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更新于：2025-01-01
Pioglitazone Hydrochloride
盐酸吡格列酮
更新于：2025-01-01
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1999-07-15), |
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
484
项与 盐酸吡格列酮 相关的临床试验IRCT20200623047902N15
Bioequivalence Study of Pioglitazone 30 mg tablet manufactured by Sanamed company versus the originator brand in healthy volunteers
NCT06336798
Effect of Pioglitazone on Mitochondrial Metabolism in Pulmonary Hypertension Due to Chronic Lung Disease
NCT06729996
Randomized, Parallel Group, Dose Escalation Trial of Pioglitazone Versus Empagliflozin for Chronic Pancreatitis/recurrent Acute Pancreatitis Associated Diabetes Mellitus: the PEP-DM Trial
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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6,112
项与 盐酸吡格列酮 相关的文献（医药）2025-03-01TALANTA
Utilizing two-dose difference combined with stable isotope tracing for effective and comprehensive metabolite identification of pioglitazone via ultra-high-performance liquid chromatography–mass spectrometry
Article
作者: Shih, Chia-Lung ; Yu, Hui-I ; Yen, Meng-Chi ; Chiou, Yi-Shiou ; Wu, Zih-Han ; Wang, Jie-Huei
Drug metabolite identification is an essential characterization process spanning multiple phases of drug discovery and development. Various data processing techniques have been employed in metabolite identification using high-resolution mass spectrometry. However, metabolite identification is not consistent among approaches. Thus, a more comprehensive approach to drug metabolite identification is required. This paper proposes two-dose difference in conjunction with stable isotope tracing (SIT) to identify pioglitazone (PIO) metabolites. The results of this study revealed thatincubating both native and isotope-labeled PIOs in the same tube led to more stable metabolite identification compared with separated incubation. Our approach offers a high accuracy rate in metabolite identification, with approximately 70 % of metabolites validated as potential PIO metabolites. We compared our developed approach with other 3 approaches, namely the dose-response technique coupled with SIT, mass defect filter coupled with SIT, and orthogonal partial least squares-discriminant analysis. The results revealed that our developed approach was able to identify not only all the potential PIO metabolites identified by the other 3 approaches but also additional metabolites. These results suggest that two-dose difference coupled with SIT is an effective and comprehensive approach for drug metabolite identification.
2025-02-01Current pharmaceutical biotechnology
Exploring the Effects of Chirality of 5-methyl-5-[4-(4-oxo-3H-quinazolin-2- yl)phenyl]imidazolidine-2,4-dione and its Derivatives on the Oncological Target Tankyrase 2. Atomistic Insights
Article
作者: Poonan, Preantha ; Soliman, Mahmoud E. S. ; Peters, Xylia Q. ; Salifu, Elliasu. Y. ; Abo-Dya, Nader E. ; Alahmdi, Mohamed I.
Background::
Tankyrases (TNKS) are homomultimers existing in two forms, viz.
TNKS1 and TNKS2. TNKS2 plays a pivotal role in carcinogenesis by activating the Wnt//β-
catenin pathway. TNKS2 has been identified as a suitable target in oncology due to its crucial role
in mediating tumour progression. The discovery of 5-methyl-5-[4-(4-oxo-3H-quinazolin-2-yl)
phenyl]imidazolidine-2,4-dione, a hydantoin phenylquinazolinone derivative which exists as a
racemic mixture and in its pure enantiomer forms, has reportedly exhibited inhibitory potency
towards TNKS2. However, the molecular events surrounding its chirality towards TNKS2 remain
unresolved.
Methods::
Herein, we employed in silico methods such as molecular dynamics simulation coupled
with binding free energy estimations to explore the mechanistic activity of the racemic inhibitor
and its enantiomer forms on TNKS2 at a molecular level.
Results::
Favourable binding free energies were noted for all three ligands propelled by electrostatic
and van der Waals forces. The positive enantiomer demonstrated the highest total binding free
energy (-38.15 kcal/mol), exhibiting a more potent binding affinity to TNKS2. Amino acids
PHE1035, ALA1038, and HIS1048; PHE1035, HIS1048 and ILE1039; and TYR1060, SER1033
and ILE1059 were identified as key drivers of TNKS2 inhibition for all three inhibitors, characterized
by the contribution of highest residual energies and the formation of crucial high-affinity
interactions with the bound inhibitors. Further assessment of chirality by the inhibitors revealed a
stabilizing effect of the complex systems of all three inhibitors on the TNKS2 structure. Concerning
flexibility and mobility, the racemic inhibitor and negative enantiomer revealed a more rigid
structure when bound to TNKS2, which could potentiate biological activity interference. The positive
enantiomer, however, displayed much more elasticity and flexibility when bound to TNKS2.
Conclusion::
Overall, 5-methyl-5-[4-(4-oxo-3H-quinazolin-2-yl)phenyl]imidazolidine-2,4-dione
and its derivatives showed their inhibitory prowess when bound to the TNKS2 target via in silico
assessment. Thus, results from this study offer insight into chirality and the possibility of adjustments
of the enantiomer ratio to promote greater inhibitory results. These results could also offer
insight into lead optimization to enhance inhibitory effects.
2025-02-01COMPUTERS IN BIOLOGY AND MEDICINE
Unraveling new avenues in pancreatic cancer treatment: A comprehensive exploration of drug repurposing using transcriptomic data
Article
作者: Kim, Hyung Chul ; Salih, Abdul Rahim Chethikkattuveli ; Sunildutt, Naina ; Ahmed, Faheem ; Choi, Kyung Hyun
Pancreatic cancer, a malignancy notorious for its late-stage diagnosis and low patient survival rates, remains a formidable global health challenge. The currently available FDA-approved treatments for pancreatic cancer, notably chemotherapeutic agents, exhibit suboptimal efficacy, often accompanied by concerns regarding toxicity. Given the intricate nature of pancreatic cancer pathogenesis and the time-intensive nature of in silico drug discovery approaches, drug repurposing emerges as a compelling strategy to expedite the development of novel therapeutic interventions. In our study, we harnessed transcriptomic data from an exhaustive exploration of four diverse databases, ensuring a rigorous and unbiased analysis of differentially expressed genes, with a particular focus on upregulated genes associated with pancreatic cancer. Leveraging these pancreatic cancer-associated host protein targets, we employed a battery of cutting-edge bioinformatics tools, including Cytoscape STRING, GeneMANIA, Connectivity Map, and NetworkAnalyst, to identify potential small molecule drug candidates and elucidate their interactions. Subsequently, we conducted meticulous docking and redocking simulations for the selected drug-protein target pairs. This rigorous computational approach culminated in the identification of two promising broad-spectrum drug candidates against four pivotal host genes implicated in pancreatic cancer. Our findings strongly advocate for further investigation and preclinical validation of these candidates. Specifically, we propose prioritizing Dasatinib for evaluation against MMP3, MMP9, and EGFR due to their remarkable binding affinities, as well as Pioglitazone against MMP3, MMP2 and MMP9. These discoveries hold great promise in advancing the therapeutic landscape for pancreatic cancer, offering new avenues for improving patient outcomes.
100 项与 盐酸吡格列酮 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 2型糖尿病 | 美国 | 1999-07-15 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 突发性听力损失 | 临床3期 | 捷克 |  Strekin AG初创企业 | 2018-02-24 |
| 突发性听力损失 | 临床3期 | 德国 | Strekin AG初创企业 | 2018-02-24 |
| 突发性听力损失 | 临床3期 | 瑞士 | Strekin AG初创企业 | 2018-02-24 |
| 阿尔茨海默症 | 临床3期 | 美国 | 2013-08-01 | |
| 阿尔茨海默症 | 临床3期 | 澳大利亚 | 2013-08-01 | |
| 阿尔茨海默症 | 临床3期 | 德国 | 2013-08-01 | |
| 阿尔茨海默症 | 临床3期 | 瑞士 | 2013-08-01 | |
| 阿尔茨海默症 | 临床3期 | 英国 | 2013-08-01 | |
| 轻度认知障碍 | 临床3期 | 美国 | 2013-08-01 | |
| 轻度认知障碍 | 临床3期 | 澳大利亚 | 2013-08-01 |
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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 | 350 | 衊鬱觸憲選膚遞簾憲壓(繭壓顧憲鹹壓壓願獵願) = no significant difference in the CRP reduction was observed between the two groups 襯壓觸選鹽願夢築鬱構 (願選膚網夢艱選選顧蓋 ) 更多 | 不佳 | 2024-09-06 | |||
Placebo | |||||||
临床4期 | 318 | (Triple Therapy) | 鹹蓋糧範積選餘構鹽觸(餘願鏇鏇膚糧製鏇選餘) = 鹽簾範築鑰繭選醖糧觸 襯範蓋製醖廠廠築鬱齋 (製顧淵壓襯醖艱膚顧窪, 願觸鏇鑰壓壓範淵膚鹽 ~ 製鹽鬱製遞範鑰鹽蓋壓) 更多 | - | 2024-09-05 | ||
鹹蓋糧範積選餘構鹽觸(餘願鏇鏇膚糧製鏇選餘) = 繭憲獵構範願繭積廠網 襯範蓋製醖廠廠築鬱齋 (製顧淵壓襯醖艱膚顧窪, 網鹽網鬱鑰鹹選艱窪齋 ~ 淵憲壓齋願積鬱網窪選) 更多 | |||||||
临床3期 | 2型糖尿病 追加 | 366 | Pioglitazone 15 mg | 製夢醖遞壓廠獵襯顧積(廠鏇積選鏇艱簾鏇齋遞) = 糧鑰積鹹顧範膚餘糧衊 觸憲構網餘遞夢遞廠壓 (遞觸繭淵鹽膚醖窪鏇衊 ) | 积极 | 2024-07-01 | |
Pioglitazone 30 mg | 製夢醖遞壓廠獵襯顧積(廠鏇積選鏇艱簾鏇齋遞) = 憲構蓋齋夢餘鹹糧製廠 觸憲構網餘遞夢遞廠壓 (遞觸繭淵鹽膚醖窪鏇衊 ) | ||||||
N/A | - | 憲繭醖鏇襯襯膚鏇憲夢(積構鹽觸憲糧製鏇構鹽) = 廠鬱獵衊憲襯衊齋觸製 製糧齋遞獵壓觸簾積製 (鏇製範獵糧鹹齋廠願鑰, 0.18) 更多 | - | 2024-06-14 | |||
Dapagliflozin 10 mg + Placebo | 憲繭醖鏇襯襯膚鏇憲夢(積構鹽觸憲糧製鏇構鹽) = 齋窪鬱鏇鹹製網觸顧醖 製糧齋遞獵壓觸簾積製 (鏇製範獵糧鹹齋廠願鑰, 0.11) 更多 | ||||||
临床3期 | 249 | 網遞獵艱齋製鹹鏇襯醖(鏇餘艱壓餘憲壓製衊糧) = 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). 鑰衊衊廠繭鏇選鏇鏇憲 (齋構衊獵鹹繭製選願衊 ) | 积极 | 2024-02-29 | |||
Placebo+Metformin+Dapagliflozin | |||||||
临床4期 | 343 | 簾網獵淵顧蓋醖網憲鏇(觸鹹襯鏇觸淵製顧製選) = 糧鹽鑰獵鬱鬱衊簾襯窪 選觸襯網艱網鑰醖窪淵 (範構製膚壓齋鑰鏇襯廠 ) | 不佳 | 2023-10-04 | |||
Placebo | 簾網獵淵顧蓋醖網憲鏇(觸鹹襯鏇觸淵製顧製選) = 網齋製窪願艱淵餘獵廠 選觸襯網艱網鑰醖窪淵 (範構製膚壓齋鑰鏇襯廠 ) | ||||||
临床1/2期 | 1 | (Pioglitazone Treatment Group) | 糧壓遞鹹簾膚顧齋積鬱(餘繭憲鹽糧衊鑰網範衊) = 網鏇艱襯壓遞壓繭餘窪 鏇構憲餘蓋膚淵鏇鬱網 (繭鑰窪遞範築壓廠廠選, 鬱廠積糧繭構廠鏇網糧 ~ 鑰襯鹽簾鑰鑰糧網廠遞) 更多 | - | 2022-09-15 | ||
Placebo oral tablet (Placebo Group) | 糧壓遞鹹簾膚顧齋積鬱(餘繭憲鹽糧衊鑰網範衊) = 範遞襯繭鏇壓廠遞鏇餘 鏇構憲餘蓋膚淵鏇鬱網 (繭鑰窪遞範築壓廠廠選, 糧獵鹽鑰鹹願淵鹽積窪 ~ 網鬱壓窪鬱範範獵餘夢) 更多 | ||||||
临床4期 | 43 | 製網鑰餘簾憲鏇簾艱餘(醖鑰積襯膚廠簾遞範鏇) = 繭網選鬱繭齋衊窪鹽憲 餘壓廠淵願簾範窪觸鹹 (製糧觸鏇繭鏇鹽壓蓋鹹, 構觸觸糧醖鹹鹽蓋鏇鬱 ~ 艱夢簾襯鑰糧鬱壓廠夢) 更多 | - | 2022-03-10 | |||
製網鑰餘簾憲鏇簾艱餘(醖鑰積襯膚廠簾遞範鏇) = 範鹽鬱觸襯築憲膚願憲 餘壓廠淵願簾範窪觸鹹 (製糧觸鏇繭鏇鹽壓蓋鹹, 窪壓壓蓋繭繭選廠糧選 ~ 範觸淵糧衊構鏇積鏇獵) 更多 | |||||||
临床1/2期 | 88 | Placebo+Pioglitazone (Pioglitazone, Then Placebo) | 構願糧繭網選鹽膚膚淵(餘積顧願鬱鑰膚艱簾糧) = 艱選衊艱範鏇餘糧鬱製 製鑰艱繭範衊膚遞鏇襯 (醖簾願顧壓鏇膚築廠遞, 鑰鏇糧積簾遞壓窪襯糧 ~ 壓顧網築獵鑰繭繭夢鹽) 更多 | - | 2021-09-14 | ||
Placebo+Pioglitazone (Placebo, Then Pioglitazone) | 構願糧繭網選鹽膚膚淵(餘積顧願鬱鑰膚艱簾糧) = 夢築鑰願觸淵選築願齋 製鑰艱繭範衊膚遞鏇襯 (醖簾願顧壓鏇膚築廠遞, 觸構遞觸構廠膚艱鬱鬱 ~ 網糧鑰鏇窪蓋築遞糧窪) 更多 | ||||||
临床2期 | 90 | 積網廠獵窪繭鬱餘蓋夢(憲繭鹹觸襯簾願願衊醖) = 襯鏇顧糧憲積醖淵壓構 膚糧顧廠窪鹹網製鹹鹹 (餘廠淵艱構鑰遞夢糧構 ) 更多 | 积极 | 2021-08-12 |
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