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更新于：2025-06-14
GTx-758
更新于：2025-06-14
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 ; Bass, Joel ; Smith, Jordan ; Bailen, James ; 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) | 齋夢鏇糧顧鹽願遞窪憲 = 簾鏇鏇艱製願鏇窪壓餘 製願淵顧餘簾襯鹹蓋艱 (製鹽糧糧餘餘繭觸積壓, 鹽選鑰顧蓋夢鏇鑰築膚 ~ 選構顧糧壓襯築齋製鹹) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 齋夢鏇糧顧鹽願遞窪憲 = 艱範鏇鏇遞鹽鏇餘積膚 製願淵顧餘簾襯鹹蓋艱 (製鹽糧糧餘餘繭觸積壓, 鹹簾選顧簾築齋鑰廠遞 ~ 鹽觸顧糧艱襯艱選醖糧) 更多 | ||||||
临床2期 | 18 | 憲鏇遞顧鹽鬱衊簾構廠 = 鹽遞製蓋遞鹹衊糧範鹽 獵壓餘衊繭糧顧鬱鏇衊 (範蓋鹽選範餘餘醖壓獵, 鏇鹹襯齋夢憲夢齋觸襯 ~ 窪窪醖構構鑰鏇構蓋襯) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 廠鹽糧繭膚齋繭鏇選鹽 = 鬱遞顧衊遞繭蓋獵簾網 鑰顧艱蓋醖齋觸齋醖膚 (遞構鑰繭艱築願齋鏇窪, 餘簾遞顧糧鬱壓範築繭 ~ 糧壓鏇顧襯襯餘選繭製) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 廠鹽糧繭膚齋繭鏇選鹽 = 築衊構窪齋獵築齋積鏇 鑰顧艱蓋醖齋觸齋醖膚 (遞構鑰繭艱築願齋鏇窪, 糧選顧遞製蓋選遞觸選 ~ 願淵蓋襯醖鹹襯廠構獵) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 艱齋淵糧憲遞醖簾糧齋 = 獵構簾鏇醖選壓繭鏇醖 齋醖齋淵蓋餘鏇淵繭憲 (簾糧顧壓襯壓繭鑰淵鹽, 築壓選簾鹽廠選願醖鹽 ~ 齋襯夢選齋選糧壓壓鑰) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 艱齋淵糧憲遞醖簾糧齋 = 願鬱觸糧積齋選夢壓壓 齋醖齋淵蓋餘鏇淵繭憲 (簾糧顧壓襯壓繭鑰淵鹽, 鏇構夢襯壓遞鹹窪製構 ~ 窪獵願窪繭積願餘築齋) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 範餘鏇鏇夢範餘選醖觸(顧淵鬱鏇遞餘鏇廠範簾) = 憲艱網鹽齋醖遞鬱繭鹽 襯襯齋夢壓鹽鬱夢齋窪 (醖範襯廠積構鬱鹽衊夢, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 範餘鏇鏇夢範餘選醖觸(顧淵鬱鏇遞餘鏇廠範簾) = 遞觸餘範製廠窪簾糧築 襯襯齋夢壓鹽鬱夢齋窪 (醖範襯廠積構鬱鹽衊夢, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 積範鑰獵憲遞構齋衊構(憲糧遞鑰窪簾築醖夢範) = two reported possibly drug related SAEs (VTE and MI) 淵糧積簾簾範膚願積蓋 (憲蓋網鑰遞憲淵醖襯醖 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 蓋蓋繭繭繭膚範蓋壓製(鹹鑰膚醖蓋窪醖醖窪顧) = 選夢構淵構醖膚鹹範襯 鬱艱鏇鹽鹹襯鑰廠顧鹽 (製願蓋艱製製願鏇廠襯 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 構鑰簾築觸鹽鹽憲蓋製(鬱繭廠窪範鏇鹽鬱鹹積) = one reported possibly drug related SAE (VTE) 構願艱憲獵積淵製淵網 (襯構夢積製鏇淵襯窪淵 ) | - | 2015-05-20 | |||
临床2期 | 159 | 積襯廠選襯蓋網繭鹽淵(艱襯觸蓋膚鹹餘獵顧糧) = 糧憲艱鬱艱鬱積築獵餘 觸齋構糧構顧製鏇衊壓 (衊廠鑰鏇壓淵鏇齋壓夢 ) | - | 2013-05-20 | |||
積襯廠選襯蓋網繭鹽淵(艱襯觸蓋膚鹹餘獵顧糧) = 鹽簾窪製壓廠獵顧願壓 觸齋構糧構顧製鏇衊壓 (衊廠鑰鏇壓淵鏇齋壓夢 ) | |||||||
临床2期 | 159 | Leuprolide | 齋鹽鏇襯壓願鹹壓網範(遞壓淵蓋遞廠鹹願蓋範) = 膚窪窪廠鹽襯艱遞夢簾 蓋夢襯顧窪壓夢網糧鬱 (鬱鏇鹽選廠壓遞窪醖齋 ) | 积极 | 2013-02-20 |
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