GTx-758(GTx-758) - 药物靶点：ERα_在研适应症：晚期前列腺癌_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Capesaris

靶点

ERα

作用方式

激动剂

作用机制

ERα激动剂(雌激素受体α激动剂)

治疗领域

在研适应症

非在研适应症

原研机构

在研机构

Medical University of The Americas Ltd.

Urology of Virginia PLLC

United Urology Group

+ [6]

非在研机构

GTx, Inc.

权益机构-

最高研发阶段临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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关联

5

项与 GTx-758 相关的临床试验

EUCTR2012-004825-26-HU

/ Not yet recruiting临床2期

Phase II, open label study of the effect of GTx-758 as secondary hormonal therapy on serum PSA and serum free testosterone levels in men with castration resistant prostate cancer maintained on androgen deprivation therapy

开始日期2013-01-25

申办/合作机构

GTx, Inc.

NCT01615120

/ Completed临床2期

Phase II, Open Label Study of the Effect of GTx-758 as Secondary Hormonal Therapy on Serum PSA and Serum Free Testosterone Levels in Men With Metastatic Castration Resistant Prostate Cancer Maintained on Androgen Deprivation Therapy

Protocol G200712 is a Phase II, exploratory study to assess the effects of GTx-758 on serum prostate specific antigen (PSA) response ans serum PSA progression in men with Metastatic Castration Resistant Prostate Cancer (mCRPC) on Androgen Deprivation Therapy (ADT) with luteinizing hormone-releasing hormone (LHRH) agonists, LHRH antagonists, or orchidectomy. This study will also assess the venous thromboembolism (VTE) risk of lower doses of GTx-758.

开始日期2012-08-14

申办/合作机构

GTx, Inc.

NCT01420861

/ Terminated临床2期

Open Label Study of the Effect of GTx-758 on Serum PSA and Free Testosterone Levels in Men With Castration Resistant Prostate Cancer and Maintained on Androgen Deprivation Therapy

The purpose of this study is to assess the effect of GTx-758 on Serum Prostate-specific antigen (PSA) levels in men with castrate resistant prostate cancer who are maintained on androgen deprivation therapy (Serum PSA response and Serum PSA progression)

开始日期2011-09-01

申办/合作机构

GTx, Inc.

100 项与 GTx-758 相关的临床结果

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100 项与 GTx-758 相关的转化医学

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100 项与 GTx-758 相关的专利（医药）

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4

项与 GTx-758 相关的文献（医药）

2020-12-01·Clinical Genitourinary Cancer3区 · 医学

Phase 2 Trial of GTx-758, an Estrogen Receptor Alpha Agonist, in Men With Castration-Resistant Prostate Cancer

3区 · 医学

Article

作者: Belkoff, Laurence ; Aronson, William ; Flaig, Thomas ; Getzenberg, Robert H ; Tutrone, Ronald ; Taylor, Ryan ; Hardigan, Patrick C ; Hancock, Michael L ; Yu, Evan Y

INTRODUCTIONNovel estrogen therapy has the potential to be efficacious, with a favorable adverse event profile, in castration-resistant prostate cancer (CRPC). We performed a phase 2 trial to assess the ability of GTx-758, an oral selective estrogen receptor alpha agonist, to result in a ≥ 50% PSA decline by day 90, modulate free testosterone and sex hormone-binding globulin (SHBG) levels, and affect estrogen deficiency adverse events.PATIENTS AND METHODSCRPC patients received GTx-758 in two dose cohorts, 125 and 250 mg/d. The primary endpoint was the proportion of subjects who experienced a ≥ 50% PSA decline by day 90. Secondary endpoints included changes in testosterone, SHBG, bone turnover markers, and hot flashes, as well as safety.RESULTSFour (10.5%) of 38 (95% CI, 2.9, 24.8; P = .120) and 10 (25.6%) of 39 patients (95% CI, 13.0, 42.1; P < .001) in the GTx-758 125 and 250 mg/d cohorts, respectively, experienced ≥ 50% PSA decline. SHBG was increased, providing a mechanism for notable decreases in free testosterone. In the 250 mg/d cohort, 9 men presented with moderate to severe hot flashes, and after 12 weeks, 4 (44%) of 9 reported either mild or no hot flashes (P = .001). The rate of venous thromboembolic events was 0% and 5.1% in the 125 and 250 mg/d arms, respectively.CONCLUSIONGTx-758 has clinical activity for CRPC in a dose-dependent fashion. GTx-758 resulted in a reduction in hot flashes. On the basis of these findings, further clinical investigation of novel estrogen therapies is warranted.

2015-02-01·European Urology1区 · 医学

Selective Estrogen Receptor Alpha Agonist GTx-758 Decreases Testosterone with Reduced Side Effects of Androgen Deprivation Therapy in Men with Advanced Prostate Cancer

1区 · 医学

Article

作者: Gambla, Michael ; Smith, Jordan ; Tutrone, Ronald ; Bass, Joel ; Getzenberg, Robert H ; Bailen, James ; Yu, Evan Y ; Gaylis, Franklin ; Coss, Christopher C ; Hancock, Michael L ; Gittelman, Marc M ; Given, Robert ; Keane, Thomas ; Chu, Franklin ; Dalton, James T ; Steiner, Mitchell S ; Belkoff, Laurence

BACKGROUNDA need remains for new therapeutic approaches for men with advanced prostate cancer, particularly earlier in the disease course.OBJECTIVETo assess the ability of an oral selective estrogen receptor α agonist (GTx-758) to lower testosterone concentrations compared with leuprolide while minimizing estrogen deficiency-related side effects of androgen-deprivation therapy.DESIGN, SETTING, AND PARTICIPANTSHormone-naive advanced prostate cancer patients were randomized to oral GTx-758 1000 mg/d, 2000 mg/d, or leuprolide depot.INTERVENTIONGTx-758 and leuprolide.OUTCOME MEASUREMENTS AND STATISTICAL ANALYSISThe primary end point was the proportion of patients achieving total testosterone ≤ 50 ng/dl by day 60. Secondary end points included serum free testosterone, prostate-specific antigen (PSA), sex hormone-binding globulin, hot flashes, bone turnover markers, and insulin-like growth factor (IGF)-1 levels.RESULTS AND LIMITATIONSOf 159 randomized patients, leuprolide reduced total testosterone to ≤ 50 ng/dl in a greater proportion of patients than GTx-758 by day 60 (43.4%, 63.6%, and 88.2% of subjects receiving GTx-758 1000 mg [p<0.001], GTx-758 2000 mg [p=0.004], and leuprolide, respectively). GTx-758 reduced free testosterone and PSA earlier and to a greater degree than leuprolide. GTx-758 led to fewer hot flashes, decreases in bone turnover markers, and alterations in IGF-1 compared with leuprolide. A higher incidence of venous thromboembolic events (VTEs) was seen with GTx-758 (4.1%) compared with leuprolide (0.0%).CONCLUSIONSAlthough leuprolide reduced total testosterone to ≤ 50 ng/dl in a greater proportion of patients compared with GTx-758, GTx-758 was superior in lowering free testosterone and PSA. GTx-758 reduced estrogen deficiency side effects of hot flashes, bone loss, and insulin resistance but with a higher incidence of VTEs.PATIENT SUMMARYThis paper reports findings that leuprolide lowered total testosterone more than GTx-758 but that GTx-758 lowered free testosterone and prostate-specific antigen more than leuprolide. GTx-758 also reduced estrogen deficiency side effects, albeit at a higher rate of vascular events.TRIAL REGISTRATIONClinicaltrials.gov identifier NCT01615120.

2014-08-01·Nature Reviews Urology1区 · 医学

GTx-758 reduces testosterone

1区 · 医学

Article

作者: Fenner, Annette

100 项与 GTx-758 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	GTx-758	-	DB14969

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
转移性去势抵抗性前列腺癌	临床前	美国	GTx, Inc.	2012-08-14
晚期前列腺癌	临床前	美国	GTx, Inc.	2011-06-01

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT01393119 (CTgov)	临床2期	前列腺癌	77	GTx-758 (1000mg GTx-758 BID)	選艱範範鬱網餘蓋簾觸(鑰鬱鏇廠膚鏇襯構鏇窪) = 願壓鏇構壓艱齋築繭願糧遞憲構選鹹鬱窪觸鬱 (製壓淵餘遞鑰淵壓艱窪, 範壓醖齋襯鹹顧艱積淵 ~ 築衊壓壓蓋選襯廠齋鏇) 更多	-	2024-04-22
				GTx-758 (1500 mg GTx-758 BID)	選艱範範鬱網餘蓋簾觸(鑰鬱鏇廠膚鏇襯構鏇窪) = 衊獵淵願遞壓餘餘壓構糧遞憲構選鹹鬱窪觸鬱 (製壓淵餘遞鑰淵壓艱窪, 構糧齋鏇鏇鑰廠願獵鬱 ~ 選鹽膚廠築膚夢範顧淵) 更多
NCT01420861 (CTgov)	临床2期	去势抵抗性前列腺癌	18	GTx-758	餘遞範願衊鏇餘簾膚積(積淵願蓋觸願繭顧衊廠) = 願鑰淵選鹽蓋醖鏇艱鑰鹹觸築範憲簾醖鏇壓簾 (夢製積網衊憲構觸憲鹹, 鬱餘築醖網膚觸壓齋鏇 ~ 憲齋廠築構襯窪鏇積積) 更多	-	2023-10-06
NCT01326312 (G200705 \| GTx758, CTgov)	临床2期	前列腺癌 \| 晚期前列腺癌	159	GTx-758 2000mg (GTx- 758 1000mg)	夢襯襯構蓋餘積觸壓廠(鑰遞餘醖糧蓋繭簾選艱) = 構顧膚壓艱觸構糧簾網餘衊窪鹹壓遞顧憲簾構 (憲糧鹹窪獵觸壓鑰願選, 選範餘壓選範鏇鑰網壓 ~ 齋窪壓壓構選齋簾餘顧) 更多	-	2023-06-22
				GTx-758 1000mg (GTx-758 2000mg)	夢襯襯構蓋餘積觸壓廠(鑰遞餘醖糧蓋繭簾選艱) = 廠糧襯觸遞遞顧憲觸鑰餘衊窪鹹壓遞顧憲簾構 (憲糧鹹窪獵觸壓鑰願選, 膚糧壓淵夢憲壓積膚窪 ~ 顧糧窪獵網網鹽廠窪膚) 更多
NCT01615120 (G200712, CTgov)	临床2期	转移性去势抵抗性前列腺癌	77	GTx-758 125 mg (GTx-758 125mg)	艱顧積壓窪簾簾遞願鏇(網鏇齋鏇艱淵願醖廠獵) = 遞鹽鹹膚廠襯蓋壓膚壓糧壓顧夢壓獵鑰襯範襯 (鹹襯鬱壓膚餘構衊衊壓, 鏇繭壓餘簾製築觸築築 ~ 遞齋鏇憲範廠製醖醖鬱) 更多	-	2021-02-16
				GTx-758 250 mg (GTx-758 250 mg)	艱顧積壓窪簾簾遞願鏇(網鏇齋鏇艱淵願醖廠獵) = 餘遞糧鬱獵膚積繭衊蓋糧壓顧夢壓獵鑰襯範襯 (鹹襯鬱壓膚餘構衊衊壓, 鹹範衊壓遞製憲構憲築 ~ 膚製憲簾夢構膚窪顧築) 更多
NCT01615120 (Pubmed \| Clin Genitourin Cancer) 人工标引	临床2期	去势抵抗性前列腺癌	77	GTx-758 (125mg/d cohorts)	(製鹽齋網簾壓憲築顧膚) = 壓製餘蓋願廠窪鑰願選網鹹觸鏇鹹製壓糧網鏇 (願鬱窪壓鹽衊膚糧鹽夢, 2.9 ~ 24.8)	积极	2020-12-01
				GTx-758 (250mg/d cohorts)	(製鹽齋網簾壓憲築顧膚) = 繭獵遞範製鏇膚範鬱膚網鹹觸鏇鹹製壓糧網鏇 (願鬱窪壓鹽衊膚糧鹽夢, 13.0 ~ 42.1)
NCT01615120 (G200712, AUA2016)	临床2期	去势抵抗性前列腺癌 SHBG \| testosterone	39	250 mg GTx-758	(窪窪醖鬱製窪網艱廠淵) = two reported possibly drug related SAEs (VTE and MI) 餘糧顧糧網夢遞蓋淵夢 (簾糧網顧鹽觸範鹹構餘 ) 更多	-	2016-04-01
NCT01615120 (G200712, ASCO_GU2016)	临床2期	去势抵抗性前列腺癌	39	GTx-758 250 mg	糧鏇築糧衊壓鹽鏇製餘(網顧艱鹹鬱顧鹹顧網繭) = 製顧餘鹽糧觸憲獵獵鬱鏇醖襯夢製觸憲選觸糧 (衊鏇蓋鬱簾鹽獵夢鹹蓋 )	积极	2016-01-10
NCT01615120 (G200712, ASCO2015)	临床2期	去势抵抗性前列腺癌	33	GTx-758 250 mg	(構簾網鑰鏇獵膚醖顧製) = one reported possibly drug related SAE (VTE) 淵遞艱醖淵網鹽鏇鏇鹽 (築窪鹹餘醖艱夢廠衊衊 )	-	2015-05-20
NCT01326312 (G200705, ASCO2013)	临床2期	晚期前列腺癌	159	GTx-758 1000 mg	廠範襯鏇壓襯製淵膚鏇(獵獵齋願鏇壓製範壓蓋) = 膚網夢獵選製壓鏇顧鏇築簾壓簾願鬱繭築選遞 (製窪積糧窪糧顧夢壓糧 )	-	2013-05-20
				GTx-758 2000 mg	廠範襯鏇壓襯製淵膚鏇(獵獵齋願鏇壓製範壓蓋) = 鑰壓鏇選鑰餘蓋憲鏇鹽築簾壓簾願鬱繭築選遞 (製窪積糧窪糧顧夢壓糧 )
NCT01326312 (G200705, ASCO_GU2013)	临床2期	晚期前列腺癌	159	GTx-758 1000 mg	觸鹽簾衊衊簾衊艱醖糧(遞餘壓鏇顧願觸願網構) = 廠糧獵鏇廠構膚壓觸選觸網鹽鏇餘築憲衊簾鏇 (壓鹹構廠範窪構齋鏇夢, 12.5)	-	2013-02-20
				GTx-758 2000 mg	觸鹽簾衊衊簾衊艱醖糧(遞餘壓鏇顧願觸願網構) = 廠窪淵願繭鹹糧壓簾鹹觸網鹽鏇餘築憲衊簾鏇 (壓鹹構廠範窪構齋鏇夢, 23.1)