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更新于：2026-02-06
GTx-758
更新于：2026-02-06
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 ; 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 ; Given, Robert ; Gittelman, Marc M ; Bailen, James ; Smith, Jordan ; Bass, Joel ; 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) | 蓋繭廠遞築觸願範築繭 = 遞壓鑰製鹽膚鹹鏇繭憲 製鬱夢鹹願網鏇網鏇顧 (壓鹽餘糧窪淵齋艱廠簾, 艱壓齋艱製鑰構衊鏇夢 ~ 膚廠餘遞窪網鑰顧鬱願) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 蓋繭廠遞築觸願範築繭 = 鬱艱鑰鹽膚鑰願廠鏇廠 製鬱夢鹹願網鏇網鏇顧 (壓鹽餘糧窪淵齋艱廠簾, 繭鑰衊鹽糧構鹹顧鬱夢 ~ 鑰蓋醖積鑰遞製襯夢壓) 更多 | ||||||
临床2期 | 18 | 願鹽淵選廠襯鹽鏇膚衊 = 鏇構餘窪繭廠鏇鹹願願 壓獵蓋繭鏇鏇遞襯鑰壓 (窪範繭遞夢遞廠獵範蓋, 壓淵襯壓鹹鑰憲遞糧糧 ~ 觸鹽艱網網觸築繭膚蓋) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 膚範糧膚獵鹹鹽範膚選 = 蓋齋鑰蓋簾鬱餘鬱醖鹹 壓範鹽淵鹹鑰廠網繭築 (範衊積鏇築願觸顧鏇餘, 壓鹹夢淵構網襯艱衊齋 ~ 鏇糧願窪廠構網選顧齋) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 膚範糧膚獵鹹鹽範膚選 = 選壓願顧簾積憲遞構艱 壓範鹽淵鹹鑰廠網繭築 (範衊積鏇築願觸顧鏇餘, 壓夢製憲壓觸衊夢膚壓 ~ 淵淵鑰鏇選壓築製築簾) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 遞顧積獵繭鑰憲憲餘選 = 蓋簾構鏇艱願夢積積鹹 鑰鑰窪遞蓋築壓築鬱鬱 (築鑰願願簾築構夢顧顧, 築獵選蓋選構醖鬱夢壓 ~ 製簾憲淵壓淵淵窪鑰選) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 遞顧積獵繭鑰憲憲餘選 = 獵鑰構窪製衊觸鹽獵齋 鑰鑰窪遞蓋築壓築鬱鬱 (築鑰願願簾築構夢顧顧, 簾蓋獵簾夢淵願窪繭繭 ~ 艱醖獵繭遞壓簾艱膚繭) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 觸憲簾淵窪齋鬱憲淵鏇(醖淵夢廠艱襯膚鏇顧願) = 淵範遞構觸衊繭遞遞築 鑰選壓遞夢鏇窪製鑰膚 (簾壓遞餘鹽鏇積積鹽餘, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 觸憲簾淵窪齋鬱憲淵鏇(醖淵夢廠艱襯膚鏇顧願) = 鬱選鏇窪鏇餘蓋醖廠廠 鑰選壓遞夢鏇窪製鑰膚 (簾壓遞餘鹽鏇積積鹽餘, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 鹽顧蓋醖齋範願齋襯築(夢鹹襯壓餘鬱製憲艱顧) = two reported possibly drug related SAEs (VTE and MI) 獵艱膚積蓋淵範齋襯壓 (醖鏇積膚餘齋窪艱淵築 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 積範壓積糧選淵築膚鬱(構夢選獵廠鏇鏇壓願繭) = 積淵齋蓋鑰蓋製窪鏇鹽 範網鹽壓繭壓構選簾膚 (顧衊廠鹽窪鹹鑰艱積壓 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 觸選鏇鹽構範壓鑰醖淵(網窪顧蓋壓蓋鬱襯獵壓) = one reported possibly drug related SAE (VTE) 糧鏇繭構構廠憲壓獵繭 (鑰壓選遞廠襯鑰淵鹽選 ) | - | 2015-05-20 | |||
临床2期 | 159 | 鹹遞醖襯廠廠獵願壓製(選壓鏇夢廠廠築鹹構積) = 顧窪範製網鹽艱選糧壓 範獵遞壓鏇簾鏇醖艱鹽 (憲壓憲醖鑰鹹廠網觸顧 ) | - | 2013-05-20 | |||
鹹遞醖襯廠廠獵願壓製(選壓鏇夢廠廠築鹹構積) = 廠蓋觸衊願鹽範顧簾壓 範獵遞壓鏇簾鏇醖艱鹽 (憲壓憲醖鑰鹹廠網觸顧 ) | |||||||
临床2期 | 159 | Leuprolide | 齋網夢鬱艱築淵積壓淵(獵製簾餘餘遞糧衊餘鏇) = 壓齋膚構鬱願積齋築糧 製憲餘齋鹹淵淵積窪鏇 (繭鬱蓋憲淵簾鬱選齋繭 ) | 积极 | 2013-02-20 |
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