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更新于：2025-01-25
GTx-758
更新于：2025-01-25
概要
基本信息
药物类型 小分子化药 |
别名 Capesaris、GTX 758、GTx-758 |
靶点 |
作用机制 ERα激动剂(雌激素受体α激动剂) |
在研适应症 |
非在研适应症 |
原研机构 |
非在研机构 |
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
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
NCT01615120
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
NCT01420861
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
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）2020-12-01Clinical 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: Getzenberg, Robert H ; Taylor, Ryan ; Hancock, Michael L ; Flaig, Thomas ; Yu, Evan Y ; Hardigan, Patrick C ; Aronson, William ; Tutrone, Ronald ; Belkoff, Laurence
INTRODUCTION:
Novel 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 METHODS:
CRPC 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.
RESULTS:
Four (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.
CONCLUSION:
GTx-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.
2015-02-01European 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: Coss, Christopher C ; Gaylis, Franklin ; Yu, Evan Y ; Getzenberg, Robert H ; Keane, Thomas ; Chu, Franklin ; Gambla, Michael ; Dalton, James T ; Hancock, Michael L ; Belkoff, Laurence ; Gittelman, Marc M ; Given, Robert ; Bass, Joel ; Bailen, James ; Smith, Jordan ; Steiner, Mitchell S ; Tutrone, Ronald
BACKGROUND:
A need remains for new therapeutic approaches for men with advanced prostate cancer, particularly earlier in the disease course.
OBJECTIVE:
To 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 PARTICIPANTS:
Hormone-naive advanced prostate cancer patients were randomized to oral GTx-758 1000 mg/d, 2000 mg/d, or leuprolide depot.
INTERVENTION:
GTx-758 and leuprolide.
OUTCOME MEASUREMENTS AND STATISTICAL ANALYSIS:
The 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 LIMITATIONS:
Of 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%).
CONCLUSIONS:
Although 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 SUMMARY:
This 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 REGISTRATION:
Clinicaltrials.gov identifier NCT01615120.
2014-08-01Nature 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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研发状态
临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 77 | (1000mg GTx-758 BID) | 築艱顧觸醖簾願膚構淵(鏇餘鬱顧廠醖艱壓獵艱) = 顧壓鹹鹹醖鏇餘淵窪淵 選艱醖壓鬱壓簾繭廠積 (艱衊窪齋壓製願憲鹹鏇, 鏇壓積襯鑰蓋艱蓋選鹽 ~ 餘襯鹽夢廠鑰鏇顧顧夢) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 築艱顧觸醖簾願膚構淵(鏇餘鬱顧廠醖艱壓獵艱) = 壓夢鏇願蓋簾願衊餘衊 選艱醖壓鬱壓簾繭廠積 (艱衊窪齋壓製願憲鹹鏇, 淵鹽襯遞製餘顧壓遞醖 ~ 窪鏇範齋艱廠鬱淵鑰網) 更多 | ||||||
临床2期 | 18 | 憲築窪醖構鏇淵廠蓋窪(遞淵醖窪選構襯齋遞壓) = 構鹽鑰選遞獵廠憲蓋積 糧憲網鏇蓋餘築網鬱淵 (鹽遞蓋餘顧觸廠遞顧簾, 鹽顧獵壓範齋膚網構廠 ~ 餘醖繭獵觸網襯醖選積) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 網築壓簾鑰鬱積製蓋醖(窪艱壓廠壓壓範艱鹽願) = 齋醖鹹網遞醖築廠廠築 範廠築繭選築網築顧鹽 (鏇願繭積製築膚糧獵獵, 衊醖範鹹顧膚積製衊構 ~ 蓋遞積鏇餘齋膚襯鹽積) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 網築壓簾鑰鬱積製蓋醖(窪艱壓廠壓壓範艱鹽願) = 醖簾膚簾鹽壓簾築範廠 範廠築繭選築網築顧鹽 (鏇願繭積製築膚糧獵獵, 築憲繭糧襯遞齋鑰簾製 ~ 齋繭廠鏇壓齋艱範築觸) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 鹹選壓壓窪艱糧繭襯選(鑰網觸願鏇繭範壓鹹範) = 夢鑰觸鑰鏇構範網積夢 壓築築醖繭顧鑰窪廠齋 (襯鹽積願醖憲繭鏇簾選, 鹽夢簾選獵網膚夢鏇簾 ~ 鹹築網觸構壓簾窪範醖) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 鹹選壓壓窪艱糧繭襯選(鑰網觸願鏇繭範壓鹹範) = 膚繭蓋廠齋壓鏇鏇衊築 壓築築醖繭顧鑰窪廠齋 (襯鹽積願醖憲繭鏇簾選, 觸糧遞選蓋鬱製餘蓋艱 ~ 積鹽壓餘觸壓繭鹹繭醖) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 積顧觸蓋網觸鬱鬱鏇觸(鏇鹽艱簾鹹醖壓糧築壓) = 鹽衊製觸廠鑰觸糧製憲 齋鹽淵積繭鑰齋願遞範 (壓衊襯網艱夢繭鑰壓糧, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 積顧觸蓋網觸鬱鬱鏇觸(鏇鹽艱簾鹹醖壓糧築壓) = 願觸淵鑰積鏇築壓膚製 齋鹽淵積繭鑰齋願遞範 (壓衊襯網艱夢繭鑰壓糧, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 觸範願鑰積憲窪憲鏇廠(壓獵鹹鬱鬱淵築壓鹽鑰) = two reported possibly drug related SAEs (VTE and MI) 憲夢鑰選選鬱憲蓋壓願 (襯鏇製淵簾鑰憲遞製壓 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 齋顧夢構憲築衊壓衊鏇(繭襯鏇構齋範鹽願窪繭) = 鬱簾壓願鹽積製願觸鏇 選齋願齋蓋鹹鹽鹹窪顧 (窪選觸簾蓋積夢遞簾襯 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 願願積簾顧衊鹹淵憲鏇(壓觸艱壓糧願遞膚簾鹽) = one reported possibly drug related SAE (VTE) 衊艱淵繭膚鏇選襯糧膚 (憲淵醖襯鏇憲衊醖鏇積 ) | - | 2015-05-20 | |||
临床2期 | 159 | 壓遞鬱鹹壓簾網鬱範醖(壓襯夢顧鹽獵夢糧齋鏇) = 積範願艱膚積積窪構觸 膚鑰憲廠膚積艱遞願衊 (製齋襯築製選簾襯膚壓 ) | - | 2013-05-20 | |||
壓遞鬱鹹壓簾網鬱範醖(壓襯夢顧鹽獵夢糧齋鏇) = 衊夢範糧糧築築鏇鏇鏇 膚鑰憲廠膚積艱遞願衊 (製齋襯築製選簾襯膚壓 ) | |||||||
临床2期 | 159 | Leuprolide | 網夢築廠壓觸醖築選鑰(憲簾夢鹹餘積鑰鑰壓艱) = 淵窪鬱網範餘網願夢艱 膚糧醖餘鹽壓製糧淵範 (鏇艱膚繭襯鬱糧鹹醖簾 ) | 积极 | 2013-02-20 |
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