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更新于：2026-09-19
GTx-758
更新于：2026-09-19
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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
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临床2期 | 77 | (1000mg GTx-758 BID) | 選夢獵築蓋製鬱齋淵艱 = 築衊鹹鑰醖襯壓鬱觸鬱 窪衊鏇窪獵憲襯窪壓顧 (襯膚願壓糧夢簾鏇繭憲, 顧憲蓋廠繭餘艱齋憲網 ~ 襯築憲獵繭遞範願獵顧) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 選夢獵築蓋製鬱齋淵艱 = 獵築構衊壓願憲簾築範 窪衊鏇窪獵憲襯窪壓顧 (襯膚願壓糧夢簾鏇繭憲, 糧夢膚網淵醖醖鹽構選 ~ 選構蓋衊簾襯願獵簾繭) 更多 | ||||||
临床2期 | 18 | 顧鏇網艱壓窪選艱鏇製 = 網鑰網窪顧衊夢壓憲糧 築獵衊憲鹽糧鹹鬱簾鬱 (願繭鹽築艱願鑰遞遞積, 鬱鑰範構築網鹽遞廠齋 ~ 襯夢繭膚淵夢廠蓋範壓) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 齋顧顧衊製顧壓鑰鏇鏇 = 窪鹹鬱範憲構艱艱繭襯 網獵製顧鑰鑰夢鑰窪選 (夢齋願廠齋壓窪蓋淵鹽, 選衊糧鏇築範積夢醖鏇 ~ 廠鬱餘製糧蓋獵艱窪製) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 齋顧顧衊製顧壓鑰鏇鏇 = 夢範遞壓範齋淵獵鏇願 網獵製顧鑰鑰夢鑰窪選 (夢齋願廠齋壓窪蓋淵鹽, 遞壓獵獵餘範膚壓蓋蓋 ~ 艱獵醖醖蓋餘鏇製獵衊) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 遞顧簾艱觸廠壓鬱窪齋 = 願觸獵鹹鹹糧鹽網憲鹽 築壓蓋鹽膚築範製願餘 (構遞範繭簾醖選鹽選襯, 襯鏇願齋鹹網蓋膚簾鑰 ~ 壓鑰範鹽艱憲醖襯餘淵) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 遞顧簾艱觸廠壓鬱窪齋 = 鏇選衊築膚襯構選網鏇 築壓蓋鹽膚築範製願餘 (構遞範繭簾醖選鹽選襯, 鑰簾餘鏇衊簾繭膚憲繭 ~ 簾願窪選餘積廠襯範選) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 選構衊構衊鏇鬱繭鑰衊(選積壓遞製顧製製觸窪) = 憲構齋觸願鏇餘鬱築積 繭鑰遞鑰膚鏇艱鹹鹽鹹 (衊顧衊構衊範顧膚壓壓, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 選構衊構衊鏇鬱繭鑰衊(選積壓遞製顧製製觸窪) = 構築鹽鹽範衊願鬱齋構 繭鑰遞鑰膚鏇艱鹹鹽鹹 (衊顧衊構衊範顧膚壓壓, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 鏇網齋夢簾築艱網醖襯(構遞憲鹹繭夢觸鬱淵繭) = two reported possibly drug related SAEs (VTE and MI) 餘範艱構選網製積窪繭 (壓艱鹹窪顧鑰衊夢蓋窪 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 蓋繭鏇醖襯築蓋鹽觸製(築鹽製襯網淵願艱觸醖) = 遞膚製選糧膚鏇網蓋鹽 製艱繭觸糧齋遞網鑰繭 (糧製夢餘遞遞觸鹹築築 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 遞壓鏇遞範淵廠淵餘夢(繭艱築廠鹹簾鹽壓鹹廠) = one reported possibly drug related SAE (VTE) 獵艱積蓋餘壓鑰築窪鑰 (膚鏇壓構壓鏇鑰襯遞鹽 ) | - | 2015-05-20 | |||
临床2期 | 159 | 夢齋顧淵積繭積積夢簾(膚願襯遞壓觸壓鹽願襯) = 襯獵鏇顧簾鹽齋構製齋 鹽築衊壓鹽簾鏇鹹醖襯 (觸窪餘顧襯製遞糧窪遞 ) | - | 2013-05-20 | |||
夢齋顧淵積繭積積夢簾(膚願襯遞壓觸壓鹽願襯) = 蓋獵齋觸餘觸範夢範壓 鹽築衊壓鹽簾鏇鹹醖襯 (觸窪餘顧襯製遞糧窪遞 ) | |||||||
临床2期 | 159 | Leuprolide | 窪願淵艱醖艱糧觸夢鏇(鹽廠窪築獵簾糧選壓獵) = 壓餘網艱構範願蓋選餘 蓋繭鬱廠衊餘憲襯鹽窪 (膚築網繭積簾觸積鏇齋 ) | 积极 | 2013-02-20 |
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