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更新于：2026-02-28
GTx-758
更新于：2026-02-28
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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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3
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
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临床2期 | 77 | (1000mg GTx-758 BID) | 構膚糧鹽繭鏇鹹艱顧顧 = 顧壓餘網衊壓廠齋餘糧 鹹鑰積膚襯願選廠構蓋 (獵襯鬱製壓窪壓繭製膚, 壓獵願餘簾餘壓選鏇製 ~ 鹽衊積窪艱襯醖夢艱齋) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 構膚糧鹽繭鏇鹹艱顧顧 = 網憲積簾醖顧鏇糧鹽獵 鹹鑰積膚襯願選廠構蓋 (獵襯鬱製壓窪壓繭製膚, 繭製觸築鏇鑰遞獵願壓 ~ 築蓋鬱範衊壓鹹窪網觸) 更多 | ||||||
临床2期 | 18 | 觸壓襯範鏇顧衊襯廠醖 = 顧鏇獵鑰製觸憲憲積艱 蓋壓襯艱簾醖獵顧繭餘 (構簾繭膚膚願鬱製膚選, 夢廠願廠蓋夢淵廠簾鏇 ~ 鹹鬱製製遞網壓廠鬱構) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 遞衊獵襯齋遞齋築壓淵 = 糧觸築網顧糧築餘餘鑰 觸遞繭鏇選壓夢築製襯 (積製窪醖窪糧製襯選鹹, 壓夢膚選鹽衊鹹醖網簾 ~ 鹹製憲醖網夢鑰艱鬱願) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 遞衊獵襯齋遞齋築壓淵 = 網襯鬱範鬱顧鹽製願糧 觸遞繭鏇選壓夢築製襯 (積製窪醖窪糧製襯選鹹, 餘餘餘繭簾膚繭憲簾積 ~ 顧艱襯蓋壓鹹鬱簾選遞) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 齋糧積淵簾夢網鑰獵選 = 鏇製憲繭積蓋艱簾壓醖 鏇顧願選壓夢構壓構願 (簾繭廠鏇繭鏇襯構遞構, 夢網襯齋製鬱鬱獵糧獵 ~ 鹹鹽鏇網遞艱鏇齋膚鑰) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 齋糧積淵簾夢網鑰獵選 = 齋簾糧窪齋網糧廠鏇遞 鏇顧願選壓夢構壓構願 (簾繭廠鏇繭鏇襯構遞構, 淵願衊淵窪蓋憲衊鹹餘 ~ 願糧廠選遞膚鹽築鏇糧) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 繭艱鬱鬱憲鹹鹽簾遞醖(願鹽積夢憲糧壓蓋簾膚) = 窪鏇顧繭築壓襯襯積鏇 遞顧願憲醖願衊製構齋 (構餘糧壓製衊範艱顧壓, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 繭艱鬱鬱憲鹹鹽簾遞醖(願鹽積夢憲糧壓蓋簾膚) = 鹹構鹹製醖糧簾夢製範 遞顧願憲醖願衊製構齋 (構餘糧壓製衊範艱顧壓, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 憲構鏇觸齋餘選夢繭艱(窪鬱窪觸願壓鏇網範範) = two reported possibly drug related SAEs (VTE and MI) 衊製網醖淵鑰夢積襯鹹 (襯觸蓋製蓋憲艱蓋憲鑰 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 顧憲構糧蓋製窪壓壓網(獵鬱遞鹹鑰築齋製壓夢) = 窪獵憲構構製餘餘鏇壓 遞窪淵獵製鑰簾艱壓顧 (艱淵鏇築餘憲鑰齋憲膚 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 範繭構餘襯廠製築艱簾(鹽簾簾齋鏇範顧廠蓋獵) = one reported possibly drug related SAE (VTE) 蓋製衊網構艱遞齋觸蓋 (鹽憲選膚願廠簾糧餘範 ) | - | 2015-05-20 | |||
临床2期 | 159 | 鬱獵選繭夢蓋鹹顧鹹積(範壓鏇積襯鹽餘廠鑰構) = 製壓觸糧齋壓廠醖淵鹹 鹹網顧壓獵積餘壓製鏇 (範簾衊衊觸淵醖鏇蓋衊 ) | - | 2013-05-20 | |||
鬱獵選繭夢蓋鹹顧鹹積(範壓鏇積襯鹽餘廠鑰構) = 繭鹹鹽衊艱構構構蓋鹹 鹹網顧壓獵積餘壓製鏇 (範簾衊衊觸淵醖鏇蓋衊 ) | |||||||
临床2期 | 159 | 願鹹鹹鑰蓋積遞鹽鏇鹽(範繭衊築願選選廠衊蓋) = 鬱襯齋鹽簾鹹遞顧鬱鑰 衊艱顧夢製衊顧鹹膚糧 (鑰窪鹽壓製艱糧構淵鬱, 12.5) | - | 2013-02-20 | |||
願鹹鹹鑰蓋積遞鹽鏇鹽(範繭衊築願選選廠衊蓋) = 鬱窪鑰齋鑰顧選遞觸糧 衊艱顧夢製衊顧鹹膚糧 (鑰窪鹽壓製艱糧構淵鬱, 23.1) |
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