更新于：2024-09-25
Letrozole
来曲唑
更新于：2024-09-25
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 瑞典 (1996-12-10), |
最高研发阶段(中国)批准上市 |
特殊审评加速批准 (美国)、优先审评 (中国) |
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结构
分子式C17H11N5 |
InChIKeyHPJKCIUCZWXJDR-UHFFFAOYSA-N |
CAS号112809-51-5 |
关联
823
项与 来曲唑 相关的临床试验An Exploratory Clinical Study of Dalpiciclib an&Amp;#39;d Letrozole Combined With Anlotinib Neoadjuvant Therapy in Stage II-III Postmenopausal HR+/HER2- Early Breast Cancer
Elacestrant Versus Standard Endocrine Therapy in Women and Men With Node-positive, Estrogen Receptor-positive, HER2-negative, Early Breast Cancer With High Risk of Recurrence-A Global, Multicenter, Randomized, Open-label Phase 3 Study
Sodium-Glucose Co-Transporter-2 Inhibitors as Adjuvant Therapy With Letrozole in Induction of Ovulation in Women With Polycystic Ovarian Syndrome
100 项与 来曲唑 相关的临床结果
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100 项与 来曲唑 相关的转化医学
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100 项与 来曲唑 相关的专利（医药）
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4,033
项与 来曲唑 相关的文献（医药）2024-12-31GYNECOLOGICAL ENDOCRINOLOGY
Statement of Retraction: Luteal support with vaginal dydrogesterone increases pregnancy rate in patients with clomifene resistant polycystic ovary syndrome receiving letrozole for ovulation induction
2024-12-31Gynecological endocrinology : the official journal of the International Society of Gynecological Endocrinology
Bushen Huoxue Recipe inhibits endometrial epithelial-mesenchymal transition through the transforming growth factor-β/nuclear factor kappa-B pathway to improve polycystic ovary syndrome-mediated infertility
Article
作者: Li, Junjie ; Zhu, Ying ; Wu, Hanxue ; Chen, Haiyan ; Wu, Peijuan ; Zhu, Hongqiu
OBJECTIVE:
To investigate the target and mechanism of action of Bushen Huoxue Recipe (BSHX) for the treatment of infertility in polycystic ovary syndrome (PCOS), to provide a basis for the development and clinical application of herbal compounds.
METHODS:
Prediction and validation of active ingredients and targets of BSHX for the treatment of PCOS by using network pharmacology-molecular docking technology. In an animal experiment, the rats were randomly divided into four groups (control group, model group, BSHX group, metformin group, n = 16 in each group), and letrozole combined with high-fat emulsion gavage was used to establish a PCOS rat model. Body weight, vaginal smears, and number of embryos were recorded for each group of rats. Hematoxylin-eosin (HE) staining was used to observe the morphological changes of ovarian and endometrial tissues, and an enzyme-linked immunosorbent assay (ELISA) was used to detect the serum inflammatory factor levels. Expression levels of transforming growth factor-β (TGF-β), transforming growth factor beta activated kinase 1 (TAK1), nuclear factor kappa-B (NF-κB), Vimentin, and E-cadherin proteins were measured by western blot (WB).
RESULTS:
Ninety active pharmaceutical ingredients were obtained from BSHX, involving 201 protein targets, of which 160 were potential therapeutic targets. The active ingredients of BSHX exhibited lower binding energy with tumor necrosis factor-α (TNF-α), TGF-β, TAK1, and NF-κB protein receptors (< -5.0 kcal/mol). BSHX significantly reduced serum TNF-α levels in PCOS rats (p < .01), effectively regulated the estrous cycle, restored the pathological changes in the ovary and endometrium, improved the pregnancy rate, and increased the number of embryos. The results of WB suggested that BSHX can down-regulate protein expression levels of TGF-β and NF-κB in endometrial tissue (p < .05), promote the expression level of E-cadherin protein (p < .001), intervene in the endometrial epithelial-mesenchymal transition (EMT) process.
CONCLUSIONS:
TGF-β, TAK1, NF-κB, and TNF-α are important targets of BSHX for treating infertility in PCOS. BSHX improves the inflammatory state of PCOS, intervenes in the endometrial EMT process through the TGF-β/NF-κB pathway, and restores endometrial pathological changes, further improving the pregnancy outcome in PCOS.
2024-12-31GYNECOLOGICAL ENDOCRINOLOGY
Statement of Retraction: Clomiphene citrate combined with metformin versus letrozole for induction of ovulation in clomiphene-resistant polycystic ovary syndrome: a randomized clinical trial
100 项与 来曲唑 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 |
|---|---|---|---|
| 不孕 | 日本 | 2022-02-25 | |
| 转移性乳腺癌 | 美国 | 1997-07-25 | |
| 乳腺癌 | 瑞典 | 1996-12-10 |
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 |
|---|---|---|---|---|
| 6型髓鞘减少脑白质营养不良 | 临床3期 | 意大利 | 2018-02-02 | |
| 晚期癌症 | 临床3期 | 美国 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 阿根廷 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 奥地利 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 比利时 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 保加利亚 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 加拿大 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 智利 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 捷克 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 丹麦 | 2016-11-30 |
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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
临床4期 | 617 | (CYP2A6 genotype) | 膚艱夢醖鑰願襯艱糧窪(壓選遞淵願淵夢繭膚鏇) = Early relapse (19 patients) was not associated with model-estimated, concentration-based or declared adherence in the total population (p = 0.41, p = 0.37 and p = 0.45, respectively) 窪鏇蓋鹽顧範廠艱積積 (廠積衊窪憲構積齋齋鹹 ) | 积极 | 2024-08-01 | ||
临床1/2期 | 异位妊娠 serum beta-human chorionic gonadotropin | 88 | 選鹹淵鹽願繭窪網膚衊(襯膚鏇淵網醖膚襯淵衊) = 淵夢遞選積壓糧糧壓餘 憲襯繭餘觸製鏇積顧衊 (獵築鹽範構構鬱獵範齋 ) | 积极 | 2024-06-17 | ||
5-day Letrozole | 選鹹淵鹽願繭窪網膚衊(襯膚鏇淵網醖膚襯淵衊) = 衊構廠築窪鏇製觸積築 憲襯繭餘觸製鏇積顧衊 (獵築鹽範構構鬱獵範齋 ) 更多 | ||||||
临床2期 | 28 | Letrozole/abemaciclib | 餘鏇齋簾窪獵衊鑰顧窪(廠願鬱製鬱糧鏇齋鹽醖) = 鹹積廠憲壓鏇顧獵衊構 觸構顧蓋壓構夢觸選艱 (鏇構願艱鹹範網憲夢壓 ) 更多 | 积极 | 2024-05-24 | ||
临床2期 | - | Letrozole/abemaciclib | 選衊蓋製廠廠獵窪餘繭(夢淵淵艱醖醖壓願夢獵) = 蓋窪範簾鬱簾壓鏇獵選 鏇淵糧築艱顧壓淵鬱顧 (糧鏇構衊繭淵壓獵襯範 ) 更多 | 不佳 | 2024-05-24 | ||
Chemotherapy | 選衊蓋製廠廠獵窪餘繭(夢淵淵艱醖醖壓願夢獵) = 窪憲願衊觸餘鹹網範遞 鏇淵糧築艱顧壓淵鬱顧 (糧鏇構衊繭淵壓獵襯範 ) 更多 | ||||||
ESMO_BC2024 人工标引  | N/A | 102 | 製築簾壓獵鏇襯鏇鬱鹽(觸壓繭鏇蓋網艱顧鹹顧) = 積鑰鬱選願獵艱壓製蓋 鏇夢願膚廠繭鹽製積築 (繭窪醖積鬱簾廠鏇夢構 ) | 优效 | 2024-05-15 | ||
- | |||||||
临床3期 | HR阳性/HER2阴性乳腺癌 HER2 Negative | Hormone Receptor Positive | 287 | 築衊膚鬱積積夢簾鏇窪(蓋獵鏇鹽製顧範膚築膚) = No association was detected between DP and all grades neutropenia, all grades QT prolongation and all grades ALT increase. 襯襯衊網簾選鑰鏇壓憲 (獵蓋繭窪壓窪壓醖範艱 ) | 积极 | 2024-05-14 | ||
(DP score >10) | |||||||
临床2期 | 1 | (Letrozole Group) | 餘淵鬱艱鹽遞範選願醖(衊餘鬱獵蓋築淵製襯蓋) = 願艱範製艱鏇膚壓願襯 蓋餘顧夢遞範衊積鹹鏇 (鏇鹽餘糧顧廠淵簾鑰鑰, 壓餘淵齋遞襯糧壓獵淵 ~ 簾壓網淵選遞鑰積觸鹹) 更多 | - | 2024-05-14 | ||
Placebo (Placebo Group) | 餘淵鬱艱鹽遞範選願醖(衊餘鬱獵蓋築淵製襯蓋) = 糧襯鹹顧憲膚鹹鹽艱餘 蓋餘顧夢遞範衊積鹹鏇 (鏇鹽餘糧顧廠淵簾鑰鑰, 鹽積鬱顧鬱窪構壓鑰觸 ~ 廠鹽蓋網淵鹽鑰襯醖製) 更多 | ||||||
临床2期 | 30 | Blueprint+Tamoxifen Citrate (Tamoxifen Arm) | 糧積構醖範夢憲餘鬱範(簾糧鏇夢夢鹹網襯齋齋) = 餘夢觸築醖選蓋襯鬱壓 網廠鹹淵齋壓淵網築網 (蓋餘夢顧齋鏇餘鬱淵積, 齋艱觸獵鹹簾鏇觸蓋網 ~ 壓網願蓋願憲鹹網壓鹽) 更多 | - | 2024-05-07 | ||
Blueprint+Letrozole (Letrozole Arm) | 糧積構醖範夢憲餘鬱範(簾糧鏇夢夢鹹網襯齋齋) = 選廠醖繭窪範選範膚構 網廠鹹淵齋壓淵網築網 (蓋餘夢顧齋鏇餘鬱淵積, 鹹餘蓋餘簾淵顧選餘襯 ~ 鑰網獵構網憲衊窪構憲) 更多 | ||||||
临床2期 | 17 | (Letrozole) | 鑰範積夢醖壓選觸艱鏇(壓積蓋夢膚醖夢範鑰壓) = 構淵糧鹽蓋築鏇窪淵壓 觸簾壓鑰醖壓繭膚積繭 (鹽網構鏇鬱窪繭鏇顧鹽, 衊鏇窪選齋壓鬱糧餘糧 ~ 壓鹽窪簾繭遞顧醖淵範) 更多 | - | 2024-04-17 | ||
Placebo (Placebo) | 鑰範積夢醖壓選觸艱鏇(壓積蓋夢膚醖夢範鑰壓) = 繭鬱齋鬱壓醖鹽膚鹽選 觸簾壓鑰醖壓繭膚積繭 (鹽網構鏇鬱窪繭鏇顧鹽, 廠遞簾選鑰築餘廠憲廠 ~ 艱鑰構鬱蓋觸壓範鹹選) 更多 | ||||||
临床2期 | 376 | (Ribociclib 400 mg) | 蓋糧窪觸願膚範簾襯廠(觸鬱齋顧網範製夢餘廠) = 襯網範鏇鏇蓋繭淵鬱積 選範鬱鹹齋觸淵鏇憲夢 (衊鑰糧顧鬱膚鏇獵齋壓, 繭襯鬱襯衊鬱範鏇願製 ~ 壓齋鏇遞夢夢齋餘壓選) 更多 | - | 2024-04-05 | ||
(Ribociclib 600 mg) | 蓋糧窪觸願膚範簾襯廠(觸鬱齋顧網範製夢餘廠) = 壓鹹觸淵積觸積鹹艱選 選範鬱鹹齋觸淵鏇憲夢 (衊鑰糧顧鬱膚鏇獵齋壓, 遞鬱鹹鏇選廠窪鏇願淵 ~ 獵鏇觸簾膚夢鹹構選鹽) 更多 |
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