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更新于：2026-02-27
Toremifene Citrate
枸橼酸托瑞米芬
更新于：2026-02-27
概要
基本信息
原研机构 |
最高研发阶段批准上市 |
首次获批日期 日本 (1995-03-31), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国) |
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结构/序列
分子式C32H36ClNO8 |
InChIKeyIWEQQRMGNVVKQW-OQKDUQJOSA-N |
CAS号89778-27-8 |
关联
50
项与 枸橼酸托瑞米芬 相关的临床试验CTR20241963
枸橼酸托瑞米芬片人体生物等效性试验
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枸橼酸托瑞米芬片在健康受试者中空腹和餐后给药条件下单中心、单剂量、随机、开放、交叉设计生物等效性试验
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枸橼酸托瑞米芬片在健康成年受试者中单次空腹状态及高脂餐后口服给药的随机、开放、两周期、两序列、交叉设计生物等效性试验方案
100 项与 枸橼酸托瑞米芬 相关的临床结果
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100 项与 枸橼酸托瑞米芬 相关的转化医学
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100 项与 枸橼酸托瑞米芬 相关的专利（医药）
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918
项与 枸橼酸托瑞米芬 相关的文献（医药）2026-01-01Cancer treatment and research communications
Treatment of ER-positive breast cancer with FDA-approved aromatase inhibitors
Review
作者: Lukong, Kiven Erique ; Kim, Nayoung
Breast cancer is a leading cause of death among women globally. Estrogen receptor (ER)-positive breast cancers account for ∼70 % of breast cancer diagnoses worldwide. Endocrine therapy is the primary treatment approach for ER-positive breast cancer. In the United States, the Food and Drug Administration (FDA) has approved several endocrine therapies for ER-positive breast cancers, including selective estrogen receptor modulators (SERMs), selective estrogen receptor downregulators/degraders (SERDs), and aromatase inhibitors (AIs). The current FDA-approved SERMs include tamoxifen, toremifene, and raloxifene, while the only SERD that has been approved to date is fulvestrant. Various generations of AIs are available for the treatment of hormone-positive breast cancers, including exemestane, letrozole, and anastrozole. Aromatase inhibitors are often utilized following relapse with therapies such as tamoxifen. Herein, we focus on and review the major FDA-approved aromatase inhibitors used to treat ER-positive breast cancer.
2025-11-22Journal of biomolecular structure & dynamics
In silico
screening of potential agonists of a glucagon-like peptide-1 receptor among female sex hormone derivatives
Article
作者: Nedyalkova, Miroslava ; Simeonov, Vasil ; Romanova, Julia ; Robeva, Ralitsa ; Yovcheva, Kirila ; Lattuada, Marco
Glucagon-like peptide-1 (GLP-1) is an intestinal hormone that exerts its pleiotropic effects through a specific GLP-1 receptor (GLP-1R). The hormone-receptor complex might regulate glucose-dependent insulin secretion, and energy homeostasis; moreover, it could decrease inflammation and provide cardio- and neuroprotection. Additionally, the beneficial influence of GLP-1 on obesity in women might lead to improvement of their ovarian function. The links between metabolism and reproduction are tightly connected, and it is not surprising that different estrogen derivatives, estrogen-receptor modulator (SERM) and progestins used for gonadal and oncological disorders might influence carbohydrate and lipid metabolism. However, their possible influence on the GLP-1R has not been studied. The docking scores and top-ranked poses of raloxifene were much higher than those observed for other investigated SERMs and estradiol per se. Among different studied progestins, drospirenone showed slightly higher affinity to GLP-1R. Herein, the same data set of the drugs is evaluated by molecular dynamics (MD) simulations and compared with the obtained docking result. Notably, it is demonstrated that the used docking protocol and the applied MD calculations ranked the same ligand (raloxifene) as the best one. In the present study, raloxifene might exert an allosteric influence on GLP-1R signaling, which might contribute to potential beneficial effects on metabolism and weight regulation. However, further experimental and clinical studies are needed to reveal if the GLP-1R modulation has a real biological impact.
2025-08-01Current computer-aided drug design
Molecular Docking and ADMET Analysis Strategy-based Stability Indicating RP-HPLC-PDA Method Development and Validation of Toremifene
Article
作者: Ahmad, Makhmur ; Khan, Shamshir ; Hashmi, Sana ; Hudda, Sharwan ; Ali, Md Sajid ; Ullah, Zabih
Background::
The purpose of this research is to develop an analytical method
and validate it according to ICH guidelines for the estimation of Toremifene by RP-HPLC-PDA
with molecular docking and ADMET analysis. From molecular docking, it came to know
the receptor affinity specifically to estrogen receptors (ERα and ERβ), which are responsible
for cancer therapy. ADMET analyses secure its therapeutic potential as well safety of the
drug.
Methods::
An isocratic method has developed by RP-HPLC-PDA (AGILENT 1100) with symmetry
of 100 mm x 4.6 mm x 5 μm particle size C18 column and optimise mobile phase is
methanol: 0.1% OPA (orthophosphoric acid) water ratio of 43:57% v/v. Under different conditions
like acidic, alkaline, oxidative, and neutral environments, toremifene was tested for degradation.
Results::
The developed method is validated in accordance with ICH guidelines. A calibration
curve with an r2 value of 0.9987 has been prepared across the range of 10 to 50 μg/ml with five
standard dilutions. The retention time of the drug is 5.575 minutes. The validation results are
system suitability (%RSD-0.76), inter-day precision (%RSD 0.14-0.29), intraday precision
(%RSD 0.08-0.34), accuracy (%RSD 0.16-0.96), and robustness (%RSD 0.16-0.35). In different
intended conditions, four peaks are in 1 N HCl, two peaks in 1 N NaOH, three peaks in 10%
H2O2 (1hr), and one peak in neutral.
Conclusion::
Toremifene, a Selective Estrogen Receptor Modulator (SERM), Drug pharmacokinetic
properties and receptor binding affinity results are helpful in designing the analytical
method. Developing the RP-HPLC-PDA method is found to be novel, simple and precise. It
could be used for testing toremifene in bulk and pharmaceutical tablet dosage forms in quality
control, as well as stability tests.
100 项与 枸橼酸托瑞米芬 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 |
|---|---|---|---|
| ER阴性乳腺癌 | 欧盟 | 1996-02-14 | |
| ER阴性乳腺癌 | 冰岛 | 1996-02-14 | |
| ER阴性乳腺癌 | 列支敦士登 | 1996-02-14 | |
| ER阴性乳腺癌 | 挪威 | 1996-02-14 | |
| 转移性乳腺癌 | 欧盟 | 1996-02-14 | |
| 转移性乳腺癌 | 冰岛 | 1996-02-14 | |
| 转移性乳腺癌 | 列支敦士登 | 1996-02-14 | |
| 转移性乳腺癌 | 挪威 | 1996-02-14 | |
| 乳腺癌 | 日本 | 1995-03-31 | |
| 乳腺癌 | 日本 | 1995-03-31 |
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 |
|---|---|---|---|---|
| 癌前状态 | 临床3期 | 美国 | 2005-01-01 | |
| 癌前状态 | 临床3期 | 阿根廷 | 2005-01-01 | |
| 癌前状态 | 临床3期 | 加拿大 | 2005-01-01 | |
| 前列腺上皮内瘤变 | 临床3期 | 美国 | 2005-01-01 | |
| 前列腺上皮内瘤变 | 临床3期 | 阿根廷 | 2005-01-01 | |
| 前列腺上皮内瘤变 | 临床3期 | 加拿大 | 2005-01-01 | |
| 骨折 | 临床3期 | 美国 | 2003-10-01 | |
| 骨折 | 临床3期 | 墨西哥 | 2003-10-01 | |
| 转移性前列腺癌 | 临床3期 | 美国 | 2003-10-01 | |
| 转移性前列腺癌 | 临床3期 | 墨西哥 | 2003-10-01 |
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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3期 | 1,589 | Placebo | 鹽壓廠衊廠製衊餘衊餘 = 衊獵衊顧獵構遞顧憲憲 觸齋壓壓鹹鹹鬱鹽糧窪 (鹹鹹齋衊範積齋衊夢選, 鏇夢簾繭鑰鑰鏇衊鹽醖 ~ 鹽壓艱鏇膚顧網獵獵壓) 更多 | - | 2023-06-12 | ||
临床4期 | 绝经前乳腺癌 辅助 | 92 | 遞蓋顧繭廠範築窪鏇膚(齋積構遞鏇糧夢積鹽範) = 願範齋餘憲壓窪鹹夢鬱 鬱廠製醖衊餘鑰築製網 (壓顧願衊壓憲窪衊襯選 ) 更多 | - | 2020-07-16 | ||
遞蓋顧繭廠範築窪鏇膚(齋積構遞鏇糧夢積鹽範) = 製製製鬱膚遞顧壓憲膚 鬱廠製醖衊餘鑰築製網 (壓顧願衊壓憲窪衊襯選 ) 更多 | |||||||
临床2期 | HR阳性乳腺癌 hormone receptor-positive | 106 | 廠鹽簾餘繭夢願鑰鏇積(願鬱積鏇築憲膚鹽構蓋) = 餘餘獵淵夢夢糧艱遞衊 蓋艱窪鹹製餘鬱鏇艱築 (夢觸製鏇夢繭襯蓋網衊 ) 更多 | 积极 | 2018-02-15 | ||
廠鹽簾餘繭夢願鑰鏇積(願鬱積鏇築憲膚鹽構蓋) = 鏇遞衊膚艱淵膚繭願壓 蓋艱窪鹹製餘鬱鏇艱築 (夢觸製鏇夢繭襯蓋網衊 ) 更多 | |||||||
临床3期 | high-grade prostatic intraepithelial neoplasia (HGPIN) | - | 齋遞簾構觸構膚願淵壓(繭觸製廠鑰餘齋壓齋蓋) = 醖夢鏇遞鹽膚範糧襯糧 淵觸憲選選積餘製網觸 (窪憲淵鏇獵網糧獵淵築 ) 更多 | - | 2013-02-10 | ||
Placebo | 齋遞簾構觸構膚願淵壓(繭觸製廠鑰餘齋壓齋蓋) = 淵顧鹽築鏇築觸鬱繭製 淵觸憲選選積餘製網觸 (窪憲淵鏇獵網糧獵淵築 ) 更多 | ||||||
临床3期 | 646 | 憲憲醖餘觸鹹積襯壓願(選廠觸衊簾糧鏇構顧觸) = 範鑰獵壓膚齋鑰齋觸願 願鏇鏇獵選製範鹽襯獵 (衊壓鬱鑰膚夢壓遞鏇製, -1.5 ~ 75.0) 更多 | 积极 | 2013-01-01 | |||
Placebo | 憲憲醖餘觸鹹積襯壓願(選廠觸衊簾糧鏇構顧觸) = 鏇觸鹽襯積淵構選製選 願鏇鏇獵選製範鹽襯獵 (衊壓鬱鑰膚夢壓遞鏇製 ) 更多 | ||||||
N/A | 27 | 壓襯獵製糧夢築製壓艱(淵淵繭憲遞憲鹽製醖壓) = 鹽獵膚蓋獵鏇築築顧築 壓夢願鏇夢願鬱蓋齋顧 (淵窪膚醖繭蓋齋構餘糧 ) 更多 | - | 2011-05-20 | |||
临床3期 | - | 膚齋壓廠範簾網蓋襯糧(觸繭遞淵遞鹹糧鑰選顧): relative risk reduction = 79.5 (95% CI, 29.8 ~ 94.0) | 积极 | 2010-05-20 | |||
Placebo | |||||||
N/A | - | 1,284 | 築鹹繭製壓夢齋膚衊顧(壓鹹顧簾範網艱鹽網鏇): OR = 0.59 (95% CI, 0.36 ~ 1.0), P-Value = <0.05 | - | 2010-04-01 | ||
Placebo | |||||||
临床3期 | - | 1,382 | 製範觸蓋觸醖鏇築夢範(顧憲築鹽顧壓範窪蓋網) = 鹹範襯膚簾鑰廠鏇憲獵 齋構繭壓廠鏇襯廠餘顧 (遞夢繭選鑰積繭鹹壓鑰 ) 更多 | - | 2009-05-20 | ||
临床2期 | 新辅助 | - | 鏇鏇夢遞鏇夢願觸構餘(遞繭遞襯遞壓糧糧網願) = 蓋網襯鹹遞鹹構壓憲鏇 積鬱鏇齋積觸鹽鹹窪觸 (壓餘鏇憲壓鹽糧糧鏇壓, 28 ~ 58) | - | 2004-07-15 |
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