A Multi-center Phase II Study of Combining Cabozantinib and Atezolizumab as the 1st Line Therapy for PD-L1 Negative Advanced/Metastatic NSCLC (Cabatezo-1)

NSCLC patients with low expression level of PD-L1, esp. those with its level less than 1%, do not derive much benefit from anti-PD-1/L1 therapy (e.g. atezoilzumab). In this study, investigators hypothesize that the combination of cabozantinib (a multi-kinase inhibitor) and atezolizumab will result in better therapeutic value.

开始日期2024-12-01

申办/合作机构

University of Kansas

[+2]

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2024-10-01

申办/合作机构

The University of Alabama at Birmingham

[+2]

NCT06475989 / Not yet recruiting临床3期

A Randomized Phase III Study of BRAF-Targeted Therapy vs Cabozantinib in RAI-Refractory Differentiated Thyroid Cancer With BRAF V600Em

This phase III trial compares the effect of cabozantinib versus combination dabrafenib and trametinib for the treatment of patients with differentiated thyroid cancer that does not respond to treatment (refractory) and which expresses a BRAF V600E mutation. Cabozantinib is in a class of medications called receptor tyrosine kinase inhibitors. It binds to and blocks the action of several enzymes which are often over-expressed in a variety of tumor cell types. This may help stop or slow the growth of tumor cells and blood vessels the tumor needs to survive. Dabrafenib is an enzyme inhibitor that binds to and inhibits the activity of a protein called B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. Trametinib is also an enzyme inhibitor. It binds to and inhibits the activity of proteins called MEK 1 and 2, which play a key role in activating pathways that regulate cell growth. This may inhibit the growth of tumor cells mediated by these pathways. The usual approach for patients with thyroid cancer is targeted therapy with dabrafenib and trametinib. This trial may help researchers decide which treatment option (cabozantinib alone or dabrafenib in combination with trametinib) is safer and/or more effective in treating patients with refractory BRAF V600E-mutated differentiated thyroid cancer.

开始日期2024-09-13

申办/合作机构

ECOG-ACRIN Medical Research Foundation, Inc.

[+1]

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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1,521

项与苹果酸卡博替尼相关的文献（医药）

2024-06-01·Artificial intelligence chemistry

Machine learning models to predict ligand binding affinity for the orexin 1 receptor

Article

作者: O'Connor, Shayna L ; James, Morgan H ; Welsh, William J ; Zhang, Vanessa Y

The orexin 1 receptor (OX1R) is a G-protein coupled receptor that regulates a variety of physiological processes through interactions with the neuropeptides orexin A and B. Selective OX1R antagonists exhibit therapeutic effects in preclinical models of several behavioral disorders, including drug seeking and overeating. However, currently there are no selective OX1R antagonists approved for clinical use, fueling demand for novel compounds that act at this target. In this study, we meticulously curated a dataset comprising over 1300 OX1R ligands using a stringent filter and criteria cascade. Subsequently, we developed highly predictive quantitative structure-activity relationship (QSAR) models employing the optimized hyper-parameters for the random forest machine learning algorithm and twelve 2D molecular descriptors selected by recursive feature elimination with a 5-fold cross-validation process. The predictive capacity of the QSAR model was further assessed using an external test set and enrichment study, confirming its high predictivity. The practical applicability of our final QSAR model was demonstrated through virtual screening of the DrugBank database. This revealed two FDA-approved drugs (isavuconazole and cabozantinib) as potential OX1R ligands, confirmed by radiolabeled OX1R binding assays. To our best knowledge, this study represents the first report of highly predictive QSAR models on a large comprehensive dataset of diverse OX1R ligands, which should prove useful for the discovery and design of new compounds targeting this receptor.

2024-05-01·Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer

Comprehensive Review of ROS1 Tyrosine Kinase Inhibitors-Classified by Structural Designs and Mutation Spectrum (Solvent Front Mutation [G2032R] and Central β-Sheet 6 [Cβ6] Mutation [L2086F])

Review

作者: Nagasaka, Misako ; Zhang, Shannon S ; Ou, Sai-Hong Ignatius ; Hagopian, Garo G

Despite ROS1 fusion-positive NSCLC accounting for approximately 1% to 2% of NSCLC, there is a long list of ROS1 tyrosine kinase inhibitors (TKIs) being developed in addition to three approved ROS1 TKIs, crizotinib, entrectinib and repotrectinib. Here, we categorized ROS1 TKIs by their structures (cyclic versus noncyclic) and inhibitory abilities (active against solvent front mutation G2032R or central β-sheet #6 [Cβ6] mutation L2086F) and summarized their reported clinical activity in order to provide a dashboard on how to use these ROS1 TKIs in various clinical situations. In addition, the less known Cβ6 mutation ROS1 L2086F confer resistances to next-generation ROS1 TKIs (repotrectinib, taletrectinib, and potentially NVL-520) that can be overcome by cabozantinib as documented in published patient reports and potentially by certain L-shaped type I ROS1 TKIs including ceritinib and gilteritinib, which is approved as a FLT3 inhibitor for relapsed refractory FLT3+ acute myeloid leukemia but have published preclinical activites against ROS1 (and ALK). Future clinical trials should investigate cabozantinib and gilteritinib to repurpose them as ROS1 TKIs that can target ROS1 L2086F Cβ6 mutation.

2024-04-01·Clinical genitourinary cancer

Real-World Results of Cabozantinib Given as Alternative Schedule in Metastatic Renal Cell Carcinoma

Article

作者: Bruchbacher, Andreas ; Franke, Johannes ; Alimohammadi, Arman ; Schmidinger, Manuela ; Laukhtina, Ekaterina ; Fajkovic, Harun

BACKGROUND:

The multikinase-inhibitor Cabozantinib is a widely used treatment strategy in metastatic renal cell carcinoma (mRCC), either in combination with the programmed cell death protein-1 (PD-1) inhibitor nivolumab or as monotherapy. Cabozantinib is given continuously at a dose of 60 mg once daily when used as a single agent and at 40 mg when combined with nivolumab. Treatment-related adverse events (TRAE's) were shown to occur frequently.

OBJECTIVE:

We aimed to assess the safety and efficacy of cabozantinib in patients with mRCC. Patients were treated in various lines. Furthermore, we analyzed the impact of an alternative treatment schedule in patients not able to maintain continuous dosing.

PATIENTS:

This is a single center retrospective study from the Medical University of Vienna.

OUTCOME MEASUREMENTS AND STATISTICAL ANALYSIS:

Overall response rates (ORR), progression free survival (PFS) and overall survival (OS) were evaluated for the entire cohort, by treatment line and by treatment schedule.

RESULTS:

Between January 2014 until April 2021, 71 patients received cabozantinib. Sixty-seven patients were eligible for full evaluation. By IMDC criteria, 32.4%, 59.2%, and 8.5% were classified as favorable, intermediate and poor risk respectively. Cabozantinib was offered as a 2nd-line or 3rd-line treatment in 38.0% and 32.4% of patients, respectively. An alternative treatment schedule was offered in 39.1% of patients. Objective responses were found in 43.3% (CR 6%) of patients and the median PFS was 10.8 months (95% CI: 5.5-16.2). When compared to continuous dosing, an alternative treatment schedule was associated with longer PFS (12.2 months (95% CI: 0-25.5) vs. 6.1 months (95% CI: 0.37-11.8) (P = .014, HR 0.46 (95% CI: 0.24-0.86), respectively) and a lower frequency and severity of TRAE's.

CONCLUSIONS:

Safety and efficacy of cabozantinib in real world is comparable to what has been observed in the pivotal trials, irrespective of the treatment line. An alternative schedule may further improve efficacy and safety.

452

项与苹果酸卡博替尼相关的新闻（医药）

2024-09-18

·GlobeNewswire-Health Care

Ipsen provides update on CONTACT-02 Phase III trial in metastatic castration-resistant prostate cancer following final overall survival analysis

Trial investigating Cabometyx® (cabozantinib) in combination with atezolizumab demonstrated a positive trend towards improvement for one of the primary endpoints of overall survival, but did not meet statistical significance Ipsen will not pursue regulatory submissions for the combination regimen in countries where we have commercialization rights (outside of the US and Japan) We remain confident in the proven profile of Cabometyx as a monotherapy and in combination with immunotherapy, across approved and potential future indications 15 September 2024 - Ipsen (Euronext: IPN; ADR: IPSEY) announced today detailed final overall survival (OS) data from the Phase III CONTACT-02 trial investigating the combination of Cabometyx® (cabozantinib) and atezolizumab in metastatic castration-resistant prostate cancer (mCRPC). The trial investigated the combination regimen versus a second novel hormonal therapy (NHT) in men previously treated with one NHT and measurable soft-tissue disease. At a median follow-up of 24.0 months, these data demonstrated a numerical but not statistically significant improvement in OS for the combination versus a second NHT (hazard ratio: 0.89; 95% confidence interval: 0.72-1.10; P=0.296). As previously announced, the trial met the other primary endpoint of progression-free survival (PFS), demonstrating a statistically significant benefit in PFS.1 Safety for the combination appeared to be consistent with the known safety profiles of the individual medicines, and no new safety signals were identified. Based on the results of the final OS analysis and anticipated challenging regulatory environment in the countries in which Ipsen has commercialization rights (outside the US and Japan), Ipsen will not pursue regulatory submissions for this combination regimen in mCRPC. We remain confident, in the proven profile of Cabometyx as a monotherapy and in combination with immunotherapy across approved indications, as well as its ongoing future potential. Ipsen wishes to thank the patients, their families and healthcare teams for their participation in this clinical trial. Cabometyx (cabozantinib) is a small molecule that inhibits multiple receptor tyrosine kinases, including VEGFRs, MET, RET and the TAM family (TYRO3, MER, AXL).2 These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis (the growth of new blood vessels that tumors need to grow), drug resistance, modulation of immune activities and maintenance of the tumor microenvironment.2,3,4,5 Exelixis granted Ipsen exclusive rights for the commercialization and further clinical development of Cabometyx outside of the U.S. and Japan. Exelixis granted exclusive rights to Takeda Pharmaceutical Company Limited (Takeda) for the commercialization and further clinical development of Cabometyx for all future indications in Japan. Exelixis holds the exclusive rights to develop and commercialize Cabometyx in the U.S. In over 65 countries outside of the United States and Japan, including in the European Union, Cabometyx is currently indicated as a:3 Monotherapy for advanced renal cell carcinoma (aRCC). as first-line treatment of adults with intermediate- or poor-risk disease. in adults following prior VEGFR-targeted therapy. A combination with nivolumab for the first-line treatment of aRCC in adults. Monotherapy for the treatment of adults living with locally advanced or metastatic differentiated thyroid carcinoma, refractory or not eligible to radioactive iodine who have progressed during or after prior systemic therapy. Monotherapy for the treatment of hepatocellular carcinoma in adults who have previously been treated with sorafenib. The detailed recommendations for the use of Cabometyx are described in the Summary of Product Characteristics (EU SmPC). Prostate cancer is the second most common cancer in men and the fourth most common cancer overall globally.6 In 2020, there were more than 1.4 million new cases of prostate cancer and about 375,300 deaths worldwide.6 Prostate cancer is considered mCRPC when it has spread beyond the prostate and does not respond to androgen-suppression therapies, a common treatment for prostate cancer.7 Men diagnosed with mCRPC often have a poor prognosis, with an estimated survival of 1-2 years.8 CONTACT-02 is a global, multicenter, randomized, Phase III, open-label study that enrolled 575 patients who were randomized 1:1 to the experimental arm of Cabometyx in combination with atezolizumab and the control arm of a second NHT (either abiraterone and prednisone or enzalutamide). The study included patients with mCRPC who have measurable extra-pelvic soft tissue metastasis and who have progressed on one prior NHT. The two primary endpoints of the trial are progression-free survival (PFS) and OS. The PFS analysis was conducted in the first 400 randomized patients (PFS in the intent-to-treat [ITT] population) and assessed by a blinded independent radiology committee (BIRC) per RECIST 1.1. The OS analysis was conducted in the ITT population (n=507). The secondary endpoint is objective response rate (ORR) per BIRC. The trial is sponsored by Exelixis and co-funded by Ipsen, Roche and Takeda. Takeda is conducting the trial in Japan. More information about CONTACT-02 is available at ClinicalTrials.gov. We are a global biopharmaceutical company with a focus on bringing transformative medicines to patients in three therapeutic areas: Oncology, Rare Disease and Neuroscience. Our pipeline is fueled by external innovation and supported by nearly 100 years of development experience and global hubs in the U.S., France and the U.K. Our teams in more than 40 countries and our partnerships around the world enable us to bring medicines to patients in more than 80 countries. Ipsen is listed in Paris (Euronext: IPN) and in the U.S. through a Sponsored Level I American Depositary Receipt program (ADR: IPSEY). For more information, visit ipsen.com. References 1 Agarwal et al. Cabozantinib Plus Atezolizumab vs Second Novel Hormonal Therapy in Patients With Metastatic Castration-Resistant Prostate Cancer (mCRPC): Primary Analyses From the Phase 3 CONTACT-02 Study. As presented at the ASCO GU congress 2024, San Francisco, USA 2 El-Khoueiry A. et al., Cabozantinib: An evolving therapy for hepatocellular carcinoma. Cancer Treatment Reviews. 2021 Jul;98:102221. DOI: 10.1016/j.ctrv.2021.102221. 3 European Medicines Agency. Cabometyx® (cabozantinib) EU Summary of Product Characteristics. Available from: https://www.ema.europa.eu/en/documents/product-information/cabometyx-epar-product-information_en.pdf. Last accessed: September 2024 4 Yakes M. et al., Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther. 2011;10:2298–2308. DOI: 10.1158/1535-7163.MCT-11-0264 5 Hsu et al., AXL and MET in Hepatocellular Carcinoma: A Systematic Literature Review. Liver Cancer 2021 DOI: 10.1159/000520501 6 Prostate cancer statistics. World Cancer Research Fund International. Available at: https://www.wcrf.org/cancer-trends/prostate-cancer-statistics/. Accessed August 2024 7 Prostate Cancer: Types of Treatment. Cancer.Net. Available at: https://www.cancer.net/cancer-types/prostate-cancer/types-treatment. Accessed September 2024 8 Moreira, D. M., et al. Predicting Time From Metastasis to Overall Survival in Castration-Resistant Prostate Cancer: Results From SEARCH. Clin Genitourin Cancer. 2017; 15: 60–66.e2 The content above comes from the network. if any infringement, please contact us to modify.

临床结果引进/卖出免疫疗法

2024-09-17

·药明康德

PFS翻3倍！小分子抗癌疗法3期积极结果登《新英格兰医学杂志》

▎药明康德内容团队编辑 Exelixis今天公布了CABINET研究的更新数据，这是一项评估Cabometyx（cabozantinib）治疗神经内分泌肿瘤（NET）患者的3期关键性临床试验：其中一组为晚期胰腺神经内分泌肿瘤（pNET）患者，另一组为晚期胰腺外神经内分泌肿瘤（epNET）患者。这些数据今天在2024年欧洲肿瘤内科学会（ESMO）大会上发布，并同时在《新英格兰医学杂志》上发表。最新结果显示出cabozantinib在主要终点无进展生存期（PFS）方面的持续改善。在pNET队列（n=95）中，中位随访时间为13.8个月时，cabozantinib组的中位PFS为13.8个月，而安慰剂组为4.4个月。Cabozantinib将疾病进展或死亡风险降低77%（HR=0.23，95%　CI：0.12-0.42；p<0.0001）。在epNET队列（n=203）中，中位随访时间为10.2个月时，HR=0.38（95% CI：0.25-0.59；p<0.0001），两组的中位PFS分别为8.4个月和3.9个月。额外的分析表明，在pNET队列中，盲法独立中央审评（BICR）评估的客观缓解率（ORR）为19%，而安慰剂组为0%。在epNET队列中，BICR评估的ORR为5%，而安慰剂组为0%。Cabozantinib与安慰剂相比的总生存期（OS）中期结果相似；pNET队列的总生存期HR为0.95（95% CI：0.45-2.00），epNET队列为0.86（95% CI：0.56-1.31）。每个队列中观察到的cabozantinib的安全性特征与其已知的安全性特征一致，未发现新的安全信号。大多数接受cabozantinib治疗的患者需要进行剂量调整或减少以管理不良事件。新闻稿指出，这些结果是Exelixis提交的cabozantinib用于治疗晚期NET成人患者的补充新药申请（sNDA）的依据。FDA已于8月受理该sNDA，并预计在2025年4月3日之前完成审评。 Cabozantinib可抑制多种酪氨酸激酶，包含MET、VEGFR-1、2、3、AXL、RET、ROS1、KIT等，这些受体酪氨酸激酶与肿瘤的生成、转移、血管增生与药物抗性有关。它在美国已获批准治疗晚期肾细胞癌、与PD-1抗体nivolumab联用作为晚期肾细胞癌一线疗法，以及治疗曾接受过sorafenib疗法的肝细胞癌（HCC）患者等多项适应症。 ▲欲了解更多前沿技术在生物医药产业中的应用，请长按扫描上方二维码，即可访问“药明直播间”，观看相关话题的直播讨论与精彩回放参考资料： [1] Exelixis Announces Final Results from Phase 3 Pivotal CABINET Study Evaluating Cabozantinib in Advanced Neuroendocrine Tumors Presented at ESMO 2024 and Published in New England Journal of Medicine. Retrieved September 16, 2024, from https://www.businesswire.com/news/home/20240913607414/en 免责声明：药明康德内容团队专注介绍全球生物医药健康研究进展。本文仅作信息交流之目的，文中观点不代表药明康德立场，亦不代表药明康德支持或反对文中观点。本文也不是治疗方案推荐。如需获得治疗方案指导，请前往正规医院就诊。版权说明：本文来自药明康德内容团队，欢迎个人转发至朋友圈，谢绝媒体或机构未经授权以任何形式转载至其他平台。转载授权请在「药明康德」微信公众号回复“转载”，获取转载须知。分享，点赞，在看，聚焦全球生物医药健康创新

临床3期临床结果临床成功

2024-09-16

·FiercePharma

ESMO: Despite survival miss, Exelixis presses on with FDA prostate cancer bid as Ipsen scraps EU plan

Cabometyx and Tecentriq showed a numerical improvement in extending the lives of patients with metastatic castration-resistant prostate cancer. The same set of clinical data on Cabometyx and Tecentriq in prostate cancer has led to two distinct regulatory plans between Exelixis and its partner Ipsen.Exelixis plans to file Cabometyx’s combination with Roche’s Tecentriq with the FDA for an approval in metastatic castration-resistant prostate cancer (mCRPC) despite the combo failing to show a statistically significant life extension benefit in a phase 3 trial.Compared with a change of novel hormonal therapy, Cabometyx and Tecentriq showed a numerical improvement in overall survival (OS) with a death risk reduction of 11%, according to the final analysis of the CONTACT-02 trial presented at the European Society for Medical Oncology (ESMO) 2024 meeting. As Exelixis announced in August alongside its second-quarter financial results, the survival number didn’t reach statistical significance.Patients in the experimental arm lived a median 14.8 months, versus about 15 months in the control group. OS is one of the dual primary endpoints of CONTACT-02.CONTACT-02 is still considered a positive trial because it has previously met its other dual primary endpoint, progression-free survival (PFS). PFS is a clinically relevant and approvable endpoint in prostate cancer, Exelixis’ chief medical officer, Amy Peterson, M.D., told Fierce Pharma via email.As investigators reported in January, the Cabometyx-Tecentriq combo reduced the risk of progress or death by 35% versus a second novel hormonal therapy. At that time, the numerical survival advantage for the combo was wider at 21%, with a median OS of 16.7 months, compared with 14.6 months for control. Exelixis had then postponed its plan for an FDA filing as the agency requested a more mature OS analysis. The mCRPC treatment landscape is evolving. Available options now include androgen receptor inhibitors, chemotherapy, PARP inhibitors and immune checkpoint inhibitors and radioligand therapy.“As a result, it may be challenging to demonstrate an effect on OS, as patients switch to new systemic therapies upon radiographic progression,” Peterson said.Back in 2014, Cabometyx as a single agent failed to significantly improve OS in patients with heavily pretreated mCRPC in the phase 3 COMET-1 trial despite a notable PFS improvement in an exploratory analysis. That phase 3 flop triggered a 70% reduction in Exelixis’ workforce at the time .In CONTACT-02, a nearly equal number of patients received subsequent therapies, with the majority receiving follow-on chemotherapy, Neeraj Agarwal, M.D., from the University of Utah Health, said during his presentation of the data at ESMO 2024.Agarwal noted that CONTACT-02 appears to have enrolled a population that has poor prognosis and high-risk factors, including about a quarter of patients with liver metastases in each arm. Rana McKay, M.D., from the University of California, San Diego, who was invited by ESMO to discuss the CONTACT-02 data during a presentation, also noted that the survival lengths of the trial participants were lower than expected, highlighting a poor prognostic population.The Cabometyx-Tecentriq pairing worked well in some of those higher-risk patients. In those with liver metastases, the combo reduced the risk of death by 32%. In patients with bone metastases, who represent about three-quarters of the trial population, the doublet lowered the risk of death by 21%.However, in patients without bone metastases, those who took Cabometyx and Tecentriq somehow lived shorter than their peers in the comparator arm did. Exelixis plans to submit an application for the regimen to the FDA this year, Peterson said. But she said it’s too early to comment on specific indications or whether a broad label is appropriate.In contrast, Ipsen, which holds Cabometyx’s rights outside of the U.S. and Japan, said it will not pursue approvals for this combination regimen in mCRPC in its territories, including Europe. The French pharma cited an “anticipated challenging regulatory environment” to explain its decision.McKay, in her presentation, highlighted that liver metastases are increasingly common in advanced prostate cancer. Those patients represent an unmet medical need as they’re associated with worse outcomes but have limited treatment options.“Our community in prostate cancer has really voted with its feet here,” McKay said. “There had been really limited settings where rPFS alone has resulted in a regulatory drug approval in the mCRPC setting. It’s really the totality of the data of rPFS, OS, safety, toxicity and quality of life.”In terms of toxicity, treatment-related adverse events at grades 3 or 4 occurred in 40% of the combo arm in CONTACT-02, versus 8% in the control group. The rate of treatment-related adverse events leading to discontinuation of any study component was 14% and 2%, respectively, in the two arms. No death was chalked up to treatment-related side effects. If the CONTACT-02 regimen wins an FDA approval, most of its usage are expected to be among those with liver metastasis, William Blair analysts said in a Tuesday note. Based on past studies, the team figured that the prevalence of liver metastasis in chemotherapy-naïve mCRPC is roughly 5% to 6%, “representing a small commercial opportunity for Exelixis.”Also at ESMO 2024, investigators provided an updated readout from the phase 3 CABINET trial for Cabometyx in advanced neuroendocrine tumors. At the final analysis, Cabometyx reduced the risk of progression or death by a whopping 77% compared with placebo in heavily pretreated advanced pancreatic neuroendocrine tumors (pNET). The reduction was 62% in advanced extra-pancreatic neuroendocrine tumors (epNET). Both analyses came from central blinded review. The trial had previously stopped early and reported data in 2023 because of strong efficacy.On OS, Cabometyx again showed numerical improvements that did not meet statistical significance; the drug reduced the risk of death by 5% in pNET and by 14% in epNET. Given that some patients in the control group went on to receive Cabometyx upon disease progression, the William Blair team argued that the lack of an OS showing will not “preclude significant clinical utility of Cabometyx.”The CABINET trial enrolled a heavily pretreated population, including patients who had tried Novartis’ radioligand therapy Lutathera. William Blair put the total addressable market for Cabometyx in late-line NETs at $900 million in the U.S.Editor's Note: The story was updated at 8 a.m. ET on Sept. 17 with additional comments from William Blair and updated data from the CABINET trial.

临床结果临床3期财报

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,

后查看更多信息

适应症	国家/地区	公司	日期
甲状腺癌	美国	Exelixis, Inc.	2021-09-17
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
胰腺神经内分泌肿瘤	申请上市	美国	Exelixis, Inc.	2024-08-06
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	-	National Cancer Institute	2024-09-13
转移性骨肉瘤	临床3期	-	National Cancer Institute	2023-01-13
不能切除的骨肉瘤	临床3期	-	National Cancer Institute	2023-01-13
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
膀胱癌	临床3期	加拿大	National Cancer Institute	2022-06-03
转移性尿道尿路上皮癌	临床3期	美国	National Cancer Institute	2022-06-03

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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


NCT05200143 (CTgov)	临床2期	难治性黑色素瘤 \| 皮肤黑色素瘤	4	Ipilimumab+Nivolumab+Cabozantinib	艱構繭衊鹹繭淵齋築獵(艱夢壓鬱範醖襯糧膚齋) = 積選衊憲顧觸繭製襯鹹選簾鬱觸鬱襯選淵積願 (糧廠獵製獵鹽壓繭窪觸, 蓋餘淵窪齋糧鬱獵廠窪 ~ 積窪壓製膚獵選繭構遞) 更多	-	2024-09-19
NCT03824691 (ARCADIA, ESMO2024) 人工标引	临床2期	尿路上皮癌	61	Cabozantinib+durvalumab	艱壓積糧憲觸網蓋糧鬱(齋繭淵鬱範鹹艱鏇糧憲) = 夢蓋淵簾齋醖範淵繭壓願鹹築積襯簾顧齋蓋憲 (齋願築構網觸艱積糧憲, 7.1 ~ 25.5) 更多	积极	2024-09-15
NCT03824691 (ARCADIA, ESMO2024) 人工标引	临床2期	尿路上皮癌	61	Cabozantinib+durvalumab	鹽遞淵鏇鹹築壓鹹齋積(繭襯醖夢鬱淵選糧淵襯) = 廠觸壓構積鬱壓觸獵構夢衊顧壓蓋積積醖鏇夢 (夢窪獵醖繭製遞餘積餘, 5.1 ~ NR) 更多	积极	2024-09-15
NCT03945773 (CaboPoint, ESMO2024)	临床2期	晚期肾细胞癌二线	127	Cabozantinib 60 mg/day after 1L nivolumab + ipilimumab	網簾衊齋餘選憲構艱醖(簾繭選憲齋鬱獵餘醖襯) = 糧壓壓構壓醖範窪艱網鑰鏇襯夢艱遞窪餘壓窪 (餘鏇製構醖網鹽鹹窪觸, 29.6 ~ 52.1) 更多	积极	2024-09-15
NCT03945773 (CaboPoint, ESMO2024)	临床2期	晚期肾细胞癌二线	127	Cabozantinib 60 mg/day after 1L CPI + VEGF-targeted therapy	網簾衊齋餘選憲構艱醖(簾繭選憲齋鬱獵餘醖襯) = 願獵廠遞製鬱構齋鏇襯鑰鏇襯夢艱遞窪餘壓窪 (餘鏇製構醖網鹽鹹窪觸, 14.6 ~ 43.9) 更多	积极	2024-09-15
NCT04413123 (phase II study of cabozantinib (Cabo) with nivolumab (Nivo) and ipilimumab (Ipi) in advanced renal cell carcinoma with divergent histologies (RCCdh), ESMO2024)	临床2期	晚期肾细胞癌	39	Cabo/Nivo/Ipi	餘壓餘蓋獵鬱憲觸衊廠(顧鬱鑰糧積簾糧積積窪) = 糧襯餘築鹽醖鑰網醖觸鏇範築淵蓋選鑰觸願簾 (艱顧觸鹹選醖憲積鹹觸, 12% ~ 31) 更多	积极	2024-09-15
ESMO2024	N/A	胰岛细胞癌	-	Cabozantinib	鹽遞獵膚醖鬱鹽鹽觸繭(鑰觸網糧淵艱衊壓繭遞) = During therapy, a total of 26 SAEs were observed including 22 SAE grade 3, 1 SAE grade 4, and 3 SAE grade 5, with SAEs including ileus, acute pain, cholangiosepsis, intestinal perforation, or stroke 願艱製壓醖襯觸艱遞觸 (廠願糧餘鬱願鬱壓蓋遞 )	-	2024-09-13
NCT04022343 (CTgov)	临床2期	局部晚期透明细胞肾细胞癌 \| 局部晚期恶性肿瘤	22	Cabozantinib	鹹繭窪蓋糧壓觸鑰鑰壓(蓋鏇夢淵廠醖築淵積繭) = 鑰襯糧衊窪鏇襯觸構壓窪壓膚鬱網淵襯獵糧積 (襯艱積簾遞選衊遞餘淵, 遞膚壓糧觸蓋鹹積選憲 ~ 範壓淵憲觸鏇願選鹽膚) 更多	-	2024-08-13
NCT03914300 (Pubmed \| J Clin Endocrinol Metab) 人工标引	临床2期	分化型甲状腺癌 RAI-refractory	11	Cabozantinib in combination with nivolumab and ipilimumab	餘夢艱壓廠遞鬱範窪窪(獵鹽築網齋艱蓋鏇遞夢) = 鏇齋積繭廠觸構鬱範窪觸獵積醖簾淵夢繭選鬱 (蓋鏇積觸艱艱顧簾艱廠 ) 更多	不佳	2024-08-12
NCT04022343 (Pubmed \| Res Sq) 人工标引	临床2期	局部晚期透明细胞肾细胞癌新辅助 VEGF \| c-MET \| Gas6 ... 更多	17	Cabozantinib	醖獵繭遞鏇顧糧選壓願(繭願構襯網觸鹹餘鬱餘) = We identified that plasma cell-free DNA (cfDNA), VEGF, c-MET, Gas6, and AXL were significantly increased while VEGFR2 decreased during cabozantinib treatments. 齋獵觸範鏇鏇網壓糧齋 (製獵膚顧遞觸艱遞夢鹽 ) 更多	积极	2024-08-08
NCT04497038 (CTgov)	临床1/2期	纤维化 \| 晚期肝细胞癌	3	Cabozantinib	觸築鹹艱網構選襯鹽襯(製選餘網製鏇艱壓壓齋) = 衊製顧選壓壓範遞窪襯膚獵蓋選壓艱醖衊蓋遞 (淵窪遞積齋鏇壓構範廠, 構選齋鏇繭膚網簾蓋蓋 ~ 築鬱壓鬱網艱鏇網艱衊) 更多	-	2024-08-06