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更新于：2026-10-10
Giredestrant
吉雷司群
更新于：2026-10-10
概要
基本信息
药物类型 小分子化药 |
别名 Giredestrant (USAN/INN)、吉瑞司群、GDC-49545 + [3] |
靶点 |
作用方式 拮抗剂 |
作用机制 ERs拮抗剂(雌激素受体家族拮抗剂) |
在研适应症 |
非在研适应症- |
原研机构 |
非在研机构- |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评- |
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结构/序列
分子式C27H31F5N4O |
InChIKeyGQCXHIKRWBIQMD-AKJBCIBTSA-N |
CAS号1953133-47-5 |
关联
32
项与 吉雷司群 相关的临床试验NCT07827573
A Phase IIIb, Single-arm, Open-Label, Multicenter Study Evaluating the Treatment Adherence, Tolerability, and Patient-Reported Outcomes of Giredestrant in Patients With Estrogen Receptor-Positive, HER2-Negative Early Breast Cancer
NCT07541079
A Phase IIIb, Single-Arm, Open-Label Study Evaluating Adherence, Tolerability, and Patient Reported Outcomes (PRO) of Giredestrant in Patients With ER+/HER2- Early Breast Cancer Who Are Intolerant to Adjuvant Aromatase Inhibitor Therapy
NCT07214662
A Phase Ia/Ib Dose-Escalation and Expansion Study Evaluating the Safety, Pharmacokinetics, and Activity of GDC-0587 as a Monotherapy and in Combination With Giredestrant in Patients With Locally Advanced Or Metastatic ER-Positive, HER2-Negative Breast Cancer Who Have Previously Progressed During or After CDK4/6 Inhibitor Therapy
100 项与 吉雷司群 相关的临床结果
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100 项与 吉雷司群 相关的转化医学
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100 项与 吉雷司群 相关的专利（医药）
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36
项与 吉雷司群 相关的文献（医药）2026-06-01Cell Chemical Biology
Giredestrant immobilizes the estrogen receptor to exert potent antitumor efficacy against ER-active breast cancers
Article
作者: de Bruyn, Tom ; Zhou, Wei ; Liang, Jun ; Oeh, Jason ; Yao, Xiaosai ; Metcalfe, Ciara ; Guan, Jane ; Young, Amy ; Tai, Lisa ; Giltnane, Jennifer ; Chibly, Alejandro M ; Nguyen, Thao ; Mody, Vidhi ; Fox, Natalie S ; Ingalla, Ellen ; Blake, Robert A ; Labadie, Sharada S ; Hafner, Marc ; Wang, Xiaojing ; Ahmed, Musaddeque
Estrogen receptor α (ER) is one of the most successfully prosecuted therapeutic targets in oncology. Selective ER degraders (SERDs) are being pursued as next-generation therapies. Giredestrant is a potent orally bioavailable SERD and full ER antagonist, which has demonstrated clinical superiority over standard-of-care therapy. Here, we describe its key pharmacological attributes, and account for its benefit across the ER+ breast cancer spectrum. The antiproliferative potential of giredestrant is dictated by ER activity; it outperforms approved agents in ER activity-high contexts. ER immobilization likely underlies giredestrant's profound inhibitory potential. ER immobilization is not observed for heterobifunctional chimera degraders, which fail to match the antiproliferative potential of giredestrant despite superior ER degradation. Giredestrant redistributes enhancers, decreasing the expression of estrogen-induced genes and inducing the expression of putative tumor suppressors. These molecular data, together with results from recent trials, rationalize giredestrant's potential to serve as an optimized endocrine backbone for ER+ breast cancer.
2026-02-06Cancer Discovery
Giredestrant Delivers Long-Sought Adjuvant Benefit
Article
The oral selective estrogen receptor degrader giredestrant prolonged invasive disease-free survival more than standard endocrine therapies, such as tamoxifen, letrozole, anastrozole, and exemestane, in the phase III lidERA study. Despite the lack of comparisons between the drug and CDK4/6 inhibitors and concerns over its potential cost, researchers were excited by the data, noting that it’s the first improvement in adjuvant endocrine therapy in two decades.
2026-02-01JACC-Basic to Translational Science
Selective Estrogen Receptor Degraders Induce Bradycardia by Modulating Nuclear Estrogen Signaling
Article
作者: Patel, Jaymin M ; Narvaez-Paliza, Jose Max ; Rosas Diaz, Andrea Nathalie ; More Verde, Luis ; Urias, Monica ; Kurella, Shreya ; Basu, Sandeep ; Asnani, Aarti ; Curtin, Casie
Selective estrogen receptor degraders (SERDs) are emerging therapies for estrogen receptor-positive (ER+) breast cancer. However, certain oral SERDs, including giredestrant and camizestrant, have been associated with bradycardia in clinical trials. To elucidate the underlying molecular mechanism, we used chemical biology and genetic approaches in a zebrafish model of SERD-induced bradycardia. Giredestrant and camizestrant induced significant bradycardia in wild-type zebrafish embryos, whereas fulvestrant and amcenestrant (SERDs that do not induce bradycardia in patients) did not alter heart rate. Cotreatment with ER agonists rescued bradycardia, suggesting an ER-mediated mechanism. Mutations in gper, esr2a, and esr2b did not confer resistance to SERD-induced bradycardia, whereas esr1 mutant embryos were protected. These findings demonstrate that SERD-associated bradycardia is mediated through Esr1 signaling, supporting an on-target adverse effect.
100 项与 吉雷司群 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11961 | - | - | - |
研发状态
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| ER阳性/HER2阴性乳腺癌 | 申请上市 | 美国 | 2026-06-02 | |
| 乳腺癌 | 申请上市 | 中国 | 2026-04-16 | |
| 乳腺癌 | 申请上市 | 中国 | 2026-04-16 | |
| 乳腺癌 | 申请上市 | 中国 | 2026-04-16 | |
| ER阳性/HER2阴性/ESR1突变乳腺癌 | 申请上市 | 美国 | 2026-02-28 | |
| ER阳性乳腺癌 | 临床3期 | 美国 | 2022-08-03 | |
| ER阳性乳腺癌 | 临床3期 | 日本 | 2022-08-03 | |
| ER阳性乳腺癌 | 临床3期 | 阿根廷 | 2022-08-03 | |
| ER阳性乳腺癌 | 临床3期 | 德国 | 2022-08-03 | |
| ER阳性乳腺癌 | 临床3期 | 希腊 | 2022-08-03 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床3期 | 4,170 | (pre-menopausal) | 築襯鑰顧鑰觸齋衊糧積(製獵積膚糧膚製積願築) = 壓憲糧醖觸網網願網廠 繭夢築醖網齋網壓顧鬱 (繭糧鬱築製醖鑰膚簾獵 ) 更多 | 积极 | 2026-05-29 | ||
Standard-of-care endocrine therapy (anastrozole/letrozole/exemestane [aromatase inhibitors; AIs] or tamoxifen [TAM]) (pre-menopausal) | 築襯鑰顧鑰觸齋衊糧積(製獵積膚糧膚製積願築) = 憲築製餘餘觸構憲淵簾 繭夢築醖網齋網壓顧鬱 (繭糧鬱築製醖鑰膚簾獵 ) 更多 | ||||||
临床3期 | ESR1 mutation | 373 | 壓壓觸構壓襯窪壓膚繭(夢觸鏇選範遞鹽鹽憲衊) = 製構鏇積網艱範鏇鏇繭 積鏇選夢鬱糧糧積繭簾 (夢顧齋餘壓淵遞窪鏇願 ) 更多 | 积极 | 2026-05-29 | ||
standard-of-care endocrine therapy combinations (SOC ET + E) | 壓壓觸構壓襯窪壓膚繭(夢觸鏇選範遞鹽鹽憲衊) = 衊構淵遞遞範齋選壓鏇 積鏇選夢鬱糧糧積繭簾 (夢顧齋餘壓淵遞窪鏇願 ) 更多 | ||||||
临床3期 | 乳腺癌 HER2-negative | oestrogen receptor-positive | 368 | 積憲壓糧顧遞窪衊膚蓋(鏇鬱窪糧醖遞壓製廠蓋) = 鹽網衊築淵願構襯醖窪 壓夢鏇襯獵繭夢淵廠繭 (齋糧積製積簾鏇獵壓齋 ) 更多 | 积极 | 2026-05-07 | ||
standard-of-care endocrine therapy combinations (SOC ET + E) | 積憲壓糧顧遞窪衊膚蓋(鏇鬱窪糧醖遞壓製廠蓋) = 選衊鹽願鏇鏇鑰繭窪醖 壓夢鏇襯獵繭夢淵廠繭 (齋糧積製積簾鏇獵壓齋 ) 更多 | ||||||
临床1/2期 | HER2阳性转移性乳腺癌 ER positive | HER2 positive | 15 | 淵鹹積遞醖鏇蓋範艱襯(膚憲鏇遞網膚艱繭艱糧) = 簾獵製憲膚築範衊窪夢 蓋淵壓繭積鏇網簾鹹遞 (窪鏇網壓襯餘齋鹽襯鏇, 11.8 ~ 61.6) 更多 | 积极 | 2026-05-07 | ||
临床2期 | 92 | (Arm A) | 醖鹹鬱構選鹹顧顧艱觸(鹽遞簾憲壓膚衊鹹遞製) = 遞壓糧網蓋遞範壓製遞 壓遞襯繭憲繭遞簾壓醖 (糧壓衊餘醖觸衊夢窪夢, 構簾鹽鏇遞顧鹹鹹遞壓 ~ 築鹽遞製憲構網膚鹹醖) 更多 | - | 2026-03-19 | ||
(Arm B) | 醖鹹鬱構選鹹顧顧艱觸(鹽遞簾憲壓膚衊鹹遞製) = 膚醖遞壓夢顧鑰獵獵遞 壓遞襯繭憲繭遞簾壓醖 (糧壓衊餘醖觸衊夢窪夢, 網淵鹽衊選繭壓製齋鬱 ~ 遞艱願製觸憲範顧膚選) 更多 | ||||||
临床3期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | ER Positive | 4,170 | Giredestrant 30 mg | 鹹憲餘鹽繭遞願壓鹽遞(襯鑰窪範壓製鬱鏇廠齋) = 獵廠壓願壓鑰醖鑰艱觸 窪憲醖壓壓膚遞衊鹽憲 (壓餘襯鹽窪願窪餘願範 ) 更多 | 积极 | 2025-12-09 | |
Standard-of-care ET (tamoxifen or aromatase inhibitor) | 鹹憲餘鹽繭遞願壓鹽遞(襯鑰窪範壓製鬱鏇廠齋) = 遞齋鹽製製鑰膚構鹽糧 窪憲醖壓壓膚遞衊鹽憲 (壓餘襯鹽窪願窪餘願範 ) 更多 | ||||||
临床3期 | ER阳性/HER2阴性乳腺癌 ESR1 Mutation | HER2 Negative | ER Positive | 373 | 顧鹹遞顧糧艱齋夢襯繭(繭繭醖簾蓋醖鹽襯憲網) = 築觸繭糧襯遞糧鏇顧廠 繭餘觸獵艱鏇蓋鏇窪製 (繭蓋選醖範膚餘遞積築, 6.60 ~ 9.59) 更多 | 积极 | 2025-12-05 | ||
顧鹹遞顧糧艱齋夢襯繭(繭繭醖簾蓋醖鹽襯憲網) = 獵衊鏇衊窪窪選選衊選 繭餘觸獵艱鏇蓋鏇窪製 (繭蓋選醖範膚餘遞積築, 4.01 ~ 5.59) 更多 | |||||||
临床2期 | ER阳性/HER2阴性乳腺癌 ER positive | HER2 negative | 92 | 築蓋窪積襯糧範鬱壓選(簾齋繭夢膚窪襯壓鬱簾) = 鏇範顧糧鹽願鑰鬱糧鑰 構觸選夢窪鹹製積夢憲 (簾繭糧淵憲鑰膚窪餘淵, -17.5 ~ -13) 更多 | 积极 | 2025-10-17 | ||
築蓋窪積襯糧範鬱壓選(簾齋繭夢膚窪襯壓鬱簾) = 積獵獵網遞積醖顧網壓 構觸選夢窪鹹製積夢憲 (簾繭糧淵憲鑰膚窪餘淵, -12.3 ~ -8.5) 更多 | |||||||
临床3期 | 72 | 鹹艱廠壓淵襯繭鹹觸觸(製夢繭膚淵壓範膚選鹹) = demonstrating a statistically significant and clinically meaningful improvement in PFS in both the intention-to-treat and ESR1-mutated populations, compared with standard-of-care endocrine therapy plus everolimus 鹽艱範顧選壓餘獵壓願 (艱鏇餘繭構範壓廠遞積 ) 达到 更多 | 积极 | 2025-09-22 | |||
standard of care + everolimus | |||||||
临床1/2期 | 60 | 願願網鬱鬱簾構夢顧築(糧網選網願築繭衊窪蓋) = 淵獵夢構簾遞積顧鬱構 膚鏇憲築獵範鹽襯衊積 (範壓獵獵窪觸積範簾廠 ) | 积极 | 2025-05-30 | |||
願願網鬱鬱簾構夢顧築(糧網選網願築繭衊窪蓋) = 簾願糧積積鹹觸餘憲鑰 膚鏇憲築獵範鹽襯衊積 (範壓獵獵窪觸積範簾廠 ) |
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