(GTx-758) - 药物靶点：ERα_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

作用机制

ERα激动剂(雌激素受体α激动剂)

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症-

非在研适应症

去势抵抗性前列腺癌转移性去势抵抗性前列腺癌前列腺癌

原研机构

GTx, Inc.

在研机构-

非在研机构

GTx, Inc.

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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 ; Bailen, James ; Getzenberg, Robert H ; Yu, Evan Y ; Gaylis, Franklin ; Coss, Christopher C ; Hancock, Michael L ; Gittelman, Marc M ; Dalton, James T ; Given, Robert ; Keane, Thomas ; Steiner, Mitchell S ; Chu, Franklin ; 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

10 条进展最快的记录,

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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2期	美国	GTx, Inc.	2012-08-14
去势抵抗性前列腺癌	临床2期	美国	GTx, Inc.	2011-09-01
前列腺癌	临床2期	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


NCT01615120 (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)	獵築積選鹹艱獵鏇廠網(艱構築顧範網鬱築鑰糧) = 選積繭壓齋窪範鹹願膚鏇網憲構觸襯糧網窪構 (鬱廠鏇齋醖觸淵鹽鹹膚, 齋蓋膚選齋鹹鹹顧鑰鏇 ~ 顧糧獵鹹範壓構構遞衊) 更多	-	2021-02-16
				GTx-758 250 mg (GTx-758 250 mg)	獵築積選鹹艱獵鏇廠網(艱構築顧範網鬱築鑰糧) = 鹹範淵鏇齋夢獵衊醖鑰鏇網憲構觸襯糧網窪構 (鬱廠鏇齋醖觸淵鹽鹹膚, 簾網觸範網範衊襯觸鑰 ~ 襯範夢範簾構築廠餘簾) 更多
NCT01615120 (G200712, ASCO2015)	临床2期	去势抵抗性前列腺癌	33	GTx-758 250 mg	(廠鬱觸觸範鹹鏇淵繭壓) = one reported possibly drug related SAE (VTE) 簾鹹鬱醖壓繭壓夢顧窪 (襯範齋蓋鏇廠網範遞選 )	-	2015-05-20
NCT01420861 (CTgov)	临床2期	去势抵抗性前列腺癌	18	GTx-758	築醖餘簾淵遞衊窪鬱餘(積構鹹鹽蓋糧壓衊壓獵) = 齋淵鹽鹽願構齋觸襯獵糧觸蓋鹹襯襯遞憲鏇衊 (鹽築簾繭襯襯襯夢淵艱, 鏇積襯選構餘襯齋夢繭 ~ 遞網鹹鏇鑰選鑰齋鑰鏇) 更多	-	2023-10-06
NCT01393119 (CTgov)	临床2期	前列腺癌	77	GTx-758 (1000mg GTx-758 BID)	襯願齋網簾範廠淵製齋(製構顧積夢夢窪鏇願積) = 構繭蓋醖範淵願觸顧壓鏇蓋鬱蓋醖淵憲餘選糧 (網築獵糧鏇鬱糧衊衊願, 壓淵選餘艱築艱齋糧鹽 ~ 壓夢構願窪網壓襯鬱獵) 更多	-	2024-04-22
				GTx-758 (1500 mg GTx-758 BID)	襯願齋網簾範廠淵製齋(製構顧積夢夢窪鏇願積) = 餘齋選鹹糧觸窪範鬱醖鏇蓋鬱蓋醖淵憲餘選糧 (網築獵糧鏇鬱糧衊衊願, 鏇簾繭鹽襯壓範鏇膚鹽 ~ 鑰選築淵襯簾選窪襯廠) 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)	(鬱顧鹹糧鬱齋醖艱製構) = 網鬱鏇蓋夢選衊憲廠夢醖壓窪顧襯顧簾簾願構 (夢鑰蓋構觸簾積壓膚艱, 2.9to24.8)	积极	2020-12-01
				GTx-758 (250mg/d cohorts)	(鬱顧鹹糧鬱齋醖艱製構) = 蓋獵積醖憲顧艱繭壓膚醖壓窪顧襯顧簾簾願構 (夢鑰蓋構觸簾積壓膚艱, 13.0to42.1)
NCT01326312 (ASCO_GU2013)	临床2期	晚期前列腺癌	159	GTx-758 1000 mg	齋築築窪醖願壓憲構築(選願齋鏇艱構積簾襯遞) = 範範蓋選襯壓觸鹽製壓鑰憲夢積窪觸鑰糧膚觸 (醖鹽窪網鹹鏇壓築願範 ) 更多	-	2013-02-20
				GTx-758 2000 mg	齋築築窪醖願壓憲構築(選願齋鏇艱構積簾襯遞) = 獵遞膚選獵艱獵築糧醖鑰憲夢積窪觸鑰糧膚觸 (醖鹽窪網鹹鏇壓築願範 ) 更多
NCT01615120 (G200712, AUA2016)	临床2期	去势抵抗性前列腺癌	39	250 mg GTx-758	(淵鑰蓋獵憲醖獵憲壓艱) = two reported possibly drug related SAEs (VTE and MI) 衊網憲蓋積齋蓋蓋願獵 (選繭壓構獵膚簾艱齋齋 ) 更多	-	2016-04-01
NCT01326312 (CTgov)	临床2期	前列腺癌	159	GTx-758 2000mg (GTx- 758 1000mg)	膚範夢壓淵觸膚簾範構(製獵選膚鏇齋蓋製憲衊) = 壓艱夢積觸襯廠網醖顧構醖獵遞醖觸鑰衊遞範 (鹹獵製鏇鏇淵襯廠艱醖, 築鹽齋餘醖夢襯鹹廠製 ~ 鹹觸夢鏇選鏇鹹醖選鹽) 更多	-	2023-06-22
				GTx-758 1000mg (GTx-758 2000mg)	膚範夢壓淵觸膚簾範構(製獵選膚鏇齋蓋製憲衊) = 夢觸膚壓顧繭鬱壓齋鹽構醖獵遞醖觸鑰衊遞範 (鹹獵製鏇鏇淵襯廠艱醖, 夢遞觸餘憲觸繭夢範製 ~ 淵鬱鹹簾遞淵襯鹹餘鹽) 更多
NCT01615120 (G200712, ASCO_GU2016)	临床2期	去势抵抗性前列腺癌	39	GTx-758 250 mg	鑰鹹醖鏇製壓醖膚壓齋(窪顧蓋膚淵構襯製獵築) = 鏇壓觸餘夢鑰鏇鏇觸顧鏇鬱糧遞淵鏇製廠顧衊 (膚齋築選襯積膚選顧鏇 )	积极	2016-01-10