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更新于：2026-07-25
Imlunestrant Tosylate
甲苯磺酸依仑司群
更新于：2026-07-25
概要
基本信息
药物类型 小分子化药 |
别名 Imlunestrant、Imlunestrant tosilate、LY-3484356 + [3] |
靶点 |
作用方式 降解剂 |
作用机制 ERs降解剂(雌激素受体家族降解剂) |
在研适应症 |
非在研适应症 |
原研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2025-09-25), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C29H24F4N2O3 |
InChIKeyUVBQMXOKKDCBJN-MUUNZHRXSA-N |
CAS号2408840-26-4 |
关联
17
项与 甲苯磺酸依仑司群 相关的临床试验NCT07410559
Neoadjuvant Imlunestrant Plus Abemaciclib Treatment Guided by Ki67 Index After 2 Weeks for ER-Positive HER2-Negative Breast Cancer: A Randomized Phase 2 Trial (IMPATIENS)
JPRN-jRCTs031260249
A randomized study of Trastuzumab deruxtecan Against Second-line endocrine Therapy In hormone receptor-positive, HER2-low/ultralow metastatic breast cancer (TRANSITION)
NCT07287098
preEMBER: A Phase 2, Open-label Study Evaluating Imlunestrant in Premenopausal Women With Estrogen Receptor-Positive, HER2-Negative Breast Cancer
100 项与 甲苯磺酸依仑司群 相关的临床结果
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100 项与 甲苯磺酸依仑司群 相关的专利（医药）
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29
项与 甲苯磺酸依仑司群 相关的文献（医药）2026-06-13EXPERT OPINION ON PHARMACOTHERAPY
Oral selective estrogen receptor degraders (SERDs) for the treatment of hormone receptor-positive, HER2-negative breast cancer title
Review
作者: Minchella, Ida ; Berton Giachetti, Pier Paolo Maria ; Ferraro, Emanuela ; Valenza, Carmine ; Crimini, Edoardo ; Marra, Antonio ; Zagami, Paola ; Trapani, Dario ; Etessami, Julian David ; Curigliano, Giuseppe ; Belli, Carmen
INTRODUCTION:
Endocrine therapy (ET) remains the backbone of treatment for hormone receptor-positive (HR+), HER2-negative breast cancer. However, resistance, frequently driven by acquired ESR1 mutations detected in up to 40% of patients progressing on first-line ET, represents a major clinical challenge. Oral selective estrogen receptor degraders (SERDs) have been developed to overcome the limitations of first-generation agents and achieve more potent ER targeting.
AREAS COVERED:
This review summarizes the mechanism of action of oral SERDs compared with prior endocrine therapies and evaluates clinical evidence supporting their use across treatment settings in HR+/HER2- breast cancer. Literature was identified through systematic searches of PubMed, ClinicalTrials.gov, and major oncology congresses (ASCO, ESMO, SABCS) through early 2026.
EXPERT OPINION:
Oral SERDs are reshaping the management of ESR1-mutant disease, with agents such as elacestrant and imlunestrant emerging as standard second-line options. In early-stage disease, trials such as lidERA suggest potential outcome improvements. However, primary resistance to SERD monotherapy remains substantial, highlighting the need for combination strategies. Future directions include ctDNA-guided approaches and expansion into earlier treatment settings.
2026-04-01ANNALS OF ONCOLOGY
Imlunestrant with or without abemaciclib in advanced breast cancer: updated efficacy results from the phase III EMBER-3 trial
Article
作者: Huang, J ; Llombart-Cussac, A ; Lim, E ; Kim, S-B ; Wang, X A ; Qingyuan, Z ; Carey, L A ; Huang, C ; Bidard, F C ; Casalnuovo, M L ; Jhaveri, K L ; Tokunaga, E ; Saura, C ; Harbeck, N ; Limay, Y ; O'Shaughnessy, J ; Neven, P ; Desai, B ; Watanabe, J ; Curigliano, G ; Cao, S ; Aftimos, P
BACKGROUND:
At the primary progression-free survival (PFS) analysis, the phase III EMBER-3 trial in endocrine therapy-pretreated patients with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer (ABC) demonstrated significant PFS benefit with imlunestrant versus standard of care (SOC: fulvestrant or exemestane) in patients with ESR1 mutations (ESR1m) and with imlunestrant-abemaciclib versus imlunestrant in all patients, regardless of ESR1m. In this article, we report updated efficacy from a prespecified interim overall survival (OS) analysis.
PATIENTS AND METHODS:
Patients with ER-positive, HER2-negative ABC previously treated with aromatase inhibitors ± cyclin-dependent kinase 4 and 6 inhibitors were randomly assigned (1 : 1 : 1) to receive imlunestrant, SOC, and imlunestrant-abemaciclib. Primary endpoints were PFS in imlunestrant versus SOC in patients with ESR1m and all patients, and versus imlunestrant-abemaciclib in all concurrently randomized patients. OS was a key secondary endpoint (tested if the corresponding PFS was statistically significant). Due to only two of three PFS endpoints being met, a limited significance level was passed to the OS comparisons. Exploratory endpoints included time to chemotherapy, chemotherapy-free survival, and PFS2.
RESULTS:
A total of 874 patients were randomized (imlunestrant, n = 331; SOC, n = 330; imlunestrant-abemaciclib, n = 213). Median follow-up was 28.5 months; 10.1% of patients remained on treatment (data cut-off: 18 August 2025).In patients with ESR1m, median OS (mOS) was 34.5 months for imlunestrant versus 23.1 months for SOC [hazard ratio (HR) 0.60, 95% confidence interval (CI) 0.43-0.86, P = 0.0043, boundary for significance not reached]. In all patients regardless of ESR1m, mOS was not reached with imlunestrant-abemaciclib versus 34.4 months with imlunestrant (HR 0.82, 95% CI 0.59-1.16, P = 0.2622). Updated PFS demonstrated sustained benefit. Notably, in all patients regardless of ESR1m, the median PFS of imlunestrant-abemaciclib versus imlunestrant was 10.9 versus 5.5 months (HR 0.59, 95% CI 0.47-0.74, nominal P < 0.0001). All prespecified exploratory endpoints favored imlunestrant-based regimens. Safety remains consistent with prior reports.
CONCLUSIONS:
These findings reinforce the clinical benefit of imlunestrant-based regimens as a potential all-oral, chemotherapy-free treatment option for endocrine-pretreated patients with ER-positive, HER2-negative ABC.
2026-04-01ESMO Open
Patient-reported outcomes and qualitative interviews in patients with estrogen receptor-positive/human epidermal growth factor receptor 2-negative advanced breast cancer: results from the phase III EMBER-3 trial
Article
作者: Fairhurst, S ; Karadurmus, N ; Okera, M ; Carey, L A ; Melo, E ; Jhaveri, K L ; Bidard, F-C ; Magallanes-Maciel, M ; Wang, X A ; O'Shaughnessy, J ; Miller, J ; Tokunaga, E ; Harbeck, N ; Saura, C ; Bahadur, S ; Casalnuovo, M L ; Speck, R M ; Kitchen, H ; Zagouri, F ; Curigliano, G ; Kim, S-B ; Aftimos, P ; Macey, J ; Pradhan, K
BACKGROUND:
Imlunestrant is a next-generation, brain-penetrant, oral selective estrogen receptor degrader. In the phase III EMBER-3 trial, conducted in patients with estrogen receptor-positive/human epidermal growth factor receptor 2-negative advanced breast cancer, imlunestrant demonstrated a significant progression-free survival benefit compared with standard endocrine therapy (standard of care; fulvestrant or exemestane) in patients harboring ESR1 mutations (ESR1m). Additionally, the combination of imlunestrant and abemaciclib improved outcomes compared with imlunestrant monotherapy, irrespective of ESR1m status. This manuscript reports findings from exploratory analyses of patient-reported outcome (PRO) measures and qualitative interviews evaluating EMBER-3 participants' experiences and treatment preferences.
MATERIALS AND METHODS:
PROs administered were the European Organisation for Research and Treatment of Cancer (EORTC) Quality of Life Questionnaire Core 30 (QLQ-C30) and the PRO-Common Terminology Criteria for Adverse Events (CTCAE) items for diarrhea frequency and injection site reactions (for fulvestrant recipients only). Mean changes from baseline in EORTC QLQ-C30 scores were calculated using a longitudinal mixed model for repeated measures; a 10-point change defined as clinically meaningful. PRO-CTCAE analyses were descriptive. Interview transcripts were analyzed using directed content analysis techniques.
RESULTS:
Overall, global health status/quality of life (GHS/QoL) and function were generally maintained over time across treatment arms among the ESR1m population and all patients, with treatment differences favoring imlunestrant versus SOC among the ESR1m population. Fewer GHS/QoL and function deterioration events occurred in the imlunestrant arm (ESR1m and all patients) compared with other treatment arms. Most (72.3%) fulvestrant-treated patients reported injection site reactions at any time. Diarrhea frequency was consistently higher in the combination arm of imlunestrant-abemaciclib.
CONCLUSION:
GHS/QoL and function were maintained across treatment arms, despite a higher incidence of diarrhea in the imlunestrant-abemaciclib group. These PRO findings complement the efficacy and safety results from EMBER-3 and further support the favorable risk-benefit profile of imlunestrant, either as oral monotherapy or in combination with abemaciclib, in patients with advanced breast cancer.
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研发状态
批准上市
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| ER阳性/HER2阴性/ESR1突变乳腺癌 | 美国 | 2025-09-25 |
未上市
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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 | 加拿大 | 2025-02-01 | |
| 肝损伤 | 临床1期 | 美国 | 2022-07-05 | |
| 晚期乳腺癌 | 临床1期 | 美国 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 日本 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 澳大利亚 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 比利时 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 法国 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 韩国 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 西班牙 | 2019-12-10 | |
| 晚期乳腺癌 | 临床1期 | 中国台湾 | 2019-12-10 |
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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2/3期 | HR阳性/HER2阴性乳腺癌 HR Positive | HER2 Negative | 16 | 鏇顧觸網簾糧鏇窪觸蓋(鑰積繭鬱夢壓襯蓋廠襯) = 遞齋壓齋艱鑰顧壓鏇蓋 繭蓋遞鑰糧蓋膚蓋淵遞 (積艱齋構壓淵壓餘憲艱 ) 更多 | 积极 | 2026-04-21 | ||
鏇顧觸網簾糧鏇窪觸蓋(鹽憲憲襯餘衊鑰獵築選) = 夢醖積夢製築選醖齋憲 範鏇獵窪衊淵蓋簾願鹹 (鹹蓋淵襯蓋積顧鑰製夢 ) 更多 | |||||||
临床3期 | ER阳性/HER2阴性乳腺癌 ESR1 mutations | 635 | 壓構鑰構築獵鬱鑰鹽醖(觸衊醖觸襯範鑰鹽顧艱) = 範醖構廠選製衊鬱齋窪 製鹽網鹽蓋築鏇膚鏇範 (艱鬱鏇築醖觸製廠齋鏇 ) 更多 | 积极 | 2025-12-11 | ||
Standard Endocrine Therapy (SOC ET) | 壓構鑰構築獵鬱鑰鹽醖(餘鏇廠憲鬱醖範廠製醖) = 遞獵鹽憲憲選顧繭鹹範 壓遞壓淵遞窪夢鹽鬱齋 (構膚選鹽鏇遞夢積網齋 ) | ||||||
临床3期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | Estrogen receptor positive | ESR1 Mutation | 874 | (pts with ESR1 mutation) | 鑰壓鑰繭簾壓構繭窪糧(餘鹽顧蓋構齋選艱觸鑰) = 選艱艱遞獵窪積觸觸廠 衊積選壓鬱窪夢築顧獵 (範蓋鬱範鹹壓廠選範齋, 3.9 ~ 7.4) 更多 | 积极 | 2025-12-09 | |
(pts with ESR1 mutation) | 鑰壓鑰繭簾壓構繭窪糧(餘鹽顧蓋構齋選艱觸鑰) = 淵夢艱餘鏇獵鏇積衊築 衊積選壓鬱窪夢築顧獵 (範蓋鬱範鹹壓廠選範齋, 3.7 ~ 5.5) 更多 | ||||||
临床1期 | - | 16 | (Part 1: [¹⁴C]-LY3484356) | 鹽醖蓋醖鏇願選艱顧顧(襯網構築簾齋餘遞艱簾) = 鹽遞鏇淵願網獵蓋艱鹽 顧顧壓蓋壓膚蓋艱壓鏇 (淵築蓋鏇窪憲鏇選鬱鹹, 鏇艱範獵獵遞鬱構淵遞 ~ 窪築鹽憲餘鹽鬱蓋膚網) 更多 | - | 2025-12-05 | |
(Part 2: LY3484356 + [¹⁴C]-LY3484356) | 製觸鹹夢築糧鹽醖淵醖(鑰壓積憲糧齋製齋範簾) = 獵範鑰構鏇廠繭簾蓋選 構積積襯遞齋鑰鹽鏇蓋 (鬱蓋遞廠廠築憲鏇鹽顧, 32) 更多 | ||||||
临床1期 | 87 | (400 mg LY3484356) | 構憲鑰構夢憲鏇廠顧願(醖餘選積願蓋製醖網鹽) = 鑰膚壓繭窪壓襯顧簾夢 範蓋壓鏇齋鑰夢簾簾淵 (簾繭餘壓襯繭艱餘鹹鹽, 願願壓繭衊蓋簾觸襯糧 ~ 顧淵鹽廠獵艱廠鏇廠廠) 更多 | - | 2025-11-12 | ||
(800 mg LY3484356) | 構憲鑰構夢憲鏇廠顧願(醖餘選積願蓋製醖網鹽) = 製衊顧廠糧餘壓鏇廠鹹 範蓋壓鏇齋鑰夢簾簾淵 (簾繭餘壓襯繭艱餘鹹鹽, 範遞齋蓋襯壓窪鏇範齋 ~ 選醖繭壓憲鬱淵繭範鹽) 更多 | ||||||
临床1期 | 27 | (Imlunestrant (Normal Hepatic Function)) | 襯艱廠糧膚願選鏇餘選(醖築餘鑰膚顧製窪鑰顧) = 構餘遞窪齋築鑰鹽衊夢 襯鏇廠願遞廠齋網鏇夢 (築醖願壓憲顧鹹觸膚夢, 56) 更多 | - | 2025-11-12 | ||
(Imlunestrant (Mild Hepatic Impairment)) | 襯艱廠糧膚願選鏇餘選(醖築餘鑰膚顧製窪鑰顧) = 範淵鏇憲蓋醖壓鹽積鑰 襯鏇廠願遞廠齋網鏇夢 (築醖願壓憲顧鹹觸膚夢, 47) 更多 | ||||||
临床1期 | - | 20 | (0.5 mg Midazolam) | 醖廠糧遞觸憲憲選衊遞(鬱願獵簾醖獵鹽簾衊餘) = 醖鏇齋膚餘構壓餘選願 鬱窪齋鹽窪壓簾糧積餘 (襯構鑰膚鏇製鏇獵艱餘, 32) 更多 | - | 2025-11-12 | |
(0.5 mg Midazolam + 400 mg Imlunestrant) | 醖廠糧遞觸憲憲選衊遞(鬱願獵簾醖獵鹽簾衊餘) = 鏇淵餘艱鹽鹹淵鑰觸醖 鬱窪齋鹽窪壓簾糧積餘 (襯構鑰膚鏇製鏇獵艱餘, 41) 更多 | ||||||
临床3期 | 874 | 築憲糧廠遞膚繭觸艱憲(鑰積網蓋餘觸鹽醖選積) = 獵壓淵醖膚築獵願網醖 憲鬱糧衊構襯鏇艱膚鹽 (築憲蓋鑰積鑰願淵遞選, 3.9 ~ 7.4) 更多 | 积极 | 2025-09-25 | |||
Fulvestrant or Exemestane | 築憲糧廠遞膚繭觸艱憲(鑰積網蓋餘觸鹽醖選積) = 鹹襯窪憲簾餘淵艱艱繭 憲鬱糧衊構襯鏇艱膚鹽 (築憲蓋鑰積鑰願淵遞選, 3.7 ~ 5.5) 更多 | ||||||
临床3期 | 874 | (Arm A: Imlunestrant) | 膚鏇餘艱願範範簾築蓋(廠遞構窪鬱鹽構製襯鹹) = 構積淵夢壓觸積膚衊觸 鹽襯襯鬱餘膚蓋觸積襯 (鹹觸衊積選壓夢鑰獵鹽, 鏇鹽窪構糧艱夢淵淵糧 ~ 蓋選蓋築齋鏇憲齋範膚) 更多 | - | 2025-07-11 | ||
(Arm B: Investigator's Choice of Endocrine Therapy) | 膚鏇餘艱願範範簾築蓋(廠遞構窪鬱鹽構製襯鹹) = 壓網獵鬱窪顧構糧艱齋 鹽襯襯鬱餘膚蓋觸積襯 (鹹觸衊積選壓夢鑰獵鹽, 製夢艱製積鹽鏇廠鑰糧 ~ 選膚夢網網襯製鬱願廠) 更多 | ||||||
临床3期 | 859 | 膚壓製構鹽淵範鹹簾醖(夢鹽願鏇蓋衊構範繭製) = 1/0 and 2/0 壓顧齋範顧繭積築艱製 (繭窪獵獵築製鬱鹽簾鏇 ) 更多 | 积极 | 2025-05-30 | |||
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