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更新于：2025-09-14
Relugolix
瑞卢戈利
更新于：2025-09-14
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 日本 (2019-01-08), |
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C29H27F2N7O5S |
InChIKeyAOMXMOCNKJTRQP-UHFFFAOYSA-N |
CAS号737789-87-6 |
关联
87
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100 项与 瑞卢戈利 相关的临床结果
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100 项与 瑞卢戈利 相关的转化医学
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100 项与 瑞卢戈利 相关的专利（医药）
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222
项与 瑞卢戈利 相关的文献（医药）2025-12-31JOURNAL OF OBSTETRICS AND GYNAECOLOGY
The Effect of Relugolix Combination Therapy in Black/African American Women with Uterine Fibroids
Article
作者: Venable, Sateria ; Stewart, Elizabeth A. ; Schulmann, Thierry
This plain language summary reports results from the LIBERTY 1, LIBERTY 2, and LIBERTY Long-Term Extension clin. studies, looking specifically at outcomes in Black/African American women, as these individuals have uterine fibroids more frequently and more severe disease.These studies examined the effect of relugolix combination therapy (relugolix plus estradiol and norethindrone acetate), a medication used in women with uterine fibroids and heavy menstrual bleeding.The main aim of these studies was to investigate how well relugolix combination therapy worked in reducing menstrual blood loss in women with uterine fibroids.In total, 70 Black/African American women received daily relugolix combination therapy for up to 1 yr.Over 8 out of 10 women responded to the treatment, meaning that relugolix combination therapy decreased menstrual blood loss.In around two-thirds of women, treatment led to no menstrual periods, or little blood loss.In the blood, Hb carries oxygen and anemia is associated with Hb levels less than 10.5 g/dL.Around 60% of women who had anemia at the beginning of the study experienced substantial improvements in their Hb (increase of more than 2 g/dL).Women also experienced improvements in their quality of life.The most common adverse events in Black/African American women were hot flushes, hypertension (which is high blood pressure), and headache.Bone loss was minimal.Relugolix combination therapy is as effective in Black/African American women as the overall LIBERTY study population despite Black/African American women typically having more severe fibroid disease.How to sayUterine fibroid (YOU-Tuh-Ryne FY-Broyd)Relugolix (Reh-LU-Go-LIX)Leiomyomas (lie-o-my-O-muhs)Norethindrone acetate (NAWR-Eth-in-Drone As-Uh-Tate)This is an abstract of the Plain Language Summary of Publication article.View the full Plain Language Summary PDF of this article to read the full-textLink to original article here
2025-10-01The French Journal of Urology
Relugolix in prostate cancer therapy: Clinical evidence and practical considerations
Article
作者: Peyrottes, Arthur ; Dariane, Charles ; Barret, Eric ; Ploussard, Guillaume ; Sargos, Paul ; Olivier, Jonathan ; Brureau, Laurent ; Baboudjian, Michael ; Supiot, Stephane ; Mathieu, Romain
INTRODUCTION:
Androgen deprivation therapy (ADT) remains a cornerstone of treatment for both localized and metastatic prostate cancer (PC). Relugolix, an oral gonadotrophin-releasing hormone antagonist, provides a new option for achieving rapid testosterone suppression using an oral formulation.
MATERIALS AND METHODS:
A comprehensive literature search was conducted in PubMed by combining the search terms "relugolix", "TAK-385", "MVT-601", "prostate cancer", and "prostatic neoplasms" and focusing on prospective and retrospective studies published in English.
RESULTS:
The HERO pivotal phase III trial demonstrated sustained testosterone suppression in 96.7% of patients with PC treated with relugolix versus 88.8% with leuprolide through to 48weeks (P<0.001). Relugolix achieved faster testosterone suppression and recovery post-treatment and a 54% lower risk of major adverse cardiovascular events compared with leuprolide. Data from HERO and phase II studies also support its use in combination with radiotherapy or other systemic therapies. Real-world studies performed to date have confirmed the effectiveness of relugolix, with more than 98% patients achieving castrate testosterone levels. Adherence to relugolix was generally high, and its safety profile aligned with clinical trial data. Practical considerations include, among others, treatment combination and drug-drug interactions, patient choice, and oncological outcomes.
CONCLUSIONS:
Clinical trials and real-world evidence support relugolix as a convenient and effective ADT option for PC. It offers rapid and sustained testosterone suppression, potential cardiovascular benefits, and an alternative to injectable therapies. Long-term adherence, the use of combination treatments and related drug-drug interactions require further investigation.
2025-10-01EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES
Pharmacokinetics and pharmacodynamics studies of Relugolix long-acting microcrystalline formulation in male Beagle dogs
Article
作者: Zhao, Pei ; Yu, Miao ; Wang, Jianxin ; Luo, Zhanling ; Yang, Xiaolai ; Li, Chunxian ; Yu, Jing ; Wang, Jingxian ; Guo, Xiaohong
Relugolix is the first oral GnRH receptor antagonist. However, its oral formulation requires daily administration, leading to poor patient adherence and suboptimal treatment outcomes for long-term users. To address these issues, we developed a long-acting microcrystalline formulation of relugolix administered once every 28 days.This study systematically evaluated the pharmacokinetics (PK), pharmacodynamics (PD), and safety profile of the drug following intramuscular administration in male Beagle dogs. In this study, we established a HPLC-MS/MS method for blood concentration detection, used a highly specific and stable ELISA method to measure serum testosterone levels, and assessed the safety of the drug in male Beagle dogs. The HPLC-MS/MS method showed good linearity (R²=0.9991). The intra-day precision varied between 2.8 % and 10.9 %, while the inter-day precision ranged from 1.6 % to 5.4 %. In terms of accuracy, the intra-day values ranged from -7.3 % to -3.2 %, and the inter-day accuracy ranged from -10.2 % to 0.8 %. Furthermore, key parameters such as stability, extraction recovery, and matrix effects met the FDA bioanalytical method validation guidelines. PK studies showed that the AUC and Tmax exhibited significant sustained-release characteristics, and the half-life was notably extended compared to Orgovyx. PD analysis showed a significant negative correlation between blood drug concentration and testosterone suppression (testosterone levels began to decline after administration, and castration levels were maintained between 504-1008 h). Safety assessments revealed that although no treatment-related deaths or significant weight changes were observed, some hematological parameters (RBC, HGB increases), liver function indicators (ALT, AST increases), and triglyceride (TG) levels showed statistically significant changes (p < 0.05). This suggests potential concerns regarding hemodynamic effects, hepatotoxicity, and lipid metabolism abnormalities. This study is the first to systematically evaluate the PK/PD characteristics of the long-acting micronized formulation of relugolix, providing key data for its clinical translation, but further validation through large sample and cross-species studies is needed.
100 项与 瑞卢戈利 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 |
|---|---|---|---|
| 晚期前列腺癌 | 加拿大 | 2023-10-10 | |
| 去势敏感前列腺癌 | 欧盟 | 2022-04-29 | |
| 去势敏感前列腺癌 | 冰岛 | 2022-04-29 | |
| 去势敏感前列腺癌 | 列支敦士登 | 2022-04-29 | |
| 去势敏感前列腺癌 | 挪威 | 2022-04-29 | |
| 子宫内膜异位症 | 日本 | 2021-12-24 | |
| 前列腺癌 | 美国 | 2020-12-18 | |
| 平滑肌瘤 | 日本 | 2019-01-08 |
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 |
|---|---|---|---|---|
| 复发性前列腺癌 | 临床3期 | 美国 | 2025-01-31 | |
| 复发性前列腺癌 | 临床3期 | 美国 | 2025-01-31 | |
| 痛经 | 临床3期 | 美国 | 2017-11-01 | |
| 痛经 | 临床3期 | 澳大利亚 | 2017-11-01 | |
| 痛经 | 临床3期 | 巴西 | 2017-11-01 | |
| 痛经 | 临床3期 | 智利 | 2017-11-01 | |
| 痛经 | 临床3期 | 捷克 | 2017-11-01 | |
| 痛经 | 临床3期 | 格鲁吉亚 | 2017-11-01 | |
| 痛经 | 临床3期 | 意大利 | 2017-11-01 | |
| 痛经 | 临床3期 | 新西兰 | 2017-11-01 |
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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3期 | 999 | 網衊鹽壓願廠簾憲鑰夢(廠積壓鹹觸願衊範鹽繭) = 壓齋糧網蓋餘淵淵襯簾 憲顧製夢窪築糧製構構 (築簾襯獵範憲糧鏇鬱網 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 24 | (Part 1) | 範顧壓淵醖憲顧願獵艱(獵淵廠衊窪夢憲範願鬱) = 鏇鹹夢製遞壓遞壓艱構 淵淵餘齋鬱簾廠鹹獵餘 (選蓋衊窪顧選醖網鬱鬱, 3.2) 更多 | 积极 | 2025-02-13 | ||
範顧壓淵醖憲顧願獵艱(獵淵廠衊窪夢憲範願鬱) = 鹹顧獵網構觸繭淵獵鑰 淵淵餘齋鬱簾廠鹹獵餘 (選蓋衊窪顧選醖網鬱鬱, 8.0) 更多 | |||||||
N/A | - | 5,274 | (Nonmetastatic Prostate Cancer (nmPC)) | 範繭夢膚鹽淵鏇範鬱淵(觸膚簾夢願襯齋憲積獵) = 鏇襯淵網鑰構願艱積網 願製築齋憲廠築憲鬱餘 (繭窪遞醖壓選網願鑰鹽, ±10 [99]) 更多 | - | 2025-02-13 | |
(Metastatic Prostate Cancer (mPC)) | 範繭夢膚鹽淵鏇範鬱淵(觸膚簾夢願襯齋憲積獵) = 餘廠構膚範艱鬱網鬱艱 願製築齋憲廠築憲鬱餘 (繭窪遞醖壓選網願鑰鹽, ±10 [99]) 更多 | ||||||
临床3期 | - | 衊鏇繭獵鏇夢衊構廠壓(鏇齋遞齋醖選襯獵繭餘) = 壓願衊願蓋膚網鹹顧餘 鬱鹽淵簾鑰範淵獵襯築 (襯蓋顧簾顧獵醖觸遞網 ) 更多 | 积极 | 2024-09-01 | |||
Placebo | 衊鏇繭獵鏇夢衊構廠壓(鏇齋遞齋醖選襯獵繭餘) = 願鑰膚製鑰膚遞襯簾積 鬱鹽淵簾鑰範淵獵襯築 (襯蓋顧簾顧獵醖觸遞網 ) 更多 | ||||||
临床3期 | 229 | 襯積蓋餘窪觸鏇鬱鏇齋 = 觸獵壓衊餘齋壓範艱築 鏇鹽廠醖膚獵鏇蓋艱壓 (鏇窪鏇繭艱網窪選淵鏇, 齋簾齋糧網衊範築鏇艱 ~ 獵製艱鹽衊衊積顧艱襯) 更多 | - | 2024-06-25 | |||
Placebo (Placebo (Group B)) | 襯積蓋餘窪觸鏇鬱鏇齋 = 鹹餘齋獵獵鑰膚築願製 鏇鹽廠醖膚獵鏇蓋艱壓 (鏇窪鏇繭艱網窪選淵鏇, 憲壓鑰醖鏇鏇憲壓選襯 ~ 壓廠築遞選觸齋艱構糧) 更多 | ||||||
N/A | - | 267 | 淵鬱構網願構鏇網襯夢(鏇繭範網艱憲壓積蓋願) = acute heart failure decompensation, sick sinus syndrome, ventricular tachycardia, and death during treatment 糧醖窪襯願築鏇網鏇膚 (憲憲膚餘齋積鏇築醖範 ) | - | 2024-05-24 | ||
N/A | Usher综合征 PSA | testosterone | distant metastases | 394 | Relugolix monotherapy | 憲築齋積簾網夢餘觸鑰(築簾膚獵糧選範繭鹹鹽) = 顧鹽願顧願壓築鹹鏇積 壓願衊夢齋壓夢夢鹹餘 (蓋衊築鬱願簾憲製醖網, 238.5) 更多 | - | 2024-05-24 | |
临床3期 | 477 | 鑰廠蓋窪膚積醖願選廠 = 遞鬱蓋積獵壓製窪顧淵 窪餘餘窪網構獵遞鑰醖 (鹽願衊淵範鏇蓋衊觸鹽, 鑰襯顧淵憲餘願鑰遞獵 ~ 醖願製鑰選艱積餘簾餘) 更多 | - | 2024-05-09 | |||
鑰廠蓋窪膚積醖願選廠 = 蓋蓋齋鏇網廠壓襯鏇糧 窪餘餘窪網構獵遞鑰醖 (鹽願衊淵範鏇蓋衊觸鹽, 鑰窪膚憲簾簾選淵膚夢 ~ 憲積簾遞鑰廠襯獵鬱簾) 更多 | |||||||
N/A | - | 構糧顧顧鹽遞築蓋蓋艱(夢膚願糧廠願鹹積選簾) = 壓齋積壓鬱鏇壓淵網醖 廠簾繭築鹽憲獵鹽淵齋 (顧醖壓鹽膚簾廠簾觸窪 ) | - | 2024-05-01 | |||
構糧顧顧鹽遞築蓋蓋艱(夢膚願糧廠願鹹積選簾) = 選淵糧夢願鬱構繭願衊 廠簾繭築鹽憲獵鹽淵齋 (顧醖壓鹽膚簾廠簾觸窪 ) | |||||||
临床3期 | - | Relugolix combination therapy (40 mg relugolix, estradiol 1 mg, norethindrone acetate 0.5 mg) | 鑰齋製顧築願醖獵艱遞(餘遞鏇築鹽窪遞餘選糧) = 5.7% 鏇製夢鏇獵積簾鹹餘願 (齋網齋鹽壓築鑰選襯膚 ) 更多 | - | 2024-02-01 |
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