苹果酸卡博替尼(Cabozantinib (s)-Malate) - 药物靶点：AXL x RET x ROS1 x TYRO3 x Tie-2 x TrkB x VEGFR1 x VEGFR2 x VEGFR3 x c-Kit x c-Met_在研适应症：神经内分泌肿瘤，高分化胰腺内分泌肿瘤，胰腺外神经内分泌肿瘤_专利_临床

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]

靶点

AXL x RET x ROS1 x TYRO3 x Tie-2 x TrkB x VEGFR1 x VEGFR2 x VEGFR3 x c-Kit x c-Met

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)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [11]

在研适应症

神经内分泌肿瘤高分化胰腺内分泌肿瘤胰腺外神经内分泌肿瘤+ [196]

非在研适应症

晚期胆管癌晚期乳腺癌肝外胆管癌+ [39]

原研机构

Exelixis, Inc.

在研机构

National Cancer InstituteIpsen Pharma SAS

Exelixis, Inc.

+ [19]

非在研机构

University of Washington

江苏豪森药业集团有限公司

EMD Serono, Inc.

权益机构

Ipsen SA

Takeda Pharmaceutical Co., Ltd.

Chugai Pharmaceutical Co., Ltd.

+ [7]

最高研发阶段批准上市

首次获批日期

美国 (2012-11-29),

甲状腺髓样癌

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

273

项与苹果酸卡博替尼相关的临床试验

NCT07187869

/ Not yet recruiting临床1期IIT

Modulation of the Bone Immune Microenvironment Following Cabozantinib Treatment of Bone Metastatic Clear Cell Renal Cell Carcinoma: Proof of Concept Study

The goal of our study is to explore how treatments affect the bone immune microenvironment and determine the best treatment options for patients with metastatic kidney cancer to the bone. This could prevent skeletal complications and improve patient outcomes.

开始日期2026-03-31

申办/合作机构

The University of Texas MD Anderson Cancer Center

[+1]

NCT06811116

/ Recruiting临床1/2期IIT

A Phase I/II Trial of Sapanisertib in Combination With Cabozantinib in β-catenin-mutated Hepatocellular Carcinoma (SAPHIRE)

This phase I/II trial studies the side effects and best dose of sapanisertib when given together with cabozantinib, and to see how well they work in treating patients with liver cancer that has spread from where it first started to other places in the body (metastatic) and contains a mutation (change) in the β-catenin gene. Sapanisertib and cabozantinib may stop the growth of tumor cells by blocking some of the enzymes needed for cell growth. Giving sapanisertib and cabozantinib together may work better than giving cabozantinib alone in treating β-catenin-mutated metastatic hepatocellular carcinoma.

开始日期2026-02-10

申办/合作机构

National Cancer Institute

NCT06502171

/ Not yet recruiting临床1期IIT

A Phase 1/1b/2 Study of Cabozantinib in Combination With Selumetinib for Plexiform Neurofibroma in Adults and Adolescents With Neurofibromatosis Type 1

Based on the clinical activity of both selumetinib and cabozantinib as monotherapies in clinical trials, the demonstrated activity of these agents in reduced doses in preclinical studies, and the non-overlapping toxicity profiles, the study will assess the tolerability and efficacy of selumetinib and cabozantinib in combination in participants with NF1 ≥16 years old with progressive and/or symptomatic PN in a phase 1/1b/2 clinical trial.
Trial Design Phase 1 This will be an open label, dose escalation phase. Dose level escalation will be determined by a rolling six design. In this design, up to 6 participants can be enrolled at a given dose level and then evaluated for dose limiting toxicity (DLT) within the DLT window. The DLT window is defined as 16 weeks in this study based on the long half-life of cabozantinib and the desire to have maximum confidence about long-term tolerability of the combination prior to proceeding to the next dose level.
Phase 1b Once the recommended phase 2 dose has been determined in phase 1, an expanded cohort of 12 participants will be enrolled in phase 1b portion of the study.
Phase 2 This will be an open label, single-arm phase using the recommended phase 2 dose.

开始日期2025-10-01

申办/合作机构

The University of Alabama at Birmingham

[+2]

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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2,436

项与苹果酸卡博替尼相关的文献（医药）

2025-12-01·Medicinal Chemistry

Reducing Cabozantinib Toxicity in Renal Cell Carcinoma Treatment through Structural Modifications

Article

作者: Lu, Yongliang ; Guo, Jiaxiang ; Yang, Yu ; Yin, Xiaotao

Background and Objectives::

Cabozantinib, a Tyrosine Kinase Inhibitor (TKI), is widely used in Renal Cell Carcinoma (RCC) therapy but often causes serious side effects such as myelosuppression, immunosuppression, and angiopathy. This study aims to identify key protein targets responsible for the therapeutic efficacy and adverse reactions of cabozantinib and to explore structural modifications to reduce toxicity while preserving efficacy.

Methods::

A non-randomized computational approach was employed, screening 400 potential protein targets using SwissTargetPrediction and ChemBL databases. Molecular docking and Structure-Activity Relationship (SAR) analysis were performed to assess interactions between cabozantinib and identified targets, focusing on structural elements contributing to toxicity.

Results::

Three primary proteins were identified as responsible for the anti-tumor effects of cabozantinib, while three others were linked to its side effects. Docking analysis revealed that the methoxyphenyl group in cabozantinib formed undesirable hydrogen bonds with toxicity-related proteins. Modulating these off-target interactions by minimizing hydrogen bonding in this region could significantly reduce adverse effects.

Conclusion::

These findings provide structural insights into cabozantinib’s dual effects and suggest optimization strategies for TKI design, offering a pathway toward safer and more effective RCC treatments.

2025-12-01·Clinical Genitourinary Cancer

Titrating Cabozantinib in Metastatic Renal Cell Carcinoma Patients Using Goldilocks Principle: A Real-World Evidence Study

Article

作者: Ahrenfeldt, Johanne ; Lyskjær, Iben ; Fristrup, Niels ; Thybo, Malou Aarønæs

INTRODUCTION:

The incidence of renal cell carcinoma (RCC) continues to rise worldwide, and this malignancy has demonstrated substantial sensitivity to both immunotherapies and targeted agents, particularly tyrosine kinase inhibitors (TKIs). Cabozantinib, a commonly utilized TKI, has shown promising efficacy across multiple clinical trials. This study aims to evaluate the real-world effectiveness of individualized cabozantinib dosing as a later-line treatment in patients with metastatic RCC (mRCC).

PATIENTS AND METHODS:

Patients with mRCC treated at the Department of Oncology, Aarhus University Hospital, Denmark, were identified to estimate the median progression free survival (mPFS) and median overall survival (mOS) from treatment initiation. Best radiological response was evaluated using RECIST 1.1. Multivariable cox regression analyses were performed, including covariates such as brain metastasis, first-line treatment, line of treatment, ECOG Performance Status, IMDC risk group, nephrectomy status, and toxicity.

RESULTS:

A total of 179 patients were included, of which 139 patients received second-line (2L) treatment, and 40 patients received third+-line (3+L) treatment. We found a mPFS of 11.2 months for 2L treatment and 11.6 months for 3+L treatment. The mOS was 15.6 months for the 2L group and 17.1 months for the 3+L group. The mPFS and mOS in the IMDC favourable risk group were 28.5 and 52.1 months, respectively. No significant differences in mPFS or mOS were observed based on prior 1L treatment or the presence of brain metastases. The mOS and mPFS found in this study are comparable to, and in some cases exceed, those reported in other real-world cohorts. Interestingly, we found treatment-related toxicity to correlate significantly with an increased survival (mOS 66.8 vs. 32.8 months, P = .016) (mPFS 14,7 vs. 8,5 months, P = .013).

CONCLUSION:

This study reinforces the existing data on effectiveness of cabozantinib as a later-line treatment for mRCC in real-world settings. We report 40 mg as the preferred landing zone. Furthermore we identify patients needing dose reductions due to toxicity as a subgroup carrying a significantly better prognosis. The results emphasize the importance of individual dosage for optimizing treatment outcomes and points out treatment-related toxicity as a surrogate marker for sufficient serum concentration of the active substance.

2025-11-03·JOURNAL OF EXPERIMENTAL MEDICINE

A high-throughput zebrafish screen identifies novel candidate treatments for kaposiform lymphangiomatosis (KLA)

Article

作者: Levin, Lotan ; Jabali, Amani ; Paran, Yael ; Yaniv, Karina ; Perlmoter, Gal ; Bassi, Ivan ; Barzilai, Aviv ; Tevet, Yaara ; Geva, Polina ; Leichner, Gil S. ; Otterstrom, Jason J. ; Lambiase, Giuseppina ; Barr, Haim ; Farag, Naama ; Egozi, Shany ; Long, Jonathan ; Avivi, Camila ; Moshe, Noga ; Greenberger, Shoshana

Kaposiform lymphangiomatosis (KLA) is a rare and aggressive disease caused by a somatic activating NRAS mutation (p.Q61R) in lymphatic endothelial cells (LECs). The development of new therapeutic avenues is hampered by the lack of animal models faithfully replicating the clinical manifestations of KLA. Here, we established a novel zebrafish model of KLA by conditionally expressing the human NRAS mutation in venous and lymphatic ECs. Mutant embryos recapitulate key clinical features of KLA, including dilated lymphatics and pericardial edema, which are reversed by trametinib, a MEK inhibitor used in KLA treatment. Leveraging this model in combination with an AI-based high-throughput drug screening platform, we identify cabozantinib, a tyrosine kinase inhibitor, and GSK690693, a competitive pan-Akt kinase inhibitor, as promising candidates for treating KLA. Notably, both drugs normalized sprouting and migration of cultured LECs from a KLA patient. Overall, our novel zebrafish model provides a powerful platform to dissect KLA pathogenesis and identify new therapeutic avenues.

710

项与苹果酸卡博替尼相关的新闻（医药）

2025-09-26

·PMLiVE

Ipsen's tumour treatment receives MHRA marketing authorisation

Ipsen has been given marketing authorisation by the UK Medicines and Healthcare products Regulatory Agency (MHRA) for cabozantinib, to be used for patients with previously treated, unresectable or metastatic neuroendocrine tumours (NETs). This is the first time the agency has authorised a treatment of this type, which can be used irrespective of tumour site or prior systemic therapy. NETS affect an estimated 35 out of every 100,000 people in England and often require multiple lines of therapy as the disease progresses. Effective treatment options are limited, with factors such as the primary tumour site complicating the determination of optimal treatment sequencing. The authorisation is based on positive data from the phase 3 CABINET trial, which assessed cabozantinib versus placebo in patients with advanced pancreatic NETs (pNETs) and extra-pancreatic NETs (epNETs). In both cohorts, cabozantinib demonstrated a statistically significant reduction in the risk of disease progression and death, with median progression-free survival improved compared with placebo. “This UK marketing authorisation marks a critical milestone in making a licensed and efficacious treatment option available to patients upon progression. We are actively engaging with NICE to ensure that individuals living with this often overlooked form of cancer in the UK have timely access to this approved therapeutic option,” said Ian Gray, UK & Ireland interim medical director at Ipsen. Cabozantinib was also granted marketing authorisation in Europe earlier this year by the European Medicines Agency (EMA). The recommendation followed a positive opinion from the Committee for Medicinal Products for Human Use (CHMP) in June. A final review by NICE is expected later this year.

临床3期临床结果上市批准

2025-09-19

·PRNewswire

Liver Cancer Therapeutics Market Size Surpasses USD 13.16 Billion by 2032, Increasing at a CAGR of 16.5% from 2025 to 2033

AUSTIN, Texas and TOKYO, Sept. 19, 2025 /PRNewswire/ -- According to DataM Intelligence, the global liver cancer therapeutics market size was valued at US$3.36 billion in 2024 and is expected to reach US$13.16 billion by 2033, growing at a CAGR of 16.5% during the forecast period 2025-2033. The liver cancer therapeutics market is entering a transformative phase, driven by the shift from traditional systemic therapies to innovative immunotherapies and targeted agents that offer improved survival outcomes. The growing adoption of combination regimens, particularly checkpoint inhibitors paired with VEGF or TKI therapies, is expected to redefine the treatment landscape and expand the eligible patient pool. At the same time, the rising prevalence of hepatocellular carcinoma worldwide, coupled with strong R&D pipelines and increasing regulatory approvals, positions this market for sustained growth. A significant advancement in liver cancer therapeutics is the approval of combination immunotherapy regimens. Notably, AstraZeneca's Imfinzi (durvalumab) plus Imjudo (tremelimumab) gained global recognition after the HIMALAYA trial demonstrated a meaningful overall survival benefit in patients with unresectable hepatocellular carcinoma. This approval provided a new first-line treatment option beyond tyrosine kinase inhibitors and VEGF-targeted therapies, offering durable survival outcomes for a subset of patients and reshaping the standard of care in advanced HCC. Another key advancement is the expansion of targeted oral therapies, which have improved safety and efficacy profiles. Drugs such as lenvatinib and cabozantinib have demonstrated substantial clinical activity as first- or second-line options, while ongoing research is investigating their use in combination with checkpoint inhibitors. The growing pipeline of next-generation TKIs and precision therapies, tailored to genetic and molecular profiles, is driving innovation, improving patient survival, and reinforcing the importance of oral targeted agents in the long-term management of HCC. Get a Sample PDF Brochure of the Report (Use Corporate Email ID for a Quick Response): The chemotherapy segment, based on therapy type, is expected to account for 39.1% of the liver cancer therapeutics market share. Chemotherapy remains a vital part of the liver cancer therapeutics market, especially for patients with intermediate-stage hepatocellular carcinoma (HCC) or those ineligible for surgical resection or transplantation. Trans-arterial chemoembolization (TACE) is a standard of care used in clinical settings and often combined with targeted therapies. Despite the rise of immunotherapies and precision drugs, chemotherapy remains vital due to its established protocols, lower costs, and widespread availability. Clinical studies are exploring the synergy of chemotherapeutic agents with immunomodulators to prolong survival and delay disease progression. The North American liver cancer therapeutics market was valued at 42.1% market share in 2024. North America is expected to dominate the liver cancer therapeutics market due to its robust healthcare infrastructure, high awareness, and significant investments in oncology research and development (R&D). For instance, in January 2025, researchers at Mount Sinai made a significant breakthrough in treating hepatocellular carcinoma (HCC), a type of liver cancer. Additionally, the rise in liver cancer incidence, driven by NAFLD, obesity, and chronic hepatitis C, has increased early diagnosis rates and demand for advanced therapeutics. The FDA's favorable regulatory pathways, including priority reviews and orphan drug designations, have accelerated drug approval, ensuring rapid market access. The liver cancer therapeutics market in the U.S. dominated the North America market with the largest revenue share in 2024, driven by the increasing investment in pharmaceuticals. The regulatory framework in the U.S. ensures only safe and effective drugs reach the market, which increases trust of patients and healthcare providers in the medicines. Furthermore, the involvement of major players and the launch of novel treatments contribute to its dominance. Regulatory approvals for innovative drugs support market expansion, making the U.S. a leader in liver cancer treatments. This environment fosters continuous innovation and growth. Get Customization in the Report as Per Your Business Requirements: Europe is the second-dominating region in the liver cancer therapeutics market, valued at 34.5% market share in 2024. The liver cancer therapeutics market in Europe is driven by the growing prevalence of hepatitis B and C infections, rising alcohol consumption, and increasing cases of non-alcoholic fatty liver disease (NAFLD). Supportive regulatory approvals for novel immunotherapies, combined with a well-established healthcare infrastructure and government-backed cancer screening programs, are driving the adoption of advanced treatment regimens. In the U.K., a high burden of liver disease linked to obesity, diabetes, and alcohol misuse is accelerating demand for effective HCC treatments. National Health Service (NHS) initiatives to expand early cancer diagnosis, along with faster access schemes for innovative oncology drugs, further drive uptake of immunotherapies and targeted therapies. The Asia-Pacific region in the Liver Cancer Therapeutics Market was valued at 23.5% market share in 2024. This region is witnessing significant growth due to the very high incidence of hepatitis B and C, particularly in China and Southeast Asia, which are leading causes of HCC. Rising investments in healthcare infrastructure, increased clinical trial activity, and expanding patient access to immuno-oncology drugs are driving market growth. In Japan, liver cancer remains a leading cause of cancer mortality, primarily associated with hepatitis virus infections and an ageing population. Strong government support for oncology research, rapid adoption of cutting-edge immunotherapies, and the presence of domestic pharmaceutical players are key factors driving therapeutic innovation and market expansion. For instance, in June 2025, Ono Pharmaceutical Co., Ltd. and Bristol-Myers Squibb K.K. received supplemental approval for their anti-PD-1 antibody, Opdivo, and BMSKK's anti-CTLA-4 antibody, Yervoy, in combination therapy in Japan to expand their use for treating unresectable hepatocellular carcinoma (HCC), a type of cancer. Purchase This Exclusive Report at Just USD 4350 Only: Key Liver Cancer Therapeutics Companies: Top companies in the liver cancer therapeutics market include AstraZeneca, Bayer AG, Eli Lilly, Bristol-Myers Squibb Company, Eisai Co., Ltd., Genentech and among others. Recent Developments in the Market In September 2025, Akeso, Inc. has dosed the first patient in its Phase II registrational trial, evaluating cadonilimab, Akeso's first-in-class PD-1/CTLA-4 bispecific antibody, in combination with lenvatinib for treating advanced hepatocellular carcinoma in patients previously treated with atezolizumab and bevacizumab. In July 2025, Apollo Proton Cancer Centre (APCC) has launched an 'Advanced Liver Cancers Clinic', an integrated clinic for primary liver cancers and liver metastases. Related Reports: Pediatric Oncology Drugs Market Size, Share, Industry, Forecast and Outlook (2024-2031) Cancer Immunotherapy Market Size, Trends & Forecast 2033 Hepatocellular Carcinoma Treatment Market Size, Share, Growth Trends and Forecast Report 2025-2033 About DataM Intelligence 4Market Research: DataM Intelligence 4Market Research is a comprehensive market intelligence platform offering syndicated and customized reports along with expert consulting across multiple industries, including chemicals, healthcare, agriculture, food & beverages, and more. With extensive experience and a strategy-focused approach, DataM provides businesses and individuals with reliable market insights, statistical forecasts, and personalized research solutions to help them make informed decisions and successfully bring innovations to market. To find out more, visit or follow us on Twitter, LinkedIn and Facebook. Contact: Mr. Sai Kiran DataM Intelligence 4market Research LLP Ground floor DSL Abacus IT Park, Industrial Development Area Uppal, Hyderabad, Telangana 500039 USA: +1 877-441-4866 Email: [email protected] Content Source: Visit Our Website: Logo: SOURCE DataM Intelligence 4 Market Research LLP WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

孤儿药临床2期上市批准免疫疗法

2025-09-19

·ioncology

鄢谢桥教授：ST-1898片在晚期肾细胞癌患者中的有效性和安全性的Ib/II期临床数据及启示丨第28届CSCO学术年会

点击蓝字，关注我们编者按：近年来，肾细胞癌的靶向治疗不断取得新突破，多靶点TKI药物研发成为热点。在第28届全国临床肿瘤学大会（CSCO）上，北京大学肿瘤医院/北京高博医院鄢谢桥教授报告了ST-1898片在晚期肾细胞癌患者中的Ib/II期临床研究结果，显示出良好的有效性和安全性。《肿瘤瞭望》特邀鄢谢桥教授就该研究的核心成果及其临床意义进行深入解读。 01 《肿瘤瞭望》：ST-1898是一个多靶点TKI。在肾癌领域，其靶点设计（如c-MET, AXL, VEGFR2等）是针对当前TKI治疗（如舒尼替尼、卡博替尼）的哪些局限性（如耐药、毒性谱）而优化的？其理论上可能带来哪些差异化优势？鄢谢桥教授北京大学肿瘤医院/北京高博医院这个问题非常好。目前国内确实缺乏新型TKI药物，我们在晚期肾癌的后线甚至一线治疗手段仍较为有限。相比之下，国外已批准卡博替尼、仑伐替尼等多靶点药物，这曾令我们非常羡慕。因此，ST-1898的研发令人振奋，我们现在也拥有了自主研发的新型TKI药物。 ST-1898是通过AI药物设计技术平台（SigmaHit®）开发的全新多靶点TKI，具有三大优势。第一，其靶点覆盖广泛，不仅包括传统的PDGFR、VEGFR，还涵盖耐药相关靶点如AXL和c-MET，以及肿瘤细胞生存依赖的c-KIT和TRK等靶点。第二，靶点抑制活性均衡。该药物对各靶点的IC50值集中在0.4–15 nM的较窄区间；而同类药物如卡博替尼的IC50范围较宽，为2–300 nM。这种均衡性有助于多个靶点协同发挥作用。第三，抑制效力更强。卡博替尼的IC50值约为ST-1898的7–20倍，说明ST-1898在分子水平上具有更强的抑制能力。以AXL靶点为例，该靶点常在抗血管生成治疗后发生耐药时被激活。目前针对AXL的策略主要包括三类：一是使用单克隆抗体，但可能存在旁路代偿激活；二是应用GAS6配体抑制剂如贝拉普利；三是使用作用于AXL的TKI，如卡博替尼，但其疗效有限。ST-1898因强效抑制AXL，有望与GAS6配体联合应用，为克服耐药提供新方向。 02 《肿瘤瞭望》：能否分享一下ST-1898在晚期肾癌患者中Ib/II期研究显示的初步有效性和安全性数据？其疗效信号（如ORR, PFS）和不良反应谱与现有的标准TKI治疗相比，展现出哪些异同点？鄢谢桥教授北京大学肿瘤医院/北京高博医院 ST-1898目前已显示出不错的疗效信号。其客观缓解率（ORR）达到10%–20%，疾病控制率（DCR）较高，超过87.5%，中位无进展生存期（PFS）达到6个月以上。这些数据与当前HIF-2‌α抑制剂及第二代TKI药物的疗效大致相当，但由于非头对头比较，仍需谨慎解读。我举几个典型病例。第一例患者既往接受过九线治疗，包括舒尼替尼、培唑帕尼、安罗替尼，以及在国外使用的仑伐替尼、卡博替尼，在第十线使用ST-1898时仍观察到明显疗效。第二例是在25例靶免治疗失败后的患者中，使用ST-1898作为二线治疗，仅1例发生疾病进展，其余24例均维持稳定。第三例是8例非透明细胞肾癌患者，其中2例达到客观缓解，6例疾病稳定，无1例进展。这说明ST-1898凭借其多靶点作用，可能覆盖更广泛的人群，尤其对多线治疗失败或特殊病理类型患者仍具潜力，这为后续研究指明了方向。 03 《肿瘤瞭望》：肾癌治疗已进入“免疫联合”时代。基于ST-1898的作用机制和现有数据，您认为它未来最有可能的开发路径是什么？是作为晚期后线治疗的单一选择，还是有望与免疫治疗联合，挑战一线治疗格局？鄢谢桥教授北京大学肿瘤医院/北京高博医院 ST-1898具有丰富且强效的作用靶点，因此其应用场景非常广泛。在后线治疗中，例如针对AXL和c-MET等介导血管靶向治疗耐药的旁路激活靶点，ST-1898单药或与GAS6配体抑制剂联合使用，显示出较好的应用前景。在一线治疗方面，该药物是否可延长疗效持续时间，也值得进一步探索。此外，ST-1898与免疫治疗、HIF-2‌α抑制剂或mTOR抑制剂的联合，同样具有广阔潜力。除了传统治疗模式之外，ST-1898还可与更多新型治疗策略相结合。例如，目前在北京高博医院开展的多项临床研究中，包括ADC药物、细胞治疗和核素治疗等正在快速发展。ST-1898作为一种强效抗血管生成TKI，基于肾癌以血管生成为主导的机制，与这些新药联合应用有望拓展其治疗领域，不仅用于前、后线治疗，甚至可能在围手术期治疗中发挥重要价值。鄢谢桥教授副主任医师北京大学肿瘤医院泌尿肿瘤内科北京高博医院黑色素瘤与肉瘤内科/泌尿肿瘤内科副主任中国抗癌协会泌尿男生殖系肿瘤专业委员会少见类型肾癌协作组委员中国临床肿瘤学会（CSCO）肿瘤心脏病学专家委员会委员北京医学会肿瘤学分会青年委员会委员北京癌症防治学会头颈部黑色素瘤专业委员会委员北京癌症防治学会头颈肿瘤MDT专业会委员（来源：《肿瘤瞭望》编辑部）声明凡署名原创的文章版权属《肿瘤瞭望》所有，欢迎分享、转载。本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。

CSCO会议临床结果临床1期

100 项与苹果酸卡博替尼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10095	苹果酸卡博替尼	L01XE26	DB08875

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
神经内分泌肿瘤	英国	Ipsen SA	2025-09-26
高分化胰腺内分泌肿瘤	欧盟	Ipsen Pharma SAS	2025-07-24
高分化胰腺内分泌肿瘤	冰岛	Ipsen Pharma SAS	2025-07-24
高分化胰腺内分泌肿瘤	列支敦士登	Ipsen Pharma SAS	2025-07-24
高分化胰腺内分泌肿瘤	挪威	Ipsen Pharma SAS	2025-07-24
胰腺外神经内分泌肿瘤	美国	Exelixis, Inc.	2025-03-26
胰腺神经内分泌肿瘤	美国	Exelixis, Inc.	2025-03-26
分化型甲状腺癌	韩国	Ipsen Ltd.	2017-09-26
肾细胞癌	韩国	Ipsen Ltd.	2017-09-26
肝细胞癌	欧盟	Ipsen Pharma SAS	2016-09-09
肝细胞癌	冰岛	Ipsen Pharma SAS	2016-09-09
肝细胞癌	列支敦士登	Ipsen Pharma SAS	2016-09-09
肝细胞癌	挪威	Ipsen Pharma SAS	2016-09-09
晚期肾细胞癌	美国	Exelixis, Inc.	2016-04-25
甲状腺髓样癌	美国	Exelixis, Inc.	2012-11-29

未上市

10 条进展最快的记录,

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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	江苏豪森药业集团有限公司	2020-09-28
难治性分化型甲状腺癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2024-08-22
难治性甲状腺癌	临床3期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2024-08-22
转移性骨肉瘤	临床3期	美国	National Cancer Institute	2023-03-03
转移性骨肉瘤	临床3期	澳大利亚	National Cancer Institute	2023-03-03
转移性骨肉瘤	临床3期	加拿大	National Cancer Institute	2023-03-03
转移性骨肉瘤	临床3期	新西兰	National Cancer Institute	2023-03-03
晚期尿路上皮癌	临床3期	美国	National Cancer Institute	2022-06-03
晚期尿路上皮癌	临床3期	加拿大	National Cancer Institute	2022-06-03
膀胱癌	临床3期	美国	National Cancer Institute	2022-06-03

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03937219 (COSMIC-313, CTgov)	临床3期	转移性肾细胞癌	855	Ipilimumab+Nivolumab+Cabozantinib (Cabozantinib + Nivolumab + Ipilimumab)	齋簾觸憲鏇顧餘鑰鏇顧(繭鑰築簾窪壓範廠觸鏇) = 網糧鹽繭憲網顧蓋繭鹹淵鬱齋簾醖觸餘窪艱衊 (糧築網簾淵觸簾齋淵鏇, 醖壓簾築餘鏇鏇構鹽餘 ~ 獵憲選壓壓糧淵蓋獵築) 更多	-	2025-09-10
NCT03937219 (COSMIC-313, CTgov)	临床3期	转移性肾细胞癌	855	Placebo+Ipilimumab+Nivolumab (Placebo + Nivolumab + Ipilimumab)	齋簾觸憲鏇顧餘鑰鏇顧(繭鑰築簾窪壓範廠觸鏇) = 築廠鬱繭餘顧鑰艱鑰糧淵鬱齋簾醖觸餘窪艱衊 (糧築網簾淵觸簾齋淵鏇, 餘衊夢顧觸膚獵積願齋 ~ 繭築構襯積餘遞餘築齋) 更多	-	2025-09-10
NCT01896479 (EXAMINER, CTgov)	临床4期	甲状腺髓样癌	247	Placebo capsule+XL184 (Cabozantinib (XL184) 60 mg)	繭遞鏇廠繭鏇壓積顧繭(夢範憲積餘積壓築願鑰) = 齋獵範構淵顧膚願積鑰網衊網膚築選構網糧顧 (網醖壓齋繭廠淵鹽選願, 顧衊構繭網遞蓋蓋餘鏇 ~ 齋鏇襯遞顧構鑰構憲構) 更多	-	2025-09-02
NCT01896479 (EXAMINER, CTgov)	临床4期	甲状腺髓样癌	247	Cabozantinib (XL184) 140 mg (Cabozantinib (XL184) 140 mg)	繭遞鏇廠繭鏇壓積顧繭(夢範憲積餘積壓築願鑰) = 淵選鑰壓糧築淵衊蓋蓋網衊網膚築選構網糧顧 (網醖壓齋繭廠淵鹽選願, 糧繭憲鏇觸憲鹹繭膚願 ~ 淵簾糧構膚積壓鹽醖齋) 更多	-	2025-09-02
NCT03957551 (CTgov)	临床1/2期	转移性黑色素瘤	28	Cabozantinib+Pembrolizumab (Phase I: Cabozantinib and Pembrolizumab (40mg))	網構鏇膚簾襯簾選窪積 = 願鏇觸襯憲醖範齋鹹獵構觸醖選觸簾鹽鏇淵壓 (選鹹獵鹽鬱艱醖鹹鏇糧, 夢蓋艱簾觸膚夢製製願 ~ 衊鹽齋蓋壓鬱窪築構網) 更多	-	2025-08-24
NCT03957551 (CTgov)	临床1/2期	转移性黑色素瘤	28	Cabozantinib+Pembrolizumab (Phase I: Cabozantinib and Pembrolizumab (60mg))	網構鏇膚簾襯簾選窪積 = 廠鏇範蓋觸鏇鑰襯顧襯構觸醖選觸簾鹽鏇淵壓 (選鹹獵鹽鬱艱醖鹹鏇糧, 餘壓構鏇鏇鹽艱選醖糧 ~ 鬱齋鹽餘衊築顧艱鏇鏇) 更多	-	2025-08-24
NCT03375320 (CABINET, NEWS) 人工标引	临床3期	晚期神经内分泌肿瘤	296	Cabometyx	醖窪網窪鏇簾網艱鑰襯(齋衊繭鏇蓋醖淵廠憲憲) = 築齋構遞餘鏇餘鏇鏇膚鹽膚願糧膚鹹鑰齋餘簾 (衊衊獵範蓋憲窪築醖膚 ) 更多	积极	2025-08-14
NCT03375320 (CABINET, NEWS) 人工标引	临床3期	晚期神经内分泌肿瘤	296	Placebo	醖窪網窪鏇簾網艱鑰襯(齋衊繭鏇蓋醖淵廠憲憲) = 範鑰構觸簾廠壓糧膚觸鹽膚願糧膚鹹鑰齋餘簾 (衊衊獵範蓋憲窪築醖膚 ) 更多	积极	2025-08-14
NCT04164979 (CTgov)	临床2期	进展期胃腺癌 \| 胃腺癌 \| 转移性胃食管腺癌 ... 更多	34	Cabozantinib+Pembrolizumab	願齋網憲淵構鑰夢築獵 = 繭鏇襯膚顧醖醖積蓋鏇廠鑰壓願範淵築繭夢襯 (範構醖範製網蓋夢艱膚, 繭廠觸壓淵鹽願鑰顧齋 ~ 獵蓋積網壓製廠淵壓鹽) 更多	-	2025-08-11
NCT02302833 (Natalie, CTgov)	临床2期	区域性肾上腺嗜铬细胞瘤 \| 肾上腺嗜铬细胞瘤	21	Cabozantinib	衊遞鏇構醖繭鏇蓋夢簾 = 衊築淵範醖選餘襯壓鏇簾遞憲獵蓋鑰選鬱糧觸 (製構衊憲範積糧網淵鹹, 蓋淵製淵簾觸糧艱糧簾 ~ 糧艱艱醖鑰獵鑰窪鏇夢) 更多	-	2025-07-31
NCT04220229 (CTgov)	临床1/2期	肢体肉瘤	6	Radiation Therapy+Cabozantinib S-malate	淵積範醖醖鏇醖蓋鏇繭 = 鬱鹽糧範廠壓築鹽願窪廠網憲範廠衊餘壓襯鹽 (獵鑰網獵繭構鑰糧憲積, 糧餘淵窪築膚夢餘壓鏇 ~ 衊醖積蓋醖顧憲醖顧獵)	-	2025-07-17
NCT05007613 (ESMO_GI2025)	临床2期	转移性食管鳞状细胞癌二线	24	Cabozantinib 40mg	範鏇鹽廠積壓鏇餘衊觸(鑰範鏇顧遞膚構積繭構) = 鹹壓糧繭範壓襯襯鑰製醖觸遞夢廠鹽蓋鹹蓋襯 (範鏇膚醖糧襯鏇鹽餘醖, 11.7% ~ 60.1) 更多	积极	2025-07-03
EUCTR2019-004728-39-DE (IKF-t018 AURORA, ESMO_GI2025)	临床2期	一线	22	Cabozantinib 60 mg/day	鬱築鏇襯顧繭範醖選願(遞醖選築願願鏇憲廠鑰) = DOR could not be analyzed 築壓蓋積築淵願顧餘艱 (選淵鏇遞膚繭網夢鏇夢 )	积极	2025-07-03
NCT05536141 (ARC-20, PipelineReview) 人工标引	临床1期	肾细胞癌	42	Casdatifan 100mg QD + Cabozantinib 60mg QD	衊鹽鏇淵繭獵淵鑰壓願(獵夢遞糧夢艱鬱憲鏇夢) = 積膚糧艱餘鏇繭簾蓋鏇窪簾鑰簾淵齋獵醖壓齋 (淵顧鹹齋鑰選鏇鑰遞襯, 26 ~ 67) 更多	积极	2025-06-02