预约演示
更新于：2026-09-08
Ribociclib Succinate
琥珀酸瑞波西利
更新于：2026-09-08
概要
基本信息
药物类型 小分子化药 |
别名 Kisqali、ribociclib、利柏西利 + [7] |
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 |
最高研发阶段批准上市 |
首次获批日期 美国 (2017-03-13), |
最高研发阶段(中国)批准上市 |
特殊审评孤儿药 (美国)、突破性疗法 (美国) |
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结构/序列
分子式C27H36N8O5 |
InChIKeyNHANOMFABJQAAH-UHFFFAOYSA-N |
CAS号1374639-75-4 |
关联
197
项与 琥珀酸瑞波西利 相关的临床试验NCT07423611
A Multicenter, Open-label, Randomized Controlled Clinical Study Comparing the Efficacy and Safety of ctDNA-guided Ribociclib Plus Endocrine Therapy Versus Chemotherapy Followed by Ribociclib Plus Endocrine Therapy as Adjuvant Treatment in Patients With HR+/HER2- Early Breast Cancer
NCT07391774
A Phase III Trial of Rx Therapy Guided by Genomic Risk Assessment For High Anatomic Stage ER-pos/HER2-neg Breast Cancer With RS Less Than or Equal to 25 (RxFINE-Low)
NCT07647328
SERAFA-1: A Single Arm, Open Label, Multicentre, Phase IIIb Study Of Camizestrant Plus Ribociclib in 1st Line Treatment of ER Positive, HER2-negative Advanced Breast Cancer Patients
100 项与 琥珀酸瑞波西利 相关的临床结果
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100 项与 琥珀酸瑞波西利 相关的转化医学
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100 项与 琥珀酸瑞波西利 相关的专利（医药）
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1,483
项与 琥珀酸瑞波西利 相关的文献（医药）2026-12-31Journal of Pharmaceutical Policy and Practice
Economic evaluation of cyclin-dependent kinases 4 and 6 inhibitors in advanced hormonal receptor-positive and human epidermal growth factor receptor 2 negative breast cancer: a nationwide budget impact analysis
Article
作者: Hamad, Anas ; Shafei, Laila ; Hisham Al-Ziftawi, Nour ; Mohamed Ibrahim, Mohamed Izham ; Bojassoum, Salha ; Elazzazy, Shereen
Background:
Several trials demonstrated improvements in clinical outcomes associated with cyclin-dependent kinase 4 and 6 (CDK4/6) inhibitors in breast cancer patients. The challenge remains regarding their high costs. Ribociclib and Abemaciclib are cost-effective in Qatar. Yet, their affordability was not studied. This budget impact analysis (BIA) is to assess the affordability of adopting CDK4/6 inhibitors in Qatar over five years duration (2024-2028).
Methods:
We ran a BIA to evaluate two scenarios: (1) Increasing abemaciclib's market share from 20% to 60%, replacing both palbociclib and ribociclib. (2) Assuming equal market share for both ribociclib and abemaciclib up to 80%, reducing palbociclib's share. The analysis considered treatment costs, patient population, and disease prevalence. All data were retrieved from the National Center for Cancer Care and Research, and costs were presented in Qatari Riyals (QAR). Sensitivity analyses were run to ensure the robustness of the conclusion. All results were compared to Qatar's budget threshold, which is QAR 453,822.
Results:
Based on a total of 173 patients using CDK4/6 inhibitors, increasing abemaciclib's market share to 60% yielded cumulative savings of QAR 14 million over five years, which is around QAR 14,613 per patient per year. However, equally increasing ribociclib's and abemaciclib's market share to 80% resulted in a modest budget increase, remaining within acceptable thresholds. Sensitivity analyses confirmed the robustness of these findings, showing that cost reductions and higher uptake rates further enhanced savings.
Conclusion:
Abemaciclib is a budget-saving option for HR+/HER2- breast cancer in Qatar, should it replace the market share by up to 60% over five years. In addition, ribociclib and abemaciclib are affordable treatment options if they equally contributes to up to 80% of the market share for the eligible advanced breast cancer patients. The results supported the concept of allocating CDK4/6 inhibitors as they were found to be affordable to the Qatari healthcare system.
2026-10-01AMERICAN JOURNAL OF OPHTHALMOLOGY
Corneal Epithelial Alterations Associated With Cyclin-Dependent Kinase 4/6 Inhibitor Therapy in Hormone Receptor–Positive Breast Cancer
Article
作者: Ozbay, Esra Kızıldag ; Ovali, Fatma Su ; Kucuk, Mehmet Fatih ; Karaca, Mustafa ; Ozbay, Mehmet Fatih ; Dogan, Berna ; Ozturk, Banu
IMPORTANCE:
Cyclin-dependent kinase 4/6 (CDK4/6) inhibitors are standard therapy for hormone receptor-positive (HR+), HER2-negative breast cancer. By blocking the G1/S cell-cycle transition, these agents may impair renewal of the corneal epithelium. No controlled study has systematically evaluated corneal epithelial changes in patients receiving CDK4/6 inhibitors.
OBJECTIVE:
To determine whether CDK4/6 inhibitor-based therapy is associated with cornealepithelial alterations independent of aromatase inhibitor exposure and tear film dysfunction.
DESIGN, SETTING, AND PARTICIPANTS:
Retrospective comparative cross-sectional study at a tertiary ophthalmology center. A total of 132 women were enrolled: 45 receiving a CDK4/6 inhibitor plus an aromatase inhibitor (CDKAI group), 44 receiving aromatase inhibitor monotherapy (AI group), and 43 age-matched postmenopausal controls without systemic oncologic therapy.
EXPOSURES:
CDK4/6 inhibitor (ribociclib, palbociclib, or abemaciclib) combined with an aromatase inhibitor; aromatase inhibitor alone; or no systemic oncologic therapy.
MAIN OUTCOMES AND MEASURES:
Prevalence and severity of punctate epitheliopathy and vortex keratopathy, assessed by a masked ophthalmologist. Secondary outcomes included Schirmer I test, tear film break-up time, and Ocular Surface Disease Index (OSDI).
RESULTS:
PE was present in 44.4% of eyes in the CDKAI group vs 4.7% in the AI group and 2.3% in controls (χ² = 34.31; P < .001). All moderate (13.3%) and severe/complicated (8.9%) PE cases occurred exclusively in the CDKAI group. Vortex keratopathy was observed in 13.3% of CDKAI patients and in none of the other groups (P = .025). Schirmer values, tear film break-up time, and OSDI scores did not differ among groups (all P > .05). Within the CDKAI group, PE was not associated with treatment duration (P = .963) or tear film parameters.
CONCLUSIONS AND RELEVANCE:
In this comparative study, CDK4/6 inhibitor-based therapy was associated with significantly higher prevalence and severity of PE and vortex keratopathy, independent of aromatase inhibitor exposure and in the absence of measurable tear film dysfunction. These findings suggest a direct cytostatic effect on the corneal epithelium. Symptom scores were low, although OSDI interpretation was limited by incomplete responses. Proactive corneal surface evaluation with fluorescein staining may be warranted during CDK4/6 inhibitor treatment.
2026-10-01BIOORGANIC & MEDICINAL CHEMISTRY
CDK4/6-targeted therapy: From clinical inhibitors to emerging strategies to overcome resistance
Review
作者: Lu, Ying ; Yan, Zitong ; Feng, Dijing ; Chen, Zhuo ; Sha, Wenjie
The Cyclin-dependent kinase 4/6 (CDK4/6) complex orchestrates the critical G1-to-S phase transition by phosphorylating the Retinoblastoma protein (Rb), establishing it as a validated therapeutic target in oncology. The clinical deployment of ATP-competitive inhibitors-Palbociclib, Ribociclib, and Abemaciclib-has revolutionized the standard of care for hormone receptor-positive breast cancer. However, the long-term efficacy of these agents is inevitably compromised by the emergence of intrinsic and acquired resistance. This multifaceted resistance landscape is driven by genomic alterations including RB1 loss, activation of compensatory bypass signaling pathways, and the adaptive scaffolding functions of CDK6. Consequently, therapeutic strategies are evolving from simple inhibition to rational intervention. In this review, we systematically elucidate these emerging interventions. On one hand, we explore strategies grounded in the optimization of occupancy-based inhibition, specifically highlighting the synergistic combination regimens and rational design of dual-target small molecules to re-sensitize resistant tumors. On the other hand, we highlight the paradigm shift toward Proteolysis Targeting Chimera (PROTAC) technology. By recruiting the ubiquitin-proteasome system to catalytically degrade target proteins, CDK4/6-PROTACs eliminate both enzymatic activity and non-catalytic scaffolding functions, offering a mechanistically distinct strategy to overcome the structural limitations of traditional inhibitors. This review summarizes the progression from clinical inhibitors to strategies for overcoming resistance, offering insights into the future development of CDK4/6-targeted therapies.
100 项与 琥珀酸瑞波西利 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 晚期乳腺癌 | 加拿大 | 2018-03-02 | |
| 转移性乳腺癌 | 加拿大 | 2018-03-02 | |
| HR阳性/HER2阴性乳腺癌 | 美国 | 2017-03-13 |
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 |
|---|---|---|---|---|
| 晚期 HER2 阳性乳腺癌 | 临床3期 | 美国 | 2022-03-28 | |
| 晚期 HER2 阳性乳腺癌 | 临床3期 | 葡萄牙 | 2022-03-28 | |
| 晚期 HER2 阳性乳腺癌 | 临床3期 | 西班牙 | 2022-03-28 | |
| 早期乳腺癌 | 临床3期 | - | 2018-03-31 | |
| HER2 阴性乳腺癌 | 临床3期 | 意大利 | 2018-02-02 | |
| 6型髓鞘减少脑白质营养不良 | 临床3期 | 意大利 | 2018-02-02 | |
| 局部晚期乳腺癌 | 临床3期 | 意大利 | 2018-02-02 | |
| 乳腺癌 | 临床3期 | 美国 | 2017-06-07 | |
| 晚期癌症 | 临床3期 | 美国 | 2016-11-30 | |
| 晚期癌症 | 临床3期 | 阿根廷 | 2016-11-30 |
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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1期 | 12 | 憲顧製糧壓襯憲襯餘鑰(蓋築艱觸夢憲鹽鬱繭網) = 選夢壓齋獵廠餘鑰衊齋 衊壓顧製選蓋壓鹽衊簾 (構憲糧膚簾選製餘簾鑰, 壓鏇獵齋壓觸鹹憲壓簾 ~ 鬱鏇鹽淵網選齋餘窪膚) 更多 | - | 2026-09-04 | |||
临床3期 | 287 | (Ribociclib+Letrozole (Core Phase)) | 窪衊構鏇夢糧構衊鏇壓(鑰繭繭齋衊餘鬱夢艱構) = 窪廠選窪選範糧鑰蓋製 蓋壓鏇觸鬱夢鏇遞醖壓 (願簾製願醖鹹夢繭鏇構, 鑰簾繭鹽蓋範衊壓鏇網 ~ 築顧製糧膚製廠夢繭艱) 更多 | - | 2026-07-10 | ||
(Alpelisib+Fulvestrant (Extension Phase)) | 繭鹹齋鬱廠襯艱膚製壓 = 襯壓窪鹽醖蓋觸壓鏇獵 壓淵遞鬱鏇積構獵觸製 (獵鹹淵憲鬱艱齋選壓蓋, 憲壓製願餘築獵窪鏇顧 ~ 蓋夢艱製獵醖繭壓淵範) 更多 | ||||||
临床3期 | HR阳性/HER2阴性小叶癌 hormone receptor-positive | human epidermal growth factor receptor 2-negative | 724 | (Early Breast Cancer) | 簾鏇鏇願糧獵鏇鑰觸顧(夢繭鏇鬱糧範壓遞鑰壓) = Patients with EBC receiving 400 mg experienced lower rates and severity of both neutropenia and QTcF prolongation than patients with advanced breast cancer receiving 600 mg. 顧遞獵鹹構艱繭構艱齋 (網壓艱醖築憲衊壓鏇鏇 ) | 积极 | 2026-06-23 | |
临床1/2期 | 去势抵抗性前列腺癌 RB expression | 46 | 顧壓蓋簾選簾簾鑰餘糧(艱夢醖觸積構構網齋壓) = 觸糧夢積鏇範鑰築鏇簾 鹹鏇觸憲製蓋鏇選獵積 (繭齋餘糧廠製鏇艱衊夢, 43 ~ 95) 更多 | 不佳 | 2026-05-29 | ||
顧壓蓋簾選簾簾鑰餘糧(艱夢醖觸積構構網齋壓) = 襯觸鬱膚鹹選顧製蓋齋 鹹鏇觸憲製蓋鏇選獵積 (繭齋餘糧廠製鏇艱衊夢, 65 ~ 93) 更多 | |||||||
N/A | 15,374 | 積鏇襯網膚選夢鹽餘衊(範窪獵觸製廠襯膚構簾) = 憲製蓋夢簾願獵鹹築鹹 廠繭積網製壓網選製蓋 (蓋壓壓糧願憲鑰鑰製遞 ) 更多 | 积极 | 2026-05-29 | |||
積鏇襯網膚選夢鹽餘衊(範窪獵觸製廠襯膚構簾) = 遞鏇糧憲憲積繭齋製廠 廠繭積網製壓網選製蓋 (蓋壓壓糧願憲鑰鑰製遞 ) 更多 | |||||||
临床2期 | HER2阳性转移性乳腺癌 HER2-positive | 12 | T-DM1 + ribociclib | 衊壓繭製餘築觸鏇膚窪(範鏇憲鏇簾餘廠獵淵廠) = 淵餘窪艱願構齋願蓋廠 憲鑰網範襯鏇夢鹽遞蓋 (簾壓築膚獵夢遞築鬱積 ) 更多 | 积极 | 2026-05-29 | |
T-DM1 + ribociclib (ER-positive) | 衊壓繭製餘築觸鏇膚窪(範鏇憲鏇簾餘廠獵淵廠) = 鑰廠鏇鏇製鑰範鹹鹹鬱 憲鑰網範襯鏇夢鹽遞蓋 (簾壓築膚獵夢遞築鬱積 ) 更多 | ||||||
N/A | 5,649 | Ribociclib + An Aromatase Inhibitor | 遞築憲顧夢淵艱餘艱獵(襯鏇選築選製繭夢築願) = 蓋糧簾窪壓遞觸構築衊 選製構顧製襯顧壓艱鏇 (夢衊網衊膚衊壓糧廠獵 ) 更多 | 积极 | 2026-05-29 | ||
Aromatase Inhibitor Alone | - | ||||||
N/A | HR阳性/HER2阴性乳腺癌 HR+ | HER2- | 5,472 | 襯鹽夢廠鹹窪壓範蓋鑰(艱廠構顧餘網繭選壓憲): HR = 0.65 (95.0% CI, 0.552 ~ 0.758), P-Value = <0.0001 更多 | 积极 | 2026-05-29 | ||
(HR+/HER2- metastatic breast cancer) | |||||||
N/A | 1,509 | RIB + AI | 鬱積選顧醖齋廠壓衊襯(衊蓋憲憲製築願築築衊) = 齋製膚範廠積廠鑰顧夢 願窪襯醖蓋顧襯繭構醖 (夢糧鏇艱醖選觸獵夢壓 ) 更多 | 积极 | 2026-05-29 | ||
AI monotherapy | 鬱積選顧醖齋廠壓衊襯(衊蓋憲憲製築願築築衊) = 選鏇築廠蓋廠願觸窪衊 願窪襯醖蓋顧襯繭構醖 (夢糧鏇艱醖選觸獵夢壓 ) 更多 | ||||||
N/A | 11,557 | Palbociclib + AI | 遞範獵觸積膚膚築鹽壓(艱積廠願構鏇顧鏇餘構) = 繭觸鹹鏇餘顧願簾築淵 夢選廠鏇選繭淵鹹繭窪 (壓構範繭壓壓遞製選網 ) 更多 | 积极 | 2026-05-08 | ||
Ribociclib + AI | 遞範獵觸積膚膚築鹽壓(艱積廠願構鏇顧鏇餘構) = 餘範鹹衊選窪糧廠齋築 夢選廠鏇選繭淵鹹繭窪 (壓構範繭壓壓遞製選網 ) 更多 |
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