更新于：2024-12-17
Topiroxostat
托匹司他
更新于：2024-12-17
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构
分子式C13H8N6 |
InChIKeyUBVZQGOVTLIHLH-UHFFFAOYSA-N |
CAS号577778-58-6 |
关联
55
项与 托匹司他 相关的临床试验一项评估托吡司特片治疗痛风伴高尿酸血症的多中心、随机、双盲、双模拟、阳性药平行对照的Ⅱ期临床研究
托吡司特片在中国健康受试者中进行的单中心、随机、开放、单次（空腹/餐后）口服给药、两制剂、两序列、四周期重复交叉的人体生物等效性试验
托匹司他片人体生物等效性研究（餐后）
100 项与 托匹司他 相关的临床结果
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100 项与 托匹司他 相关的转化医学
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100 项与 托匹司他 相关的专利（医药）
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411
项与 托匹司他 相关的文献（医药）2025-01-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Design, synthesis, and evaluation of 4-(4-methyl-4H-1,2,4-triazol-3-yl)piperidine derivatives as potential glutaminyl cyclase isoenzyme inhibitors for the treatment of cancer
Article
作者: He, Pan ; Wang, Zhuoran ; Zhou, Qingqing ; Qin, Feixia ; Xiong, Wei ; Gao, Ying ; Zhu, Fangyi ; Wu, Haiqiang ; Wu, Zhenxin ; Li, Chenyang
Upregulated glutaminyl cyclase isoenzyme (isoQC) contributes to cancer development by catalyzing pE-CD47 generation and thus enhancing CD47-SIRPα binding and subsequent "don't eat me" signals. We thus consider that isoQC could represent a novel target for cancer therapy. We previously prepared a series of diphenyl conjugated imidazole derivatives (DPCIs) and evaluated their use as glutaminyl cyclase (QC) inhibitors. Here, a new series of DPCIs was rationally designed and synthesized. As anticipated, the analogues exhibited considerably improved inhibitory potency against both QC and isoQC. Crucially, these chemicals exhibited marked selectivity toward isoQC. Further assessments established that one selected compound (27) did not affect the viability of A549, H1299, PC9, or HEK293T cells or the body weight of mice. This compound did, however, reduce pE-CD47 levels in infected A549 cells (isoQC_OE and isoQC_KD) and exhibited apparent anti-cancer effects in vivo by downregulating the level of pE-CD47 via the inhibition of isoQC activity. Taken together, these findings indicated that the compounds synthesized in this study could represent potential QC/isoQC inhibitors for the treatment of cancers.
2025-01-01JOURNAL OF INORGANIC BIOCHEMISTRY
Anticancer dinuclear Ir(III) complex activates Nrf2 and interferes with NAD(H) in cancer cells
Article
作者: Řezníčková, Eva ; Bárta, Ondřej ; Štarha, Pavel ; Milde, David ; Kryštof, Vladimír
Dinuclear complex [Ir2(μ-L1)(η5-Cp*)2Cl2](PF6)2 (1) exhibits low micromolar cytotoxic activity in vitro in various human cancer cells (GI50 = 1.7-3.0 μM) and outperformed its mononuclear analogue [Ir(η5-Cp*)Cl(L2)]PF6 (2; GI50 > 40.0 μM); Cp* = pentamethylcyclopentadienyl, L1 = 4-chloro-2,6-bis[5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl]pyridine, L2 = 5-(pyridin-2-yl)-1,3,4-thiadiazol-2-amine. Compound 1 upregulated the Keap1/Nrf2 oxidative stress-protective pathway in the treated MV4-11 acute myeloid leukemia cells. In connection with the redox-mediated mode of action of 1, its NADH-oxidizing activity was detected in solution (1H NMR), while NAD+ remained intact (with formate as a hydride source). Surprisingly, only negligible NADH oxidation was detected in the presence of the reduced glutathione and ascorbate. Following the results of in-solution experiments, NAD(H) concentration was assessed in 1-treated MV4-11 cancer cells. Besides the intracellular NADH oxidation in the presence of 1, the induced oxidative stress also led to a decrease of NAD+, resulting in depletion of both NAD+/NADH coenzymes. The discussed findings provide new insight into the biochemical effects of catalytic anticancer compounds that induce cell death via a redox-mediated mode of action.
2024-12-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Molecular descriptors and in silico studies of 4-((5-(decylthio)-4-methyl-4n-1,2,4-triazol-3-yl)methyl)morpholine as a potential drug for the treatment of fungal pathologies
Article
作者: Gutyj, Bogdan ; Myroslava, Ohloblina ; Tüzün, Burak ; Parchenko, Volodymyr ; Poustforoosh, Alireza ; Inna, Bushuieva
The article explores the polypharmacological profiling of 4-((5-(decylthio)-4-methyl-4H-1,2,4-triazole-3-yl)methyl)morpholine as a potential antimicrobial agent. The study utilized 15148 electronic pharmacophore models of organisms, ranked by the Tversky index. Detailed analysis revealed classical bonding patterns with selected enzymes, identifying key amino acid residues involved in complex formation. Protein target prediction was conducted through various stages using the Galaxy web service, including ligand structure creation, pharmacophore alignment, and target ranking. The activities of the molecules against 1G6C, 2W6O, 3G7F, 3OWU, 4IVR, and 4TZT proteins were compared. Docking studies with PyMOL and Discovery Studio Visualizer revealed binding to thymidine kinase, thiamine phosphate synthase, and biotin carboxylase with promising binding affinities. These interactions suggest potential antibacterial and antiviral effects, warranting further virtual screening and in-depth studies for the development of effective antimicrobial drugs. Calculations of the molecules were made with the gaussian package program. Calculations were made on the 6-31++g** basis set at B3LYP, HF, and M062X levels with Gaussian software. Afterwards, the 0-100 ns interaction of the molecule with the highest activity was examined.
100 项与 托匹司他 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 |
|---|---|---|---|
| 痛风 | 日本 | 2013-06-28 | |
| 痛风 | 日本 | 2013-06-28 | |
| 痛风 | 日本 | 2013-06-28 | |
| 高尿酸血症 | 日本 | 2013-06-28 | |
| 高尿酸血症 | 日本 | 2013-06-28 | |
| 高尿酸血症 | 日本 | 2013-06-28 |
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 |
|---|---|---|---|---|
| 糖尿病肾病 | 临床2期 | 日本 | 2014-12-30 | |
| 糖尿病肾病 | 临床2期 | 日本 | 2014-12-30 |
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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
N/A | 慢性肾病 serum urate levels | urinary albumin excretion | - | 壓糧製襯範鏇鏇鏇鬱蓋(簾糧鹹繭憲淵築憲鏇襯) = 窪淵鑰衊窪鹽鏇觸夢餘 鏇衊獵艱願鏇鑰鑰網齋 (獵鬱鬱夢範齋獵襯範壓 ) | 积极 | 2015-05-21 | ||
Placebo | 壓糧製襯範鏇鏇鏇鬱蓋(簾糧鹹繭憲淵築憲鏇襯) = 繭夢艱積衊廠繭網齋網 鏇衊獵艱願鏇鑰鑰網齋 (獵鬱鬱夢範齋獵襯範壓 ) |
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