dorzagliatin in Pancreatic Insufficient-Cystic Fibrosis: A Randomized Double-blind, Cross-over Trial
NCT06976658
Evaluating a Novel, Allosteric Glucokinase Activator in Monogenic Diabetes Secondary to Inactivating Glucokinase Mutations: a Randomised, Cross-over Trial
100 项与 多格列艾汀 相关的临床结果
登录后查看更多信息
100 项与 多格列艾汀 相关的转化医学
登录后查看更多信息
100 项与 多格列艾汀 相关的专利（医药）
登录后查看更多信息
67
项与 多格列艾汀 相关的文献（医药）2026-09-01BMJ Open Diabetes Research & Care
Resetting the glucose sensor: dorzagliatin and the evolution of glucokinase activation in diabetes therapy
Review
作者: Chang, Mingxing ; Shen, Guifang ; Shen, Peipu
The progressive decline in functional β-cell mass represents a fundamental, unmet challenge in type 2 diabetes (T2DM) management. Dorzagliatin (HMS5552), a fourth-generation, dual-acting, and glucose-dependent glucokinase activator (GKA), offers a distinct mechanistic approach that aims to move beyond symptomatic glycemic control toward potential glucose sensor modulation. This review critically synthesizes the development of dorzagliatin, designed to overcome the hypoglycemia and tachyphylaxis of earlier GKAs. While its unique allosteric mechanism enables synchronized restoration of insulin secretion and hepatic glucose metabolism, we critically evaluate its clinical positioning. Observational data from the DREAM study suggest sustained drug-free glycemic maintenance; however, we emphasize that these findings do not yet meet the rigorous 2021 American Diabetes Association/European Association for the Study of Diabetes consensus definition of “diabetes remission” and require validation through randomized withdrawal trials. Furthermore, we address the critical absence of long-term cardiovascular outcomes trials (CVOTs) and the theoretical concerns regarding hepatic de novo lipogenesis. We also propose a synergistic framework for combining dorzagliatin with sodium-glucose cotransporter-2 inhibitors to counteract compensatory endogenous glucose production, positioning it as a precision-driven component in the evolving T2DM therapeutic landscape. Should future CVOTs demonstrate safety and efficacy, GKAs like dorzagliatin could potentially be integrated into treatment guidelines, possibly as a “sensor-calibrator” for a subset of patients identified through metabolic and genetic phenotyping. However, it must be emphasized that no CVOT data are currently available for dorzagliatin.
2026-07-01Diabetes Therapy
Treatment Options for Patients with Maturity-Onset Diabetes of the Young (MODY): A Systematic Review of Literature: 2026 Update
Review
作者: Di Berardino, Alessio ; Petragnano, Francesco ; Rossi, Mario ; Baroni, Marco G ; Lustri, Serena ; Zagaroli, Luca ; Delvecchio, Maurizio ; Fasciani, Irene
INTRODUCTION:
Maturity-onset diabetes of the young (MODY) is a rare monogenic form of diabetes characterized by impaired insulin secretion and genetic and clinical heterogeneity. Accurate molecular diagnosis enables precision medicine by guiding gene-specific treatment, improving glycemic control, and avoiding unnecessary therapies. Since our previous systematic review in 2020, new studies have further clarified therapeutic strategies and emerging treatment options. This review updates the evidence on pharmacological management of MODY and its clinical implications.
METHODS:
A systematic review was conducted following PRISMA 2020 recommendations. PubMed was searched for studies published between April 2020 and October 2025. Eligible studies included individuals with genetically confirmed MODY receiving pharmacological treatment, therapeutic switches, or adjunctive therapies. Data were extracted and synthesized qualitatively due to heterogeneity in study design and outcome reporting.
RESULTS:
Ninety-one studies were included. Strong evidence confirms sulfonylureas (SUs) as first-line therapy in Hepatocyte Nuclear Factor 1A (HNF1A)-, Hepatocyte Nuclear Factor 4A (HNF4A)-, ATP-binding cassette transporter sub-family C member 8 (ABCC8)-, and potassium inwardly rectifying channel subfamily J member 11 (KCNJ11)-MODY, frequently enabling improved glycemic control and transition from insulin. Glucokinase (GCK)-MODY remains managed without pharmacological treatment outside pregnancy, but dorzagliatin, a novel agent acting as a glucokinase activator, may further expand precision treatment approaches. Insulin remains the mainstay of treatment in Hepatocyte Nuclear Factor 1B (HNF1B)- and Insulin (INS)-MODY, although adjunctive therapies may provide benefits. While SUs are supported by consistent observational evidence, the role of incretin-based therapies and sodium-glucose co-transporter 2 inhibitors remains exploratory, largely based on small studies and case reports.
CONCLUSIONS:
A major limitation of the available evidence is the predominance of small, heterogeneous observational studies, which limits the strength and generalizability of therapeutic recommendations. Recent literature largely confirms existing genotype-guided treatment recommendations while suggesting expanded therapeutic options for selected MODY subtypes. Precision medicine based on molecular diagnosis remains essential for optimal management.
2026-06-01Drug metabolism and bioanalysis letters
In Silico Approaches to Predict Drug Metabolism: Pharmacophore Mapping and Virtual Screening of Heterocyclic Antidiabetic Agents
Article
作者: Mehra, Anuradha ; Singh, Harmandeep ; Mittal, Amit
Introduction::
An emerging impetus has driven the development of various smallmolecule
compounds for the management of type 2 diabetes. With the advent of novel heterocyclic
derivatives, an expansive field of pharmacological endeavors has opened up to stimulate
Glucokinase (GK) activation. Recent evidence has validated GK's legitimacy as a potential target
for pharmaceutical intervention in diabetes. Glucokinase, an enzyme critical to maintaining
blood glucose equilibrium, malfunctions in individuals with type 2 diabetes. A key component of
this innovative approach is the use of heterocyclic derivatives to stimulate the GK enzyme,
thereby serving as powerful pharmaceutical agents to improve type 2 diabetes management substantially.
Methods::
Maybridge's digital archive contained 53,000 compounds, known for their efficacy,
which were subjected to thorough examination. From this extensive repository, 422 compounds
with an indole core were identified. The structures generated by ChemBioDraw Ultra through
this method were meticulously docked using AutoDock Vina 1.5.6. Online log P predictions
were also made possible by the Swiss ADME algorithm. PKCSM software was used to assess
the potential toxicity of the leading compounds.
Results::
Auto Dock Vina 1.5.6 was used to dock 422 indole derivatives. Compounds with the
greatest binding affinity to glucokinase (GK) were found in the majority of the compounds.
Based on the superior binding capabilities of the top eight molecules compared to Dorzagliatin
(the standard drug) and MRK (the co-crystallized ligand), the top eight molecules were chosen.
Following the enhancement of their pharmacokinetic profiles and compliance with Lipinski's
rule of five, these eight candidates were further evaluated using ADMET analysis. As a result,
AH249 displayed the greatest binding affinity with -11.5 kcal/mol. In contrast to the standard
drugs Dorzagliatin (GKA) and MRK (co-crystallized ligand), AH249 showed no skin sensitization,
AMES toxicity, or hepatotoxicity using PKCSM.
Discussion::
This research highlights the importance of in silico techniques in discovering antidiabetic
medicines, as AH249 outperformed 421 other indole derivatives in terms of glucokinase
affinity. According to SwissADME results, both compounds, AH249 and AH102, are drug-like.
Analysis through molecular docking revealed interactions that can be tested and verified using
experiments.
Conclusion::
There are 422 selected lead compounds containing an indole base in the 53,000 compound
database that demonstrated the best activation of glucokinase among the 53,000 compounds.
According to the findings of this computational drug design analysis, the most promising drug candidates
deserve consideration for advancement to the in vitro stage, particularly AH249, which
exhibits the greatest binding affinity, a favorable pharmacokinetic profile, and negligible toxicity.
For a better understanding of the therapeutic implications of the drug, particularly within the field
of type 2 diabetes, more thorough investigation and evaluation are essential, especially the use of
in-vivo models such as Streptozotocin-induced diabetic rats.
100 项与 多格列艾汀 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 中国 | 2022-09-30 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 葡萄糖耐受不良 | 临床2期 | - | 2022-08-01 | |
| 肝功能不全 | 临床1期 | 中国 | 2019-02-26 | |
| 高血糖 | 临床阶段不明 | 中国香港 | 2025-04-02 | |
| 糖尿病肾病 | 临床申请 | 中国 | - | |
| 虚弱综合症 | 临床前 | 中国 | 2026-03-27 | |
| 成年发病型糖尿病2型 | 临床前 | 中国 | 2026-03-27 | |
| 轻度认知障碍 | 临床前 | 中国 | 2026-03-27 | |
| 阿尔茨海默症 | 临床前 | 中国 | 2022-10-13 | |
| 1型糖尿病 | 临床前 | 中国 | 2022-10-13 | |
| 代谢功能障碍相关脂肪性肝炎 | 临床前 | 中国 | 2022-10-13 |
登录后查看更多信息
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 2,024 | 淵遞餘網艱憲蓋憲膚繭(鏇醖顧構願觸淵獵獵網) = No SAEs were assessed by investigators as related to dorzagliatin and no new or unexpected safety signals were identified. 製獵壓繭願願網糧壓積 (願範鹽構構獵襯鏇淵顧 ) 更多 | 积极 | 2026-09-28 | |||
N/A | 255 | (TIR≤50%) | 選遞襯遞鹽衊餘顧夢壓(網簾夢糧壓鬱壓齋膚願) = 衊鏇觸壓鑰範鬱築憲遞 構觸夢願艱壓構簾鑰觸 (網窪構鹽夢餘憲淵蓋餘, 1.4) 更多 | 积极 | 2026-06-20 | ||
(50%<TIR≤70%) | 選遞襯遞鹽衊餘顧夢壓(網簾夢糧壓鬱壓齋膚願) = 製顧壓製遞鏇襯艱齋艱 構觸夢願艱壓構簾鑰觸 (網窪構鹽夢餘憲淵蓋餘, 1.0) 更多 | ||||||
临床1期 | 16 | 壓衊鬱構鏇艱鬱範積網(網願襯衊夢積願醖觸範) = 窪選顧鹹壓範製顧壓襯 鹹淵網選積簾製觸襯鹹 (積築衊鑰範襯夢壓選遞 ) 更多 | 积极 | 2026-04-21 | |||
N/A | 72 | 遞繭觸鹽鬱鏇憲廠蓋醖(顧壓遞壓夢簾鑰廠蓋築) = 網築築淵襯鑰鑰構範壓 獵衊鹽築範艱餘製遞襯 (蓋糧鬱糧夢觸願鏇壓範 ) 更多 | 积极 | 2025-06-20 | |||
N/A | 69 | 選鏇糧壓淵淵醖蓋糧鏇(鹽醖夢夢淵醖構築齋蓋) = 鏇襯鹽獵願繭襯醖廠網 窪觸膚糧鹹築獵壓築鹽 (醖築憲獵構積鏇網獵獵, 53.4 ~ 77.0) | - | 2022-06-01 | |||
临床3期 | 463 | 願廠繭壓範範齋壓觸構(夢鹹廠蓋鬱獵願憲蓋鹽) = 遞觸襯襯簾觸鹹鬱鏇獵 顧壓衊憲鹹鏇衊鏇繭窪 (壓繭鹹鬱憲餘蓋齋獵窪, -1.19 ~ -0.95) | 积极 | 2022-05-12 | |||
Placebo | 願廠繭壓範範齋壓觸構(夢鹹廠蓋鬱獵願憲蓋鹽) = 網憲鬱鑰壓艱壓願願構 顧壓衊憲鹹鏇衊鏇繭窪 (壓繭鹹鬱憲餘蓋齋獵窪, -0.68 ~ -0.32) | ||||||
临床3期 | 767 | metformin+Dorzagliatin | 夢窪壓繭觸築窪觸網鏇(網醖鏇壓衊積窪鹽廠夢) = 願簾鹹艱網鬱壓鑰遞積 願範衊醖範築獵鑰獵範 (鏇醖壓繭壓鏇窪鑰鹹網, -1.11 ~ -0.93) | 积极 | 2022-05-12 | ||
metformin+Placebo | 夢窪壓繭觸築窪觸網鏇(網醖鏇壓衊積窪鹽廠夢) = 簾積餘製範廠簾網網構 願範衊醖範築獵鑰獵範 (鏇醖壓繭壓鏇窪鑰鹹網, -0.45 ~ -0.26) | ||||||
N/A | 2型糖尿病 追加 | 767 | 顧壓齋網蓋鏇艱鬱齋築(製範夢壓遞積膚壓醖襯) = 餘鹽醖壓蓋糧範淵遞憲 鏇繭艱顧築獵鬱淵夢艱 (醖鬱製齋築積齋壓鏇窪 ) | 积极 | 2021-06-01 | ||
Placebo | 顧壓齋網蓋鏇艱鬱齋築(製範夢壓遞積膚壓醖襯) = 艱製淵艱艱膚繭壓簾製 鏇繭艱顧築獵鬱淵夢艱 (醖鬱製齋築積齋壓鏇窪 ) | ||||||
N/A | 463 | Dorzagliatin 75 mg | 壓簾構積鹹鹹鹽獵糧簾(繭糧觸鏇願遞糧鹹獵廠) = 衊窪繭壓鏇鹹鑰膚艱夢 蓋淵窪獵糧蓋壓膚餘選 (淵鬱構鑰憲壓膚鹽積夢 ) 更多 | 积极 | 2021-06-01 | ||
Placebo | 膚憲網壓鬱鏇衊衊鹽壓(廠憲選壓繭積餘簾憲淵) = 鑰襯鏇壓積窪構淵築壓 網製夢願窪廠選艱廠鏇 (願願觸繭艱遞鹽顧襯顧 ) | ||||||
临床3期 | 463 | 憲齋鑰蓋觸壓遞蓋簾鏇(膚衊觸網觸糧壓鏇繭鬱) = 夢選淵窪膚鏇遞餘願選 膚餘糧顧繭艱窪鹹遞蓋 (醖餘範選網選顧鬱壓選 ) 更多 | 积极 | 2020-06-18 | |||
Placebo | 憲齋鑰蓋觸壓遞蓋簾鏇(膚衊觸網觸糧壓鏇繭鬱) = 膚範範艱簾觸廠顧繭壓 膚餘糧顧繭艱窪鹹遞蓋 (醖餘範選網選顧鬱壓選 ) 更多 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
提出任何生物医药研究问题
让每一步生物医药决策都精准制胜
基于十亿级生物数据与全球情报的精准 AI，赋能早期药物发现
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即接入生物医药数据包
智慧芽新药库数据也通过智慧芽开放平台，以MCP或API服务形式对外开放。立即使用我们的MCP服务定制您的LLM智能体。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用