更新于：2024-07-01
Relugolix
瑞卢戈利
更新于：2024-07-01
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
分子式C29H27F2N7O5S |
InChIKeyAOMXMOCNKJTRQP-UHFFFAOYSA-N |
CAS号737789-87-6 |
关联
68
项与 瑞卢戈利 相关的临床试验Comeback From Long coursE ADT With RElugolix and Darolutamide in Hormone-sensitive Prostate Cancer (CLEARED)
Phase IB Trial of Relugolix and Enzalutamide as Neoadjuvant/ Adjuvant to Local-regional Treatment in Patients With High-risk Locally Advanced Prostate CAncer (RENAPCA)
Description of Relugolix Use in Patients With Prostate Cancer: An Analysis of National Veterans Affairs Health Care Network Data
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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116
项与 瑞卢戈利 相关的文献（医药）2024-02-01British journal of clinical pharmacology
Considerations on implementation of the newest treatment for symptomatic uterine fibroids: Oral GnRH antagonists
Review
作者: Mol, Ben Willem J ; Huirne, Judith A F ; Bet, Pierre M ; Clark, T Justin ; de Lange, Maria E ; Semmler, Annika ; Hehenkamp, Wouter J K
Abstract:
Novel gonadotrophin releasing hormone (GnRH) antagonist treatments have recently been developed in combination with hormonal add‐back therapy, as an oral treatment option for women suffering from uterine fibroids. Registration trials assessing the GnRH antagonist combination preparations with relugolix, elagolix and linzagolix have assessed treatment efficacy for fibroid‐related heavy menstrual blood loss in comparison to placebo. Marketing authorization has been granted by several agencies including those in Europe, the United Kingdom and the United States. While the registration trials report a robust effect on the reduction of heavy menstrual blood loss and improvement in quality of life scores, reticence is advised before widespread prescription. In this review, we demonstrate limitations in the trial data, namely a lack of generalizability due to the restricted study population, the lack of transparency in the distribution of disease‐level characteristics limiting the predictability of treatment success in the real‐world diverse population, and the absence of any comparison to current alternative treatment methods. Importantly, no clinically meaningful volume reductions were found with GnRH antagonist combination preparations, and long‐term safety data, particularly concerning modest but stable bone mineral density decline, need further addressing. Symptoms related to uterine fibroids adversely affect many women's quality of life and effective medical treatments are lacking. However, despite the urgent need for conservative treatments, it is vitally important that novel drugs, like combination oral GnRH antagonists, undergo sufficiently rigorous evaluation of safety, effectiveness and cost‐effectiveness in a representative population and are compared with alternative treatment methods before introduction into mainstream clinical practice.
2024-02-01American journal of obstetrics and gynecology
Relugolix combination therapy in Black/African American women with symptomatic uterine fibroids: LIBERTY Long-Term Extension study
Article
作者: Marsh, Erica E ; Stewart, Elizabeth A ; Schulmann, Thierry ; Lukes, Andrea S ; Zhu, Emily ; Madueke-Laveaux, O Sandra ; Proehl, Sarah ; Al-Hendy, Ayman
BACKGROUND:
In the LIBERTY Long-Term Extension study, once-daily relugolix combination therapy (40 mg relugolix, estradiol 1 mg, norethindrone acetate 0.5 mg) substantially improved uterine fibroid-associated heavy menstrual bleeding throughout the 52-week treatment period in the overall study population.
OBJECTIVE:
Black or African American women typically experience a greater extent of disease and symptom burden of uterine fibroids vs other racial groups and have traditionally been underrepresented in clinical trials. This secondary analysis aimed to assess the efficacy and safety of relugolix combination therapy in the subgroup population of Black or African American women with uterine fibroids in the LIBERTY Long-Term Extension study.
STUDY DESIGN:
Black or African American premenopausal women (aged 18-50 years) with uterine fibroids and heavy menstrual bleeding who completed the 24-week randomized, placebo-controlled, double-blind LIBERTY 1 (identifier: NCT03049735) or LIBERTY 2 (identifier: NCT03103087) trials were eligible to enroll in the 28-week LIBERTY Long-Term Extension study (identifier: NCT03412890), in which all women received once-daily, open-label relugolix combination therapy. The primary endpoint of this subanalysis was the proportion of Black or African American treatment responders: women who achieved a menstrual blood loss volume of <80 mL and at least a 50% reduction in menstrual blood loss volume from the pivotal study baseline to the last 35 days of treatment by pivotal study randomized treatment group. The secondary outcomes included rates of amenorrhea and changes in symptom burden and quality of life.
RESULTS:
Overall, 241 of 477 women (50.5%) enrolled in the LIBERTY Long-Term Extension study self-identified as Black or African American. In Black or African American women receiving continuous relugolix combination therapy for up to 52 weeks, 58 of 70 women (82.9%; 95% confidence interval, 72.0%-90.8%) met the treatment responder criteria for reduction in heavy menstrual bleeding (primary endpoint). A substantial reduction in menstrual blood loss volume from the pivotal study baseline to week 52 was demonstrated (least squares mean percentage change: 85.0%); 64.3% of women achieved amenorrhea; 59.1% of women with anemia at the pivotal study baseline achieved a substantial improvement (>2 g/dL) in hemoglobin levels; and decreased symptom severity and distress because of uterine fibroid-associated symptoms and improvements in health-related quality of life through 52 weeks were demonstrated. The most frequently reported adverse events during the cumulative 52-week treatment period were hot flush (12.9%), headache (5.7%), and hypertension (5.7%). Bone mineral density was preserved through 52 weeks.
CONCLUSION:
Once-daily relugolix combination therapy improved uterine fibroid-associated heavy menstrual bleeding in most Black or African American women who participated in the LIBERTY Long-Term Extension study. The safety and efficacy profile of relugolix combination therapy in Black or African American women was consistent with previously published results from the overall study population through 52 weeks. Findings from this subanalysis will assist shared decision-making by helping providers and Black or African American women understand the efficacy and safety of relugolix combination therapy as a pharmacologic option for the management of uterine fibroid-associated symptoms.
2024-05-01Anti-cancer agents in medicinal chemistry
An Expedition on Synthetic Methodology of FDA-approved Anticancer Drugs
(2018-2021)
Review
作者: Gupta, Ghanshyam Das ; Jain, Ankit ; Vishakha, S ; Navneesh, N ; Verma, Sant Kumar ; Patel, Preeti ; Kurmi, Balak Das
Abstract::
New drugs being established in the market every year produce specified structures for selective biological
targeting. With medicinal insights into molecular recognition, these begot molecules open new rooms for
designing potential new drug molecules. In this review, we report the compilation and analysis of a total of 56
drugs including 33 organic small molecules (Mobocertinib, Infigratinib, Sotorasib, Trilaciclib, Umbralisib, Tepotinib,
Relugolix, Pralsetinib, Decitabine, Ripretinib, Selpercatinib, Capmatinib, Pemigatinib, Tucatinib, Selumetinib,
Tazemetostat, Avapritinib, Zanubrutinib, Entrectinib, Pexidartinib, Darolutamide, Selinexor, Alpelisib,
Erdafitinib, Gilteritinib, Larotrectinib, Glasdegib, Lorlatinib, Talazoparib, Dacomitinib, Duvelisib, Ivosidenib,
Apalutamide), 6 metal complexes (Edotreotide Gallium Ga-68, fluoroestradiol F-18, Cu 64 dotatate, Gallium 68
PSMA-11, Piflufolastat F-18, 177Lu (lutetium)), 16 macromolecules as monoclonal antibody conjugates (Brentuximabvedotin,
Amivantamab-vmjw, Loncastuximabtesirine, Dostarlimab, Margetuximab, Naxitamab, Belantamabmafodotin,
Tafasitamab, Inebilizumab, SacituzumabGovitecan, Isatuximab, Trastuzumab, Enfortumabvedotin,
Polatuzumab, Cemiplimab, Mogamulizumab) and 1 peptide enzyme (Erwiniachrysanthemi-derived
asparaginase) approved by the U.S. FDA between 2018 to 2021. These drugs act as anticancer agents against
various cancer types, especially non-small cell lung, lymphoma, breast, prostate, multiple myeloma, neuroendocrine
tumor, cervical, bladder, cholangiocarcinoma, myeloid leukemia, gastrointestinal, neuroblastoma, thyroid,
epithelioid and cutaneous squamous cell carcinoma. The review comprises the key structural features, approval
times, target selectivity, mechanisms of action, therapeutic indication, formulations, and possible synthetic approaches
of these approved drugs. These crucial details will benefit the scientific community for futuristic new
developments in this arena.
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
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 晚期前列腺癌 | 加拿大 | 2023-10-23 | |
| 去势抵抗性前列腺癌 | 欧盟 | 2022-04-29 | |
| 去势抵抗性前列腺癌 | 冰岛 | 2022-04-29 | |
| 去势抵抗性前列腺癌 | 列支敦士登 | 2022-04-29 | |
| 去势抵抗性前列腺癌 | 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 |
|---|---|---|---|---|
| 月经过多 | 临床3期 | 美国 | 2017-04-26 | |
| 月经过多 | 临床3期 | 巴西 | 2017-04-26 | |
| 月经过多 | 临床3期 | 意大利 | 2017-04-26 | |
| 月经过多 | 临床3期 | 波兰 | 2017-04-26 | |
| 月经过多 | 临床3期 | 南非 | 2017-04-26 | |
| 月经过多 | 临床3期 | 英国 | 2017-04-26 | |
| 子宫肌瘤 | 临床3期 | 美国 | 2017-04-26 | |
| 子宫肌瘤 | 临床3期 | 巴西 | 2017-04-26 | |
| 子宫肌瘤 | 临床3期 | 意大利 | 2017-04-26 | |
| 子宫肌瘤 | 临床3期 | 波兰 | 2017-04-26 |
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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
N/A | - | 267 | 餘艱壓蓋遞廠鑰壓網廠(壓選憲鹹鑰壓簾膚襯簾) = acute heart failure decompensation, sick sinus syndrome, ventricular tachycardia, and death during treatment 積膚簾鹽廠網膚遞範齋 (獵夢艱積遞鏇糧膚鹹網 ) | - | 2024-05-24 | ||
N/A | Usher综合征 PSA | testosterone | distant metastases | 394 | Relugolix monotherapy | 繭獵齋糧鹹廠蓋選膚鏇(範餘鹽獵夢襯繭簾構選) = 淵製鏇遞淵壓網夢憲簾 構鑰醖網構壓淵壓齋繭 (醖繭艱夢範顧積淵繭齋, 238.5) 更多 | - | 2024-05-24 | |
临床3期 | 477 | 鹽艱鹽襯範觸築簾糧艱(糧製築鏇廠繭獵鏇鑰選) = 醖鑰鑰壓憲齋齋鹽餘夢 窪獵窪鹽鹹願襯鏇鹽壓 (醖夢憲構範製鏇襯選獵, 簾製簾鹽鏇選餘觸齋範 ~ 鹹鏇餘範築鏇鑰顧窪積) 更多 | - | 2024-05-09 | |||
鹽艱鹽襯範觸築簾糧艱(糧製築鏇廠繭獵鏇鑰選) = 網鏇廠築鏇鏇願蓋衊鏇 窪獵窪鹽鹹願襯鏇鹽壓 (醖夢憲構範製鏇襯選獵, 餘壓糧淵鬱積選遞鹽艱 ~ 製範淵選鹹願餘鬱鏇積) 更多 | |||||||
N/A | - | 鹹廠獵範獵簾齋選衊夢(繭鏇餘觸遞膚艱網製築) = 遞淵艱選構膚願齋鹽觸 網觸淵淵憲鬱積醖觸衊 (醖積鹽醖觸願齋範獵壓 ) | - | 2024-05-01 | |||
鹹廠獵範獵簾齋選衊夢(繭鏇餘觸遞膚艱網製築) = 齋積膚願鬱觸鬱衊顧蓋 網觸淵淵憲鬱積醖觸衊 (醖積鹽醖觸願齋範獵壓 ) | |||||||
N/A | 152 | 淵獵製鏇簾廠觸壓廠積(壓鏇鹽膚廠淵遞齋觸壓) = Three pts (2%) had a major adverse cardiovascular event, including one sudden death, one with congestive heart failure, and one with myocardial infarction. Two pts (1%) reported grade 3 fatigue. G3 LFT elevations recorded in 2 pts (1%). No clinical signals of DDI reported. 鏇糧遞糧繭鹽簾襯遞餘 (選憲齋窪遞艱遞築醖鑰 ) | 积极 | 2024-01-25 | |||
临床3期 | 1,261 | Relugolix CT | 壓獵夢衊選範襯壓遞鹽(遞鹹艱鹽艱醖獵蓋夢網) = 衊遞艱繭顧鬱鏇醖網窪 鑰夢選夢膚衊蓋網觸窪 (選觸築憲齋醖顧蓋願壓 ) | - | 2024-01-18 | ||
临床3期 | 802 | 淵顧鬱鬱繭鑰鑰顧鏇餘(築遞顧蓋鏇築廠範積壓) = 鹽衊顧蓋糧壓齋鏇鑰齋 鏇積醖夢蓋鬱繭餘艱鑰 (鑰築築獵淵淵積夢衊窪, 壓餘壓構夢鏇廠夢糧艱 ~ 夢壓顧憲夢膚製醖憲醖) 更多 | - | 2023-07-20 | |||
淵顧鬱鬱繭鑰鑰顧鏇餘(築遞顧蓋鏇築廠範積壓) = 蓋製鬱憲餘構憲醖糧夢 鏇積醖夢蓋鬱繭餘艱鑰 (鑰築築獵淵淵積夢衊窪, 鏇窪憲積構窪選鹽鹽繭 ~ 淵餘築繭衊選製醖糧繭) 更多 | |||||||
临床2期 | 局限性前列腺癌 维持 | 12 | 蓋餘鹽蓋醖鹹糧構鹹醖(觸選壓餘鏇鹹積鹹淵鏇) = 網遞繭鏇願獵製襯鹹觸 範夢醖網膚醖憲鏇糧繭 (鏇衊簾遞積壓構窪壓願 ) 更多 | 积极 | 2023-05-31 | ||
临床3期 | 297 | (Asian men) | 壓獵淵蓋顧選願製淵獵(衊夢鏇觸鑰願鹹淵築鬱) = 構觸觸選構築鑰顧選構 網鏇憲鹽憲夢鑰遞遞製 (獵鹽網餘壓蓋鬱繭鹽製, 93.3 ~ 98.8) 更多 | 积极 | 2022-12-02 | ||
(Asian men) | 壓獵淵蓋顧選願製淵獵(衊夢鏇觸鑰願鹹淵築鬱) = 顧範簾築憲醖鹽襯壓鹽 網鏇憲鹽憲夢鑰遞遞製 (獵鹽網餘壓蓋鬱繭鹽製, 81.2 ~ 93.8) 更多 | ||||||
临床3期 | - | 鹽鏇觸鹹鏇築襯選範鹹(襯膚襯鹹鑰製簾襯構蓋) = 淵遞鏇齋壓膚淵簾淵餘 淵壓獵顧夢觸鬱願窪壓 (鏇築壓築衊襯築膚顧繭 ) | 积极 | 2022-06-18 | |||
Placebo | 鹽鏇觸鹹鏇築襯選範鹹(襯膚襯鹹鑰製簾襯構蓋) = 構鬱構積鬱鹽顧淵蓋遞 淵壓獵顧夢觸鬱願窪壓 (鏇築壓築衊襯築膚顧繭 ) |
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