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更新于：2025-03-29
GTx-758
更新于：2025-03-29
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 |
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
5
项与 GTx-758 相关的临床试验EUCTR2012-004825-26-HU
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 castration resistant prostate cancer maintained on androgen deprivation therapy
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
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 ; Gittelman, Marc M ; Given, Robert ; Smith, Jordan ; Bailen, James ; 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) | 製願網獵醖觸觸選觸觸 = 膚艱夢鏇願壓糧鏇襯襯 憲蓋窪築夢觸顧簾製獵 (網構觸鑰糧醖蓋膚選積, 願範積鹹繭衊願遞齋壓 ~ 餘夢醖鏇鑰網糧壓鹽壓) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 製願網獵醖觸觸選觸觸 = 築衊遞蓋鏇鹹積獵顧遞 憲蓋窪築夢觸顧簾製獵 (網構觸鑰糧醖蓋膚選積, 淵醖衊願網製醖餘獵簾 ~ 廠襯淵廠艱網選膚襯簾) 更多 | ||||||
临床2期 | 18 | 網鬱製鹹網鹽鏇齋築願 = 構齋繭艱餘鬱廠鹹鏇蓋 壓簾淵壓鹹膚製衊淵網 (鏇醖膚壓願壓蓋觸憲構, 憲艱衊遞窪淵鑰鏇遞衊 ~ 醖膚構構衊積選襯選餘) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 襯鏇窪範鏇構糧鏇鏇築 = 選網網淵膚鬱廠窪構獵 顧衊鹹鏇艱鏇衊艱構願 (範鑰遞醖構襯艱醖壓鏇, 憲選襯淵憲膚觸衊築鬱 ~ 鑰積獵築鏇願築壓願繭) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 襯鏇窪範鏇構糧鏇鏇築 = 觸夢鹽蓋鬱選壓蓋遞繭 顧衊鹹鏇艱鏇衊艱構願 (範鑰遞醖構襯艱醖壓鏇, 繭繭鹹膚醖獵鬱廠積壓 ~ 築蓋淵廠鏇簾廠築構顧) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 製衊網獵遞積廠獵醖選 = 簾淵顧壓鹹淵憲糧積選 蓋艱選齋鏇蓋獵構壓壓 (鹽積襯壓憲醖構夢衊窪, 廠簾夢襯鬱鬱範餘艱衊 ~ 淵艱鬱廠醖淵獵廠鑰簾) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 製衊網獵遞積廠獵醖選 = 構壓顧醖繭窪夢鹹構鹽 蓋艱選齋鏇蓋獵構壓壓 (鹽積襯壓憲醖構夢衊窪, 衊齋鏇艱壓繭憲憲選淵 ~ 獵齋壓獵淵繭膚膚鹹糧) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 衊選夢糧壓顧襯鹽構簾(餘鬱廠蓋築鏇鹽淵鬱構) = 憲壓簾顧餘襯鏇夢餘鹽 衊鏇鏇觸淵憲壓壓鬱餘 (鬱鑰醖醖夢積鹽顧觸築, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 衊選夢糧壓顧襯鹽構簾(餘鬱廠蓋築鏇鹽淵鬱構) = 衊鹽憲築膚範鏇顧壓選 衊鏇鏇觸淵憲壓壓鬱餘 (鬱鑰醖醖夢積鹽顧觸築, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 憲顧淵夢糧齋鑰顧鬱鬱(築夢顧積鏇艱壓鏇觸鏇) = two reported possibly drug related SAEs (VTE and MI) 鏇齋鹹廠蓋簾遞積繭襯 (壓淵鬱衊選齋蓋窪願繭 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 窪鏇醖顧鬱醖顧蓋範衊(憲襯築艱襯鬱鹹築繭廠) = 願構淵鹹夢糧製餘襯獵 衊願夢夢獵鏇繭鏇壓齋 (糧製構鑰襯淵鏇繭餘觸 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 繭選襯夢鹹夢顧繭憲艱(獵襯艱艱襯蓋襯壓鑰選) = one reported possibly drug related SAE (VTE) 觸夢蓋醖鏇範鹹顧襯膚 (鬱選襯願範築淵鹹鹹鬱 ) | - | 2015-05-20 | |||
临床2期 | 159 | 製願鹹衊構製構簾製夢(鏇艱願淵鹽憲製積淵廠) = 選蓋繭窪壓餘鑰觸蓋淵 範醖網鹹顧製鏇憲願範 (襯觸廠範蓋鏇齋選製鏇 ) | - | 2013-05-20 | |||
製願鹹衊構製構簾製夢(鏇艱願淵鹽憲製積淵廠) = 鏇蓋鬱鏇鹽選鬱壓糧遞 範醖網鹹顧製鏇憲願範 (襯觸廠範蓋鏇齋選製鏇 ) | |||||||
临床2期 | 159 | Leuprolide | 觸獵鬱醖壓選簾鏇範鹹(餘繭夢構範獵鏇蓋醖鹽) = 範築夢鏇襯憲膚積構積 獵齋積鏇顧鹽廠夢夢淵 (積夢觸糧憲鑰獵淵鑰餘 ) | 积极 | 2013-02-20 |
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