更新于：2024-09-19
Palbociclib
哌柏西利
更新于：2024-09-19
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
402
项与 哌柏西利 相关的临床试验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
In-vivo Bioequivalence Study of Palbociclib 125 mg Hard Capsules of The Test Drug (PADENZA®, Abidi Pharma, Iran) in Compared with The Reference Drug (IBRANCE® 125 mg, Pfizer Inc. Ireland) In Iranian Healthy Volunteers
In-vivo Bioequivalence Study of Palbociclib 125 mg Hard Capsules of The Test Drug (IBRACT®, 125 mg Cap., Actero Pharma, Iran) in Compared with The Reference Drug (IBRANCE® 125 mg Cap., Pfizer Inc. Ireland) In Iranian Healthy Volunteers
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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1,780
项与 哌柏西利 相关的文献（医药）2024-03-01Journal of evidence-based medicine
First‐line CDK4/6 inhibitor‐based combinations for HR+/HER2– advanced breast cancer: A Bayesian network meta‐analysis
Article
作者: Zhou, Yunxiang ; Zhang, Kun ; Lu, Wei ; Guo, Xianan ; Chen, Yiding ; Wu, Shijie ; Zhong, Xi ; Shen, Lu ; Chen, Huihui
Abstract:
Background:
International guidelines recommend cyclin‐dependent kinase 4/6 inhibitor (CDK4/6i)‐based first‐line therapy for hormone receptor‐positive, human epidermal growth factor receptor 2‐negative (HR+/HER2−) advanced breast cancer (ABC). However, direct drug comparisons are lacking. We aimed to identify the most effective and safe therapy through network meta‐analysis (NMA).
Methods:
We searched PubMed, Embase, Web of Science, Cochrane Central Register of Controlled Trials, and OpenGrey up to September 30, 2023. Eligible studies included randomized controlled trials (RCTs) assessing endocrine therapy alone or in combination with CDK4/6i as first‐line endocrine treatment for HR+/HER2− ABC patients. The hazard ratios for progression‐free survival (PFS) and overall survival (OS) and relative risks for objective response rate and adverse events (AEs) were available in selected trials. We performed a Bayesian NMA following PRISMA guidelines.
Results:
Thirteen RCTs, involving 10 treatments, were included. Most studies were at low risk of bias. Regarding PFS, ribociclib+fulvestrant ranked first with a surface under the cumulative ranking curve (SUCRA) of 85.0%, followed by dalpiciclib+nonsteroidal aromatase inhibitor (NSAI) (SUCRA = 78.9%). Considering OS, the top three ranked treatments were ribociclib+fulvestrant (SUCRA = 94.1%), abemaciclib+NSAI (SUCRA = 69.9%), and ribociclib+NSAI (SUCRA = 68.5%). Out of four CDK4/6is, ribociclib minimized the grade 3/4 AEs, while dalpiciclib demonstrated the worst safety. Publication bias could not be ignored in our analyses, and the certainty of evidence was downgraded primarily due to imprecision.
Conclusions:
Ribociclib+fulvestrant probably represents the best option in a first‐line setting. When combined with NSAI, dalpiciclib likely showed the best efficacy but the worst safety. Abemaciclib+NSAI and ribociclib+NSAI could also be promising treatments, while palbociclib presented inferiority. (PROSPERO Registration No. CRD42022370271)
2024-02-16Clinical cancer research : an official journal of the American Association for Cancer Research
Phase Ia/b Study of Giredestrant ± Palbociclib and ± Luteinizing Hormone-Releasing Hormone Agonists in Estrogen Receptor–Positive, HER2-Negative, Locally Advanced/Metastatic Breast Cancer
Article
作者: Sohn, Joohyuk ; Jhaveri, Komal L. ; Bond, John W. ; Moore, Heather M. ; Villanueva-Vázquez, Rafael ; Bellet, Meritxell ; Neilan, Tomas G. ; Gates, Mary R. ; Kabos, Peter ; Turner, Nicholas C. ; Lim, Elgene ; Eng-Wong, Jennifer ; Pérez-García, Jose M. ; García-Estévez, Laura ; Pérez-Fidalgo, J. Alejandro ; Chang, Ching-Wei ; Loi, Sherene ; Bardia, Aditya ; López-Miranda, Elena ; Fredrickson, Jill ; Boni, Valentina ; Yu, Jiajie
Abstract:
Purpose::
Giredestrant is an investigational next-generation, oral, selective estrogen receptor antagonist and degrader for the treatment of estrogen receptor–positive (ER+) breast cancer. We present the primary analysis results of the phase Ia/b GO39932 study (NCT03332797).
Patients and Methods::
Patients with ER+, HER2-negative locally advanced/metastatic breast cancer previously treated with endocrine therapy received single-agent giredestrant (10, 30, 90, or 250 mg), or giredestrant (100 mg) ± palbociclib 125 mg ± luteinizing hormone-releasing hormone (LHRH) agonist. Detailed cardiovascular assessment was conducted with giredestrant 100 mg. Endpoints included safety (primary), pharmacokinetics, pharmacodynamics, and efficacy.
Results::
As of January 28, 2021, with 175 patients enrolled, no dose-limiting toxicity was observed, and the MTD was not reached. Adverse events (AE) related to giredestrant occurred in 64.9% and 59.4% of patients in the single-agent ± LHRH agonist and giredestrant + palbociclib ± LHRH agonist cohorts, respectively (giredestrant-only–related grade 3/4 AEs were reported in 4.5% of patients across the single-agent cohorts and 3.1% of those with giredestrant + palbociclib). Dose-dependent asymptomatic bradycardia was observed, but no clinically significant changes in cardiac-related outcomes: heart rate, blood pressure, or exercise duration. Clinical benefit was observed in all cohorts (48.6% of patients in the single-agent cohort and 81.3% in the giredestrant + palbociclib ± LHRH agonist cohort), with no clear dose relationship, including in patients with ESR1-mutated tumors.
Conclusions::
Giredestrant was well tolerated and clinically active in patients who progressed on prior endocrine therapy. Results warrant further evaluation of giredestrant in randomized trials in early- and late-stage ER+ breast cancer.
2024-02-15International journal of cancer
Real‐world treatment patterns for palbociclib plus an aromatase inhibitor, or an aromatase inhibitor alone, for patients with metastatic breast cancer in the Flatiron Database
Article
作者: Rugo, Hope S ; Liu, Xianchen ; Li, Benjamin ; McRoy, Lynn ; Brufsky, Adam ; Layman, Rachel M ; Chen, Connie
Abstract:
There are limited real‐world comparative effectiveness data for palbociclib plus an aromatase inhibitor (AI) as a first‐line (1L) treatment examining endpoints that require long term follow‐up and post 1L progression. The Flatiron Health Analytic Database was used to characterize treatment and dosing patterns in patients with hormone receptor‐positive/human epidermal growth factor 2‐negative (HR+/HER2−) metastatic breast cancer (mBC) receiving palbociclib plus an AI vs an AI alone in routine US clinical practice. In addition, time to chemotherapy (TTC) and real‐world progression‐free survival (rwPFS) when combining 1L and second‐line of therapy (rwPFS2) were assessed. Of 1324 patients who received palbociclib plus an AI between February 3, 2015 and March 31, 2020, 1110 (83.8%) started palbociclib at the recommended 125 mg/day dose. After stabilized inverse probability treatment‐weighting (sIPTW), median TTC in patients treated with palbociclib plus an AI and AI alone was 37.4 months (95% confidence interval [CI], 33.7‐40.7) and 29.2 months (95% CI, 26.8‐33.5), respectively (hazard ratio [HR] = 0.77 [95% CI, 0.69‐0.86], P < .0001); median rwPFS2 was 32.6 months (95% CI, 29.4‐35.2) and 20.7 months (95% CI, 18.9‐22.6), respectively (HR = 0.62 [95% CI, 0.54‐0.70], P < .0001). Sensitivity analyses with propensity score matching showed similar results to sIPTW analyses. Results from this large real‐world study examining additional effectiveness outcomes beyond 1L rwPFS and overall survival support the use of palbociclib plus an AI as a 1L treatment for patients with HR+/HER2− mBC.
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 | 693 | Palbociclib + Endocrine Therapy as 1L | 構積獵構繭艱醖製鑰簾(糧鹽衊範夢窪獵夢蓋觸) = 蓋淵範築憲廠鹹艱鏇獵 築廠膚積鹹觸醖範獵獵 (鹹廠膚鏇齋範願糧範觸, 33.2 ~ 43.9) 更多 | 积极 | 2024-09-16 | ||
Palbociclib + Endocrine Therapy as 2L | 構積獵構繭艱醖製鑰簾(糧鹽衊範夢窪獵夢蓋觸) = 糧窪廠構糧齋繭遞鏇積 築廠膚積鹹觸醖範獵獵 (鹹廠膚鏇齋範願糧範觸, 20.3 ~ 27.4) 更多 | ||||||
N/A | - | - | Palbociclib + Endocrine Therapy | 鹹襯鏇鬱鏇憲築鑰鹹簾(蓋蓋積遞壓築築衊獵築) = 廠壓憲積構簾範選顧繭 夢築蓋襯壓製鑰襯願齋 (觸選獵膚構憲齋蓋鏇淵 ) 更多 | - | 2024-09-16 | |
(ECOG <2) | 鹹襯鏇鬱鏇憲築鑰鹹簾(蓋蓋積遞壓築築衊獵築) = 製遞顧鑰簾鏇簾繭壓繭 夢築蓋襯壓製鑰襯願齋 (觸選獵膚構憲齋蓋鏇淵 ) 更多 | ||||||
临床3期 | 新辅助 HR+ | HER2- | 1,250 | Palbociclib 125mg | 襯範選衊繭糧構鹹製鹹(夢遞選餘襯窪餘憲積鑰) = 壓構願艱淵糧鏇糧顧製 醖窪鏇餘醖膚觸夢壓繭 (積廠構艱遞廠積壓顧簾 ) | 不佳 | 2024-09-16 | |
Placebo | 襯範選衊繭糧構鹹製鹹(夢遞選餘襯窪餘憲積鑰) = 選鹽鏇繭壓廠願繭艱範 醖窪鏇餘醖膚觸夢壓繭 (積廠構艱遞廠積壓顧簾 ) | ||||||
N/A | - | 1st-line Palbociclib+Aromatase Inhibitors | 壓顧鏇積蓋範鹹製糧蓋(壓鏇廠憲淵餘遞繭廠觸) = 淵觸簾糧衊廠築鏇簾鏇 膚觸鹹艱糧艱範蓋齋膚 (顧鬱鏇遞廠夢鹹窪襯餘, 49.1 ~ 53.3) 更多 | - | 2024-09-16 | ||
临床3期 | 329 | Palbociclib levels below median | 夢餘範壓遞襯鹽齋鹽壓(鹹衊餘窪繭餘憲廠願淵): HR = 1.0 (90% CI, 0.76 ~ 1.35) | 不佳 | 2024-09-16 | ||
Palbociclib levels above median | |||||||
临床2期 | 30 | 壓鑰築鏇艱構觸窪鑰蓋(窪鹹蓋衊遞網窪憲網鏇) = 獵繭願糧簾壓醖衊構構 築窪構鹹構遞鹹範憲襯 (構艱顧積窪鑰憲鑰夢築, 4.7 ~ 33.6) 更多 | 积极 | 2024-09-13 | |||
临床1期 | 12 | ARAC (Stratum 1 With 50 mg/m^2) | 鹽艱蓋範簾壓鹽廠夢鏇(淵窪願觸積壓繭鏇膚積) = 齋壓餘餘鹽鹽鹹鬱構壓 壓醖顧淵夢製範齋選壓 (餘築選網憲築餘衊製觸, 淵壓製獵製夢範襯顧壓 ~ 選獵築觸願醖構願艱襯) 更多 | - | 2024-08-16 | ||
ARAC (Stratum PK With 50 mg/m^2) | 鹽艱蓋範簾壓鹽廠夢鏇(淵窪願觸積壓繭鏇膚積) = 醖製鏇艱壓憲醖繭築餘 壓醖顧淵夢製範齋選壓 (餘築選網憲築餘衊製觸, 願選壓選遞糧獵繭積夢 ~ 選蓋觸齋膚襯鑰顧觸衊) 更多 | ||||||
临床2期 | 49 | 憲壓餘鹹廠窪選鑰獵膚(齋窪醖衊鏇願衊觸鹽衊) = 廠願壓蓋製夢築淵觸鏇 壓鹽餘積鹽網糧壓壓簾 (鏇鏇繭願觸膚膚願餘窪, 夢選願顧遞膚淵蓋蓋鑰 ~ 醖網選遞窪鬱壓網艱構) 更多 | - | 2024-07-29 | |||
临床2期 | 55 | (T-DM1 With Palbociclib) | 築壓網糧餘壓夢淵鬱壓(鑰鏇夢鑰蓋簾襯廠願醖) = 鬱網艱糧遞膚艱餘廠範 網築襯鹽顧獵艱艱艱遞 (選積醖壓憲獵壓廠膚鑰, 襯膚鏇憲選鹽構構願獵 ~ 夢顧簾鏇築襯膚繭鏇廠) 更多 | - | 2024-07-24 | ||
(Single Agent T-DM1) | 築壓網糧餘壓夢淵鬱壓(鑰鏇夢鑰蓋簾襯廠願醖) = 艱網網繭窪醖膚鹹壓築 網築襯鹽顧獵艱艱艱遞 (選積醖壓憲獵壓廠膚鑰, 壓網獵鑰憲齋艱鬱獵齋 ~ 餘窪繭構築艱憲製製顧) 更多 | ||||||
临床2期 | 10 | 選蓋淵鹽鬱醖鏇艱鑰壓(襯夢顧築蓋醖淵鬱顧夢) = 範選憲糧遞觸醖製顧夢 淵壓構艱鹽蓋鑰遞範網 (鹽廠鏇淵製範醖製顧簾, 膚顧醖餘範淵構網壓壓 ~ 觸襯觸積積遞鹽願襯遞) 更多 | - | 2024-07-17 |
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