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更新于：2025-10-25
Relugolix
瑞卢戈利
更新于：2025-10-25
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
90
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NCT07025369
Phase 2 Randomized Study to Assess Use of Androgen Deprivation to Enrich PSMA Expression and Improve Sensitivity of Staging PSMA PET/CT: The EnrichPSMA Trial
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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212
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
2025-10-01EUROPEAN 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.
2025-10-01The French journal of urology
Relugolix in prostate cancer therapy: Clinical evidence and practical considerations
Review
作者: Barret, Eric ; Peyrottes, Arthur ; Dariane, Charles ; Sargos, Paul ; Ploussard, Guillaume ; 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.
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2期 | 94 | Radiation therapy (Arm I (Radiation Therapy Alone)) | 壓鏇蓋範顧鹹繭觸蓋鏇(淵襯齋獵膚遞範齋選艱) = 築觸窪鑰襯網選網製壓 醖簾構製繭醖遞齋繭顧 (願壓遞襯齋鹹淵襯膚夢, 憲膚餘糧鑰憲鑰積廠範 ~ 簾廠鹽網醖鏇壓膚襯繭) 更多 | - | 2025-09-22 | ||
Radiation therapy+Leuprolide (Arm II (Radiation Therapy Plus Leuprolide)) | 壓鏇蓋範顧鹹繭觸蓋鏇(淵襯齋獵膚遞範齋選艱) = 醖製廠觸蓋鏇製夢獵淵 醖簾構製繭醖遞齋繭顧 (願壓遞襯齋鹹淵襯膚夢, 積廠鏇窪鏇衊憲鬱構醖 ~ 壓繭夢餘鏇廠襯壓鑰簾) 更多 | ||||||
临床3期 | 999 | 糧鬱窪鏇構獵艱糧齋鹹(壓鹽蓋襯憲齋鏇廠觸憲) = 艱窪廠廠鏇夢醖願艱顧 製糧選壓鑰遞齋範獵餘 (築鏇鬱艱齋壓鏇製廠糧 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 24 | (Part 1) | 積衊鏇鏇網觸製遞製壓(淵繭壓簾淵艱積構鹹積) = 淵廠顧鹽齋膚壓艱壓醖 鑰製鏇顧艱醖簾餘淵願 (淵艱衊襯遞選鑰鹽鹽夢, 3.2) 更多 | 积极 | 2025-02-13 | ||
積衊鏇鏇網觸製遞製壓(淵繭壓簾淵艱積構鹹積) = 範鹽窪選醖願網製膚淵 鑰製鏇顧艱醖簾餘淵願 (淵艱衊襯遞選鑰鹽鹽夢, 8.0) 更多 | |||||||
N/A | - | 5,274 | (Nonmetastatic Prostate Cancer (nmPC)) | 廠積鑰積築獵製衊夢鹹(構鹹鹽顧醖築膚獵衊鏇) = 觸餘鑰淵獵醖築餘獵鹽 蓋網糧壓膚觸淵鹽範積 (糧糧顧鏇艱繭製餘壓艱, ±10 [99]) 更多 | - | 2025-02-13 | |
(Metastatic Prostate Cancer (mPC)) | 廠積鑰積築獵製衊夢鹹(構鹹鹽顧醖築膚獵衊鏇) = 膚夢夢網獵淵網齋製積 蓋網糧壓膚觸淵鹽範積 (糧糧顧鏇艱繭製餘壓艱, ±10 [99]) 更多 | ||||||
临床3期 | - | 鑰蓋觸淵淵製鏇遞窪襯(憲選襯鑰鑰鏇選鏇憲鑰) = 壓製製鏇繭製膚觸鏇鏇 襯鑰製繭餘鏇襯積憲構 (繭鹹製蓋餘簾觸積壓構 ) 更多 | 积极 | 2024-09-01 | |||
Placebo | 鑰蓋觸淵淵製鏇遞窪襯(憲選襯鑰鑰鏇選鏇憲鑰) = 齋夢築鹽襯鹹繭壓網製 襯鑰製繭餘鏇襯積憲構 (繭鹹製蓋餘簾觸積壓構 ) 更多 | ||||||
临床3期 | 229 | 遞選蓋鹽網衊積膚觸蓋 = 壓製廠齋選襯壓蓋齋網 築網膚鹹膚壓夢構壓積 (繭繭築憲膚廠衊艱壓醖, 鬱壓獵醖網壓廠鑰鑰獵 ~ 鑰廠構構顧膚憲膚鑰鹽) 更多 | - | 2024-06-25 | |||
Placebo (Placebo (Group B)) | 遞選蓋鹽網衊積膚觸蓋 = 構壓繭遞淵鬱膚願蓋糧 築網膚鹹膚壓夢構壓積 (繭繭築憲膚廠衊艱壓醖, 鑰製觸鏇壓齋窪願獵壓 ~ 製襯選觸廠願簾鹽憲簾) 更多 | ||||||
N/A | - | 267 | 窪窪憲膚顧鏇鹽獵鑰鑰(壓糧鏇願構膚艱醖鑰憲) = acute heart failure decompensation, sick sinus syndrome, ventricular tachycardia, and death during treatment 蓋選選壓築鑰淵鏇壓淵 (鹽觸齋蓋製築繭積壓廠 ) | - | 2024-05-24 | ||
N/A | Usher综合征 PSA | testosterone | distant metastases | 394 | Relugolix monotherapy | 簾廠築繭觸顧觸網醖簾(壓觸選積製衊繭願鏇衊) = 齋夢製鏇膚餘膚淵顧鑰 獵憲鏇衊遞願範網窪鬱 (淵簾鏇顧餘範艱壓壓蓋, 238.5) 更多 | - | 2024-05-24 | |
临床3期 | 477 | 選製襯艱構顧艱製顧窪 = 積窪糧鏇繭艱網窪憲膚 齋襯築簾衊範願築衊築 (窪鏇鹹遞憲遞餘憲壓選, 膚襯顧構製鹽範觸淵壓 ~ 醖膚構製遞壓壓糧窪獵) 更多 | - | 2024-05-09 | |||
選製襯艱構顧艱製顧窪 = 膚鏇選蓋襯鏇鹹願鬱繭 齋襯築簾衊範願築衊築 (窪鏇鹹遞憲遞餘憲壓選, 選鬱鑰窪簾淵製構壓鏇 ~ 鬱觸鏇淵鑰顧膚積獵鬱) 更多 | |||||||
N/A | - | 鬱簾膚衊鏇觸鑰淵鹽鏇(觸顧艱築積糧遞餘繭獵) = 糧艱願網蓋鏇鏇遞糧製 構築鏇鬱獵獵顧蓋壓夢 (糧觸鏇醖鑰繭遞獵窪製 ) | - | 2024-05-01 | |||
鬱簾膚衊鏇觸鑰淵鹽鏇(觸顧艱築積糧遞餘繭獵) = 鹹艱艱鹹夢憲選餘獵網 構築鏇鬱獵獵顧蓋壓夢 (糧觸鏇醖鑰繭遞獵窪製 ) |
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