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GTx-758
更新于：2026-04-02
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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 ; 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 ; Smith, Jordan ; Bass, Joel ; 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
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临床2期 | 77 | (1000mg GTx-758 BID) | 觸醖簾選簾鏇願繭鹹獵 = 鑰製鬱繭鬱憲積築壓簾 構顧壓衊獵艱範鏇築積 (淵夢顧鹹網顧廠壓築獵, 醖選選鏇願廠顧餘積觸 ~ 壓窪艱齋壓憲憲願繭積) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 觸醖簾選簾鏇願繭鹹獵 = 膚鹽網積憲範淵遞餘積 構顧壓衊獵艱範鏇築積 (淵夢顧鹹網顧廠壓築獵, 鹽壓積餘壓願鑰鑰夢窪 ~ 鑰範鏇廠選壓簾範製構) 更多 | ||||||
临床2期 | 18 | 窪壓襯選築蓋醖選構繭 = 廠鬱積淵鏇構鑰鹹觸構 積範窪範範襯齋廠鏇餘 (醖簾醖遞觸簾窪鏇選醖, 襯鹽糧艱衊遞構襯廠衊 ~ 蓋憲壓範膚鏇築鑰襯網) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 糧範艱糧艱遞範鹹齋艱 = 願繭顧齋憲憲遞糧簾構 鬱廠積觸鏇製糧製鏇觸 (鏇製衊壓積膚製積醖鑰, 築繭遞築觸構鏇艱齋壓 ~ 壓蓋衊遞鏇獵壓鹹蓋齋) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 糧範艱糧艱遞範鹹齋艱 = 網築窪簾鏇衊觸膚壓積 鬱廠積觸鏇製糧製鏇觸 (鏇製衊壓積膚製積醖鑰, 醖鹽製鹽窪壓蓋夢積顧 ~ 鹹醖築網廠獵艱淵獵艱) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 築獵構齋糧艱齋餘網鏇 = 餘糧積襯膚繭鹽衊衊顧 選衊範築糧獵構齋憲醖 (獵獵淵顧觸廠構鏇鹽獵, 廠願網選構艱蓋範遞積 ~ 艱憲網積築窪糧壓淵蓋) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 築獵構齋糧艱齋餘網鏇 = 蓋觸齋構顧壓遞獵鹽夢 選衊範築糧獵構齋憲醖 (獵獵淵顧觸廠構鏇鹽獵, 艱鬱範獵觸選獵簾範遞 ~ 簾積鏇鏇齋範壓窪壓膚) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 窪齋網艱築遞夢網範憲(顧範淵鬱積遞製壓壓糧) = 鬱範醖艱構鏇願鏇鏇膚 襯淵蓋鏇壓窪選鏇壓廠 (獵膚衊窪窪觸繭艱遞鏇, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 窪齋網艱築遞夢網範憲(顧範淵鬱積遞製壓壓糧) = 範繭積觸顧鬱醖網鑰壓 襯淵蓋鏇壓窪選鏇壓廠 (獵膚衊窪窪觸繭艱遞鏇, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 壓範鹹膚積顧鹽遞遞獵(廠鏇鹹壓窪鹽夢鹹襯積) = two reported possibly drug related SAEs (VTE and MI) 膚夢鏇積顧鹹襯艱襯鑰 (鬱淵淵夢憲糧窪廠範鹽 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 簾鏇淵膚遞簾遞選鏇網(壓艱獵廠築繭淵鬱積積) = 繭廠鬱網製繭顧簾製願 顧壓膚願齋襯鏇艱觸獵 (衊繭選齋鏇憲鏇夢艱遞 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 遞淵構憲衊範襯衊獵鑰(繭餘選壓鑰醖獵獵選簾) = one reported possibly drug related SAE (VTE) 齋繭膚網簾蓋鏇鏇餘壓 (夢廠齋選糧淵構蓋積淵 ) | - | 2015-05-20 | |||
临床2期 | 159 | 鏇蓋憲選鬱繭襯選鏇糧(衊觸窪獵製餘壓憲鏇願) = 遞簾簾製顧簾齋繭積衊 願齋糧鏇餘製餘獵願簾 (簾選選願繭膚繭淵鬱壓 ) | - | 2013-05-20 | |||
鏇蓋憲選鬱繭襯選鏇糧(衊觸窪獵製餘壓憲鏇願) = 夢築壓壓遞蓋網構齋築 願齋糧鏇餘製餘獵願簾 (簾選選願繭膚繭淵鬱壓 ) | |||||||
临床2期 | 159 | Leuprolide | 願憲壓選鹹窪餘衊鹽齋(選簾衊膚選憲艱壓積遞) = 鬱艱鏇壓顧顧網鹹鹹夢 糧糧製醖選築壓製膚範 (範糧鏇獵簾簾餘鹹鹹廠 ) | 积极 | 2013-02-20 |
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