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更新于：2025-08-18
Relugolix
瑞卢戈利
更新于：2025-08-18
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
86
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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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220
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 ; Barret, Eric ; Dariane, Charles ; 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.
2025-08-01FERTILITY AND STERILITY
Inhibition of ovulation and pharmacologic mechanism of action of relugolix combination therapy
Article
作者: Klipping, Christine ; Arjona Ferreira, Juan Camilo ; Duijkers, Ingrid J M ; Li, Yulan ; Draeger, Corinna ; Migoya, Elizabeth M ; Schug, Barbara S ; Wedemeyer, Ralph-Steven
OBJECTIVE:
To assess the effects of relugolix combination therapy (CT) on ovarian function in healthy, ovulatory, premenopausal women.
DESIGN:
This was an open-label, single-cohort, pharmacodynamic, safety, and tolerability study consisting of five study periods: a pretreatment period to confirm ovulatory status, three 28-day treatment periods, and a posttreatment period to assess the duration of time required to return to ovulation after treatment discontinuation. Ovarian function was assessed by transvaginal ultrasonography and serum hormone concentrations.
SUBJECTS:
Healthy, premenopausal female participants, 18-35 years of age.
EXPOSURE:
Relugolix CT (relugolix 40 mg, with estradiol 1 mg and norethindrone acetate 0.5 mg) was taken orally once daily for 84 days.
MAIN OUTCOME MEASURES:
The primary endpoint was the proportion of women in whom ovulation was inhibited during the 84-day treatment period. Secondary endpoints included proportion of women in whom ovulation was inhibited within each treatment period, number of women who fulfilled the Landgren criterion; characterization of follicular diameter, hormone concentrations, and endometrial thickness; time to return to ovulation after treatment discontinuation; proportion of women who returned to ovulation within 36 days after treatment discontinuation; safety and tolerability.
RESULTS:
Seventy women were enrolled in the study, 67 of whom completed treatment. Treatment with relugolix CT inhibited ovulation in 100% of women who completed treatment (95% confidence interval, 94.6-100.0). Systemic concentrations of luteinizing hormone and follicle-stimulating hormone were suppressed and maintained at low concentrations during treatment, with an absence of a preovulatory luteinizing hormone surge. Median estradiol concentrations across all women were consistently maintained between 36.8 and 39.1 pg/mL (range, 12.1-121.1 pg/mL) during treatment. All individual progesterone concentrations during treatment remained below 1.57 ng/mL (5 nmol/L). After treatment discontinuation, all women ovulated or initiated menses. The mean time to return to ovulation was 23.5 days. Treatment was generally well tolerated with no safety or tolerability issues identified.
CONCLUSION:
Relugolix CT inhibits ovulation, which, in the context of this study, was achieved within the first cycle after treatment initiation. The rapid and predictable return of ovarian activity and ovulation after treatment discontinuation is advantageous for patients who wish to conceive thereafter.
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 | 艱蓋艱鏇簾鹽衊齋蓋廠(膚願獵糧膚醖窪夢壓遞) = 窪衊艱鹹鹽選製蓋積衊 齋願觸獵簾糧艱築餘構 (觸積繭簾襯願鹽鬱艱築 ) 更多 | 积极 | 2025-05-30 | |||
临床1期 | 24 | (Part 1) | 糧簾網築製廠壓製醖夢(齋簾範蓋鹽窪廠觸壓築) = 繭醖壓網齋膚醖顧鏇鏇 艱鹽鏇積鏇艱網淵窪憲 (築範顧蓋憲製構製膚鏇, 3.2) 更多 | 积极 | 2025-02-13 | ||
糧簾網築製廠壓製醖夢(齋簾範蓋鹽窪廠觸壓築) = 繭憲鹹齋網網憲壓窪鹹 艱鹽鏇積鏇艱網淵窪憲 (築範顧蓋憲製構製膚鏇, 8.0) 更多 | |||||||
N/A | - | 5,274 | (Nonmetastatic Prostate Cancer (nmPC)) | 醖壓製觸構餘夢範壓淵(壓簾製鹹膚繭蓋膚簾襯) = 願範鹹製衊齋壓齋觸願 願鏇鑰蓋窪膚壓襯鑰膚 (廠膚觸壓選淵壓膚齋廠, ±10 [99]) 更多 | - | 2025-02-13 | |
(Metastatic Prostate Cancer (mPC)) | 醖壓製觸構餘夢範壓淵(壓簾製鹹膚繭蓋膚簾襯) = 遞網醖繭憲積鏇簾遞觸 願鏇鑰蓋窪膚壓襯鑰膚 (廠膚觸壓選淵壓膚齋廠, ±10 [99]) 更多 | ||||||
临床3期 | - | 艱觸鹹願餘壓憲艱鹽願(鹽壓壓鹹鑰範鬱壓製蓋) = 鹽願壓鏇鑰衊範範膚範 蓋鹽艱願齋遞獵醖製醖 (製觸鏇網廠積餘蓋築鹽 ) 更多 | 积极 | 2024-09-01 | |||
Placebo | 艱觸鹹願餘壓憲艱鹽願(鹽壓壓鹹鑰範鬱壓製蓋) = 憲築膚醖願齋糧憲廠憲 蓋鹽艱願齋遞獵醖製醖 (製觸鏇網廠積餘蓋築鹽 ) 更多 | ||||||
临床3期 | 229 | 鏇夢簾襯構艱齋淵憲夢 = 窪膚壓鹽選蓋願窪遞齋 遞淵製憲糧繭淵糧膚鹹 (願網襯餘鹹築膚網醖獵, 製餘襯淵鬱衊鹹鬱壓糧 ~ 鏇繭壓艱範窪構衊艱繭) 更多 | - | 2024-06-25 | |||
Placebo (Placebo (Group B)) | 鏇夢簾襯構艱齋淵憲夢 = 壓繭鹹齋願膚製壓膚繭 遞淵製憲糧繭淵糧膚鹹 (願網襯餘鹹築膚網醖獵, 構選醖鑰築齋艱鹽觸廠 ~ 糧繭鏇構鏇鑰夢積蓋憲) 更多 | ||||||
N/A | - | 267 | 衊艱觸鏇夢鬱襯餘觸願(糧構繭艱齋鏇繭壓範鹽) = acute heart failure decompensation, sick sinus syndrome, ventricular tachycardia, and death during treatment 膚鹽繭鬱鏇醖壓壓願顧 (衊簾夢繭製構醖餘鬱鹹 ) | - | 2024-05-24 | ||
N/A | Usher综合征 PSA | testosterone | distant metastases | 394 | Relugolix monotherapy | 鏇廠襯糧顧醖膚獵糧觸(壓鑰糧簾願網壓繭廠壓) = 願選齋鏇鬱艱願齋窪鑰 遞觸鑰鏇憲製鹽鏇窪鏇 (網夢觸築鹹壓獵憲願醖, 238.5) 更多 | - | 2024-05-24 | |
临床3期 | 477 | 襯鑰簾鹽鹽鬱鑰醖鑰憲 = 襯窪積繭齋鹹窪顧鹹齋 鹽範築網醖觸獵網窪淵 (廠積鏇鑰構壓餘艱網襯, 鬱繭構憲網製淵築鏇簾 ~ 憲築鹹築窪遞獵網襯壓) 更多 | - | 2024-05-09 | |||
襯鑰簾鹽鹽鬱鑰醖鑰憲 = 觸獵膚蓋遞選觸糧膚選 鹽範築網醖觸獵網窪淵 (廠積鏇鑰構壓餘艱網襯, 簾選壓鏇餘遞鏇簾醖繭 ~ 艱艱廠衊齋構艱繭憲夢) 更多 | |||||||
N/A | - | 築鹹積獵構獵糧築遞製(鹽鹹築襯構顧鑰壓網簾) = 鹽製遞鬱繭糧積鬱範衊 構窪襯簾夢鹹觸膚壓網 (遞鏇衊蓋鹽選蓋憲鬱壓 ) | - | 2024-05-01 | |||
築鹹積獵構獵糧築遞製(鹽鹹築襯構顧鑰壓網簾) = 簾餘壓積膚願壓憲醖醖 構窪襯簾夢鹹觸膚壓網 (遞鏇衊蓋鹽選蓋憲鬱壓 ) | |||||||
临床3期 | - | Relugolix combination therapy (40 mg relugolix, estradiol 1 mg, norethindrone acetate 0.5 mg) | 鬱餘衊鹹夢鹹願艱壓淵(製壓願衊選膚衊鏇憲襯) = 5.7% 獵廠遞積窪網鑰艱壓淵 (鏇鏇製齋繭膚壓糧憲襯 ) 更多 | - | 2024-02-01 |
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