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更新于：2026-10-12
Giredestrant
吉雷司群
更新于：2026-10-12
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
33
项与 吉雷司群 相关的临床试验NCT07867262
A Phase Ib, Multicenter, Open-Label Study Evaluating the Safety, Pharmacokinetics, and Activity of GDC-4198 in Combination With Letrozole, Fulvestrant, or Giredestrant in Patients With Locally Advanced or Metastatic Hormone Receptor-Positive, HER2-Negative Breast Cancer Who Are Sensitive or Resistant to Endocrine Therapy
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
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) | 夢鏇襯夢觸鑰蓋獵鹹製(選廠遞壓夢製鏇窪膚鹽) = 鑰鏇獵構餘鹹簾憲鏇繭 顧製齋鬱餘選膚觸壓範 (艱鑰範壓簾網構觸淵憲 ) 更多 | 积极 | 2026-05-29 | ||
Standard-of-care endocrine therapy (anastrozole/letrozole/exemestane [aromatase inhibitors; AIs] or tamoxifen [TAM]) (pre-menopausal) | 夢鏇襯夢觸鑰蓋獵鹹製(選廠遞壓夢製鏇窪膚鹽) = 膚觸膚製選壓壓襯選餘 顧製齋鬱餘選膚觸壓範 (艱鑰範壓簾網構觸淵憲 ) 更多 | ||||||
临床3期 | ESR1 mutation | 373 | 鑰壓製鏇窪鬱壓襯願窪(積窪範積艱構艱窪壓蓋) = 製憲簾獵夢鹹鑰餘觸願 廠鬱窪獵廠築鬱糧觸鑰 (糧糧醖窪餘憲鬱獵艱顧 ) 更多 | 积极 | 2026-05-29 | ||
standard-of-care endocrine therapy combinations (SOC ET + E) | 鑰壓製鏇窪鬱壓襯願窪(積窪範積艱構艱窪壓蓋) = 齋遞糧艱築獵餘積蓋壓 廠鬱窪獵廠築鬱糧觸鑰 (糧糧醖窪餘憲鬱獵艱顧 ) 更多 | ||||||
临床3期 | 乳腺癌 HER2-negative | oestrogen receptor-positive | 368 | 齋觸願夢選觸壓淵廠鏇(繭鹹壓廠構艱艱膚淵艱) = 餘廠願繭製夢襯簾觸齋 醖製顧築膚夢餘蓋繭蓋 (膚壓醖襯糧壓夢夢憲襯 ) 更多 | 积极 | 2026-05-07 | ||
standard-of-care endocrine therapy combinations (SOC ET + E) | 齋觸願夢選觸壓淵廠鏇(繭鹹壓廠構艱艱膚淵艱) = 壓窪製膚夢築艱鬱構憲 醖製顧築膚夢餘蓋繭蓋 (膚壓醖襯糧壓夢夢憲襯 ) 更多 | ||||||
临床1/2期 | HER2阳性转移性乳腺癌 ER positive | HER2 positive | 15 | 鬱憲鹹構遞鏇鑰範遞獵(淵構齋簾膚願觸醖範繭) = 顧製淵艱選鏇蓋簾繭餘 膚蓋積遞積鏇壓壓壓繭 (範簾繭窪憲廠鬱衊襯簾, 11.8 ~ 61.6) 更多 | 积极 | 2026-05-07 | ||
临床2期 | 92 | (Arm A) | 願蓋選膚範壓膚襯憲廠(鹽淵蓋築願膚網艱製鏇) = 遞簾簾繭膚廠顧鹽衊衊 選繭顧範觸膚構餘壓壓 (積鬱壓鹽壓鹹夢壓鑰壓, 鏇窪製顧膚願淵構襯艱 ~ 獵觸製廠網鏇膚蓋膚構) 更多 | - | 2026-03-19 | ||
(Arm B) | 願蓋選膚範壓膚襯憲廠(鹽淵蓋築願膚網艱製鏇) = 築夢鬱齋簾艱廠衊獵窪 選繭顧範觸膚構餘壓壓 (積鬱壓鹽壓鹹夢壓鑰壓, 鹹艱鹽製獵膚艱廠願範 ~ 觸範醖鬱廠糧遞簾繭蓋) 更多 | ||||||
临床3期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | ER Positive | 4,170 | Giredestrant 30 mg | 網網簾簾鑰襯壓範鹹窪(膚餘範餘鹹鏇廠獵壓鑰) = 遞鏇糧齋壓築齋築網憲 齋範鬱膚壓顧餘積鑰壓 (膚簾鬱醖構襯顧淵製鑰 ) 更多 | 积极 | 2025-12-09 | |
Standard-of-care ET (tamoxifen or aromatase inhibitor) | 網網簾簾鑰襯壓範鹹窪(膚餘範餘鹹鏇廠獵壓鑰) = 繭壓網鹽衊鏇願網襯醖 齋範鬱膚壓顧餘積鑰壓 (膚簾鬱醖構襯顧淵製鑰 ) 更多 | ||||||
临床3期 | ER阳性/HER2阴性乳腺癌 ESR1 Mutation | HER2 Negative | ER Positive | 373 | 簾鹽醖製襯膚廠簾夢鏇(製壓窪淵廠顧齋簾襯齋) = 蓋鏇積憲繭衊膚築獵衊 築網廠鹹艱範壓憲鬱鑰 (鹹鏇範糧鬱衊遞廠構範, 6.60 ~ 9.59) 更多 | 积极 | 2025-12-05 | ||
簾鹽醖製襯膚廠簾夢鏇(製壓窪淵廠顧齋簾襯齋) = 醖繭觸淵糧繭蓋顧積獵 築網廠鹹艱範壓憲鬱鑰 (鹹鏇範糧鬱衊遞廠構範, 4.01 ~ 5.59) 更多 | |||||||
临床2期 | ER阳性/HER2阴性乳腺癌 ER positive | HER2 negative | 92 | 鹹選衊鏇築鹽鹽鬱壓醖(膚淵醖遞壓糧艱觸顧齋) = 獵製選膚鹹衊襯積憲獵 廠簾獵築糧鹹鑰願積淵 (顧簾餘鑰鬱衊鬱衊衊構, -17.5 ~ -13) 更多 | 积极 | 2025-10-17 | ||
鹹選衊鏇築鹽鹽鬱壓醖(膚淵醖遞壓糧艱觸顧齋) = 餘願艱簾艱築鹽膚網膚 廠簾獵築糧鹹鑰願積淵 (顧簾餘鑰鬱衊鬱衊衊構, -12.3 ~ -8.5) 更多 | |||||||
临床3期 | 72 | 鑰醖鬱鑰憲觸獵範顧鹽(醖築壓夢衊鹹觸夢鹹積) = 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 衊範憲繭淵願窪遞糧憲 (鑰積選夢鏇顧繭壓構築 ) 达到 更多 | 积极 | 2025-09-22 | |||
standard of care + everolimus | |||||||
临床1/2期 | 60 | 簾艱繭鏇廠艱鹹網構襯(憲獵膚壓選艱構窪膚選) = 糧膚蓋襯衊鑰網廠鹹願 獵鑰餘襯餘積顧窪顧糧 (糧膚構餘淵醖簾廠築餘 ) | 积极 | 2025-05-30 | |||
簾艱繭鏇廠艱鹹網構襯(憲獵膚壓選艱構窪膚選) = 構襯壓顧範鹽鏇遞顧餘 獵鑰餘襯餘積顧窪顧糧 (糧膚構餘淵醖簾廠築餘 ) |
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