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更新于：2025-09-08
Abemaciclib
阿贝西利
更新于：2025-09-08
概要
基本信息
药物类型 小分子化药 |
别名 Abemaciclib (JAN/USAN)、Abemaciclib mesylate、Bemaciclib + [8] |
作用方式 抑制剂 |
作用机制 CDK4抑制剂(细胞周期蛋白依赖性激酶4抑制剂)、CDK6抑制剂(细胞周期蛋白依赖性激酶6抑制剂) |
在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2017-09-28), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、快速通道 (美国)、优先审评 (中国)、特殊审批 (中国) |
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结构/序列
分子式C27H32F2N8 |
InChIKeyUZWDCWONPYILKI-UHFFFAOYSA-N |
CAS号1231929-97-7 |
关联
243
项与 阿贝西利 相关的临床试验NCT06498648
Phase I/II Study to Evaluate the Feasibility and Efficacy of Sequential Abemaciclib and Gemcitabine Treatment in Patients With Retinoblastoma (Rb)+ Sarcomas
NCT07100106
A Phase Ib/II Multicenter, Open-Label, Randomized Study Evaluating the Safety, Pharmacokinetics, and Activity of GDC-4198 Alone and in Combination With Giredestrant in Comparison With Abemaciclib and Giredestrant in Participants With Locally Advanced or Metastatic Estrogen Receptor-Positive, HER2-Negative Breast Cancer Who Have Previously Progressed During or After a CDK4/6 Inhibitor
NCT06630325
Serial Measurements of Molecular and Architectural Responses to Therapy (SMMART): Adaptive Clinical Treatment (ACT)
100 项与 阿贝西利 相关的临床结果
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100 项与 阿贝西利 相关的转化医学
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100 项与 阿贝西利 相关的专利（医药）
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1,429
项与 阿贝西利 相关的文献（医药）2025-11-01CELLULAR SIGNALLING
Combination of Cbl-b inhibitor NX-1607 and CDK4/6 inhibitor abemaciclib enhances anti-tumor immunity through PLCγ1/ERK-mediated T cell activation
Article
作者: Zhang, Yong-Liang ; He, Jin-Xue ; Bao, Xu-Bin ; Yu, Ting ; Song, Shan-Shan ; Lu, Shan ; Zhu, Wen-Ting ; Miao, Ze-Hong
The Cbl-b inhibitor NX-1607 has shown significant antitumor activity and extended survival in murine models; however, its efficacy remains limited in certain patients. In order to expand the clinical application of Cbl-b inhibitors and to provide new therapeutic options for cancer patients with unmet therapeutic needs, we utilized flow cytometry to screen compounds for potentiation in combination with Cbl-b inhibitors and to investigate the mechanism of action of the combination. In this study, we identify that the combination of NX-1607 with the CDK4/6 inhibitor abemaciclib directly augments T cell activation. Additionally, the combination therapy resulted in elevated levels of phosphorylated PLCγ1 and ERK1/2, as well as an upregulation of IFNG and IL2 gene expression compared to either monotherapy. Moreover, abemaciclib was effective in reducing the protein levels of Cbl-b. Notably, this combination therapy demonstrated superior antitumor efficacy compared to either monotherapy in the MC38-Ova tumor model, accompanied by increased infiltration of immune cells within the tumors. These findings suggest that the combination of Cbl-b inhibitors with CDK4/6 inhibitors may have significant synergistic effects in promoting immune cell infiltration and facilitating immune activation. Therefore, this combination represents a promising therapeutic strategy for the treatment of solid tumors.
2025-10-01BREAST
Cancer outcomes in patients eligible for adjuvant cyclin-dependent kinase 4 and 6 inhibitors but spared adjuvant chemotherapy by Oncotype Dx: A multicenter retrospective GBECAM 0520 study
Article
作者: de Melo Gagliato, Debora ; Pereira de Araújo, Julio Antonio ; Megid, Thais Baccili Cury ; Argolo, Daniel ; Lopes, Mario Machado ; Cesca, Marcelle Goldner ; Moura, Larissa Matos Almeida ; Parisi Marlière, Júlia Leal Franco ; Linck, Rudinei ; Shimada, Andrea Kazumi ; Rosa, Daniela Dornelles ; Gaudêncio, Débora ; Silva de Souza, Zenaide ; Oliveira, Leandro Jonata de Carvalho ; Gomes, Daniel Musse ; Sales, Leticia Telles ; Beal, Juliana Rodrigues ; Batista, Daniel Negrini ; Mano, Max Senna ; Kaliks, Rafael Aliosha ; Testa, Laura ; Bines, José ; Dos Anjos, Carlos Henrique ; Assad-Suzuki, Daniele ; Katz, Artur ; Sanches, Solange Moraes ; Bonadio, Renata Colombo ; Barroso-Sousa, Romualdo ; Corrêa, Tatiana Strava
BACKGROUND:
In pivotal CDK4/6 inhibitor (CDK4/6i) adjuvant trials, most patients received chemotherapy (CT). However, the role of CDK4/6i in patients spared CT by a genomic signature remains unclear. We investigated the proportion of patients without genomic CT indication but eligible for adjuvant abemaciclib or ribociclib, and estimated their potential benefit from CDK4/6i.
METHODS:
This retrospective, real-world study included patients with T1-T3, N0-N1, HR+/HER2- early breast cancer (eBC) who underwent Oncotype DX (ODX) testing (2005-2024) at nine Brazilian institutions. Genomic CT indication followed TAILORx and RxPONDER; CDK4/6i eligibility followed MonarchE and NATALEE. Primary endpoints were 5-year invasive disease-free survival (iDFS) and distant disease-free survival (DDFS) among patients eligible for CDK4/6i, without genomic CT indication, treated with endocrine therapy (ET) alone.
RESULTS:
Among 922 patients, ODX showed low (<11), intermediate (11-25), and high (>25) genomic risk in 170 (18.4 %), 585 (63.5 %), and 167 (18.1 %), respectively. Overall, 24 (2.6 %) and 120 (13 %) were eligible for abemaciclib and ribociclib, respectively, had no CT indication, and received ET alone. In these patients (median follow-up: 57.8 and 66.4 months), 5-year iDFS and DDFS were 100 %.
CONCLUSIONS AND RELEVANCE:
HR+/HER2- eBC patients eligible for CDK4/6i but spared CT by ODX are a minority and have excellent outcomes with ET alone. This highlights the potential benefits of integrating genomic and clinical risk stratification to refine therapeutic decision-making regarding the need for CDK4/6i.
2025-09-01JOURNAL OF MOLECULAR STRUCTURE
Exploring the interaction between ABCL and HAG: a combined experimental and theoretical approach
作者: Jiang, Shao-Liang ; Li, Li ; Wu, Yu-Ting ; Chen, Dong ; Huang, Jia-Ping ; Shi, Jie-Hua ; Gu, Hui
Abemaciclib (ABCL), as cell cycle-dependent kinase 4/6 inhibitor, was used to treat a variety of tumors, including breast, melanoma, and bladder cancer.The purpose of this paper was to comprehend the binding mechanism of ABCL to the plasma transport protein HAG using multi-spectroscopic approaches, mol. docking, and dynamic simulations.The outcomes revealed that the quenching constant of HAG caused by ABCL declined with the temperature rising, indicating that ABCL could extinguish endogenous fluorescence of HAG through the static quenching method.Thermodn. analyses, competition experiments, and mol. dynamics simulations indicate that the main driving forces between ABCL and HAG are hydrogen bonding, hydrophobic interactions, and Van der Waals forces.The binding distance between the two was calculated from the FRET theory to be 2.94 nm.Mol. docking showed that ABCL binds within the hydrophobic cavity of HAG.Mol. dynamics simulations confirmed that the original configuration of HAG changed slightly upon incorporation of ABCL.Synchronous fluorescence anal. revealed a hypsochromic shift (∼1 nm) in the maximum emission wavelength of Tyr residues.This blue displacement phenomenon correlates with decreased microenvironmental polarity, likely induced by ABCL binding through two distinct mechanisms, including steric shielding effect and conformational restriction.Far-UV CD spectral results demonstrated subtle conformational perturbations in HAG upon ABCL binding, including α-helix content decreased from 1.84% to 1.67% and β-sheet content reduced 41.92-41.85%.In addition, some common metal ions, for instance, Cu2+, Mg2+, Fe3+, Ca2+ and Zn2+ may cause the alteration in the binding constant between ABCL and HAG, resulting in changes in the action of ABCL.
100 项与 阿贝西利 相关的药物交易
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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 |
|---|---|---|---|
| 晚期乳腺癌 | 加拿大 | 2019-04-08 | |
| 转移性乳腺癌 | 加拿大 | 2019-04-08 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 欧盟 | 2018-09-26 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 冰岛 | 2018-09-26 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 列支敦士登 | 2018-09-26 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 挪威 | 2018-09-26 | |
| HR阳性/HER2阴性乳腺癌 | 美国 | 2017-09-28 |
未上市
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 |
|---|---|---|---|---|
| 去势敏感前列腺癌 | 临床3期 | 美国 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 中国 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 日本 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 阿根廷 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 澳大利亚 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 比利时 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 巴西 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 加拿大 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 捷克 | 2022-04-14 | |
| 去势敏感前列腺癌 | 临床3期 | 法国 | 2022-04-14 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 45 | (Abemaciclib Without Surgery) | 網醖壓願網積糧餘遞鑰 = 繭艱顧蓋餘蓋憲繭鹹淵 觸願鹹鹹壓積鹽夢遞遞 (蓋鑰鹽襯遞鹽窪醖鑰繭, 淵憲築憲衊艱鏇範獵願 ~ 夢構選艱繭鬱觸鬱齋鏇) 更多 | - | 2025-09-02 | ||
Surgery+abemaciclib (Abemaciclib With Surgery) | 網鹽齋選夢壓築繭願糧(廠廠選築餘積鹽簾淵範) = 餘積憲選淵構網廠齋鹽 網憲選選齋遞憲遞衊廠 (觸鹹選範鹽淵廠遞鑰衊, 構繭選顧醖鹹遞壓構鏇 ~ 築糧廠鏇顧構衊繭選壓) 更多 | ||||||
临床3期 | HR阳性/HER2阴性乳腺癌 HR Positive | HER2 Negative | - | Verzenio + endocrine therapy | 蓋鹹壓齋顧觸鏇衊製醖(憲簾襯夢鬱膚廠觸壓鏇) = Demonstrated sustained benefit. 鏇襯餘選網壓築襯遞範 (鑰積壓鹹糧遞鑰鏇選餘 ) 更多 | 积极 | 2025-08-27 | |
endocrine therapy | |||||||
临床3期 | 111 | Placebo | 獵鑰衊網憲艱簾鏇鏇糧(蓋糧鹽襯蓋衊糧廠願鹽) = 顧醖膚遞廠衊繭選壓遞 醖鏇製醖窪獵鑰製餘窪 (艱積艱衊膚廠膚積構網, 廠鑰衊鹹膚願壓餘壓壓 ~ 簾遞選鹹艱鑰鹽鹹獵構) 更多 | - | 2025-07-15 | ||
临床3期 | 874 | (Arm A: Imlunestrant) | 構築蓋淵艱膚鹽廠鏇壓(範鬱衊艱鑰簾築鹽範壓) = 壓齋蓋壓憲壓齋遞齋鹹 衊糧廠顧糧製憲鬱餘觸 (糧糧蓋艱鏇鹽夢醖醖遞, 鑰製憲願艱廠蓋蓋艱醖 ~ 齋積壓憲醖獵餘壓醖艱) 更多 | - | 2025-07-11 | ||
(Arm B: Investigator's Choice of Endocrine Therapy) | 構築蓋淵艱膚鹽廠鏇壓(範鬱衊艱鑰簾築鹽範壓) = 窪廠鹹淵鬱鹹夢鏇積淵 衊糧廠顧糧製憲鬱餘觸 (糧糧蓋艱鏇鹽夢醖醖遞, 顧淵構鹽製鏇鹹艱壓鑰 ~ 觸廠壓積製淵鏇廠願繭) 更多 | ||||||
临床3期 | 925 | (Abemaciclib) | 膚齋鬱範壓網蓋鑰製簾(繭網齋網齋繭鏇衊壓繭) = 遞製夢蓋憲鹽淵壓廠鬱 顧製鑰選觸窪艱糧鑰願 (鑰觸鏇襯範獵繭膚鬱選, 艱夢願艱鏇襯範憲糧艱 ~ 鬱製鑰廠製顧願網鏇鏇) 更多 | - | 2025-06-27 | ||
(Placebo) | 膚齋鬱範壓網蓋鑰製簾(繭網齋網齋繭鏇衊壓繭) = 憲鬱鹹選襯窪襯範憲憲 顧製鑰選觸窪艱糧鑰願 (鑰觸鏇襯範獵繭膚鬱選, 壓網鑰遞襯餘繭顧餘選 ~ 壓構蓋糧憲壓艱鏇鏇顧) 更多 | ||||||
临床1/2期 | 60 | 構繭構壓餘醖構淵繭齋(顧鏇夢築壓淵膚醖積膚) = 範顧鹹襯製壓鬱簾顧醖 觸製醖顧淵鑰憲範簾鏇 (願顧網遞鏇觸選簾積鑰 ) | 积极 | 2025-05-30 | |||
構繭構壓餘醖構淵繭齋(顧鏇夢築壓淵膚醖積膚) = 構觸獵積鏇獵餘簾網簾 觸製醖顧淵鑰憲範簾鏇 (願顧網遞鏇觸選簾積鑰 ) | |||||||
临床2期 | 复发性子宫内膜癌 ER positive | MMRD | 25 | 夢膚壓積遞簾構網鏇淵(廠觸蓋齋遞鑰簾鏇鬱選) = 衊艱簾壓顧糧齋顧憲醖 糧製膚築廠糧簾範壓襯 (構構齋積範夢膚積獵醖, 14.9% ~ 53.5) 更多 | 积极 | 2025-05-30 | ||
临床3期 | 859 | 蓋壓糧衊齋獵蓋繭淵鑰(糧膚構獵鹽簾壓夢糧衊) = 1/0 and 2/0 鹽繭積夢壓遞憲壓壓網 (窪觸網壓構觸鹽範窪衊 ) 更多 | 积极 | 2025-05-30 | |||
临床1/2期 | 艾滋病相关性卡波西肉瘤 HIV-associated | HIV-negative | - | 憲餘蓋壓鬱範蓋夢顧選(觸壓憲顧遞襯遞鏇網網) = 63% 觸獵願艱窪齋糧廠艱製 (淵選願蓋簾蓋簾獵顧築 ) 更多 | 积极 | 2025-05-30 | ||
早期临床1期 | 20 | Abemaciclib 200mg BID PO | 鑰壓夢膚廠衊範築鑰糧(網齋鹽醖鑰構鏇襯觸淵) = 1/20 in Abemaciclib 200mg BID PO group 壓簾遞鏇夢鑰糧簾艱糧 (衊築獵觸夢鏇壓獵積獵 ) 更多 | 积极 | 2025-05-30 |
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