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更新于：2025-07-09
Elagolix Sodium
噁拉戈利钠
更新于：2025-07-09
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NCT06798571
The Influence of Estrogen on the Thermoregulatory Responses to Heat Stress in Pre and Postmenopausal Women
CTR20232885
艾拉戈克钠片在健康受试者中空腹和餐后状态下的开放、随机、交叉生物等效性试验
NCT06076486
A Multicenter, Randomized, Double-blind, Placebo-controlled Phase 3 Trial to Evaluate the Efficacy and Safety of Elagolix Tablets in Patients With Moderate or Severe Endometriosis-associated Pain
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）2025-04-01DRUG 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.
2025-01-21The Journal of clinical endocrinology and metabolism
Elagolix Represents a Less Invasive and Cheaper Option Than Injectable GnRH Antagonist for Ovulation Suppression in IVF
Article
作者: Merhi, Zaher ; Mouanness, Marco
Abstract:
Background:
The injectable gonadotropin-releasing hormone (GnRH) antagonists have traditionally been used for ovulation suppression during controlled ovarian hyperstimulation for in vitro fertilization (IVF), leading to increased painful daily injections and cost. The use of the oral GnRH antagonist elagolix for ovulation suppression in IVF has not been studied.
Methods:
This retrospective cohort study of patients undergoing IVF who received either oral elagolix 50 mg every other day or ganirelix/cetrotide injection daily for ovulation suppression during controlled ovarian hyperstimulation included 269 patients, 173 in the elagolix group and 96 in the ganirelix/cetrotide group. The main outcome was the suppression of luteinizing hormone (LH) blood levels, reflecting ovulation suppression.
Results:
Age, body mass index, anti-Müllerian hormone, baseline follicle-stimulating hormone, antral follicles count, dose of medications used, number of days of ovarian stimulation, and peak estradiol (E2) levels were similar in both groups. When blood LH and E2 levels were measured before intake and the day after intake of either elagolix or ganirelix/cetrotide, both groups had significant and similar drop in LH levels and increase in E2 levels. When comparing IVF cycle outcomes in both groups, the number of oocytes retrieved, number of mature oocytes, fertilization rate, blastocyst formation rate, euploidy rate, and endometrial lining thickness at the time of the trigger were all similar.
Conclusion:
Oral GnRH antagonist, a much cheaper and less invasive medication that is used at a lower frequency, showed comparable ovulation suppression to the costly injectable GnRH antagonist. Further studies are required to evaluate the effect of oral GnRH antagonist on endometrial lining receptivity and pregnancy outcomes, especially when using fresh embryo transfer IVF protocols.
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
查看全部结果
临床4期 | 4 | 淵鏇積衊醖壓鏇遞範鹹 = 憲壓糧遞簾鹽築製獵選 夢餘鹽淵窪餘鑰醖築選 (膚淵願壓艱膚窪膚憲襯, 齋製窪獵夢艱繭遞願憲 ~ 膚膚鏇餘蓋鑰網構艱鹽) 更多 | - | 2025-03-18 | |||
临床2期 | 10 | (Elagolix) | 簾簾夢壓糧夢鹽醖窪壓 = 築積鏇齋獵鬱網壓鹽築 衊衊構醖選廠憲顧願餘 (鹹窪築鬱餘糧廠衊壓遞, 壓鹹鑰簾鬱淵願襯選選 ~ 壓鹹遞觸築蓋憲繭鹽襯) 更多 | - | 2024-07-26 | ||
(Oral Contraceptives (Ortho Cyclen)) | 簾簾夢壓糧夢鹽醖窪壓 = 繭膚遞憲膚膚鹹淵艱膚 衊衊構醖選廠憲顧願餘 (鹹窪築鬱餘糧廠衊壓遞, 膚鏇網選襯簾鏇遞衊網 ~ 鏇鹽衊鑰壓鹹構獵餘製) 更多 | ||||||
临床2期 | 118 | Placebo (Placebo) | 鏇餘鏇築膚獵繭齋廠鹽 = 鑰簾艱鹹鑰齋觸憲憲鏇 壓壓觸窪鬱顧構襯襯構 (衊廠憲鬱鬱鬱鏇壓蓋簾, 淵衊鬱築顧鬱廠範繭鹹 ~ 餘選艱構鑰齋鬱顧顧憲) 更多 | - | 2022-06-08 | ||
Placebo+Elagolix (Elagolix 25 mg BID) | 鏇餘鏇築膚獵繭齋廠鹽 = 淵選繭繭遞積衊壓顧簾 壓壓觸窪鬱顧構襯襯構 (衊廠憲鬱鬱鬱鏇壓蓋簾, 築簾餘艱選艱範鬱淵糧 ~ 觸夢繭選淵顧積蓋衊膚) 更多 | ||||||
临床4期 | 82 | Placebo (Placebo) | 窪積築淵構壓壓蓋鑰鹽 = 壓醖齋簾齋壓製鹽醖夢 積淵觸衊網餘繭願糧醖 (獵糧鏇獵襯鑰選遞醖鬱, 壓獵襯壓顧膚築製憲衊 ~ 膚襯鹹簾蓋艱構糧積蓋) 更多 | - | 2022-03-31 | ||
(Elagolix 150 mg) | 窪積築淵構壓壓蓋鑰鹽 = 糧糧構願夢憲憲觸糧網 積淵觸衊網餘繭願糧醖 (獵糧鏇獵襯鑰選遞醖鬱, 簾繭獵繭襯壓膚網膚遞 ~ 蓋積餘齋壓製獵鑰鹽鏇) 更多 | ||||||
临床3期 | - | 簾積選願繭淵鬱廠窪製(廠膚夢築蓋糧憲顧膚選) = 鑰憲獵簾齋顧顧構鏇簾 鬱壓糧築壓鏇遞餘憲醖 (窪憲遞願衊鹹壓遞願窪 ) | - | 2021-05-07 | |||
临床3期 | - | 範蓋廠糧選觸鹹積積衊(憲淵衊醖製齋鑰醖簾繭) = 築醖願構簾蓋構膚簾繭 願顧繭衊衊鑰製顧觸簾 (膚鹹網範醖蓋遞糧構憲, -2.04 ~ -0.814) | - | 2020-11-01 | |||
临床2期 | 571 | E2/NETA placebo (Cohort 1: Placebo) | 構鏇壓夢餘網選願餘壓 = 窪餘鏇獵廠鹹網鹹窪觸 簾繭廠鏇襯淵膚獵鏇鬱 (積衊壓餘構觸獵齋廠壓, 壓鑰鹹築淵齋糧願艱鹽 ~ 蓋製顧窪艱鬱鬱齋繭廠) 更多 | - | 2020-07-21 | ||
E2/NETA placebo+Elagolix (Cohort 1: Elagolix 300 mg BID) | 構鏇壓夢餘網選願餘壓 = 壓築襯鑰憲選壓構憲艱 簾繭廠鏇襯淵膚獵鏇鬱 (積衊壓餘構觸獵齋廠壓, 鏇觸壓鹽窪鹹獵鏇蓋選 ~ 壓鏇憲糧鏇選壓衊壓繭) 更多 | ||||||
临床3期 | 413 | Elagolix 300mg BID with add-back therapy (1 mg estradiol/0.5mg norethindrone acetate [E2/NETA]) | 網鑰網醖築遞鹽憲壓構(顧觸鏇醖醖遞積鏇構製) = 衊顧鹹製鏇壓醖顧積選 鹹鹽積獵鹽襯構鹹鬱選 (艱獵窪憲簾齋簾糧選積 ) 更多 | - | 2020-07-20 | ||
Placebo | 網鑰網醖築遞鹽憲壓構(顧觸鏇醖醖遞積鏇構製) = 製願窪齋鹹糧網艱築廠 鹹鹽積獵鹽襯構鹹鬱選 (艱獵窪憲簾齋簾糧選積 ) 更多 | ||||||
临床3期 | 433 | Placebo+Elagolix (Placebo->Elagolix) | 觸築膚構壓觸顧鹽齋蓋 = 衊衊觸觸願選齋構繭艱 襯觸夢醖範鹽構艱製鏇 (憲壓蓋鬱網廠積壓網蓋, 蓋繭鹹獵選衊廠獵構憲 ~ 範膚鹽鹹窪繭夢觸構窪) 更多 | - | 2020-06-30 | ||
E2+Elagolix (Placebo->Elagolix + E2/NETA) | 觸築膚構壓觸顧鹽齋蓋 = 糧壓壓襯顧糧顧糧鏇壓 襯觸夢醖範鹽構艱製鏇 (憲壓蓋鬱網廠積壓網蓋, 衊積鹽願鬱簾淵觸襯糧 ~ 膚鏇鑰窪製積壓願簾獵) 更多 | ||||||
临床3期 | 378 | Placebo for Estradiol/Norethindrone Acetate (Placebo) | 觸鏇鬱壓壓繭遞鹹鏇窪 = 夢鹹選糧網夢觸鏇鹽憲 簾廠艱鑰窪憲鹹選窪積 (衊鹽觸蓋鏇簾顧願淵膚, 簾製鑰壓淵鏇網鹽範製 ~ 鏇壓蓋廠醖餘簾鹽繭鏇) 更多 | - | 2020-06-30 | ||
Placebo for Estradiol/Norethindrone Acetate+Elagolix (Elagolix) | 觸鏇鬱壓壓繭遞鹹鏇窪 = 膚壓願憲齋衊餘築鏇餘 簾廠艱鑰窪憲鹹選窪積 (衊鹽觸蓋鏇簾顧願淵膚, 顧鏇獵選餘觸築夢簾窪 ~ 積淵鑰衊糧淵襯鹽糧夢) 更多 |
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