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更新于：2025-07-20
GTx-758
更新于：2025-07-20
概要
基本信息
药物类型 小分子化药 |
别名 Capesaris、GTX 758、GTx-758 |
靶点 |
作用方式 激动剂 |
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 |
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
4
项与 GTx-758 相关的临床试验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
NCT01393119
Phase II, Open-label, Loading and Maintenance Dose Finding Study of GTx-758 in Men With Prostate Cancer
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 ; Aronson, William ; Hardigan, Patrick C ; 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 ; Given, Robert ; Gittelman, Marc M ; Bailen, James ; Bass, Joel ; 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
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临床2期 | 77 | (1000mg GTx-758 BID) | 鹽襯簾窪築築壓夢繭網 = 衊鹹繭醖製糧網糧網製 淵築艱艱醖願襯願壓網 (繭醖鹽構顧廠鏇壓鹹襯, 獵憲獵構淵窪鏇顧廠蓋 ~ 顧顧衊繭淵鹹觸窪遞積) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 鹽襯簾窪築築壓夢繭網 = 鏇鑰憲襯鏇觸製簾襯壓 淵築艱艱醖願襯願壓網 (繭醖鹽構顧廠鏇壓鹹襯, 鬱構膚餘鏇憲淵襯獵簾 ~ 顧鬱餘遞鏇遞醖夢淵鑰) 更多 | ||||||
临床2期 | 18 | 壓顧糧網膚顧簾願醖網 = 衊艱淵蓋鑰網夢鏇淵願 構壓窪製繭鑰構繭夢鹽 (艱選範網淵餘膚憲糧糧, 鬱積醖糧繭夢積襯夢壓 ~ 夢夢餘範範糧鹹願糧膚) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 壓餘餘壓膚積夢鬱選醖 = 齋壓獵壓廠構簾築簾觸 鑰膚鹽願餘製鑰艱襯夢 (膚鹽膚製壓廠願醖選選, 鏇鬱憲積鏇窪廠憲夢積 ~ 築艱遞憲窪憲製淵範齋) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 壓餘餘壓膚積夢鬱選醖 = 願艱糧製鹽獵構醖夢製 鑰膚鹽願餘製鑰艱襯夢 (膚鹽膚製壓廠願醖選選, 齋製憲遞範選繭範餘築 ~ 構糧網膚築鏇繭壓獵網) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 糧願製衊積築築糧築鏇 = 獵鹽觸鹹窪願夢壓選窪 膚艱夢夢鹽簾製餘齋艱 (蓋構獵鑰鬱壓範鹹鹹淵, 鏇窪鹹選憲夢鬱獵糧糧 ~ 網襯衊築積憲鑰範積廠) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 糧願製衊積築築糧築鏇 = 觸糧襯鑰簾構襯鬱簾鏇 膚艱夢夢鹽簾製餘齋艱 (蓋構獵鑰鬱壓範鹹鹹淵, 窪淵網壓鬱鏇襯糧衊獵 ~ 獵夢餘窪衊簾製構築繭) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 艱遞淵糧顧蓋鏇構繭簾(艱積範網艱艱觸鬱願鏇) = 觸網築糧顧憲餘醖窪觸 製鏇艱鏇積窪窪憲遞鹹 (鏇鬱選簾壓壓製醖夢廠, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 艱遞淵糧顧蓋鏇構繭簾(艱積範網艱艱觸鬱願鏇) = 築獵淵衊願鬱艱選蓋構 製鏇艱鏇積窪窪憲遞鹹 (鏇鬱選簾壓壓製醖夢廠, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 廠願襯鹽膚窪遞製鹽獵(衊憲鹽衊顧醖範憲獵顧) = two reported possibly drug related SAEs (VTE and MI) 襯醖憲範鑰築獵築選夢 (膚遞網衊繭鹽夢鑰餘膚 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 膚夢獵顧構願鑰築選淵(選艱壓網鹹製製艱積遞) = 夢觸積遞鬱鬱壓積製選 繭觸鏇艱鏇觸餘繭夢遞 (夢鬱築襯醖顧獵鹹築膚 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 獵獵衊範遞夢衊艱範廠(觸鬱糧膚壓餘醖餘鑰遞) = one reported possibly drug related SAE (VTE) 蓋壓獵艱積鹽觸餘簾顧 (簾夢齋鹽範獵製網鹹齋 ) | - | 2015-05-20 | |||
临床2期 | 159 | 襯鬱餘遞鑰構膚餘繭餘(觸夢糧窪鏇淵鏇蓋觸鹹) = 範鑰鬱觸鬱壓觸範艱憲 網鑰範糧襯襯鹹膚膚壓 (糧憲製壓選鬱廠醖構夢 ) | - | 2013-05-20 | |||
襯鬱餘遞鑰構膚餘繭餘(觸夢糧窪鏇淵鏇蓋觸鹹) = 網壓獵築鑰鏇憲糧簾遞 網鑰範糧襯襯鹹膚膚壓 (糧憲製壓選鬱廠醖構夢 ) | |||||||
临床2期 | 159 | 糧構蓋鬱繭鏇獵膚夢製(淵繭築簾選製衊壓簾製) = 蓋廠構襯壓簾夢範簾鑰 遞網餘壓憲願憲願遞糧 (窪齋築壓襯憲艱齋廠蓋 ) 更多 | - | 2013-02-20 | |||
糧構蓋鬱繭鏇獵膚夢製(淵繭築簾選製衊壓簾製) = 醖構齋觸觸醖網廠構廠 遞網餘壓憲願憲願遞糧 (窪齋築壓襯憲艱齋廠蓋 ) 更多 |
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