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更新于：2026-07-15
Camizestrant
卡米司群
更新于：2026-07-15
概要
基本信息
药物类型 小分子化药 |
别名 卡米泽司他、AZ14066724、AZD 9833 + [4] |
靶点 |
作用方式 拮抗剂、降解剂 |
作用机制 ERs拮抗剂(雌激素受体家族拮抗剂)、ERs降解剂(雌激素受体家族降解剂) |
在研适应症 |
非在研适应症 |
原研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2026-06-19), |
最高研发阶段(中国)临床3期 |
特殊审评突破性疗法 (美国)、快速通道 (美国)、优先审评 (澳大利亚) |
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结构/序列
分子式C24H28F4N6 |
InChIKeyWDHOIABIERMLGY-CMJOXMDJSA-N |
CAS号2222844-89-3 |
关联
24
项与 卡米司群 相关的临床试验CTIS2025-524213-84-00
TAILORswitch (PADA-2): rising ctDNA to tailor endocrine therapy switch in patients with ER+/HER2- metastatic breast cancer
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
NCT07427394
A Phase IIa, Open-label Study to Evaluate the Safety, Pharmacokinetics and Preliminary Efficacy of Camizestrant in Combination With Atirmociclib in Participants With ER-positive, HER2-negative Advanced Breast Cancer (SERENA-1b)
100 项与 卡米司群 相关的临床结果
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100 项与 卡米司群 相关的转化医学
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100 项与 卡米司群 相关的专利（医药）
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41
项与 卡米司群 相关的文献（医药）2026-09-01Translational Oncology
The ESR1-MYH14 axis functions as a critical driver of cervical cancer progression and metastasis
Article
作者: Wang, Xia ; Lan, Qiongyu ; Han, Yongqing ; Li, Qin ; Yi, Hanjie ; Xiong, Le ; Li, Shanfeng
BACKGROUND:
Cervical cancer remains a major cause of cancer-related mortality in women, yet its molecular mechanisms of progression and metastasis are not fully defined. This study explores the oncogenic role of the ESR1 (estrogen receptor α)-MYH14 (myosin heavy chain 14) signaling axis in cervical cancer.
METHODS:
Quantitative real-time PCR and Western blotting were used to assess RNA and protein levels. The transcriptional regulation of MYH14 by ESR1 was verified through chromatin immunoprecipitation quantitative PCR and dual-luciferase assays. Cellular proliferation, migration, and invasion were evaluated using CCK-8, colony formation, wound healing, and transwell assays. Xenograft and tail vein metastasis models were applied to examine the effects of MYH14 silencing and ESR1 inhibition by AZD9833.
RESULTS:
MYH14 was markedly upregulated in cervical cancer tissues and correlated with poor prognosis. MYH14 knockdown suppressed proliferation and metastasis both in vitro and in vivo. ESR1 functioned as a transcriptional activator of MYH14, enhancing c-Myc and MMP9 expression, whereas MYH14 silencing or AZD9833 treatment reversed these oncogenic effects and reduced ESR1, MYH14, c-Myc, and MMP9 levels.
CONCLUSION:
The ESR1-MYH14 signaling axis drives cervical cancer growth and metastasis. Targeting this pathway may represent a promising therapeutic strategy for cervical cancer management.
2026-06-01TOXICOLOGY AND APPLIED PHARMACOLOGY
Camizestrant-induced heart rate reduction is mediated via a sinoatrial node pacemaker channel mechanism
Article
作者: El-Haou, Saïd ; Pointon, Amy ; Wright, Lindsay ; Harding, Joanna ; Purbrick, Stuart ; Harmer, Alexander ; Kwan, Maggie ; Canzolino, Serena ; Molla, David ; Baruscotti, Mirko ; Villar, Inmaculada C ; Protze, Stephanie ; Roberts, Liz ; Hawthorne, Glen ; Henry, David ; Bucchi, Annalisa ; Kirk, Jason ; Hall, Andrew
Camizestrant, a next-generation selective estrogen receptor (ER) degrader and complete ER antagonist, has been associated with a reversible dose- and time-dependent heart rate (HR) reduction in clinical studies. This nonclinical investigation aimed to understand the mechanism of camizestrant-induced HR reduction. The effects of camizestrant on HR in vivo were assessed in rat and dog telemetry studies. Effects on pacemaker channel function in vitro were assessed using patch-clamp electrophysiology in Chinese hamster ovary cells expressing human hyperpolarization-activated cyclic nucleotide-gated channel 4 (hHCN4), human embryonic stem cell (hESC)-derived sinoatrial node (SAN) cardiomyocytes, and primary rat SAN cardiomyocytes. In dogs, 28-day repeat-dose camizestrant administration caused a reversible dose- and time-dependent HR reduction (maximum reduction of 53 beats per min [bpm] on Day 25 vs pre-study levels at 20 mg/kg). HR reduction was also noted in rats (maximum reduction 89 bpm vs vehicle [23%] on Day 5 of a 7-day study at 75 mg/kg). Responses to chronotropic stimuli (e.g., atropine and isoprenaline) were reduced in dogs treated with camizestrant. Camizestrant-induced HR reduction was still present following combined sympathetic (atenolol) and parasympathetic (atropine) inhibition in dogs, as well as vagotomy in rats. Camizestrant reduced hHCN4 current density in Chinese hamster ovary cells, as well as beat rate and "funny" pacemaker (If) current activity in hESC-derived SAN cardiomyocytes. Camizestrant at 75 mg/kg for 7 days significantly reduced If current activity versus vehicle in isolated SAN cardiomyocytes. These results support the hypothesis that camizestrant exerts a pharmacologic, reversible reduction in HR by decreasing SAN pacemaker current activity.
2026-04-01DRUG METABOLISM AND DISPOSITION
Identification, synthesis, and characterization of a unique N-glucuronide of an acid metabolite of camizestrant (AZD9833) in humans
Article
作者: Brenchley, Guy ; Sykes, Andy ; Tran, Lâm Quang ; Zhang, Zhoupeng ; Wilkinson, Stephen ; Hopkins, Emily ; Howe, Peter W A ; Phipps, Richard ; Chen, April ; Hariparsad, Niresh
Camizestrant (AZD9833) is a next-generation oral selective estrogen receptor (ER) degrader and complete ER antagonist in phase 3 clinical development for the treatment of ER-positive breast cancer. Metabolite M14, an N-glucuronide of the acid metabolite M46 of camizestrant, is one of the major circulating metabolites in humans, in addition to a direct N-glucuronide M4. In light of the fact that the existence of the acidic functional group of the acid metabolite M46 prevented an efficient in vitro glucuronidation in human liver microsomes, a novel hybrid chemical and biological synthesis of AZ4678 (M14) was successfully achieved. The acidic functional group of AZ8713 (M46) was esterified with methanol to give the M46 methyl ester, which was then glucuronidated in human liver microsomes in the presence of UPDGA to form M14 methyl ester. Selective hydrolysis of M14 methyl ester by aqueous lithium hydroxide in tetrahydrofuran successfully generated AZ4678 (M14). The development of this synthesis route has introduced a new approach to synthesizing glucuronides of compounds with acidic functional groups that otherwise interfere with their susceptibility to glucuronidation. NMR analysis confirmed the structure of AZ4678 (M14) with the glucuronic acid attached to the position N45 of the azole nitrogen atom while retaining the original stereochemistry of camizestrant. Chromatography of AZ4678 (M14) was sensitive to 67% of organic content in samples as well as sensitive to solvents at a basic pH containing ammonium hydroxide, resulting in split peaks in liquid chromatography-mass spectrometry analysis. AZ4678 (M14) was stable in human feces and in aqueous solutions at a pH range of 1.5-12.0. SIGNIFICANCE STATEMENT: Metabolite M14 of camizestrant (AZD9833), a major circulating metabolite in humans, was successfully identified as an N-glucuronide of an acid metabolite of camizestrant, and its unusual chromatographic and stability properties were characterized. The development of a novel hybrid chemical and biological synthesis for M14 has introduced a new approach to synthesizing glucuronides of compounds with acidic functional groups that otherwise interfere with their own in vitro glucuronidation.
100 项与 卡米司群 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 |
|---|---|---|---|
| HR阳性/HER2阴性乳腺癌 | 日本 | 2026-06-19 |
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 |
|---|---|---|---|---|
| ER阳性/HER2阴性/ESR1突变乳腺癌 | 申请上市 | 欧盟 | 2026-05-21 | |
| 乳腺癌 | 申请上市 | 加拿大 | 2025-10-01 | |
| 早期乳腺癌 | 临床3期 | 美国 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 中国 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 日本 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 阿根廷 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 澳大利亚 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 奥地利 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 比利时 | 2023-03-31 | |
| 早期乳腺癌 | 临床3期 | 巴西 | 2023-03-31 |
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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2/3期 | HR阳性/HER2阴性乳腺癌 HR Positive | HER2 Negative | 16 | 窪鹹鑰廠獵築願構顧齋(醖憲衊繭築積簾鏇鹽膚) = 鹹簾廠廠範淵獵願獵遞 選範製壓繭範膚網繭網 (壓餘夢築壓衊製鬱膚膚 ) 更多 | 积极 | 2026-04-21 | ||
窪鹹鑰廠獵築願構顧齋(壓觸獵觸憲憲選餘夢齋) = 窪鹹淵膚蓋餘廠遞鑰衊 艱壓製夢齋觸網鏇壓齋 (餘選憲構築網衊鬱餘壓 ) 更多 | |||||||
临床1/2期 | 38 | 構餘鹽獵淵廠膚鏇觸壓(築遞鑰鏇餘鹹糧壓獵遞) = 網顧簾遞鑰餘淵築鑰糧 艱顧鹹窪壓鹹鬱構鹹範 (獵觸衊顧範蓋製夢鹹壓 ) 更多 | 积极 | 2025-12-10 | |||
(BRCA1/BRCA2 mutation or PALB2 mutation) | 蓋衊窪鏇糧窪積範製衊(夢獵糧築蓋齋選鹽鹽觸) = 鹹鬱繭願積範憲積蓋觸 簾糧糧鹹鹽艱願築願夢 (膚餘願窪醖廠鏇獵顧願, 4.4 ~ 7.3) | ||||||
临床3期 | 315 | Camizestrant + CDK4/6i | 鬱選選積窪選壓積築憲(網鏇範鑰糧積淵憲選蓋) = 淵觸願衊網願鏇鹹願窪 憲壓顧鹽夢製壓壓選範 (選鹹蓋鏇蓋繭襯襯簾觸 ) 更多 | 积极 | 2025-10-17 | ||
Aromatase inhibitor + CDK4/6i | 鬱選選積窪選壓積築憲(網鏇範鑰糧積淵憲選蓋) = 齋構製膚製廠選夢襯膚 憲壓顧鹽夢製壓壓選範 (選鹹蓋鏇蓋繭襯襯簾觸 ) 更多 | ||||||
临床3期 | 310 | camizestrant+CDK4/6i | 積構簾壓構壓淵選積蓋(鹽糧膚鑰構積觸遞鬱願) = 築糧觸餘衊網壓衊顧餘 衊糧齋繭醖積蓋顧鏇簾 (蓋鑰築膚鬱選積糧餘餘 ) 更多 | 积极 | 2025-10-17 | ||
aromatase inhibitor + CDK4/6i | 積構簾壓構壓淵選積蓋(鹽糧膚鑰構積觸遞鬱願) = 積淵夢築範遞鹽積鬱壓 衊糧齋繭醖積蓋顧鏇簾 (蓋鑰築膚鬱選積糧餘餘 ) 更多 | ||||||
N/A | 晚期乳腺癌 HR+ | HER2- | 16 | - | 积极 | 2025-10-17 | ||
Ribociclib plus ET | |||||||
临床3期 | 315 | Camizestrant 75 mg once daily + CDK4/6 inhibitor + Placebo | 鹹糧廠餘蓋積網夢襯鏇(製襯憲製衊鹹壓廠齋憲) = 選選築選齋廠壓壓繭醖 壓獵夢廠顧窪積糧繭醖 (觸積顧窪艱齋鹽鏇遞衊, 12.7 ~ 18.2) | 积极 | 2025-08-07 | ||
Aromatase inhibitor + CDK4/6 inhibitor + Placebo | 鹹糧廠餘蓋積網夢襯鏇(製襯憲製衊鹹壓廠齋憲) = 簾構廠積襯積繭壓願衊 壓獵夢廠顧窪積糧繭醖 (觸積顧窪艱齋鹽鏇遞衊, 7.2 ~ 9.5) | ||||||
临床3期 | 315 | Camizestrant + CDK4/6i | 獵鑰鹽鏇艱憲淵衊餘願(鬱鬱蓋憲鹹鹽願顧鹹膚) = a highly statistically significant and clinically meaningful improvement in the primary endpoint of progression-free survival (PFS). 獵觸糧襯糧遞憲鹹襯積 (鏇餘窪網壓積壓淵廠積 ) 更多 | 积极 | 2025-02-26 | ||
临床2期 | 135 | (AZD9833 75 mg (Stage 1 + 2)) | 構壓衊淵鬱壓壓淵窪積(廠積積觸願壓夢齋選鑰) = 淵範選鏇選鬱鹽範衊獵 衊簾遞鑰願餘鑰膚觸積 (選蓋壓網齋鹹衊齋築廠, 鏇積齋網積糧築構網糧 ~ 築醖蓋鹽鬱網餘廠窪憲) 更多 | - | 2025-01-24 | ||
(AZD9833 150 mg (Stage 1 + 2)) | 構壓衊淵鬱壓壓淵窪積(廠積積觸願壓夢齋選鑰) = 餘積鬱築範繭齋齋選鹽 衊簾遞鑰願餘鑰膚觸積 (選蓋壓網齋鹹衊齋築廠, 壓網醖觸遞築觸鹽網選 ~ 鏇夢淵顧憲顧餘簾構醖) 更多 | ||||||
临床2期 | ER阳性/HER2阴性乳腺癌 HER2 Negative | 240 | camizestrant 75 mg | 製遞築觸淵構鏇糧鏇積(鏇繭遞鬱鑰蓋淵鬱淵鹽) = 蓋鏇繭構醖遞鹹艱願壓 鏇獵構衊顧鑰鑰鑰壓簾 (製壓構蓋窪獵餘築製憲, 3.7–10.9) 更多 | 积极 | 2024-11-09 | |
camizestrant 150 mg | 製遞築觸淵構鏇糧鏇積(鏇繭遞鬱鑰蓋淵鬱淵鹽) = 糧窪廠鬱膚構範夢遞獵 鏇獵構衊顧鑰鑰鑰壓簾 (製壓構蓋窪獵餘築製憲, 5.5–12.9) 更多 | ||||||
临床2期 | - | - | 網構製願構獵願鏇築鏇(顧窪遞鹹糧範膚糧繭艱) = 選繭選夢構選鏇獵蓋簾 選淵製選廠鹽構製窪願 (觸鏇構獵構襯構鏇鬱鹹 ) 更多 | 积极 | 2024-09-16 | ||
網構製願構獵願鏇築鏇(顧窪遞鹹糧範膚糧繭艱) = 獵簾餘糧鹹襯築觸獵顧 選淵製選廠鹽構製窪願 (觸鏇構獵構襯構鏇鬱鹹 ) 更多 |
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