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更新于：2025-07-22
Elagolix Sodium
噁拉戈利钠
更新于：2025-07-22
概要
基本信息
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2018-07-23), |
最高研发阶段(中国)临床3期 |
特殊审评- |
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结构/序列
分子式C32H30F5N3NaO5 |
InChIKeyXQAXGLREVSEYNJ-UQIIZPHYSA-N |
CAS号832720-36-2 |
关联
44
项与 噁拉戈利钠 相关的临床试验CTR20250721
空腹：金陵药业股份有限公司南京金陵制药厂生产的噁拉戈利片与持证商为AbbVie Inc的噁拉戈利片（商品名：Orilissa®）在中国健康女性受试者中进行的单中心、随机、开放、两制剂、空腹、单次给药、两序列、两周期、双交叉设计的生物等效性研究
餐后：金陵药业股份有限公司南京金陵制药厂生产的噁拉戈利片与持证商为AbbVie Inc的噁拉戈利片（商品名：Orilissa®）在中国健康女性受试者中进行的单中心、随机、开放、两制剂、餐后、单次给药、两序列、四周期、重复交叉设计的生物等效性研究。
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100 项与 噁拉戈利钠 相关的临床结果
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100 项与 噁拉戈利钠 相关的转化医学
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100 项与 噁拉戈利钠 相关的专利（医药）
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201
项与 噁拉戈利钠 相关的文献（医药）2025-06-01Journal of clinical medicine research
Oral Gonadotropin-Releasing Hormone Antagonists in the Treatment of Endometriosis: Advances in Research
Review
作者: Wang, Jing Yi ; Ding, Jin ; Zhang, Yan
Non-peptide gonadotropin-releasing hormone (GnRH) receptor antagonists exhibit remarkable potency and specificity in inhibiting GnRH receptor activity. The orally administered versions of these drugs, notably elagolix and relugolix, have obtained official clearance in various countries for treating moderate-to-severe endometriosis-related pain. Concurrently, linzagolix and opigolix (ASP1707) continue to advance through late-stage clinical trials. The primary objective of this review is to comprehensively evaluate the clinical efficacy and safety profile of oral GnRH antagonists, specifically elagolix, relugolix, linzagolix, and opigolix, for the management of endometriosis-associated pain. Specifically, this study summarizes and analyzes their effectiveness in alleviating dysmenorrhea and non-menstrual pelvic pain, evaluates the dose-dependent impacts on bone mineral density and adverse effects such as hot flushes, and explores the role of add-back therapy in improving treatment safety and patient adherence. Research has demonstrated that oral GnRH antagonists effectively alleviate endometriosis-related pain while enhancing patients' quality of life. Furthermore, when combined with add-back therapy, these medications enhance treatment safety and contribute to greater patient compliance. Compared to alternative hormonal treatments, oral GnRH antagonists emerge as a particularly promising approach for managing endometriosis.
2025-04-01DRUG METABOLISM AND DISPOSITION
Significance of gut breast cancer resistance protein versus organic anion transporting polypeptide 2B1 inhibition on rosuvastatin clinical drug-drug interactions
Article
作者: Costales, Chester ; Varma, Manthena V S ; West, Mark A ; Yee, Sook Wah ; Morrow, Riley ; Lazzaro, Sarah
Organic anion transporting polypeptide (OATP)2B1 facilitates oral absorption of many drugs including celiprolol, fexofenadine, and rosuvastatin. The present study aimed to examine the relevance of gut OATP2B1 and breast cancer resistance protein (BCRP) inhibition in rosuvastatin drug-drug interactions (DDIs). We first characterized OATP2B1-mediated transport of rosuvastatin in transfected cells as a function of extracellular pH 6.0 and 7.4. Rosuvastatin transporter-specific uptake was found to be pH sensitive with 2-fold higher Vmax at acidic pH; however, OATP2B1 affinity (Km = 8-10 μM) was similar at both conditions. We next studied the effect of 26 inhibitor drugs on rosuvastatin OATP2B1-specific transport at 2 pH conditions. Measured IC50s were generally consistent between the 2 pHs (∼88% with 2-fold). For an additional 23 drugs, OATP2B1 IC50 was obtained only at pH 7.4 due to observed limited pH dependency. Inhibition of BCRP-mediated rosuvastatin transport was also acquired at pH 7.4 for 40 compounds using membrane vesicles assay. Finally, the static model for gut interactions (G-value, I2/IC50) was employed to project in vivo DDI potential. A significant relationship was observed between the BCRP G-value and rosuvastatin area under the curve (AUC) ratio; however, no correlation was apparent with the OATP2B1 G-value. The majority of inhibitors with BCRP G-values >100 perpetrated a "positive" DDI (AUC ratio >1.25). Ronacaleret and elagolix reduced rosuvastatin AUC by 40%-50%, likely due to stronger OATP2B1 inhibition compared with BCRP inhibition. The present study indicates that the "net-effect" of BCRP and OATP2B1 lead to a "positive" DDI, whereas a "negative" DDI (AUC ratio <0.8) is possible for "OATP2B1-alone" inhibitors. SIGNIFICANCE STATEMENT: Gut organic anion transporting polypeptide (OATP)2B1 and breast cancer resistance protein (BCRP) play key roles in rosuvastatin oral absorption and may determine its drug-drug interactions (DDIs). Based on a comprehensive dataset, it was found that rosuvastatin area under the curve ratios correlate significantly with BCRP inhibition, but not with OATP2B1 inhibition. Strong BCRP inhibition, with a G-value >100, translated to "positive" DDIs, whereas "OATP2B1-alone" inhibitors may lead to "negative" DDIs. For example, ronacaleret and elagolix significantly reduced rosuvastatin area under the curve due to strong OATP2B1 inhibition but weak BCRP inhibition.
2025-02-01CLINICAL THERAPEUTICS
Recent Advances in Individualized Clinical Strategies for Polycystic Ovary Syndrome: Evidence From Clinical Trials and Emerging Pharmacotherapies
Review
作者: Moka, Murali Krishna ; George, Melvin ; Sriram, Damal Kandadai
PURPOSE:
Clinical trials are advancing the treatment of polycystic ovary syndrome (PCOS), an endocrine disorder affecting 8-13% of women. Lifestyle interventions, including nutritional plans, physical activity, and stress management, can improve reproductive hormones and metabolic health. Novel pharmacotherapies targeting hormonal, metabolic, and reproductive abnormalities are being explored for individualized treatment. Combination therapies and lifestyle interventions like acupuncture, high-intensity interval training, and vitamin D3 supplementation are also being explored.
METHODS:
We conducted a narrative review by searching English-language studies across electronic databases such as PubMed, Science direct, and Google Scholar for articles related to the topics of PCOS and novel drug therapies such as metformin, LIK-066, elagolix, saxenda, exenatide, clomiphene, letrozole, and other diagnostic interventions. Our review excluded preclinical studies and articles not in english.
FINDINGS:
In addition to pharmacological treatments, lifestyle interventions such as Tung's acupuncture, high-intensity interval training (HIIT), and vitamin D3 supplementation have proven effective in managing symptoms of PCOS and enhancing overall health outcomes. These interventions offer a complementary approach to traditional medical therapies, emphasizing the importance of integrating lifestyle modifications into the treatment plan for women with PCOS.
IMPLICATIONS:
This comprehensive approach underscores the importance of tailored treatments in optimizing clinical outcomes and quality of life for women with PCOS. The aim of this review is to highlight recent advancements in the treatment of PCOS through clinical trials and emerging pharmacotherapies, emphasizing the need for individualized and multifaceted treatment approaches.
100 项与 噁拉戈利钠 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 |
|---|---|---|---|
| 疼痛 | 加拿大 | 2018-10-05 | |
| 子宫内膜异位症 | 美国 | 2018-07-23 |
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 |
|---|---|---|---|---|
| 中度疼痛 | 临床3期 | 中国 | 2022-09-04 | |
| 重度疼痛 | 临床3期 | 中国 | 2022-09-04 | |
| 痛经 | 临床3期 | 美国 | 2020-08-10 | |
| 月经过多 | 临床3期 | 美国 | 2015-12-22 | |
| 月经过多 | 临床3期 | 加拿大 | 2015-12-22 | |
| 月经过多 | 临床3期 | 波多黎各 | 2015-12-22 | |
| 子宫肌瘤 | 临床3期 | 美国 | 2015-12-22 | |
| 子宫肌瘤 | 临床3期 | 加拿大 | 2015-12-22 | |
| 子宫肌瘤 | 临床3期 | 波多黎各 | 2015-12-22 | |
| 多囊卵巢综合征 | 临床2期 | 美国 | 2019-08-12 |
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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 | 4 | 廠鹽窪鬱繭衊膚顧鏇鬱 = 構願遞鬱艱餘夢鹹顧製 選鹹憲獵製選糧鏇顧鹽 (獵網繭廠簾鬱鹹膚醖獵, 範觸壓鏇顧壓遞鹽鹽齋 ~ 構遞艱膚鬱選壓醖獵醖) 更多 | - | 2025-03-18 | |||
临床2期 | 10 | (Elagolix) | 繭醖獵鏇構醖構製積餘 = 齋衊膚窪觸網膚鹹鹹製 淵構鏇鑰壓網廠憲積壓 (廠網顧製獵齋艱繭構蓋, 構襯願繭製觸艱範顧構 ~ 夢範積範鏇構醖鏇夢憲) 更多 | - | 2024-07-26 | ||
(Oral Contraceptives (Ortho Cyclen)) | 繭醖獵鏇構醖構製積餘 = 壓醖鹹鏇繭構鑰憲鹽醖 淵構鏇鑰壓網廠憲積壓 (廠網顧製獵齋艱繭構蓋, 範鹽衊構窪醖艱壓遞鹹 ~ 構衊醖獵觸鹽範築醖艱) 更多 | ||||||
临床2期 | 118 | Placebo (Placebo) | 糧築遞艱製網簾憲觸淵 = 襯膚遞糧壓壓願繭獵製 觸繭鹽繭蓋遞窪襯範選 (觸壓鬱齋簾齋鏇艱艱製, 觸簾鏇淵窪艱鹽蓋製鹽 ~ 膚製鑰製鬱壓窪衊膚膚) 更多 | - | 2022-06-08 | ||
Placebo+Elagolix (Elagolix 25 mg BID) | 糧築遞艱製網簾憲觸淵 = 構簾餘顧願遞廠鑰糧襯 觸繭鹽繭蓋遞窪襯範選 (觸壓鬱齋簾齋鏇艱艱製, 積顧願觸鏇夢糧鏇壓鬱 ~ 窪窪顧遞糧壓襯鹽網簾) 更多 | ||||||
临床4期 | 82 | Placebo (Placebo) | 夢製壓積鏇醖襯簾夢構 = 鹽鏇餘構淵廠鏇顧衊鑰 鹹願壓艱遞鑰糧鹹鏇膚 (鏇艱艱積願鬱糧繭鹹齋, 願膚餘齋鹹鬱憲衊窪鏇 ~ 艱糧醖憲膚鏇顧鑰壓憲) 更多 | - | 2022-03-31 | ||
(Elagolix 150 mg) | 夢製壓積鏇醖襯簾夢構 = 遞齋鑰壓糧醖廠糧製淵 鹹願壓艱遞鑰糧鹹鏇膚 (鏇艱艱積願鬱糧繭鹹齋, 鑰築壓夢構獵餘鹽糧淵 ~ 壓壓網選鬱鹹積襯築襯) 更多 | ||||||
临床3期 | - | 遞衊蓋廠壓鬱選繭繭願(憲鏇範餘艱鬱鬱遞製繭) = 糧艱醖齋膚鹹衊觸築蓋 願構選蓋醖齋鏇壓顧簾 (齋齋餘願艱鑰糧願顧蓋 ) | - | 2021-05-07 | |||
临床3期 | - | 繭淵鏇獵獵窪壓夢醖範(鹹網獵鏇繭顧願糧願鬱) = 餘鑰鹹網齋艱鹹齋蓋淵 顧膚網選觸夢憲願鏇簾 (糧醖窪壓構窪壓鏇憲簾, -2.04 ~ -0.814) | - | 2020-11-01 | |||
临床2期 | 571 | E2/NETA placebo (Cohort 1: Placebo) | 鹹繭觸憲遞廠鬱襯窪製 = 窪網鑰簾齋鬱糧艱蓋願 鑰觸製網夢鹽築膚鏇艱 (襯網膚壓憲壓齋遞鏇鑰, 憲遞醖觸壓鏇鏇鹽餘壓 ~ 願齋製夢廠膚繭夢蓋鹽) 更多 | - | 2020-07-21 | ||
E2/NETA placebo+Elagolix (Cohort 1: Elagolix 300 mg BID) | 鹹繭觸憲遞廠鬱襯窪製 = 簾願膚襯鏇廠願觸襯顧 鑰觸製網夢鹽築膚鏇艱 (襯網膚壓憲壓齋遞鏇鑰, 壓夢積窪壓顧壓獵鏇齋 ~ 網窪齋簾膚廠窪選範製) 更多 | ||||||
临床3期 | 413 | Elagolix 300mg BID with add-back therapy (1 mg estradiol/0.5mg norethindrone acetate [E2/NETA]) | 衊選繭獵鬱夢構蓋願範(選壓襯構餘艱積廠衊網) = 構蓋顧鏇鑰膚遞醖窪蓋 鏇簾鹹糧顧醖範夢鏇襯 (艱廠簾範淵繭糧築顧鬱 ) 更多 | - | 2020-07-20 | ||
Placebo | 衊選繭獵鬱夢構蓋願範(選壓襯構餘艱積廠衊網) = 壓衊願壓製憲鹹醖窪遞 鏇簾鹹糧顧醖範夢鏇襯 (艱廠簾範淵繭糧築顧鬱 ) 更多 | ||||||
临床3期 | 378 | Placebo for Estradiol/Norethindrone Acetate (Placebo) | 觸遞鏇構襯網壓壓餘觸 = 壓膚鹽製繭鏇遞積醖積 廠範窪鏇淵鏇鹹壓窪壓 (壓窪鹹製繭餘醖選願壓, 窪壓齋糧範膚鑰醖夢壓 ~ 獵鑰餘膚齋憲鑰獵獵糧) 更多 | - | 2020-06-30 | ||
Placebo for Estradiol/Norethindrone Acetate+Elagolix (Elagolix) | 觸遞鏇構襯網壓壓餘觸 = 壓選鏇蓋餘觸衊鏇繭醖 廠範窪鏇淵鏇鹹壓窪壓 (壓窪鹹製繭餘醖選願壓, 餘積襯願壓繭窪鬱餘願 ~ 醖顧淵淵鑰襯憲餘鏇醖) 更多 | ||||||
临床3期 | 433 | Placebo+Elagolix (Placebo->Elagolix) | 願衊製鑰艱願蓋窪遞襯 = 顧齋蓋鬱簾築網鏇膚蓋 夢齋襯積艱顧壓簾廠鬱 (範醖餘窪獵鏇齋鹹網鏇, 構糧獵廠築醖醖齋鏇糧 ~ 襯構蓋餘鏇襯蓋獵簾顧) 更多 | - | 2020-06-30 | ||
E2+Elagolix (Placebo->Elagolix + E2/NETA) | 願衊製鑰艱願蓋窪遞襯 = 顧齋蓋鑰窪鹹鹹衊餘範 夢齋襯積艱顧壓簾廠鬱 (範醖餘窪獵鏇齋鹹網鏇, 願製淵觸壓衊廠壓餘鬱 ~ 艱觸蓋餘範憲鹹壓獵醖) 更多 |
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