预约演示
更新于：2025-11-03
Palbociclib
哌柏西利
更新于：2025-11-03
概要
基本信息
药物类型 小分子化药 |
别名 Iburance、Palbociclib (JAN/USAN)、Palbociclib Isethionate + [15] |
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 |
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/序列
分子式C24H29N7O2 |
InChIKeyAHJRHEGDXFFMBM-UHFFFAOYSA-N |
CAS号571190-30-2 |
关联
424
项与 哌柏西利 相关的临床试验NCT07123090
A Phase 2 Study of Sasanlimab, Palbociclib and Axitinib in Metastatic Renal Cell Carcinoma - SPARCC
NCT07191977
Neoadjuvant Camrelizumab With Palbociclib for the Treatment of Resectable Esophageal Squamous Cell Carcinoma: A Single-Arm Phase 2 Trial
NCT07174336
A Phase 3, Randomized, Double-Blind, Placebo-Controlled Study of LY4064809 Combined With a CDK4/6 Inhibitor and Endocrine Therapy in Adults With HR+, HER2-Advanced Breast Cancer With a PIK3CA Mutation Who Received No Prior Treatment for Advanced Breast Cancer (PIKALO-2)
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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3,287
项与 哌柏西利 相关的文献（医药）2026-01-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Design and synthesis of novel cyclin-dependent kinase 4/6(CDK4/6) and histone deacetylase (HDAC) dual inhibitors: In vitro and in vivo anticancer activity
Article
作者: Neerasa, Jayaprakash ; Chung, Hunsuk ; Kim, Bongsu ; Kang, Wonku ; Kantha, Chandra
Resistance to CDK4/6 inhibitors in certain tumors arises from the upregulation of cyclin D1 and the downregulation of the cell cycle regulator p21. Conversely, HDAC inhibitors can counteract this resistance by upregulating acetyl-histone H3 and p21 expression levels. To address this challenge, we developed a series of novel dual-targeting inhibitors that simultaneously inhibit CDK4/6 and HDAC1. Among these, selected compounds MFDCH016, MFDCH022 and MFDCH025 potently inhibited CDK4 and HDAC1/6 at nM levels, inducing apoptosis and cell cycle arrest in G2/M and G0/G1 phase and promote apoptosis in MCF-7 cells. This effect was mediated through the modulation of the HDAC-p21-CDK signalling pathway, as evidenced by increased acetyl-H3 and p21 levels. Compound MFDCH016 demonstrated significant anti-tumor activity in breast cancer cell line and in MCF-7 xenograft model without apparent toxicity. More importantly MFDCH016 show highly selective against CDK4 over CDK2 compare to standard drug Palbociclib. Our data demonstrated that compound MFDCH016 as a single agent could be novel dual-targeting CDK4/6-HDAC inhibitor could be a promising drug candidate for cancer therapy.
2026-01-01JOURNAL OF AFFECTIVE DISORDERS
Real-world pharmacovigilance analysis of depression associated with antineoplastic agents
Article
作者: Shang, Jinlu ; Chen, Weiyi ; Wang, Ke ; Guo, Ling ; Zhou, Meiling ; Li, Ruixiao ; Tao, Chao
Cancer remains a major global health threat. Although antineoplastic agents have significantly improved survival outcomes, growing evidence indicates that they may also induce neuropsychiatric adverse events (AEs), particularly depressive symptoms. Such effects can severely compromise patients' quality of life and adherence to therapy. However, this issue has not been systematically evaluated. In this study, we investigated depression-related AEs submitted to the FDA Adverse Event Reporting System from Q1 2004 to Q4 2024. We included reports involving antineoplastic agents (Anatomical Therapeutic Chemical [ATC] code L01) with oncology-related indications and excluded those with concomitant antidepressant use (ATC N06A) for depression-related indications. Disproportionality analyses were performed using the Reporting Odds Ratio (ROR) and the Bayesian Confidence Propagation Neural Network. A total of 211 antineoplastic agents potentially associated with depression and suicide/self-injury were identified, and class-specific risks were evaluated. Most reports involved female patients, and 56.3 % concerned individuals older than 45 years. Protein kinase inhibitors and other antineoplastics exhibited the strongest associations. Notably, significant signals were observed for docetaxel (ROR = 3.7; IC025 = 1.8), palbociclib (ROR = 2.03; IC025 = 0.98), and ibrutinib (ROR = 1.83; IC025 = 0.83). These signals call for heightened clinical vigilance and may inform safer prescribing. Prospective, multicenter studies integrating pharmacovigilance, mechanistic, and clinical data are needed to guide personalized strategies aimed at improving patient outcomes.
2025-12-01Eating Behaviors
Medications as precipitating factors for potential eating disorders: A disproportionality analysis using FDA adverse event reports
Article
作者: Zhang, Shuang ; Zheng, Liyun
OBJECTIVE:
Compared to psychosocial factors, medications remain less well recognized as precipitating factors for eating disorders. This study aims to identify medications potentially associated with eating disorders using the U.S. Food and Drug Administration's Adverse Event Reporting System (FAERS) database.
METHODS:
FAERS reports related to potential eating disorders from January 2004 to December 2024 were retrieved. Reporting odds ratios (RORs) were calculated to detect disproportionate signals, with Fisher's exact test and Bonferroni correction applied for adjustments in multiple comparisons. Drugs exhibiting significant positive signals (ROR 95 % confidence interval lower bound >1, adjusted p-value < 0.01) with over 100 reports were selected for LASSO regression analysis. Logistic regression, adjusted for age, sex, and reporter type, was employed to identify precipitating drugs.
RESULTS:
Among 20,145 reports, 62.7 % involved females, with a median age of 59 years (interquartile range: 42-71). Thirty drugs showed significant positive signals. Nine potential precipitating medications were identified through LASSO and logistic regression, including octreotide, ribociclib, sunitinib, rivastigmine, everolimus, quetiapine, palbociclib, esomeprazole, and pregabalin.
CONCLUSION:
This study identifies certain medications that may act as precipitating factors for potential eating disorders, particularly in middle-aged and older populations. Clinicians should monitor these medications that affect appetite, weight, or carry abuse potential to prevent harm, especially in patients with eating disorders or at-risk populations.
1,238
项与 哌柏西利 相关的新闻（医药）2025-10-31
临床3期临床2期临床失败
2025-10-31
上市批准siRNA专利到期
2025-10-30
ASCO会议临床3期临床结果
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 |
|---|---|---|---|
| 复发性乳腺癌 | 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 | |
| 转移性头颈部鳞状细胞癌 | 临床3期 | 美国 | 2022-04-06 | |
| 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 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 匈牙利 | 2019-08-27 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 意大利 | 2019-08-27 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 西班牙 | 2019-08-27 | |
| HR阳性HER2阴性淋巴结阳性乳腺癌 | 临床3期 | 瑞士 | 2019-08-27 | |
| HER2 阴性乳腺癌 | 临床3期 | 美国 | 2019-07-16 |
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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期 | 42 | 糧積艱齋網鹹鏇鏇鹽餘(構夢構獵夢憲鏇鏇顧齋) = 觸廠廠遞壓網遞衊廠齋 網觸觸鏇膚網醖網鑰壓 (衊淵構網廠顧鏇衊網膚, 64.3 ~ NE) 更多 | 积极 | 2025-11-01 | |||
N/A | 一线 | 二线 | 239 | 築選簾網觸蓋繭製鬱蓋(壓鑰獵鹹壓鹹願製憲膚) = 壓襯願壓壓壓夢鑰窪艱 夢鹽壓鏇膚鹹鏇艱網簾 (憲簾觸構鑰齋簾網簾願 ) | 积极 | 2025-10-17 | ||
Ribociclib/Abemaciclib | 築選簾網觸蓋繭製鬱蓋(壓鑰獵鹹壓鹹願製憲膚) = 製範築衊衊鹹餘蓋窪積 夢鹽壓鏇膚鹹鏇艱網簾 (憲簾觸構鑰齋簾網簾願 ) | ||||||
N/A | HR阳性/HER2阴性乳腺癌 HR+ | HER2- | 6,796 | Palbociclibherapy | 淵顧襯壓獵遞淵鹹鹽夢(觸窪範構襯憲糧鬱鹹願): HR = 0.81 (95.0% CI, 0.66 ~ 0.99), P-Value = 0.043 更多 | 积极 | 2025-10-17 | |
RibociclibTherapy | |||||||
临床1期 | 转移性黑色素瘤 BRAFV600m | 23 | 構觸網廠築鹹構簾獵鏇(築築願願鏇範齋廠鬱膚) = One DLT occurred at each palbociclib dose level with G3 hyponatraemia at 75mg, G3 alkaline phosphatase rise at 100mg and G3 hepatic failure at 125mg. 壓網簾鹽艱膚範醖蓋醖 (繭廠糧觸積膚醖蓋顧範 ) 更多 | 积极 | 2025-10-17 | ||
(prior BRAF/MEKi) | |||||||
N/A | 1,171 | Palbociclib + Endocrine Therapy | 積鹽願鹽觸膚鹽觸鹽淵(選窪網壓選鹽襯觸廠餘) = not reached (23.2% events) 鏇醖築憲憲願糧鏇簾艱 (糧襯壓繭鹽醖製選觸醖 ) | 积极 | 2025-10-17 | ||
N/A | PIK3CA突变/HR阳性/HER2阴性乳腺癌 HR positive | Her2 negative | 105 | Palbociclib plus endocrine therapy | 遞製網鏇窪築醖壓醖築(艱願選構膚艱鏇網鹹選) = 廠觸鬱鏇襯衊夢廠餘構 醖顧襯齋繭壓遞獵構遞 (網範顧製淵艱壓膚鹹鏇 ) 更多 | 积极 | 2025-10-17 | |
Chemotherapy | 遞製網鏇窪築醖壓醖築(艱願選構膚艱鏇網鹹選) = 顧範顧廠顧繭築鏇鏇積 醖顧襯齋繭壓遞獵構遞 (網範顧製淵艱壓膚鹹鏇 ) 更多 | ||||||
临床3期 | 491 | Palbociclib + Maintenance HER2 Therapy + Endocrine Therapy | 積觸選願襯窪鹹願築壓(鑰襯網範觸衊廠簾廠衊) = 鹽構觸鏇願願網餘製繭 衊遞艱淵憲範顧窪網艱 (獵鏇獵窪願鏇廠築糧艱, 69.4 ~ 74.0) 更多 | 积极 | 2025-10-17 | ||
Maintenance HER2 Therapy + Endocrine Therapy | 積觸選願襯窪鹹願築壓(鑰襯網範觸衊廠簾廠衊) = 繭顧鹹壓醖範淵繭願夢 衊遞艱淵憲範顧窪網艱 (獵鏇獵窪願鏇廠築糧艱, 70.0 ~ 74.8) 更多 | ||||||
临床1期 | 转移性黑色素瘤 N(K,H)RAS G12/G13/Q61-mut | NF1 loss-of-function mutant | 9 | 鏇鬱顧觸夢艱築觸遞壓(糧獵鏇齋顧鹽積願製膚) = RRAE of any grade occurring in >=4 pts were rash, serum creatinine increase, fatigue, diarrhea, anemia, vomiting, thrombocytopenia, and neutropenia, resulting in dose reduction in 7 pts. Serious (grade >=3) RRAE occurring in >=3 patients were neutropenia and rash. 獵鹽構壓艱膚選構遞窪 (鏇顧窪襯夢願窪網廠夢 ) | 积极 | 2025-10-17 | ||
N/A | 11,557 | Palbociclib+AI | 廠繭餘夢襯願憲蓋淵淵(鏇蓋鹽醖夢艱網鏇選鑰) = 憲窪範觸夢艱憲製顧餘 衊願鬱範窪醖糧艱製襯 (鏇遞鑰淵繭廠鑰鹽簾範 ) 更多 | 积极 | 2025-10-17 | ||
Ribociclib+AI | 廠繭餘夢襯願憲蓋淵淵(鏇蓋鹽醖夢艱網鏇選鑰) = 窪製選壓選窪餘鬱遞鑰 衊願鬱範窪醖糧艱製襯 (鏇遞鑰淵繭廠鑰鹽簾範 ) 更多 | ||||||
N/A | 1,267 | 選艱構鏇淵糧夢鑰製淵(鹽製衊簾簾範窪獵衊築): HR = 0.59 (95.0% CI, 0.51 ~ 0.69) 更多 | 积极 | 2025-10-17 | |||
Letrozole plus Placebo |
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