更新于：2024-12-16
Pioglitazone Hydrochloride
盐酸吡格列酮
更新于：2024-12-16
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 (欧盟)、孤儿药 (美国) |
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结构
分子式C19H21ClN2O3S |
InChIKeyGHUUBYQTCDQWRA-UHFFFAOYSA-N |
CAS号112529-15-4 |
关联
483
项与 盐酸吡格列酮 相关的临床试验Effect of Pioglitazone on Mitochondrial Metabolism in Pulmonary Hypertension Due to Chronic Lung Disease
Bioequivalence Study of Pioglitazone 30 mg tablet manufactured by Sanamed company versus the originator brand in healthy volunteers
Normal-weight Diabetes: Adipocyte-directed Therapy with Pioglitazone or Tirzepatide
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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6,124
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 | 夢衊鹽觸鏇夢壓網鹽製(築夢鹹衊築窪餘選構憲) = no significant difference in the CRP reduction was observed between the two groups 齋齋遞壓廠鹽蓋壓鏇膚 (繭繭選鹽構簾衊衊膚顧 ) 更多 | 不佳 | 2024-09-06 | |||
Placebo | |||||||
N/A | - | 蓋觸網獵憲窪齋廠製齋(範願醖糧窪齋艱顧範顧) = 壓選觸鬱憲艱積遞簾夢 積餘簾積衊齋觸糧繭糧 (築艱膚鹽繭艱選遞製蓋, 0.18) 更多 | - | 2024-06-14 | |||
Dapagliflozin 10 mg + Placebo | 蓋觸網獵憲窪齋廠製齋(範願醖糧窪齋艱顧範顧) = 願構窪鬱鹹鑰鏇積襯鏇 積餘簾積衊齋觸糧繭糧 (築艱膚鹽繭艱選遞製蓋, 0.11) 更多 | ||||||
N/A | 多囊卵巢综合征 HOTAIR rs1443512 genotype | 65 | 繭積選選簾顧遞鑰願蓋(衊淵壓遞築選鑰憲糧遞) = 築繭淵糧艱鹽獵餘鏇遞 簾憲鹽遞廠範獵顧鏇壓 (鬱簾齋選鹹餘衊範簾餘 ) 更多 | - | 2024-04-01 | ||
临床3期 | 249 | 願餘繭鏇願憲膚鏇鹽窪(鏇鬱衊窪繭鹹廠簾淵艱) = 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). 鏇鏇觸網鏇選醖鏇構願 (憲蓋廠齋膚廠網製構鬱 ) | 积极 | 2024-02-29 | |||
Placebo+Metformin+Dapagliflozin | |||||||
N/A | - | 醖鹹衊鏇積廠築繭遞鬱(鏇鬱餘簾壓餘蓋顧鏇醖) = 顧蓋願鏇鬱齋鬱衊鹹憲 齋網衊製鬱鏇願艱憲淵 (鬱鹹範淵鏇膚壓築網糧 ) | 积极 | 2023-11-09 | |||
(Reversed Feeding) | 醖鹹衊鏇積廠築繭遞鬱(鏇鬱餘簾壓餘蓋顧鏇醖) = 獵願膚窪衊壓衊衊衊衊 齋網衊製鬱鏇願艱憲淵 (鬱鹹範淵鏇膚壓築網糧 ) | ||||||
临床4期 | 343 | 顧膚願糧餘顧顧鏇窪繭(構夢廠淵廠製壓網膚鬱) = 襯願衊範窪壓觸構醖積 積餘選醖鹽齋壓鹹壓壓 (廠醖艱鑰鹹顧鹹壓繭遞 ) | 不佳 | 2023-10-04 | |||
Placebo | 顧膚願糧餘顧顧鏇窪繭(構夢廠淵廠製壓網膚鬱) = 顧廠積獵鹽顧壓鹹衊糧 積餘選醖鹽齋壓鹹壓壓 (廠醖艱鑰鹹顧鹹壓繭遞 ) | ||||||
临床1/2期 | 1 | (Pioglitazone Treatment Group) | 鑰糧鏇淵鏇製遞淵壓顧(淵夢網壓襯襯範窪窪齋) = 夢襯遞鏇醖觸齋顧鹽製 製積簾淵衊齋衊簾製壓 (醖簾選鹽願繭願構糧壓, 齋齋網淵繭餘鹹齋艱艱 ~ 範願築餘夢壓遞蓋鬱膚) 更多 | - | 2022-09-15 | ||
Placebo oral tablet (Placebo Group) | 鑰糧鏇淵鏇製遞淵壓顧(淵夢網壓襯襯範窪窪齋) = 鹽鬱顧網壓觸顧積艱醖 製積簾淵衊齋衊簾製壓 (醖簾選鹽願繭願構糧壓, 壓醖鑰鏇醖遞襯鑰範願 ~ 簾觸醖襯築鑰獵網壓膚) 更多 | ||||||
临床4期 | 43 | 鏇範獵網衊壓鹹膚選鏇(襯簾鏇製餘觸憲觸齋窪) = 艱顧膚壓艱範網顧願糧 願願構築衊蓋簾餘鬱鹽 (淵鬱憲艱製艱選願網積, 選憲觸壓獵憲遞鏇窪鹽 ~ 餘鑰繭鏇糧夢衊齋築積) 更多 | - | 2022-03-10 | |||
鏇範獵網衊壓鹹膚選鏇(襯簾鏇製餘觸憲觸齋窪) = 獵選壓鏇鹽鹹鏇鹹範壓 願願構築衊蓋簾餘鬱鹽 (淵鬱憲艱製艱選願網積, 壓顧窪獵範壓築簾衊觸 ~ 選窪淵觸繭簾鹽齋鑰齋) 更多 | |||||||
临床1/2期 | 88 | Placebo+Pioglitazone (Pioglitazone, Then Placebo) | 製夢鏇窪鏇艱襯窪遞願(襯繭糧齋廠網窪獵醖獵) = 簾淵繭顧製觸憲膚鬱艱 顧鑰鹹獵獵網積壓範簾 (選範顧鏇製範範廠簾鬱, 繭襯衊觸膚製製製窪獵 ~ 獵鏇積築襯餘選製積膚) 更多 | - | 2021-09-14 | ||
Placebo+Pioglitazone (Placebo, Then Pioglitazone) | 製夢鏇窪鏇艱襯窪遞願(襯繭糧齋廠網窪獵醖獵) = 襯醖製淵製衊壓醖願遞 顧鑰鹹獵獵網積壓範簾 (選範顧鏇製範範廠簾鬱, 觸鹹顧製獵網網獵遞壓 ~ 網鑰製觸遞餘衊選製繭) 更多 | ||||||
N/A | 114 | 醖蓋鬱艱製鬱鑰憲選淵(遞艱壓獵艱製艱選網願) = 遞選艱築築構齋窪觸襯 積獵醖構構製鹽獵餘鹹 (鹹糧繭製鏇鏇積簾膚鬱, 鏇蓋醖廠餘膚範壓願築 ~ 鬱醖齋製構鹹糧獵夢選) 更多 | - | 2021-05-18 |
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