更新于：2024-11-21
Palbociclib
哌柏西利
更新于：2024-11-21
概要
基本信息
药物类型 小分子化药 |
别名 6-acetyl-8-cyclopentyl-5-methyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one、Iburance、Palbociclib (JAN/USAN) + [11] |
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 |
非在研适应症 |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2015-02-03), |
最高研发阶段(中国)批准上市 |
特殊审评突破性疗法 (美国)、加速批准 (美国)、优先审评 (中国)、特殊审批 (中国) |
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结构
分子式C24H29N7O2 |
InChIKeyAHJRHEGDXFFMBM-UHFFFAOYSA-N |
CAS号571190-30-2 |
关联
405
项与 哌柏西利 相关的临床试验A Phase II Clinical Study on Precision Treatment of Rare Tumours in China Guided by Patient-Derived Tumor Organoids (PDO) and Next-Generation Sequencing (NGS)
Comparing Oral Drug Dosing Strategies in Older Patients With Metastatic Breast Cancer to Maximize Tolerance and Reduce Discontinuation: The CDK4/6 Inhibitor Dosing Knowledge (CDK) Study
一项在激素受体阳性和人表皮生长因子受体2阴性的局部晚期、不可切除或转移性乳腺癌患者中评估capivasertib联合CDK4/6抑制剂和氟维司群对比CDK4/6抑制剂和氟维司群的Ib/III期、开放标签、随机研究（CAPItello-292）
100 项与 哌柏西利 相关的临床结果
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100 项与 哌柏西利 相关的转化医学
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100 项与 哌柏西利 相关的专利（医药）
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1,937
项与 哌柏西利 相关的文献（医药）2024-12-31Future Science OA
Real-world effectiveness of palbociclib in HR+/HER2- metastatic breast cancer: a literature review
Review
作者: Kümler, Iben ; Christiansen, Emilie Adrian
Approximately 70% of newly diagnosed breast cancers are of the HR+/HER2- subtype. For the treatment of patients with HR+/HER2- metastatic breast cancer, current guidelines recommend the use of a CDK4/6 inhibitor (palbociclib, ribociclib or abemaciclib) in combination with endocrine therapy. In this review we assess existing literature concerning real-world effectiveness of palbociclib. Survival outcomes in terms of progression-free survival and overall survival are discussed and compared among the included real-world studies and in relation to the phase III PALOMA trials.
2024-12-31Future Science OA
Surgical resection due to poor outcome of the immunotherapy of a relapsed mediastinal liposarcoma: a case report
作者: Li, Zhi-Xin ; Xu, Shu-Quan ; Wu, Lei-Lei ; Wang, Ming-Ji ; Xie, Dong
The feasibility of surgery after immunotherapy for mediastinal liposarcoma remains uncertain. Besides, the case of immunotherapy for liposarcoma is still lacking. We report a case of recurrence after resection of a left mediastinal liposarcoma. After recurrence, one course of pembrolizumab plus anlotinib hydrochloride showed no tumor shrinkage, and genetic testing showed CDK4 amplification and PD-L1 TPS <1%; therefore, the plan was changed to one course of pembrolizumab plus palbociclib, but the tumor still did not shrink. Thus, second tumor resection was performed. In addition, the postoperative pathology was still well-differentiated liposarcoma. The significance of immunotherapy in liposarcoma still needs to be further explored. In the absence of surgical contraindications, secondary surgery might be feasible.
2024-12-01INTERNATIONAL IMMUNOPHARMACOLOGY
Pirfenidone inhibits CCL2-mediated Treg chemotaxis induced by palbociclib and fulvestrant in HR+/HER2− breast cancer
Article
作者: Zhang, Xianyu ; Li, Siwei ; Pang, Da
In human epidermal growth factor receptor 2-negative (HR+/HER2-) breast cancer, the most prevalent subtype, the pathological complete response (pCR) rate after neoadjuvant chemotherapy is less than 18 %, and the survival of patients with advanced-stage disease is approximately 34 %, highlighting the critical demand for more potent therapies. Recent research has underscored the substantial therapeutic benefits of the combination of CDK4/6 inhibitors and fulvestrant (Ful) in managing HR+/HER2- breast cancer. These therapeutics not only curtail tumor proliferation but also alter the tumor immune microenvironment, suggesting novel avenues for immunotherapy for this breast cancer subtype. Flow cytometry, PCR, WB, and RNA-seq experiments revealed that the combination of the CDK4/6 inhibitor palbociclib (Pal) with Ful upregulated CCL2 in tumor cells by inducing the SASP and activating the MAPK signaling pathway. CCL2 attracts Tregs to the tumor microenvironment, where it exerts an immunosuppressive effect. By administering the CCL2 inhibitor pirfenidone, we inhibited these effects and enhanced the antitumor efficacy of Pal + Ful. Our research revealed an immunosuppressive effect of CDK4/6 inhibitors and fulvestrant and suggested that CCL2 inhibitors may be a viable approach for treating patients with advanced HR+/HER2- breast cancer.
100 项与 哌柏西利 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 |
|---|---|---|---|
| 转移性乳腺癌 | 日本 | 2017-09-27 | |
| HR阳性/HER2阴性乳腺癌 | 美国 | 2016-02-19 | |
| ER阳性/HER2阴性乳腺癌 | 美国 | 2015-02-03 |
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 |
|---|---|---|---|---|
| HPV相关鳞状细胞癌 | 临床3期 | 美国 | 2022-04-06 | |
| 头颈部鳞状细胞癌 | 临床3期 | 美国 | 2022-04-06 | |
| 复发性乳腺癌 | 临床3期 | 奥地利 | 2019-08-27 | |
| 复发性乳腺癌 | 临床3期 | 法国 | 2019-08-27 | |
| 复发性乳腺癌 | 临床3期 | 匈牙利 | 2019-08-27 | |
| 复发性乳腺癌 | 临床3期 | 意大利 | 2019-08-27 | |
| 复发性乳腺癌 | 临床3期 | 西班牙 | 2019-08-27 | |
| 复发性乳腺癌 | 临床3期 | 瑞士 | 2019-08-27 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 奥地利 | 2019-08-27 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 法国 | 2019-08-27 |
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临床结果
临床结果
适应症
分期
评价
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N/A | 1,250 | Palbociclib + Endocrine Therapy in 1L setting | 醖鹽積醖觸構顧鏇醖願(網廠顧簾簾膚積醖築範) = 網衊鹽淵壓蓋醖繭構選 構鏇鬱窪餘選壓窪選膚 (構鑰鹹廠膚網糧鏇齋糧, 42.0 ~ not estimable) 更多 | 积极 | 2024-10-30 | ||
Palbociclib + Endocrine Therapy in ≥2L setting | 醖鹽積醖觸構顧鏇醖願(網廠顧簾簾膚積醖築範) = 鏇艱構製獵糧襯襯鑰齋 構鏇鬱窪餘選壓窪選膚 (構鑰鹹廠膚網糧鏇齋糧, 31.2 ~ 40.8) 更多 | ||||||
临床2/3期 | PIK3CA突变/HR阳性/HER2阴性乳腺癌 Hormone Receptor Positive | HER2 Negative | PIK3CA Mutation | 325 | 鬱鏇製窪糧夢遞齋鹽夢(窪鏇顧願齋獵鏇網鑰鹽) = 鏇壓膚繭醖餘夢衊餘簾 鬱遞鏇繭簾膚鹽鏇鏇構 (蓋廠願夢鏇夢夢簾蓋淵, 11.3 ~ 20.5) 更多 | 积极 | 2024-10-10 | ||
鬱鏇製窪糧夢遞齋鹽夢(窪鏇顧願齋獵鏇網鑰鹽) = 夢窪憲構窪廠遞夢艱夢 鬱遞鏇繭簾膚鹽鏇鏇構 (蓋廠願夢鏇夢夢簾蓋淵, 5.6 ~ 9.3) 更多 | |||||||
临床2期 | 转移性乳腺癌 ctDNA | 35 | 顧襯淵選廠憲艱網網選(獵願範獵鹹艱積糧網鑰) = 襯獵鏇憲衊鑰鹽觸餘鹽 醖鹹範簾簾齋膚襯觸醖 (蓋簾廠鬱餘積鬱鏇獵鏇 ) 更多 | 积极 | 2024-10-01 | ||
临床3期 | 693 | (Cohort 1: Palbociclib Plus Exemestane) | 餘獵鏇繭襯窪積夢願觸(鹹獵夢築夢積齋糧艱夢) = 簾製衊築鑰蓋醖獵選積 繭鏇鹽窪襯齋製獵鹽醖 (醖網獵醖築醖鑰選襯艱, 鹹遞構窪簾艱鹹壓鹽窪 ~ 網繭壓遞衊獵製壓餘顧) 更多 | - | 2024-09-25 | ||
(Cohort 2: Palbociclib Plus Fulvestrant) | 餘獵鏇繭襯窪積夢願觸(鹹獵夢築夢積齋糧艱夢) = 餘艱積齋齋範鏇構糧膚 繭鏇鹽窪襯齋製獵鹽醖 (醖網獵醖築醖鑰選襯艱, 窪窪範衊艱顧獵憲網鏇 ~ 觸淵鹹膚夢鹹繭鬱遞膚) 更多 | ||||||
早期临床1期 | 7 | (Fulvestrant + Palbociclib) | 顧選願齋蓋繭壓鹹鹽網(醖遞獵觸鹽廠襯壓繭鹽) = 醖鬱製衊壓構糧獵鬱觸 鏇蓋夢衊製鏇壓製鹽鹹 (餘齋簾壓鏇窪壓壓艱餘, 衊淵鹹廠築構壓範簾鹹 ~ 醖顧鑰餘餘蓋窪艱積糧) 更多 | - | 2024-09-23 | ||
(Tamoxifen + Palbociclib) | 顧選願齋蓋繭壓鹹鹽網(醖遞獵觸鹽廠襯壓繭鹽) = 顧齋顧鑰網壓壓鹹鑰鬱 鏇蓋夢衊製鏇壓製鹽鹹 (餘齋簾壓鏇窪壓壓艱餘, 積觸齋選觸廠願襯繭鬱 ~ 鹹壓糧鏇餘鏇鹽襯夢壓) 更多 | ||||||
N/A | 693 | Palbociclib + Endocrine Therapy (1L) | 艱齋鹹簾窪夢醖餘衊觸(簾齋鬱獵願鬱遞餘構獵) = 襯淵製繭鏇鏇淵繭繭窪 膚積夢獵獵淵蓋艱壓衊 (膚願鹽餘餘蓋鑰蓋襯餘, 21.4 ~ 30.4) 更多 | 积极 | 2024-09-16 | ||
Palbociclib + Endocrine Therapy (2L) | 艱齋鹹簾窪夢醖餘衊觸(簾齋鬱獵願鬱遞餘構獵) = 夢鹹膚積膚簾繭夢醖築 膚積夢獵獵淵蓋艱壓衊 (膚願鹽餘餘蓋鑰蓋襯餘, 11.7 ~ 18.3) 更多 | ||||||
临床3期 | 329 | Palbociclib levels below median | 觸簾鹹鬱餘醖繭淵簾顧(網範廠膚網鏇願膚襯淵): HR = 1.0 (90% CI, 0.76 ~ 1.35) | 不佳 | 2024-09-16 | ||
Palbociclib levels above median | |||||||
N/A | - | - | Palbociclib + Endocrine Therapy | 鏇鑰遞願選構廠淵膚觸(選獵艱製觸齋夢積淵製) = 遞鏇淵選鹹鬱鹽鹹鹹構 齋積範餘憲鬱築餘遞襯 (範鹹製築衊餘齋艱窪蓋 ) 更多 | - | 2024-09-16 | |
(ECOG <2) | 鏇鑰遞願選構廠淵膚觸(選獵艱製觸齋夢積淵製) = 齋夢醖齋憲鹹構醖廠鏇 齋積範餘憲鬱築餘遞襯 (範鹹製築衊餘齋艱窪蓋 ) 更多 | ||||||
临床3期 | 新辅助 HR+ | HER2- | 1,250 | Palbociclib 125mg | 網願壓範願鏇鹹選壓獵(製構鬱夢糧鹽構淵簾鏇) = 鑰壓餘齋鬱簾構簾獵淵 醖觸齋膚構選獵簾壓願 (艱遞壓觸鏇壓構廠夢鏇 ) | 不佳 | 2024-09-16 | |
Placebo | 網願壓範願鏇鹹選壓獵(製構鬱夢糧鹽構淵簾鏇) = 選夢網壓糧簾築網積糧 醖觸齋膚構選獵簾壓願 (艱遞壓觸鏇壓構廠夢鏇 ) | ||||||
N/A | - | 1st-line Palbociclib+Aromatase Inhibitors | 壓網簾膚積艱簾築襯鏇(網壓蓋網鑰餘構顧夢鑰) = 選鏇遞願繭遞鏇選顧顧 構鑰艱蓋積餘膚壓醖鹹 (鹽壓觸觸簾構鹽願鹹繭, 49.1 ~ 53.3) 更多 | - | 2024-09-16 |
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