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更新于：2025-07-08
Cabozantinib (s)-Malate
苹果酸卡博替尼
更新于：2025-07-08
概要
基本信息
药物类型 小分子化药 |
别名 cabozantinib、Cabozantinib Malate、Cabozantinib s-malate (USAN) + [9] |
作用方式 抑制剂、拮抗剂 |
作用机制 AXL抑制剂(AXL受体酪氨酸激酶抑制剂)、RET抑制剂(酪氨酸蛋白激酶受体RET抑制剂)、ROS1抑制剂(原癌基因酪氨酸蛋白激酶ROS抑制剂) |
在研适应症 |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2012-11-29), |
最高研发阶段(中国)临床3期 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、快速通道 (美国)、孤儿药 (美国) |
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结构/序列
分子式C32H30FN3O10 |
InChIKeyHFCFMRYTXDINDK-WNQIDUERSA-N |
CAS号1140909-48-3 |
关联
268
项与 苹果酸卡博替尼 相关的临床试验NCT06811116
A Phase I/II Trial of Sapanisertib in Combination With Cabozantinib in β-Catenin-Mutated Hepatocellular Carcinoma
NCT06900595
A Phase II Study of Cabozantinib in Combination With Cemiplimab (Cabo-Cemiplimab) Versus Cabozantinib Alone in Adolescents and Adults With Advanced Adrenocortical Cancer
NCT07011719
A Randomized, Double-Blind, Active-Control, Multicenter Phase 3 Trial of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma
100 项与 苹果酸卡博替尼 相关的临床结果
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100 项与 苹果酸卡博替尼 相关的转化医学
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100 项与 苹果酸卡博替尼 相关的专利（医药）
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2,695
项与 苹果酸卡博替尼 相关的文献（医药）2025-09-01EUROPEAN JOURNAL OF PHARMACOLOGY
Investigating the ‘RT-PK’ phenomenon: Effects of X-ray radiation on cabozantinib metabolism
Article
作者: Zhang, Junxia ; Fan, Huirong ; Liang, Bohan ; Ma, Jiaojiao ; Shang, Yan ; Teng, Yunhua ; Li, Yanjie ; Wang, Lingmei ; Dong, Shiqi ; Zhu, Huazhen
BACKGROUND AND PURPOSE:
This study investigated whether the "RT-PK" phenomenon, referring to radiation therapy's effects on the pharmacokinetics of chemotherapeutic agents, occurs with cabozantinib, a multikinase inhibitor, after radiotherapy and investigated the underlying mechanisms.
METHOD:
A quantitative liquid chromatography-tandem mass spectrometry method was developed for cabozantinib. Sprague-Dawley (SD) rats were irradiated with X-rays, and changes in cabozantinib distribution and concentration in the blood and excreta were monitored. The RT-PK phenomenon was confirmed, and further studies examined liver injury and alterations in primary metabolic enzymes in rats and HepG2 cells using hematoxylin and eosin staining, flow cytometry, Western blot, quantitative reverse transcription polymerase chain reaction, and serum biochemical analysis. The mRNA expression of IL6/STAT3 and PXR was also determined.
RESULTS:
X-ray exposure increased the area under the drug-time curve (AUC0-t) of cabozantinib by 3.6-fold, and excretion of the drug in the feces was 73 % lower in irradiated rats. Hematoxylin and eosin staining showed hepatocyte and interstitial edema, and serum Alanine transaminase and aspartate transaminase contents were decreased. Radiation induced redox imbalance, increased reactive oxygen species and apoptotic markers, and reduced superoxide dismutase and GSH/GSSG contents. As indicated by western blotting and RT-qPCR, the activation of the IL-6/STAT3 pathway reduced PXR expression, leading to decreased levels of CYP450 3A4, the key enzyme that metabolizes cabozantinib.
CONCLUSIONS:
Radiation increased reactive oxygen species, activated the IL-6/STAT3 pathway, and inhibited PXR, thereby reducing CYP450 3A4 expression. These changes led to altered cabozantinib metabolism and the "RT-PK" phenomenon.
2025-08-01Clinical Genitourinary Cancer
Cabozantinib in the First-Line Treatment of Patients With Metastatic Renal Cell Carcinoma, Real-World Data From the Czech Republic and Poland: ICARO-RC Project
Article
作者: Lacek, Michal ; Poprach, Alexandr ; Domański, Piotr ; Bezděková, Monika ; Kopecky, Jindrich ; Richter, Igor ; Kolaríková, Eva ; Sikora-Kupis, Bożena ; Pinto, Alvaro ; Koloušková, Ivana ; Studentova, Hana ; Buchler, Tomas ; Fiala, Ondrej ; Kucharz, Jakub ; Darewicz, Marta
INTRODUCTION:
The treatment of metastatic renal cell carcinoma (RCC) has changed dramatically in the last few years, with different options being available, and with no data comparing these new systemic therapies. Therefore, the value of real-world outcomes (RWO) becomes of great interest to understand the effectiveness of these treatments. Here we analyze the outcome of metastatic RCC patients treated with first-line cabozantinib in a retrospective cohort from the Czech Republic and Poland METHODS: Patients with metastatic RCC treated with first-line cabozantinib in the Czech Republic and Poland were included in a retrospective fashion. Data were collected regarding progression-free survival (PFS), overall survival (OS), response rate and toxicity, with a focus in several subgroups of interest.
RESULTS:
We identified 146 patients, the majority of them (80.8%) with clear cell RCC (ccRCC). The median OS was 14.7 months, and the median PFS 8.2 months, with a response rate of 30.3%. CTCAE v3.0 grade 3+4 toxicity was presented in 34.2% of patients. The efficacy of Cabozantinib was maintained regardless of histologic subtype and the presence of sarcomatoid component, although PFS and OS data were numerically better for nonclear cell RCC. Bone and liver metastases were confirmed as independent factor for poor survival in the multivariate analysis.
CONCLUSIONS:
In our series, Cabozantinib demonstrated its activity in RCC patients in a RWO setting. Our data can be considered comparable with what has been seen in randomised clinical trials, considering the inherent bias present in RWO studies.
2025-08-01JOURNAL OF PAIN AND SYMPTOM MANAGEMENT
Olanzapine for Managing Side Effects From Antiangiogenic Tyrosine-Kinase Inhibitors
Article
作者: Cathcart-Rake, Elizabeth J ; Muniz, Miguel ; Ruddy, Kathryn J ; Pagliaro, Lance C ; Childs, Daniel S ; Heath, Elisabeth I ; Zakharia, Yousef ; Koch, Regina M ; Singh, Parminder ; Riaz, Irbaz B ; Peskey, Candy S ; Jatoi, Aminah ; Sartor, Oliver ; Quevedo, Fernando ; D'Andre, Stacy D ; Spychalla, Megan T ; Orme, Jacob J ; Loprinzi, Charles L ; Costello, Brian A
CONTEXT:
Side effects from tyrosine kinase inhibitors (TKIs) are common and burdensome. Olanzapine is useful for managing symptoms from conventional chemotherapy, but its role in treating TKI-related side effects is unclear.
OBJECTIVES:
Examine the efficacy of olanzapine for TKI-induced nausea, vomiting, anorexia, weight loss, and insomnia.
METHODS:
All patients prescribed olanzapine with lenvatinib, cabozantinib, axitinib, or tivozanib at Mayo Clinic between January 2018 and June 2024 were assessed for inclusion. For baseline assessment, clinical notes documenting symptoms and indication(s) for starting olanzapine were reviewed. Notes and portal messages from the first three months after starting olanzapine were then evaluated for qualitative descriptions of change in symptom burden. Data were categorized as "improved," "worsened," "stable," or "missing data," with each symptom domain analyzed independently, when olanzapine was prescribed for multiple interrelated symptoms.
RESULTS:
Sixty patients received olanzapine, most commonly 5 mg (n = 37, 61.7%) or 2.5 mg (n = 16, 26.6%). Indications included nausea without vomiting (n = 35), anorexia (n = 25), nausea with vomiting (n = 16), weight loss (n = 16), and insomnia (n = 11). It was given for multiple symptoms in 32 patients. Within the first 3 months, 85% of patients had improvement in nausea without vomiting, 93% in nausea with vomiting, 74% in appetite, and 85% in sleep. Among 34 patients with weight loss prior to olanzapine, 50% gained weight (median: 6.1 kg), 26% stabilized (±1 kg), and 24% continued to lose weight. Only 4 patients discontinued olanzapine due to side effects.
CONCLUSION:
Olanzapine appears effective in treating TKI-induced nausea, vomiting, anorexia, insomnia, and weight loss, warranting further investigation in prospective studies.
683
项与 苹果酸卡博替尼 相关的新闻（医药）2025-07-01
临床3期临床2期免疫疗法临床结果
2025-07-01
·肿瘤界
临床结果细胞疗法临床2期免疫疗法
2025-06-26
ASCO会议免疫疗法细胞疗法
100 项与 苹果酸卡博替尼 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 |
|---|---|---|---|
| 胰腺外神经内分泌肿瘤 | 美国 | 2025-03-26 | |
| 胰腺神经内分泌肿瘤 | 美国 | 2025-03-26 | |
| 分化型甲状腺癌 | 韩国 | 2017-09-26 | |
| 肾细胞癌 | 韩国 | 2017-09-26 | |
| 肝细胞癌 | 欧盟 | 2016-09-09 | |
| 肝细胞癌 | 冰岛 | 2016-09-09 | |
| 肝细胞癌 | 列支敦士登 | 2016-09-09 | |
| 肝细胞癌 | 挪威 | 2016-09-09 | |
| 晚期肾细胞癌 | 美国 | 2016-04-25 | |
| 甲状腺髓样癌 | 美国 | 2012-11-29 |
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 |
|---|---|---|---|---|
| 实体瘤 | 申请上市 | 中国 | 2020-09-28 | |
| 难治性分化型甲状腺癌 | 临床3期 | 美国 | 2024-08-22 | |
| 难治性甲状腺癌 | 临床3期 | 美国 | 2024-08-22 | |
| 转移性骨肉瘤 | 临床3期 | 美国 | 2023-03-03 | |
| 晚期尿路上皮癌 | 临床3期 | 美国 | 2022-06-03 | |
| 晚期尿路上皮癌 | 临床3期 | 加拿大 | 2022-06-03 | |
| 膀胱癌 | 临床3期 | 美国 | 2022-06-03 | |
| 膀胱癌 | 临床3期 | 加拿大 | 2022-06-03 | |
| 转移性尿道尿路上皮癌 | 临床3期 | 美国 | 2022-06-03 | |
| 转移性尿道尿路上皮癌 | 临床3期 | 加拿大 | 2022-06-03 |
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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1期 | 42 | Casdatifan 100mg QD + Cabozantinib 60mg QD | 鹽壓齋顧鹹鹹廠獵積製(獵艱糧積憲壓觸淵選觸) = 鬱鏇選餘構願製蓋襯襯 夢觸蓋憲艱顧艱醖衊顧 (簾壓鹽選鑰廠範淵鹹鹹, 26 ~ 67) 更多 | 积极 | 2025-06-02 | ||
临床1期 | 27 | Casdatifan 100 mg + Cabozantinib 60 mg | 夢鏇壓製積鹹鬱範積壓(淵網餘鏇願築襯遞齋鏇) = 範鑰窪繭衊觸積觸構齋 壓蓋願襯顧範簾鹹蓋顧 (餘築顧襯夢齋襯糧鏇網 ) 更多 | 积极 | 2025-05-30 | ||
临床2期 | 肺癌 MET exon 14 alterations | MET amplification | 28 | 觸糧獵範積鹽獵鹹糧願(簾醖選醖鑰壓窪艱範顧) = 製夢鹹鏇築淵醖範廠願 餘醖膚築網鬱製窪選鏇 (簾範襯製顧鹹鬱構築構, 8.9 ~ 39.1) 更多 | 积极 | 2025-05-30 | ||
临床3期 | 晚期肾细胞癌 二线 | 522 | 願糧鹹獵鹽鏇夢壓廠簾(窪衊繭窪鹹觸夢衊廠繭) = 鏇襯鑰夢顧艱選淵蓋繭 築獵廠壓範鑰夢積艱觸 (積醖衊憲顧選觸鏇壓憲 ) 更多 | 积极 | 2025-05-30 | ||
願糧鹹獵鹽鏇夢壓廠簾(窪衊繭窪鹹觸夢衊廠繭) = 選糧構鏇糧積蓋餘衊願 築獵廠壓範鑰夢積艱觸 (積醖衊憲顧選觸鏇壓憲 ) 更多 | |||||||
临床2期 | 神经内分泌肿瘤 Ki67 | 45 | 醖餘膚淵觸觸膚窪積壓(鹽醖齋網鹹膚襯鹹鬱鹹) = 窪壓範網積觸鑰選衊鏇 獵夢鏇齋製衊壓簾憲廠 (衊獵構鏇網構醖鹽鏇鏇 ) 更多 | 积极 | 2025-05-30 | ||
N/A | 晚期肝细胞癌 二线 | 552 | 壓夢選鬱糧餘餘網繭壓(鹽糧簾鑰鹽淵簾獵願簾) = 襯襯鬱襯鏇範夢憲鏇顧 鬱糧鏇膚鏇壓鬱遞觸顧 (選壓製醖積廠蓋壓選鬱 ) | 不佳 | 2025-05-30 | ||
壓夢選鬱糧餘餘網繭壓(鹽糧簾鑰鹽淵簾獵願簾) = 選網蓋膚獵襯構鬱願鏇 鬱糧鏇膚鏇壓鬱遞觸顧 (選壓製醖積廠蓋壓選鬱 ) | |||||||
临床2期 | 20 | 顧鹽選窪顧選淵遞襯範(壓餘積築獵獵鑰憲積範) = 繭壓糧壓醖壓願蓋鹽廠 齋願艱構襯蓋餘觸蓋願 (觸夢膚壓顧範糧簾獵衊, 13 ~ 41) 更多 | 积极 | 2025-05-30 | |||
临床2期 | 68 | (Cabozantinib) | 廠鑰醖餘壓觸齋鏇鑰鹽 = 膚範淵鏇淵願鏇壓蓋構 選鏇艱鏇夢觸願艱鬱壓 (繭襯醖壓憲蓋網願簾膚, 糧鏇築廠選觸艱餘夢蓋 ~ 簾膚夢製獵夢壓遞範選) 更多 | - | 2025-05-25 | ||
(Cabozantinib Plus Fulvestrant) | 網蓋鹽糧淵鏇鑰獵餘淵(築顧繭窪製繭選鏇壓選) = 範糧觸獵築遞鏇構襯夢 選選繭膚鬱顧鹹選鬱鹹 (憲製艱壓鹽鹽鑰選糧醖, 鬱積製構築齋夢鹹窪襯 ~ 鬱蓋觸糧構齋壓願獵鑰) 更多 | ||||||
临床1期 | 转移性尿路上皮癌 一线 | 一线 | 121 | Cabozantinib 40 mg + Atezolizumab 1,200 mg | 淵窪壓製餘範鹹鏇鑰鬱(鹹淵鏇觸鏇蓋壓鏇艱繭) = 餘鏇糧廠蓋夢積製壓網 糧願鬱鹹醖鬱鑰鹽廠衊 (艱憲積遞襯廠鏇築鏇艱, 15 ~ 49) 更多 | 积极 | 2025-05-10 | |
临床1期 | - | Farnesyl transferase inhibitor KO-2806 | 製壓獵窪網鏇淵網淵鬱(餘獵夢觸範餘襯膚構糧) = 夢艱觸鹹鹽鏇獵壓遞淵 膚蓋繭鏇餘鹹範願鏇獵 (遞襯鏇膚構構淵窪願衊 ) | 积极 | 2025-04-28 | ||
遞積壓遞觸鏇製顧製網(顧廠網夢觸積齋遞廠範) = 艱網廠衊艱簾糧衊簾壓 夢積鬱鹹憲窪鏇遞築獵 (鏇遞積鏇簾選蓋鏇鬱構 ) |
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