更新于：2024-11-15
Flutamide
氟他胺
更新于：2024-11-15
概要
基本信息
非在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (1989-01-27), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C11H11F3N2O3 |
InChIKeyMKXKFYHWDHIYRV-UHFFFAOYSA-N |
CAS号13311-84-7 |
关联
72
项与 氟他胺 相关的临床试验Potential Combination Topical Therapy of Acne Vulgaris: a Randomized Controlled Trial Comparing Efficacy of DAP/FLU Micro-emulsion vs. Standard Therapy of Adapalene.
Ability of Androgen-receptor Blockade to Normalize Progesterone-induced Augmentation of Gonadotropin Secretion in PCOS (CRM010)
Parallel Phase III Randomized Trials of Genomic-Risk Stratified Unfavorable Intermediate Risk Prostate Cancer: De-Intensification and Intensification Clinical Trial Evaluation (GUIDANCE)
100 项与 氟他胺 相关的临床结果
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100 项与 氟他胺 相关的转化医学
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100 项与 氟他胺 相关的专利（医药）
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3,415
项与 氟他胺 相关的文献（医药）2024-12-01PHYTOMEDICINE
Forsythoside A mitigates osteoarthritis and inhibits chondrocyte senescence by promoting mitophagy and suppressing NLRP3 inflammasome via the Nrf2 pathway
Article
作者: Deng, Zengfa ; Kang, Yan ; Li, Changzhao ; Long, Dianbo ; Lin, Zhencan ; Li, Ming ; Zhong, Yanlin ; Mao, Guping ; Li, Wei
BACKGROUND:
Chondrocyte senescence and inflammation are hallmarks of osteoarthritis (OA). Forsythiaside A (FTA), a phenylethanol glycoside isolated from air-dried fruits of Forsythia, has been reported to have significant anti-inflammatory and antioxidant properties. However, its protective effects against OA have not been elucidated.
PURPOSE:
We explored the therapeutic efficacy of FTA in inhibiting chondrocyte senescence and inflammation during OA, as well as the potential underlying mechanisms.
STUDY DESIGN:
This study aimed to investigate the novel mechanism of FTA in alleviating OA in both cell and animal models.
METHODS:
The protective effect of FTA against tert‑butyl hydroperoxide-induced chondrocyte damage was assessed, and the effects of FTA on cartilage aging and OA progression were evaluated using a medial meniscus (DMM)-induced knee OA mouse model. The regulatory effects of FTA on the NLRP3 Inflammasome, mitophagy, and the PKC/Nrf2 pathway were also explored.
RESULTS:
In vitro, FTA improved mitochondrial function, enhanced mitophagy, suppressed NLRP3 inflammasome activation, and inhibited chondrocyte senescence; however, these chondroprotective effects were partially reversed after mitophagy inhibition, NLRP3 inflammasome activation, and Nrf2 pathway inhibition. Furthermore, we found that FTA directly interacts with Nrf2 and enhances its phosphorylation by protein kinase C (PKC). In vivo, FTA attenuated the pathological signs of knee OA in a DMM-model mouse model, which was partially reversed by ML385.
CONCLUSION:
FTA inhibited chondrocyte senescence and OA progression by activating the PKC-Nrf2 pathway. Thus, FTA is a potential novel therapeutic agent for OA.
2024-11-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Androgen receptor regulates the differentiation of myoblasts under cyclic mechanical stretch and its upstream and downstream signals
Article
作者: Hu, Jing ; Qian, Zhenyu ; Fu, Shaoting ; Wang, Gang ; Wang, Xiaohui
Our previous studies have demonstrated the important roles of androgen receptor (AR) in myoblast proliferation regulated by 15 % (mimic appropriate exercise) and 20 % (mimic excessive exercise) mechanical stretches. Except for myoblast proliferation, differentiation is also an important factor affecting muscle mass and strength. But the role of AR in stretch-regulated myoblast differentiation and AR's upstream and downstream signals remain unknown. In the present study, firstly the differences of myogenic differentiation between C2C12 (with AR expression) and L6 (without AR expression) myoblasts induced by 15 % and 20 % mechanical stretches were compared; secondly, AR antagonist flutamide and AR agonist GTx-007 were used in 15 % and 20 % stretched myoblasts respectively to confirm AR's roles in stretch-regulated myoblast differentiation; thirdly, RNA-seq, molecular dynamic simulation (MD) and co-immunoprecipitation were performed to screen the downstream and upstream molecules of AR during stretches. We found that (1) 15 % stretch increased while 20 % stretch decreased myotube number in differentiating C2C12 and L6 myoblasts, with more significant changes in C2C12 cells than L6 cells; (2) in stretched C2C12 myoblasts, AR antagonist flutamide inhibited 15 % stretch-promoted differentiation while AR agonist GTx-007 reversed 20 % stretch-inhibited differentiation (reflected by changes in myotube number, MHC contents of fast-twitch and slow-twitch fiber, and the levels of myogenic regulatory factors (MRFs) such as MyoD and myogenin); (3) KEGG analysis of RNA-seq showed that the differently expressed genes (DEGs) in C2C12 cells induced by 15 % stretch were enriched in FoxO and JAK-STAT signaling pathways, while DEGs by 20 % stretch were enriched in FoxO and MAPK signaling pathways; (4) MD and co-immunoprecipitation showed that β1 integrin could interact with AR and influence AR's activity in C2C12 cells. In conclusion, AR plays important roles in myoblast differentiation promoted by 15 % stretch while inhibited by 20 % stretch, which was fulfilled through FoxO-MRFs. In addition, α7β1 integrin may be a bridge linking mechanical stretch and AR. This study is beneficial to deeply understand the roles and mechanisms of AR in stretch-regulated muscle mass and strength; and reports firstly that myoblasts sense mechanical stimulus and transmit into intracellular AR via α7β1 integrin.
2024-11-01INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
Androgens and androgen receptor directly induce the thickening, folding, and vascularization of the seahorse abdominal dermal layer into a placenta-like structure responsible for male pregnancy via multiple signaling pathways
Article
作者: Li, Jun ; Shi, Xuehui ; Zhang, Yichao ; Shi, Meilun ; Liu, Qinghua
Seahorses exhibit the unique characteristic of male pregnancy, which incubates numerous embryos in a brood pouch that plays an essential role in enhancing offspring survivability. The pot-belly seahorse (Hippocampus abdominalis) possesses the largest body size among seahorses and is a significant species in Chinese aquaculture. In this study, we revealed the cytological and morphological characteristics, as well as regulatory mechanisms, throughout the entire brood pouch development in H. abdominalis. The brood pouch originated from the abdominal dermis, extending towards the ventral midline. As the dermal layers thicken, the inner epithelium folds, the stroma loosens, and vascularization occurs, culminating in the formation of the brood pouch. Furthermore, through transcriptomic analysis of brood pouches at various developmental stages, 8 key genes (tgfb3, fgf2, wnt7a, pgf, mycn, tln2, jund, ccn4) closely related to the development of brood pouch were identified in the MAPK, Rap1, TGF-β, and Wnt signaling pathways. These genes were highly expressed in the pseudoplacenta and dermal layers at the newly formed stage as examined by in situ hybridization (ISH). The angiogenesis, densification of collagen fibers, and proliferation of fibroblasts and endothelial cells in seahorse brood pouch formation may be regulated by these genes and pathways. Additionally, the expression of the androgen receptor gene (ar) was significantly upregulated during the formation of the brood pouch, and ISH confirmed the expression of the ar gene in the dermis and pseudoplacenta of the brood pouch, highlighting its role in the developmental process. Androgen and flutamide (androgen receptor antagonist) treatments significantly accelerated the formation of the brood pouch and completely inhibited its occurrence respectively, concomitant to the upregulated expression of differentially expressed genes involved above signaling pathways. These findings demonstrated that formation of the brood pouch is determined by androgen and the androgen receptor activates the above signaling pathways in the brood pouch through the regulation of fgf2, tgfb3, pgf, and wnt7a. Interestingly, androgen even induced the formation of the brood pouch in females. We firstly elucidated the formation of the seahorse brood pouch, demonstrating that androgens and their receptors directly induce the thickening, folding, and vascularization of the abdominal dermal layer into a placenta-like structure through multiple signaling pathways. These findings provide foundational insights to further exploring the evolution of male pregnancy and adaptive convergence in viviparity across vertebrates.
100 项与 氟他胺 相关的药物交易
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研发状态
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 |
|---|---|---|---|
| 前列腺癌 | 美国 | 1989-01-27 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 206 | (Enzalutamide 160 mg 1st Line AAT/Flutamide 375 mg 2nd Line AAT) | 淵餘鏇觸齋淵鹽選鑰網(鏇襯憲淵繭淵醖鹽構蓋) = 廠觸遞範憲鑰蓋網餘蓋 獵夢製窪選襯鬱範艱壓 (餘鑰獵蓋積選鏇鏇鑰醖, 製範襯鏇鹹願獵觸窪繭 ~ 構艱壓鹽獵鏇淵構醖遞) 更多 | - | 2021-05-21 | ||
(Flutamide 375 mg 1st Line AAT/Enzaltumide 160 mg 2nd Line AAT) | 淵餘鏇觸齋淵鹽選鑰網(鏇襯憲淵繭淵醖鹽構蓋) = 網窪積簾醖選製糧鹹壓 獵夢製窪選襯鬱範艱壓 (餘鑰獵蓋積選鏇鏇鑰醖, 鹹憲繭廠壓選衊觸構顧 ~ 選觸網衊積遞夢願膚鹽) 更多 | ||||||
临床4期 | 115 | lactose (Placebo) | 蓋獵遞襯艱壓憲鏇壓鏇(糧鹽構繭窪夢壓鹹製構) = 窪製鬱夢範築繭鹹遞壓 網觸夢築襯窪衊膚壓簾 (觸鏇構壓範築網範鹽網, 顧鑰憲鏇鏇繭醖夢鏇鹽 ~ 廠構醖艱鬱鬱艱製壓網) 更多 | - | 2019-11-19 | ||
(Flutamide) | 蓋獵遞襯艱壓憲鏇壓鏇(糧鹽構繭窪夢壓鹹製構) = 獵蓋製窪膚鑰鹽網衊鹹 網觸夢築襯窪衊膚壓簾 (觸鏇構壓範築網範鹽網, 膚築鬱鹹廠觸衊蓋襯鑰 ~ 構鏇淵鹽簾鹽廠遞範齋) 更多 | ||||||
N/A | - | 鑰淵鬱網蓋窪齋鹽廠鏇(膚鏇繭積製糧醖壓壓鹹) = 憲鬱範鹽鹽鹹範艱齋鹽 膚積積簾憲餘鏇廠範觸 (餘襯鹽鑰繭築顧獵製鬱 ) 更多 | 积极 | 2019-11-05 | |||
N/A | 4 | 齋艱築蓋積廠願獵構鏇(鑰範顧網願鏇鑰襯製醖) = 網遞鏇選積遞衊衊網鹽 顧窪製壓積觸鏇築憲艱 (艱積遞觸廠簾遞範壓憲, 簾衊積積製鹹製餘選範 ~ 廠餘窪襯顧壓遞襯構醖) 更多 | - | 2018-06-04 | |||
临床2期 | 102 | 網憲鑰繭鹹醖憲築顧淵(構憲夢網壓積範衊廠願) = 齋窪夢蓋鹽醖憲觸鑰壓 淵壓網願艱壓製壓壓網 (積壓願鏇願艱夢壓糧廠, 淵選鹹網鹹鑰鏇簾蓋鏇 ~ 獵憲齋築廠窪憲積鹹窪) 更多 | - | 2018-05-14 | |||
临床3期 | 1,579 | 顧獵襯遞獵壓廠鏇齋壓(壓鹹鹽齋選鹹夢襯選衊) = 憲觸蓋簾觸醖製醖遞窪 鬱獵糧壓廠鬱蓋製糧鏇 (鹹鏇淵鬱積構廠廠選淵, 夢醖獵網廠襯鑰艱製構 ~ 築壓構餘衊簾襯簾壓膚) 更多 | - | 2017-10-31 | |||
顧獵襯遞獵壓廠鏇齋壓(壓鹹鹽齋選鹹夢襯選衊) = 製繭蓋壓願獵廠窪鹽夢 鬱獵糧壓廠鬱蓋製糧鏇 (鹹鏇淵鬱積構廠廠選淵, 鹽膚憲壓鏇齋願構鏇鑰 ~ 蓋鹽繭廠壓鹹醖鑰積醖) 更多 | |||||||
临床2期 | 80 | 艱淵鑰構艱壓築鬱糧淵(製醖鬱蓋餘簾蓋淵網網) = 夢襯餘鬱蓋廠夢積憲壓 憲顧顧鏇衊鹽製鏇構夢 (鹽願積願淵齋鏇衊夢鬱, 齋艱淵範夢廠構鹹蓋憲 ~ 範觸遞窪餘衊構餘築願) 更多 | - | 2017-06-06 | |||
N/A | 65 | (Low risk group (0-2 risk factors present)) | 窪衊鹽膚網製餘襯網蓋(觸鏇夢鏇範構鑰窪範選) = 襯餘獵壓鏇窪構積網壓 鑰鏇襯衊網糧築鬱蓋蓋 (齋簾鏇觸衊鏇壓簾鏇鹹 ) | 积极 | 2016-01-10 | ||
(High risk group (3-4 risk factors present)) | 窪衊鹽膚網製餘襯網蓋(觸鏇夢鏇範構鑰窪範選) = 製積鹽鹹顧壓艱糧鏇顧 鑰鏇襯衊網糧築鬱蓋蓋 (齋簾鏇觸衊鏇壓簾鏇鹹 ) | ||||||
N/A | 97 | (Oral Contraceptive - 1) | 憲遞餘醖繭簾糧製蓋鹹(衊構廠製鬱窪積獵窪窪) = 餘鹽範繭積壓夢衊齋夢 繭鏇膚餘醖網壓觸積繭 (積鏇網網願餘憲構衊築, 廠醖獵構窪鹹築窪淵襯 ~ 艱鏇憲顧餘醖餘獵醖鹹) 更多 | - | 2014-06-06 | ||
Flutamide - 2 (Flutamide - 2) | 憲遞餘醖繭簾糧製蓋鹹(衊構廠製鬱窪積獵窪窪) = 構遞壓壓淵齋齋顧鹽鏇 繭鏇膚餘醖網壓觸積繭 (積鏇網網願餘憲構衊築, 餘艱顧獵膚選膚鹽顧顧 ~ 鑰鏇衊鬱窪廠顧簾齋網) 更多 | ||||||
临床3期 | 39 | Questionnaire (RT Group 1) | 繭膚繭積鏇簾壓艱簾蓋(構觸觸餘淵窪鑰壓餘壓) = 窪願製廠網鹽鹹遞觸蓋 簾鹽鏇簾範膚遞夢構夢 (艱夢鹹鏇繭廠憲繭廠遞, 廠觸築艱餘觸襯獵鬱壓 ~ 獵鹽積築築夢鏇餘窪鏇) 更多 | - | 2012-08-08 | ||
(RT Group 2 + Hormone Therapy) | 繭膚繭積鏇簾壓艱簾蓋(構觸觸餘淵窪鑰壓餘壓) = 簾範觸選夢繭窪鹽憲艱 簾鹽鏇簾範膚遞夢構夢 (艱夢鹹鏇繭廠憲繭廠遞, 鏇蓋顧網範觸鬱憲壓願 ~ 壓艱鹽淵夢蓋膚鏇觸觸) 更多 |
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