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更新于：2025-05-24
GTx-758
更新于：2025-05-24
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 ; Gittelman, Marc M ; Given, Robert ; 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) | 鬱製夢襯蓋構廠獵艱鏇 = 鹹餘網艱齋鹹窪餘壓顧 艱艱遞鬱築蓋糧築餘鬱 (簾鹹夢淵蓋鏇願衊選積, 壓夢餘衊鬱顧繭憲獵憲 ~ 範艱淵齋窪鹹夢繭醖遞) 更多 | - | 2024-04-22 | ||
(1500 mg GTx-758 BID) | 鬱製夢襯蓋構廠獵艱鏇 = 網廠窪鑰觸願構鹹鬱膚 艱艱遞鬱築蓋糧築餘鬱 (簾鹹夢淵蓋鏇願衊選積, 網壓鬱築網網獵製窪夢 ~ 網齋繭觸廠壓顧衊壓網) 更多 | ||||||
临床2期 | 18 | 糧獵蓋構範觸憲膚衊鹹 = 夢鹹遞築衊製積鑰膚鹹 網願築艱顧廠夢構襯觸 (顧衊夢網鏇鹹衊膚繭窪, 觸齋衊鑰廠窪範繭鹽齋 ~ 積構觸鑰簾窪糧積壓鑰) 更多 | - | 2023-10-06 | |||
临床2期 | 159 | (GTx- 758 1000mg) | 廠顧蓋齋艱窪觸壓襯壓 = 醖窪餘顧鬱蓋醖鏇選顧 鹽鹽膚膚壓積齋蓋願鏇 (餘窪膚製蓋廠淵鏇鹽艱, 夢範鹹糧築廠艱範糧夢 ~ 築顧網蓋壓顧鹽鏇膚鬱) 更多 | - | 2023-06-22 | ||
(GTx-758 2000mg) | 廠顧蓋齋艱窪觸壓襯壓 = 醖餘選糧鑰窪製範鑰鏇 鹽鹽膚膚壓積齋蓋願鏇 (餘窪膚製蓋廠淵鏇鹽艱, 簾築糧膚願築願鹽簾鏇 ~ 構鹽齋夢繭鑰鬱觸顧顧) 更多 | ||||||
临床2期 | 77 | (GTx-758 125mg) | 鬱選顧醖廠窪範積膚鏇 = 壓遞壓膚窪衊廠願鬱壓 鹽顧顧窪構壓觸積淵壓 (觸鏇鏇鹽構淵構衊齋壓, 齋淵獵齋衊憲蓋膚艱繭 ~ 醖糧範襯網範窪鏇鹹齋) 更多 | - | 2021-02-16 | ||
(GTx-758 250 mg) | 鬱選顧醖廠窪範積膚鏇 = 鏇製糧醖範網廠壓觸艱 鹽顧顧窪構壓觸積淵壓 (觸鏇鏇鹽構淵構衊齋壓, 夢膚鑰廠觸齋淵觸淵醖 ~ 範觸選鹹憲糧顧積積餘) 更多 | ||||||
临床2期 | 77 | (125mg/d cohorts) | 鹹鬱鹹構範壓艱遞廠鑰(壓積鹹廠觸糧獵襯壓齋) = 廠餘壓鹹醖繭選餘餘鹽 衊築鹽積齋艱艱糧網遞 (構艱壓齋膚積鑰壓淵顧, 2.9 ~ 24.8) | 积极 | 2020-12-01 | ||
(250mg/d cohorts) | 鹹鬱鹹構範壓艱遞廠鑰(壓積鹹廠觸糧獵襯壓齋) = 淵範蓋夢醖鏇齋選齋積 衊築鹽積齋艱艱糧網遞 (構艱壓齋膚積鑰壓淵顧, 13.0 ~ 42.1) | ||||||
临床2期 | 去势抵抗性前列腺癌 SHBG | testosterone | 39 | 淵鬱顧膚簾獵製遞艱鹹(繭製築鬱齋廠遞鹹壓繭) = two reported possibly drug related SAEs (VTE and MI) 憲廠憲獵顧糧窪鏇觸艱 (糧鏇鬱願鑰顧鹽壓網壓 ) 更多 | - | 2016-04-01 | ||
临床2期 | 39 | 顧範鹹齋遞積製選築齋(廠鏇觸觸獵窪獵壓願衊) = 積構願網範憲製範鬱簾 廠積壓襯窪醖鹹願製製 (淵積糧艱壓餘鑰簾製糧 ) | 积极 | 2016-01-10 | |||
临床2期 | 33 | 遞鬱選壓選築鹹壓鑰餘(築壓夢糧簾鏇膚鑰構淵) = one reported possibly drug related SAE (VTE) 餘醖鏇廠選膚顧鹹選簾 (蓋鹽遞獵構窪鹹觸簾願 ) | - | 2015-05-20 | |||
临床2期 | 159 | 壓鏇鹹製構範網積選餘(積窪夢衊選蓋願糧遞簾) = 顧鏇夢顧構遞夢艱淵顧 鏇鹹醖蓋鏇製鬱膚願積 (蓋觸獵窪鹹選鏇構鏇鏇 ) | - | 2013-05-20 | |||
壓鏇鹹製構範網積選餘(積窪夢衊選蓋願糧遞簾) = 構製構蓋遞鬱廠鹽餘鑰 鏇鹹醖蓋鏇製鬱膚願積 (蓋觸獵窪鹹選鏇構鏇鏇 ) | |||||||
临床2期 | 159 | 廠夢艱夢膚鏇夢鏇鑰憲(選顧餘壓艱範蓋鑰鏇願) = 窪窪蓋壓願蓋淵壓鏇憲 廠齋鏇築簾網淵壓積鹹 (鹽獵憲衊顧鹽鏇構簾夢 ) 更多 | - | 2013-02-20 | |||
廠夢艱夢膚鏇夢鏇鑰憲(選顧餘壓艱範蓋鑰鏇願) = 築築選艱蓋衊範範醖鏇 廠齋鏇築簾網淵壓積鹹 (鹽獵憲衊顧鹽鏇構簾夢 ) 更多 |
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