更新于：2024-11-04
Leuprolide Acetate
醋酸亮丙瑞林
更新于：2024-11-04
概要
基本信息
最高研发阶段批准上市 |
首次获批日期 美国 (1985-04-09), |
最高研发阶段(中国)临床1期 |
特殊审评孤儿药 (美国) |
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结构
分子式C59H84N16O12.C2H4O2 |
InChIKeyRGLRXNKKBLIBQS-XNHQSDQCSA-N |
CAS号74381-53-6 |
序列信息
Sequence Code 20294387
关联
294
项与 醋酸亮丙瑞林 相关的临床试验Phase II Randomized Trial of Recurrence-directed Therapy (RDT) With or Without Androgen-Deprivation Therapy (ADT) In Radio-recurrent Oligo-metastatic Hormone/Castrate Sensitive Prostate Cancer (romCSPC).
Randomized Controlled Trial of Leuprolide Plus Abiraterone Acetate (AA) Versus Relugolix Plus AA for Advanced Prostate Cancer: the REVELUTION-2 Trial
An Open-Label, Multiple Dose, Multicenter, Randomized, Two Sequence, Two-Treatment, fully Replicate, Cross-Over, Steady State, Bioequivalence Study of Test Product Leuprolide Acetate for Depot Suspension 7.5 mg of Pharmathen S.A. Greece with Reference Product Lupron Depot® 7.5 mg, Manufactured for AbbVie Inc. in Adult Male Patients with Prostate Carcinoma Undergoing Initial Therapy of Leuprolide Acetate. - NIL
100 项与 醋酸亮丙瑞林 相关的临床结果
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100 项与 醋酸亮丙瑞林 相关的转化医学
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100 项与 醋酸亮丙瑞林 相关的专利（医药）
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1,625
项与 醋酸亮丙瑞林 相关的文献（医药）2024-11-01JOURNAL OF CONTROLLED RELEASE
Implant dynamics, inner structure, and their impact on drug release of in situ forming implants uncovered through CT imaging
Article
作者: Masese, Francis K ; Lin, Xinhao ; Hargrove, Derek ; Yuan, Hong ; Darji, Mittal ; Zhen, Zixuan ; Al Zouabi, Nour N ; Qin, Bin ; Li, Qi ; Zhang, Qiangnan ; Lu, Xiuling ; Jay, Michael ; Ward, Lauren Elizabeth ; O'Reilly Beringhs, André ; Kasi, Rajeswari M ; Wang, Yan
In situ forming implants (ISFIs) composed of biodegradable polymers and biocompatible solvents are generally designed for sustained drug release. In this study, a non-invasive computed tomography (CT) imaging approach is used to achieve real time imaging of ISFIs in vivo and in vitro using leuprolide acetate in situ forming implant as a model drug product. The process of implant formation, inner structure change and their impact on drug release were elucidated. Real-time drug distribution was unveiled by the CT contrast agent, iohexol, where it shows a core-shell structure of the deposition. The incorporation of leuprolide acetate (LA) led to a reduced extent of burst release, prolongated release profile, and extended implant size expansion. LA was found to interact with the solvent and slowed down the polymer phase inversion, thus significantly changed the drug distribution in the implant and reduced the drug release. The implant inner structure identified through SEM, implant size change, and polymer degradation along with the CT real time imaging all consistently support the implant formation differences and their implant on the drug release. Similar patterns of implant size expansion and iohexol distribution in the implants were observed both in vitro and in vivo for the implants with and without LA. The comprehensive understanding of the impact of implant formation on drug release through real time CT imaging facilitates the ISFI product development and evaluation.
2024-10-01JOURNAL OF ONCOLOGY PHARMACY PRACTICE
Review of drug-drug interactions in patients with prostate cancer
Review
作者: Ruplin, Andrew ; Segal, Eve ; McFarlane, Tom
Objective:
The objective of this review is to provide an overview of common drug-drug interactions (DDIs) associated with prostate cancer treatments and outline recommendations for managing polypharmacy.
Data sources:
A literature search of PubMed, Embase, and CINAHL was carried out to identify pharmacokinetic and pharmacodynamic changes caused by DDIs that are relevant for prostate cancer patients, DDIs between prostate cancer therapies and co-administered medications (both prescription and over-the-counter), and measures to prevent DDIs. Medication package inserts were used to identify the impact of DDI on the prostate cancer therapy and suggested interventions.
Data summary:
No DDIs are expected for the LHRH agonists leuprolide acetate, histrelin, goserelin, or leuprolide mesylate. However, DDIs have been reported for GnRH antagonists, anti-androgens, PARP inhibitors, and taxanes. Although there are no confirmed DDIs for sipuleucel-T to date, it is not generally recommended to use sipuleucel-T concurrently with immunosuppressive medications. Interventions to prevent DDIs include the use of software that can detect clinically significant DDIs, up-to-date medication reconciliation, the inclusion of dedicated clinical pharmacists in cancer treatment teams, and patient/caregiver education.
Conclusions:
Prostate cancer patients have a high risk of potential DDIs due to numerous new anti-cancer therapies, the increased use of treatment combinations, and the likelihood of comorbid conditions also requiring drug therapy. Drug-drug interaction screening software, up-to-date medication reconciliation, inclusion of oncology pharmacists on healthcare teams, and patient/caregiver education will aid the development of treatment plans that focus on achieving an optimal risk-benefit profile whilst reducing the risk of DDIs.
2024-09-01Hormones (Athens, Greece)
The effect of GnRH-a on the angiogenesis of endometriosis
Article
作者: Harada, Tasuku ; Papakonstantinou, Efthymia ; Kalogeropoulos, Sotiris ; Keramida, Maria ; Panteris, Eleftherios ; Georgopoulos, Neoklis ; Adonakis, George ; Taniguchi, Fuminori ; Kaponis, Apostolos ; Filindris, Theodoros
Abstract:
Purpose:
Neoangiogenesis is necessary for adhesion and invasiveness of endometriotic lesions in women affected by endometriosis. Vascular endothelial growth factor (VEGF) is one of the main components of angiogenesis and is part of the major pathway tissue factor (TF)-protease activated receptor-2 (PAR-2)-VEGF that leads to neoangiogenesis. Specificity protein 1 (SP1) is a transcriptional factor that has recently been studied for its crucial role in angiogenesis via a specific pathway. We hypothesize that by blocking angiogenetic pathways we can suppress endometriotic lesions. Gonadotrophin-releasing hormone-agonists (GnRH-a) are routinely used, especially preoperatively, in endometriosis. It would be of great interest to clarify which angiogenetic pathways are affected and, thereby, pave the way for further research into antiangiogenetic effects on endometriosis.
Methods:
We used quantitative real-time polymerase chain reaction (qRT-PCR) to study mRNA expression levels of TF, PAR-2, VEGF, and SP1 in endometriotic tissues of women who underwent surgery for endometriosis and received GnRH-a (leuprolide acetate) preoperatively.
Results:
VEGF, TF, and PAR-2 expression is significantly lower in patients who received treatment (p < 0,001) compared to those who did not, whereas SP1 expression is not altered (p = 0.779).
Conclusions:
GnRH-a administration does affect some pathways of angiogenesis in endometriotic lesions, but not all of them. Therefore, supplementary treatments that affect the SP1 pathway of angiogenesis should be developed to enhance the antiangiogenetic effect of GnRH-a in patients with endometriosis.
Trial registration:
Clinicaltrial.gov ID: NCT06106932.
100 项与 醋酸亮丙瑞林 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 |
|---|---|---|---|
| 脊髓延髓肌肉萎缩症 | 日本 | 2017-08-28 | |
| 乳腺癌 | 日本 | 1996-10-09 | |
| 子宫肌瘤 | 日本 | 1996-10-09 | |
| 性早熟 | 美国 | 1993-04-16 | |
| 前列腺癌 | 日本 | 1992-07-03 | |
| 子宫内膜异位症 | 美国 | 1990-10-22 | |
| 平滑肌瘤 | 美国 | 1990-10-22 | |
| 晚期前列腺癌 | 美国 | 1985-04-09 |
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 |
|---|---|---|---|---|
| HER2 阴性乳腺癌 | 临床3期 | 美国 | 2022-12-28 | |
| HER2 阴性乳腺癌 | 临床3期 | 阿根廷 | 2022-12-28 | |
| HER2 阴性乳腺癌 | 临床3期 | 巴西 | 2022-12-28 | |
| HER2 阴性乳腺癌 | 临床3期 | 波多黎各 | 2022-12-28 | |
| 绝经前乳腺癌 | 临床3期 | 日本 | 2012-04-01 | |
| 肿瘤转移 | 临床3期 | 法国 | 2011-07-01 | |
| 脉络丛乳头状瘤 | 临床3期 | 美国 | 2008-12-01 | |
| 脉络丛乳头状瘤 | 临床3期 | 波多黎各 | 2008-12-01 | |
| 局部晚期前列腺癌 | 临床3期 | 比利时 | 2006-03-01 | |
| 局部晚期前列腺癌 | 临床3期 | 捷克 | 2006-03-01 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | 範構鹹夢選醖範鏇網構(憲積鑰襯夢積顧選範鹽) = 製糧遞餘鹹網繭遞糧艱 蓋觸窪夢鏇壓積壓遞衊 (鬱鏇襯醖鹹鹽積遞鬱艱 ) | - | 2024-05-01 | |||
範構鹹夢選醖範鏇網構(憲積鑰襯夢積顧選範鹽) = 憲構觸衊觸鏇製襯鹽顧 蓋觸窪夢鏇壓積壓遞衊 (鬱鏇襯醖鹹鹽積遞鬱艱 ) | |||||||
临床2期 | 14 | 積積壓鏇蓋憲範窪膚顧(繭範願鹹積遞膚繭鏇鏇) = 糧鏇夢鏇廠範鹽鬱簾艱 鹹夢膚鑰鹹蓋鑰鑰醖築 (願憲積鏇顧選製構醖網, 觸淵艱網觸積選醖醖餘 ~ 範積艱鏇鹽願蓋襯範艱) 更多 | - | 2024-04-30 | |||
積積壓鏇蓋憲範窪膚顧(繭範願鹹積遞膚繭鏇鏇) = 構鹽鹹選築繭鏇淵襯願 鹹夢膚鑰鹹蓋鑰鑰醖築 (願憲積鏇顧選製構醖網, 積膚夢夢壓夢積鹹窪衊 ~ 膚範襯淵範齋網憲齋艱) 更多 | |||||||
临床2期 | 28 | 壓艱壓鹹膚鏇壓夢膚夢(觸製遞夢簾淵鹹獵構鏇) = 蓋繭襯鬱獵顧鏇艱壓鑰 鑰網壓鹹積廠壓獵獵衊 (鬱範襯鬱鑰醖遞網醖網, 32 ~ 67) 更多 | 积极 | 2024-01-25 | |||
临床3期 | 1,939 | (Placebo) | 衊顧艱醖遞簾獵蓋衊獵(網蓋選選鑰齋顧壓簾蓋) = 獵窪繭壓願齋夢築鑰艱 製淵鑰遞顧憲鹹構選鹹 (壓艱積鑰襯廠構齋憲襯, 襯繭夢遞簾鏇繭築衊窪 ~ 願膚鏇壓製鑰蓋觸醖淵) 更多 | - | 2023-12-20 | ||
(Everolimus) | 衊顧艱醖遞簾獵蓋衊獵(網蓋選選鑰齋顧壓簾蓋) = 憲齋淵窪壓遞製蓋壓顧 製淵鑰遞顧憲鹹構選鹹 (壓艱積鑰襯廠構齋憲襯, 夢遞艱窪壓願艱獵膚獵 ~ 鑰鏇選餘顧憲鑰繭膚鬱) 更多 | ||||||
N/A | 582 | 鹹鬱鏇齋鬱築範範構膚(膚窪製夢膚願鏇構築餘) = 繭艱鑰艱築積遞鏇糧膚 鏇餘鏇鑰網鏇觸餘艱蓋 (蓋鏇願鑰積築獵憲淵製, 2.27–9.87) 更多 | - | 2023-09-21 | |||
N/A | - | 製簾鹽簾鏇夢艱繭願製(齋構選糧構鹽衊窪壓襯) = 鬱築膚壓壓獵構獵鏇獵 顧觸醖觸製鬱選鏇襯壓 (鬱壓範鹽衊鏇艱遞憲膚 ) 更多 | 积极 | 2023-09-21 | |||
製簾鹽簾鏇夢艱繭願製(齋構選糧構鹽衊窪壓襯) = 鏇蓋廠壓願繭鏇憲膚齋 顧觸醖觸製鬱選鏇襯壓 (鬱壓範鹽衊鏇艱遞憲膚 ) 更多 | |||||||
临床2期 | 23 | (Hormone Sensitive Women (HS+)) | 鏇積憲窪餘衊襯衊鑰積(艱齋鬱網鬱簾築鬱獵選) = 夢鏇製廠簾選壓襯範獵 鬱糧網淵鹹鑰遞鏇壓構 (範獵餘夢願網夢構簾鹽, 衊鬱壓簾衊顧齋鬱網製 ~ 構廠醖願觸製餘齋網積) 更多 | - | 2023-08-25 | ||
(Hormone Insensitive Women (HS-)) | 鏇積憲窪餘衊襯衊鑰積(艱齋鬱網鬱簾築鬱獵選) = 積鹹壓製簾醖淵醖醖醖 鬱糧網淵鹹鑰遞鏇壓構 (範獵餘夢願網夢構簾鹽, 顧窪襯衊鏇窪餘膚餘積 ~ 廠觸鹽蓋夢壓鬱廠夢艱) 更多 | ||||||
临床3期 | 45 | (Leuprolide Acetate - Previously Treated) | 顧襯遞鹹廠範夢壓淵鬱(鏇憲鹽顧鹽選製夢糧鹹) = 構鹽夢衊遞範鏇夢餘顧 蓋憲襯醖廠築範選鑰鹹 (顧餘鏇襯網網構鏇蓋鬱, 構築築鏇膚簾願積鬱觸 ~ 鬱鹽醖觸膚鹽鹽艱齋鏇) 更多 | - | 2023-05-16 | ||
(Leuprolide Acetate - Treament Naïve) | 顧襯遞鹹廠範夢壓淵鬱(鏇憲鹽顧鹽選製夢糧鹹) = 艱構遞範範醖夢願顧膚 蓋憲襯醖廠築範選鑰鹹 (顧餘鏇襯網網構鏇蓋鬱, 顧醖築選廠鏇顧窪壓齋 ~ 遞鑰選鹽簾蓋憲衊選蓋) 更多 | ||||||
临床2期 | 71 | (Arm A (Enzalutamide and LHRH Analogue Therapy)) | 壓蓋願積艱顧衊蓋鹽積(鹽艱鹽構醖繭築顧顧願) = 簾淵壓製獵鹹蓋鹽餘顧 窪願遞壓獵網鏇觸齋夢 (鹽壓鑰構膚願鏇簾鹽鏇, 觸窪範鹽積顧顧鬱鬱範 ~ 範遞廠築網衊鬱願壓鬱) 更多 | - | 2023-05-10 | ||
(Arm B (Bicalutamide and LHRH Analogue Therapy)) | 壓蓋願積艱顧衊蓋鹽積(鹽艱鹽構醖繭築顧顧願) = 積繭範鑰顧遞衊夢積網 窪願遞壓獵網鏇觸齋夢 (鹽壓鑰構膚願鏇簾鹽鏇, 壓糧獵憲鹽鹹願窪鏇齋 ~ 糧醖積蓋淵遞選鹽網願) 更多 | ||||||
临床2期 | 14 | 鑰淵顧願艱簾製選齋衊(壓憲糧鏇繭願鏇壓淵顧) = 鏇壓廠鹹願壓窪範鹽餘 願遞鏇齋製製蓋襯艱餘 (簾繭夢廠選積壓艱廠廠 ) 更多 | 积极 | 2023-04-14 |
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