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2025-01-01

申办/合作机构

The University of Alabama at Birmingham

[+2]

NCT05859217

/ Not yet recruiting临床2期IIT

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]

NCT06341712

/ Recruiting临床2期

A Phase II, Randomized, Open-label Study to Assess the Efficacy, Safety, and Pharmacokinetics (PK) of Maintenance Cabozantinib (XL184) Plus Best Supportive Care (BSC) Versus BSC in Children, Adolescents and Young Adults (AYA) With Unresectable Residual Osteosarcoma Either at Diagnosis or at First Relapse After Standard Treatment

The participants of this study will be children, adolescents, and young adults with residual osteosarcoma, which cannot be removed completely through surgery.
Participants will have achieved a partial response or stable disease at the end of conventional chemotherapy. Osteosarcoma is cancer of the bone. The cancer cells make immature bone cells, known as osteoid.
Osteosarcoma is very rare, but it is the most common type of bone cancer in children and teens. It is most common in teens and young adults.
In this study, participants will receive either cabozantinib and best supportive care or the best supportive care alone. Best supportive care will be provided at the investigator's discretion and according to institutional guidelines.
It includes antibiotics, nutritional support, correction of metabolic disorders, optimal symptom control and pain management (including radiotherapy), etc. but does not include tumor specific therapy.
Cabozantinib will be taken by mouth (orally), as a tablet, once a day. Cabozantinib will be provided to participants who tolerate it for as long as their disease does not progress. Participants in the study receiving best supportive care alone may switch to treatment with cabozantinib and best supportive care if their disease progresses and if other eligibility criteria are met.
Participants may withdraw consent to participate at any time.
The estimated duration of the study for participants is 24 months, however a participant could remain in the study longer if demonstrating treatment benefit.

开始日期2024-11-22

申办/合作机构

Ipsen SA

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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1,805

项与苹果酸卡博替尼相关的文献（医药）

2025-02-01·Current computer-aided drug design

Discovery of Novel Pyrimidine Based Small Molecule Inhibitors as VEGFR-2 Inhibitors: Design, Synthesis, and Anti-cancer Studies

Article

作者: Dabhade, Pratap S. ; Mokale, Santosh N. ; Dhawale, Sachin A.

Background::

Receptor tyrosine kinases (RTKs) are potent oncoproteins in cancer that, when mutated or overexpressed, can cause uncontrolled growth of cells, angiogenesis, and metastasis, making them significant targets for cancer treatment. Vascular endothelial growth factor receptor 2 (VEGFR2), is a tyrosine kinase receptor that is produced in endothelial cells and is the most crucial regulator of angiogenic factors involved in tumor angiogenesis. So, a series of new substituted N-(4-((2-aminopyrimidin-5-yl)oxy)phenyl)-N-phenyl cyclopropane1,1-dicarboxamide derivatives as VEGFR-2 inhibitors have been designed and synthesized.

Methods::

Utilizing H-NMR, C13-NMR, and mass spectroscopy, the proposed derivatives were produced and assessed. HT-29 and COLO-205 cell lines were used for the cytotoxicity tests. The effective compound was investigated further for the Vegfr-2 kinase inhibition assay, cell cycle arrest, and apoptosis. A molecular docking examination was also carried out with the Maestro-12.5v of Schrodinger.

Results::

In comparison to the reference drug Cabozantinib (IC50 = 9.10 and 10.66 μM), compound SP2 revealed promising cytotoxic activity (IC50 = 4.07 and 4.98 μM) against HT-29 and COLO-205, respectively. The synthesized compound SP2 showed VEGFR-2 kinase inhibition activity with (IC50 = 6.82 μM) against the reference drug, Cabozantinib (IC50 = 0.045 μM). Moreover, compound SP2 strongly induced apoptosis by arresting the cell cycle in the G1 phase. The new compounds' potent VEGFR-2 inhibitory effect was noted with key amino acids Asp1044, and Glu883, and the hydrophobic interaction was also observed in the pocket of the VEGFR-2 active site by using a docking study.

Conclusion::

The results demonstrate that at the cellular and enzyme levels, the synthetic compounds SP2 are similarly effective as cabozantinib. The cell cycle and apoptosis data demonstrate the effectiveness of the suggested compounds. Based on the findings of docking studies, cytotoxic effects, in vitro VEGFR-2 inhibition, apoptosis, and cell cycle arrest, this research has given us identical or more effective VEGFR-2 inhibitors.

2025-02-01·Clinical Genitourinary Cancer

A Prospective Non-interventional Real-World Study of cabozantinib in Pretreated Patients With Advanced Renal Cell Carcinoma Refractory to Vascular Endothelial Growth Factor-Targeted Therapy (CASSIOPE)

Article

作者: Basso, Umberto ; Bigot, Pierre ; Staehler, Michael ; Rastogi, Priti ; Verzoni, Elena ; Bedke, Jens ; Hamberg, Paul ; Gajate, Pablo ; Procopio, Giuseppe ; Qvick, Bryan ; Barthelemy, Philippe ; De Vivo, Rocco ; Dutailly, Pascale ; Eymard, Jean-Christophe ; Suarez, Cristina ; Rink, Michael ; Perrot, Valérie ; Laramas, Mathieu ; Guillot, Aline ; Lázaro-Quintela, Martín

BACKGROUND:

There is a lack of published data on real-world cabozantinib use in patients with advanced renal cell carcinoma after prior vascular endothelial growth factor (VEGF)-targeted therapy.

METHODS:

CASSIOPE was a real-world, prospective, multicenter, non-interventional postauthorization safety study of cabozantinib in adult patients with advanced renal cell carcinoma in Europe following prior VEGF-targeted treatment (NCT03419572). Endpoints included cabozantinib utilization (dose modifications due to adverse events [AEs; primary endpoint], dose, dose modifications, and treatment duration), safety, effectiveness (progression-free survival [PFS], overall survival [OS], best overall response [BOR]), and healthcare resource utilization.

FINDINGS:

Full analysis set (FAS)/safety population comprised 679 patients; 433 of these initiated cabozantinib at 60 mg/day (recommended dose) (primary safety population). Median age (FAS) was 67 (range, 29-93) years; most were male (73·0%), had clear-cell histology (85·7%), metastatic disease at cabozantinib initiation (97·8%), and prior nephrectomy (80·3%). In the primary safety population, 77·1% experienced dose modification owing to an AE. In the safety population, the median daily dose was 40·0 (range, 7·8-60·0) mg/day and the median treatment duration was 7·8 (< 0·1-15·2) months. Treatment-emergent and treatment-related AEs were experienced by 95·9% and 90·4% of patients, respectively. Median PFS (FAS) assessed by the local investigator using any method was 8·3 months, and 1-year OS rate was 74%. Approximately one-third of all patients had a BOR of partial response and 6 had a complete response.

INTERPRETATION:

Second- or later-line cabozantinib was effective and manageable in a real-world setting and had a safety profile consistent with previous studies.

2025-02-01·CANCER TREATMENT REVIEWS

Dynamics of resistance to immunotherapy and TKI in patients with advanced renal cell carcinoma

Review

作者: Mollica, Veronica ; Santoni, Matteo ; Massari, Francesco ; Rizzo, Alessandro

Immune-based combinations are the cornerstone of the first-line treatment of metastatic renal cell carcinoma patients, leading to outstanding outcomes. Nevertheless, primary resistance and disease progression is a critical clinical challenge. To properly address this issue, it is pivotal to understand the mechanisms of resistance to immunotherapy and tyrosine kinase inhibitors, that tumor eventually develop under treatment. In this review of the literature, we aim at exploring resistance mechanisms arising in patients treated with first-line immune-based combinations in order to understand the biological pattern that should be investigated to overcome them. In more detail, mechanisms of resistance to nivolumab and pembrolizumab are divided into intrinsic to cancer cells and extrinsic (stromal or immune cells). Regarding axitinib, the increased expression of Nuclear protein 1 (NUPR1) or decreased levels of insulin receptor (INSR) characterize resistant cells. The secretion of non-VEGF pro-angiogenic factors, such as PDGF-BB, IL-1β, MMP-9, Gro-α, IL-8, IL-6, and CCL-2, can lead to resistance to cabozantinib. The reactivation of pathways previously targeted by lenvatinib or the activation of alternative pathways, such as EGFR-PAK2-ERK pathway, underlie the development of resistance to lenvatinib. Exploring resistance mechanism that arise during first-line therapy can lead to the development of treatment strategy able to overcome them in order to improve duration of response and patients outcomes.

514

项与苹果酸卡博替尼相关的新闻（医药）

2025-01-20

·今日头条

我国首款EGFR ex20ins肺癌新药舒沃替尼，成功斩获获FDA优先审评

2025年1月7日，我国自研的一款EGFR外显子20插入突变（EGFR exon20ins）的靶向药物——舒沃替尼（Sunvozertinib）的新药上市申请，正式获得美国食品药品监督管理局（FDA）受理，并被授予优先审评资格，用于EGFR 20ins突变的局部晚期或转移性非小细胞肺癌（NSCLC）的治疗！此前，舒沃替尼已先后获得中美的突破性疗法认定（BTD），它也是EGFR exon20ins肺癌领域，首个且目前唯一斩获中、美BTD大满贯的抗癌新药！ ▲截图源自“PR Newswire” 一、舒沃替尼：获中美双重认证的肺癌靶向药舒沃替尼（Sunvozertinib，舒沃哲®，代号DZD9008）是一种口服、不可逆、选择性酪氨酸激酶抑制剂，具有良好的安全性和令人鼓舞的抗肿瘤活性，该药于2023 年 8 月，获中国国家药品监督管理局（NMPA）批准，用于在的治疗。值得一提的是，舒沃替尼片也是我国首个获批上市的国研EGFR外显子20插入突变（EGFR exon20ins）的靶向疗法。 2024年4月，该药被列入《2024版中国临床肿瘤学会（CSCO）非小细胞肺癌诊疗指南》，作为EGFR exon20ins 非小细胞肺癌（NSCLC）后线治疗的唯一Ⅰ级推荐方案。二、EGFR 20ins肺癌的新曙光，客观缓解率超60% 2023年8月，舒沃替尼在我国获批，此次获批主要基于一项WU-KONG6临床研究（NCT05668988）的结果。该研究共入组104例EGFR 20ins非小细胞肺癌（NSCLC）患者，在数据截止时（2022 年 10 月 17 日），最后一名入组患者已接受约 6 个月的随访。结果显示：在 97 名可评估疗效分析的患者中， 59 名（61%）的患者达到肿瘤缓解，换言之，确认的客观缓解率（ORR）高达61%（95% CI，范围：50–71）（详见下图）。总之，在这项 2 期研究中，sunvozertinib 对接受铂类化疗治疗的EGFR外显子 20ins 型 NSCLC 患者表现出抗肿瘤疗效，且安全性可控。 ▼独立评审委员会（IRC）评估的肿瘤大小变化 ▲图源“Lancet”，版权归原作者所有，如无意中侵犯了知识产权，请联系我们删除三、舒沃替尼为EGFR-TKI耐药的晚期肺癌患者带来曙光，无进展生存超7个月除了EGFR 20ins非小细胞肺癌外，近期研究发现，舒沃替尼在治疗人表皮生长因子受体 2 外显子 20 插入型（HER2 exon20ins）肺腺癌方面，也具有不俗的疗效。《抗癌药物》杂志近期报道了首例应用舒沃替尼治疗HER2 exon20ins肺腺癌的病例报告。 ▲截图源自“Anti-Cancer Drugs” 该患者为一位67岁的女性，16年前（2007年）确诊为肺腺癌，IIIa期，T2N2M0。该患者曾先后接受过吉非替尼、泊齐替尼、卡博替尼、仑伐替尼等治疗。但遗憾的是，最终无一例外，都出现了耐药性，尤其是在使用仑伐替尼2个月后，出现呼吸困难，哮鸣音加重，意识改变，卧床不起，无法活动等严重耐药表现，胸部CT显示双肺多发斑片状高密度病灶，提示对治疗有抵抗力。遂停用仑伐替尼，又因该患者此前进行肺组织活检发现存在HER2基因突变，p.Y772_A775dup外显子20非移码插入突变，故而改用舒沃替尼治疗。结果显示：在舒沃替尼治疗3天后，患者喘息、呼吸困难好转，精神状态清楚；继续治疗1周后，患者能够行走，出院后继续使用该药治疗。1个月后随访发现，患者呼吸平稳，意识清晰。胸部CT扫描显示癌性病灶缩小（详见下图）。 ▲图源“Anti-Cancer Drugs”，版权归原作者所有，如无意中侵犯了知识产权，请联系我们删除综上，舒沃替尼可以稳定患者的病情，实现 87 天的无进展生存期。这一新发现或将为 TKI 治疗失败的 HER2 外显子 20 插入型（HER2 exon20ins）患者提供新的治疗选择。四、小编寄语我国抗癌新药的研发速度，正以前所未有的中国速度，迈向世界前列！除了舒沃替尼外，还有多款针对EGFR突变的抗癌新药正在研发或即将上市,为晚期肺癌患者带来了新的希望与选择！全球肿瘤医生网小编温馨提示广大癌友，即便是标准治疗方案失败，亦或是现有治疗药物耐药，也要考虑出现新药靶点的可能，并尝试进行基因检测，以争取更多的治疗机会。看不懂检测报告的患者，也可将基因检测报告、近期病理检查、治疗经历等，提交至全球肿瘤医生网医学部，进行初步评估。五、参考资料 [1]Wang M,et al.Sunvozertinib for patients in China with platinum-pretreated locally advanced or metastatic non-small-cell lung cancer and EGFR exon 20 insertion mutation (WU-KONG6): single-arm, open-label, multicentre, phase 2 trial[J]. The Lancet Respiratory Medicine, 2024, 12(3): 217-224. https://www-thelancet-com.libproxy1.nus.edu.sg/journals/lanres/article/PIIS2213-2600(23)00379-X/abstract [2]Luan T,et al.First Case Report of Sunvozertinib for the treatment of Her2 exon 20 insertion in Lung Adenocarcinoma[J]. 2024. https://journals-lww-com.libproxy1.nus.edu.sg/anti-cancerdrugs/fulltext/2024/09000/first_case_report_of_sunvozertinib_for_the.8.aspx 本文为全球肿瘤医生网原创，未经授权严禁转载

优先审批突破性疗法CSCO会议临床结果临床2期

2025-01-09

·Business Wire

Exelixis Provides Update on Oncologic Drugs Advisory Committee Meeting for Cabozantinib (CABOMETYX®) for the Treatment of Patients with Previously Treated Advanced Neuroendocrine Tumors

ALAMEDA, Calif.--( BUSINESS WIRE )-- Exelixis, Inc. (Nasdaq: EXEL) today announced it has been notified by the U.S. Food and Drug Administration (FDA) that the supplemental New Drug Application (sNDA) for cabozantinib (CABOMETYX ® ) for the treatment of adults with previously treated advanced pancreatic neuroendocrine tumors (pNET) and advanced extra-pancreatic (epNET) will no longer be the subject of discussion at an Oncologic Drugs Advisory Committee meeting. The sNDA remains under consideration by FDA with a Prescription Drug User Fee Act action date of April 3, 2025. About Exelixis Exelixis is a globally ambitious oncology company innovating next-generation medicines and regimens at the forefront of cancer care. Powered by drug discovery and development excellence, we are rapidly evolving our product portfolio to target an expanding range of tumor types and indications with our clinically differentiated pipeline of small molecules, antibody-drug conjugates and other biotherapeutics. This comprehensive approach harnesses decades of robust investment in our science and partnerships to advance our investigational programs and extend the impact of our flagship commercial product, CABOMETYX ® (cabozantinib). Exelixis is driven by a bold scientific pursuit to create transformational treatments that give more patients hope for the future. For information about the company and its mission to help cancer patients recover stronger and live longer, visit www.exelixis.com , follow @ExelixisInc on X (Twitter), like Exelixis, Inc. on Facebook and follow Exelixis on LinkedIn. Exelixis Forward-Looking Statements This press release contains forward-looking statements, including, without limitation, statements related to: the FDA’s plans to discuss the sNDA for cabozantinib for the treatment of adults with previously treated advanced pNET and advanced epNET at an ODAC meeting; the therapeutic potential of cabozantinib as a treatment for patients with previously treated advanced pNET and advanced epNET; the regulatory review process with respect to Exelixis’ sNDA for cabozantinib in previously treated advanced pNET and advanced epNET, including the Prescription Drug User Fee Act target action date assigned by the FDA; and Exelixis’ scientific pursuit to create transformational treatments that give patients more hope for the future. Any statements that refer to expectations, projections or other characterizations of future events or circumstances are forward-looking statements and are based upon Exelixis’ current plans, assumptions, beliefs, expectations, estimates and projections. Forward-looking statements involve risks and uncertainties. Actual results and the timing of events could differ materially from those anticipated in the forward-looking statements as a result of these risks and uncertainties, which include, without limitation: complexities and the unpredictability of the regulatory review and approval processes in the U.S. and elsewhere, including the risk that the FDA may not approve cabozantinib as a treatment for pNET or epNET in a timely fashion, if at all; unexpected concerns that may arise as a result of the occurrence of adverse safety events or additional data analyses of clinical trials evaluating cabozantinib; Exelixis’ ability to protect its intellectual property rights; market competition, including the potential for competitors to obtain approval for generic versions of CABOMETYX; changes in economic and business conditions; and other factors affecting the ability of Exelixis to obtain regulatory approval for cabozantinib in new indications detailed from time to time under the caption “Risk Factors” in Exelixis’ most recent Annual Report on Form 10-K and subsequent Quarterly Reports on Form 10-Q, and in Exelixis’ future filings with the Securities and Exchange Commission. All forward-looking statements in this press release are based on information available to Exelixis as of the date of this press release, and Exelixis undertakes no obligation to update or revise any forward-looking statements contained herein, except as required by law. Exelixis, the Exelixis logo and CABOMETYX are registered U.S. trademarks of Exelixis.

申请上市抗体药物偶联物加速审批

2025-01-08

·PRNewswire

Clarivate Identifies Eleven Potential Blockbuster and Transformative Drugs in Annual Drugs to Watch Report

Anticipated advancements in obesity, oncology, gene therapy and other areas poised to revolutionize patient care LONDON, Jan. 8, 2025 /PRNewswire/ -- Clarivate Plc (NYSE:CLVT) a leading global provider of transformative intelligence, today announced the release of the twelfth annual Drugs to Watch™ report, a trusted guide to the therapies poised to redefine the future of healthcare. This year, the highly anticipated resource highlights 11 drugs projected to achieve blockbuster status or revolutionize treatment paradigms within five years. Since its inception, Drugs to Watch has identified over 98 transformative therapies, cementing its role as an essential resource for navigating the ever-evolving pharmaceutical landscape. This year's report, powered by insights from the Clarivate Cortellis intelligence suite of products, highlights 11 therapies that have recently launched or are set to debut in 2025. These innovations, addressing critical challenges in areas such as obesity, oncology, and gene therapy, are forecast to achieve blockbuster sales by 2030 or dramatically improve patient outcomes on a global scale. The report also explores pivotal trends shaping the industry, including the surging demand for obesity treatments, the transformative potential of gene editing, and the growing impact of regulatory innovation. The report offers an in-depth analysis of the chronic disease market in Mainland China, spotlighting five therapies expected to exceed $1 billion in annual sales over the next five years or deliver transformative outcomes for patients. It also explores critical topics shaping global healthcare, including regulatory advancements, the role of radiopharmaceutical theranostics in oncology, and the growing use of real-world data (RWD) and patient-reported outcomes (PROs) to drive health equity and enhance regulatory submissions. Henry Levy, President, Life Sciences & Healthcare, Clarivate, remarked: "Innovation in the life sciences is reaching unprecedented heights, and this year's Drugs to Watch™ report once again demonstrates the industry's ability to deliver therapies that address unmet medical needs and challenge existing paradigms of care. At Clarivate, we take pride in the precision and reliability of our predictions—last year, we identified 13 molecules as Drugs to Watch, with 12 already approved and launched and one poised for launch. This track record reflects the strength of our comprehensive data and deep expertise. By continuing to provide actionable insights, we empower the sector to navigate opportunities, overcome challenges and drive progress in advancing global health." Mike Ward, Global Head of Thought Leadership, Life Sciences & Healthcare, Clarivate, stated: "2025 represents a turning point for the life sciences sector as it embraces cutting-edge technologies such as AI and machine learning to enhance drug discovery and development. This year's report captures the dynamic forces at play, including groundbreaking progress in precision oncology, the rise of radiopharmaceuticals, and the growing focus on addressing global health disparities." The 2025 Drugs to Watch™ report highlights key trends reshaping the life sciences landscape, emphasizing the transformative impact of emerging technologies and therapeutic breakthroughs. Advances in AI and machine learning are streamlining drug discovery, clinical trials, and real-world data integration, enabling precision medicine approaches. The obesity market is undergoing a revolution driven by next-generation GLP-1 therapies, while radiopharmaceutical theranostics are redefining cancer treatment with a "see it and treat it" paradigm. Gene editing technologies are unlocking new opportunities in personalized medicine, and evolving regulatory frameworks are fostering greater emphasis on patient-reported outcomes and health equity. Together, these trends showcase the sector's resilience and its ability to navigate challenges while driving innovation to improve patient care worldwide. This year's drugs to watch exemplify the fusion of innovation and dedication to advancing patient care in an increasingly complex healthcare ecosystem. The Drugs to Watch™ 2025 list include: AWIQLI® (LAI 287; insulin icodec) developed by Novo Nordisk | Type 1 and type 2 diabetes mellitus AWIQLI®, the first once-weekly, subcutaneous insulin, has launched in Australia, Canada, the EU, Mainland China, and Japan. Its weekly dosing offers a significant advantage over daily basal insulin, potentially reducing the treatment burden for patients with type 1 or type 2 diabetes (T1DM and T2DM). CagriSema (cagrilintide + semaglutide) developed by Novo Nordisk | Obesity and type 2 diabetes mellitus CagriSema, combining cagrilintide, a long-acting amylin analog, with semaglutide, promises superior efficacy over semaglutide (OZEMPIC/WEGOVY®) and tirzepatide (MOUNJARO/ZEPBOUND®) in treating obesity and type 2 diabetes. This next-generation GLP-1 therapy leverages the benefits of GLP-1s, such as enhanced insulin secretion and appetite reduction, while incorporating amylin's effects, including slowed glucose absorption and release. If approved, CagriSema will be the first fixed-dose combination of amylin and GLP-1 receptor agonists in the obesity and T2DM markets. COBENFY™ (KarXT; xanomeline-trospium) developed by Bristol Myers Squibb | Schizophrenia and psychosis related to Alzheimer's disease Amid setbacks for emerging schizophrenia treatments, the approval of COBENFY marks a transformative milestone as the first drug in over 30 years with a novel mechanism of action for treating schizophrenia. Combining xanomeline and trospium, COBENFY selectively targets M1 and M4 receptors, rather than traditional dopamine pathways, while minimizing cholinergic side effects. While further data is needed to assess its effectiveness in Alzheimer's disease-related psychosis, COBENFY shows strong commercial potential if proven effective in treating AD-related hallucinations and delusions. EBGLYSS™ (lebrikizumab) developed by Eli Lilly and Co and Almirall | Atopic dermatitis EBGLYSS™, the third biologic targeting IL-13 for atopic dermatitis, follows DUPIXENT® (dupilumab) and ADBRY®/ADTRALZA® (tralokinumab) to market. Its less frequent dosing, more selective IL-13 inhibition, and strong efficacy and safety data position it as a likely first-line treatment for moderate-to-severe atopic dermatitis when topical corticosteroids are inadequate. Fitusiran developed by Alnylam® Pharmaceuticals Inc and Sanofi | Hemophilia A and B Fitusiran, shown to be effective in phase 3 trials for both hemophilia A and B, regardless of inhibitor status, has the potential to offer a new approach to hemophilia treatment. This small interfering RNA (siRNA) therapy works by inhibiting SerpinPC1 mRNA, reducing antithrombin levels, promoting thrombin generation, and helping to rebalance hemostasis to prevent bleeds. Leveraging Alnylam® Pharmaceuticals' ESC-GalNAc conjugate technology, fitusiran could become the first antithrombin-lowering therapy based on a double-stranded RNA molecule, pending approval. GSK-3536819 (MenABCWY) developed by GSK plc | Meningococcus GSK plc's GSK-3536819 vaccine candidate, a 5-in-1, first-generation formulation, targets the five groups of Neisseria meningitidis (A, B, C, W, and Y) responsible for most invasive meningococcal disease (IMD) cases worldwide. It combines the antigenic components of GSK's licensed meningococcal vaccines, BEXSERO (MenB) and MENVEO (MenACWY), both of which have established efficacy and safety profiles. IMDELLTRA™ (tarlatamab-dlle) developed by Amgen | Small-cell lung cancer (SCLC) IMDELLTRA™ is a first-in-class immunotherapy for extensive-stage small cell lung cancer (ES-SCLC). Using Amgen's bispecific T cell engager (BiTE®) molecules, it targets CD3 on T cells and DLL3 on tumor cells, enabling T cells to attack and lyse the tumor. DLL3 is expressed on the surface of SCLC cells in more than 85% of patients but is minimally expressed on healthy cells making it an attractive target. This mechanism positions IMDELLTRA as a potential standard of care for previously treated ES-SCLC. mRESVIA (mRNA-1345) developed by Moderna Inc | RSV With its U.S. FDA approval in May 2024, mRESVIA® joined AREXVY and ABRYSVO, both featured in Drugs to Watch 2024, as respiratory syncytial virus (RSV) vaccines currently available for adults ages 60 years and older, helping further support the public health initiative to reduce the RSV-related disease burden. Even with available vaccines, RSV infections continue to be a public health concern, particularly for infants and older adults (65 years and older). SEL-212 developed by Sobi® and Cartesian Therapeutics Inc/Selecta Biosciences Inc | Gout SEL-212 is a novel, once-monthly treatment combining pegylated uricase (pegadricase; SEL-037) with ImmTOR™, an immune tolerance technology designed to inhibit the formation of anti-drug antibodies (ADAs). For this application, ImmTOR consists of SEL-110.36, an inhibitor of uricase-specific ADA. This approach may help overcome the limitations of reduced efficacy and tolerability seen with other biologic treatments, such as KRYSTEXXA® (pegloticase), in patients with chronic gout. Vepdegestrant (ARV-471) developed by Arvinas Inc and Pfizer Inc | Breast cancer A global collaboration between Arvinas Inc and Pfizer Inc, vepdegestrant may become the first PROteolysis Targeting Chimera (PROTAC®) protein degrader on the market. Designed to target and degrade the estrogen receptor (ER) protein, early studies suggest PROTAC-induced degradation is more complete than with oral selective estrogen receptor degraders (SERDs). This offers potential for overcoming endocrine resistance in breast cancer. Label expansions, including combination with IBRANCE® (palbociclib), are being explored. Zanzalintinib (XL092) developed by Exelixis Inc | Colorectal cancer, renal cell carcinoma and squamous cell carcinoma of head and neck Zanzalintinib is a third-generation oral tyrosine kinase inhibitor targeting VEGF receptors, MET, and TAM kinases involved in tumor growth and immunosuppression. Currently in phase 3 trials for non-clear-cell renal cell carcinoma (nccRCC), colorectal cancer (CRC) and squamous cell carcinoma of the head and neck (SCCHN), the company anticipates one potential zanzalintinib launch per year starting as early as 2026. Compared to CABOMETYX® (cabozantinib), zanzalintinib may offer benefits, including approval for nccRCC histology and a broader patient population. Access the Drugs to Watch 2025 report from Clarivate, here. For more Drugs to Watch updates and analyses throughout the year, visit the Drugs to Watch web page and follow Clarivate for Life Sciences & Healthcare on LinkedIn and X. Join the conversation, using #DrugstoWatch. To learn more about how Clarivate can help healthcare companies inform and shape the drug discovery, development and delivery process, visit here. Methodology for the Clarivate Drugs to Watch 2025 Report To identify this year's Drugs to Watch, Clarivate drew from the expertise of over 160 analysts covering hundreds of diseases, drugs and markets, along with 11 integrated data sets that span the R&D and commercialization lifecycle, including: Cortellis Competitive Intelligence™, Disease Landscape & Forecast, Epidemiology Intelligence, BioWorld™, Cortellis Regulatory Intelligence™, Drug Timeline & Success Rates, Cortellis Clinical Trials Intelligence™, Cortellis Deals Intelligence™, Access & Reimbursement payer studies, Clarivate Real-World Data and Analytics, Web of Science™, Derwent Innovation™, and other industry sources including biopharma company press releases, filings and peer-reviewed publications. Candidate drugs in phase 2 or phase 3 trials, at pre-registration or registration stage, or already launched in 2024 were selected for analysis, including both novel treatments and already-marketed drugs pursuing new indications that could be particularly impactful. Drugs launched prior to 2024 were excluded. The dataset was filtered for drugs that had total forecast sales of $1 billion or more by 2030. Clarivate experts and analysts evaluated each drug in its individual context, based on factors such as expected approval or launch dates, competitive landscape, regulatory status, trial results, market dynamics and other key factors, and added novel drugs that, while likely to fall short of blockbuster status, are poised to be therapeutic game-changers. Please note that Clarivate analysts generated the data shown in this report prior to December 31, 2024. The Drugs to Watch 2025 Report and the treatments referenced in this release are based on Clarivate's current expectations per existing data, but actual results derived from the drugs named in the report and here may differ significantly. Clarivate is committed to comprehensively supporting customers across the entire drug, device and medical technology lifecycles to advance human health. By combining patient journey data, therapeutic area expertise, artificial intelligence and analytics in ways that unlock hidden insights, data-driven decisions and accelerating innovation, Clarivate's end-to-end research intelligence is designed to enable customers to make informed evidence-based decisions. About Clarivate Clarivate™ is a leading global provider of transformative intelligence. We offer enriched data, insights & analytics, workflow solutions and expert services in the areas of Academia & Government, Intellectual Property and Life Sciences & Healthcare. For more information, please visit . Media Contact: Catherine Daniel Director, External Communications, Life Sciences & Healthcare [email protected] SOURCE Clarivate Plc WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

疫苗临床3期免疫疗法

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
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	美国	National Cancer Institute	2024-08-22
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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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


NCT03375320 (CABINET, ASCO_GI2025)	临床3期	胃肠胰神经内分泌肿瘤	203	Cabozantinib 60 mg daily	築鹽顧顧餘鹽淵製選簾(憲醖衊鏇鹽範蓋觸壓願) = 製糧夢夢願齋醖鹹獵襯廠構選築鹹繭衊窪廠憲 (範衊構齋淵蓋餘選淵廠, 6.0 ~ 16.7) 更多	积极	2025-01-23
				Placebo	築鹽顧顧餘鹽淵製選簾(憲醖衊鏇鹽範蓋觸壓願) = 衊廠觸衊夢壓築遞構鹽廠構選築鹹繭衊窪廠憲 (範衊構齋淵蓋餘選淵廠, 3.9 ~ 11.0)
JPRN-jRCT1080224637 (ASCO_GI2025)	临床1/2期	转移性结直肠癌 MET amplification \| RAS \| BRAF	35	Cabozantinib	鑰餘淵鹹廠簾製膚窪襯(憲壓網夢壓壓廠糧廠積) = 簾齋憲餘衊壓蓋鏇獵夢繭糧齋願繭廠餘鬱鏇艱 (鏇醖築蓋餘鬱築範繭夢, 0.2 ~ 36) 更多	不佳	2025-01-23
				Panitumumab	壓獵艱製選齋齋製遞壓(鹹餘襯鹹艱顧鏇膚願構) = 構衊願艱鬱膚膚繭製網窪淵廠醖獵顧獵簾艱願 (積憲醖蓋鬱遞繭鹽鑰鏇 )
NCT04963283 (ASCO_GI2025)	临床2期	转移性微卫星稳定结直肠癌	49	Cabozantinib 40 mg	構窪構繭淵鬱餘糧鬱網(醖壓鬱簾糧顧廠廠糧壓) = 鹹簾範顧夢繭築網窪積鹽艱鏇鏇製遞鑰遞醖蓋 (窪觸鹹顧觸範艱願製鹽, 0.264 ~ 0.557) 更多	积极	2025-01-23
NCT03468218 (CTgov)	临床2期	鼻旁窦鳞状细胞癌 \| 口腔鳞状细胞癌复发 \| 口咽部鳞状细胞癌 ... 更多	36	Cabozantinib+pembrolizumab	蓋廠構簾窪顧糧築襯襯(齋選廠餘淵淵願製夢廠) = 鬱鬱鹹醖艱醖觸構鹹範壓網鏇選鹽範壓糧構製 (遞餘衊夢廠憲壓繭夢廠, 築製鬱糧艱蓋蓋鏇鬱鏇 ~ 醖鑰窪製範鏇鏇遞夢淵) 更多	-	2024-12-27
NCT03945773 (CaboPoint, CTgov)	临床2期	转移性肾细胞癌 \| 局部晚期肾细胞癌 \| 转移性透明细胞性肾细胞癌	127	Cabozantinib (Cohort A)	繭鏇廠窪襯築憲衊淵蓋(蓋窪製餘齋遞淵範鹹壓) = 鑰壓艱壓鹽遞夢選窪繭構蓋衊遞築蓋窪鏇網積 (艱糧顧壓夢選廠簾製衊, 憲選窪範襯襯糧獵廠鏇 ~ 繭醖鏇艱鬱餘製鏇鑰淵) 更多	-	2024-12-19
				Cabozantinib (Cohort B)	製構膚衊製夢淵廠遞願(獵衊觸衊範觸鑰齋襯艱) = 廠窪齋選選廠遞齋願選鏇鏇鹹憲顧鏇簾鏇壓壓 (鑰憲鑰築製網選淵鹽構, 餘顧築範製鑰鹹網餘襯 ~ 鏇淵壓壓齋簾範鏇醖窪) 更多
NCT03370718 (SAT-175, CTgov)	临床2期	肾上腺皮质癌	18	Cabozantinib	獵製繭齋簾選構餘獵廠(蓋網鏇範獵膚醖餘選鑰) = 遞鏇餘鏇繭鬱鹹夢壓蓋製夢淵憲願壓壓顧蓋積 (餘淵衊鹽壓鹽範淵餘齋, 壓憲願範遞憲襯鬱願遞 ~ 網憲醖鑰夢簾簾築窪鹽) 更多	-	2024-12-10
ESMO_ASIA2024 人工标引	N/A	晚期肾细胞癌一线	41	Cabozantinib plus Nivolumab	襯衊餘餘網範膚遞簾鑰(廠鏇遞選鏇顧鹽齋鏇積) = 鏇鏇鑰築鬱獵廠衊憲製遞蓋鹽壓鹹簾遞鹹鬱遞 (顧膚鹹積顧淵範觸鏇選 ) 更多	积极	2024-12-07
				Cabozantinib	襯衊餘餘網範膚遞簾鑰(廠鏇遞選鏇顧鹽齋鏇積) = 鑰壓窪顧鹽觸壓鑰膚膚遞蓋鹽壓鹹簾遞鹹鬱遞 (顧膚鹹積顧淵範觸鏇選 ) 更多
NCT04091750 (CTgov)	临床2期	不可切除的黑色素瘤	14	ipilimumab+Nivolumab+Cabozantinib	簾鑰製觸鬱糧觸廠鹹廠(範窪糧網鹽顧襯範齋鹹) = 範襯鏇壓憲淵齋廠淵膚夢齋糧選範鏇顧鹽範糧 (鹽鑰選製餘顧醖鬱窪衊, 積選蓋願齋淵範齋窪廠 ~ 顧淵鹹鹽選選憲積選鬱) 更多	-	2024-11-27
NCT03534804 (PemCab, CTgov)	临床2期	晚期尿路上皮癌 \| 膀胱癌 \| 转移性尿路上皮癌	37	Cabozantinib+pembrolizumab	鬱製窪壓蓋襯觸遞窪築(範鏇觸衊鑰鑰遞積襯範) = 觸鏇繭糧積鹹選窪簾艱醖獵醖廠蓋衊繭襯膚獵 (鑰選製製簾窪範鹽糧簾, 襯製淵獵廠鬱膚醖糧構 ~ 廠鏇選衊蓋醖蓋廠齋衊) 更多	-	2024-11-26
NCT03375320 (CABINET \| A021602, CTgov)	临床3期	高分化胰腺内分泌肿瘤 \| 胰腺神经内分泌肿瘤 \| 类癌 ... 更多	298	Cabozantinib S-malate (Arm Ia (Cabozantinib S-malate, Extra-pancreatic NET Cohort [epNET]))	衊餘壓鏇淵構範顧憲鏇(築遞獵廠艱廠遞獵襯齋) = 網製鹹窪蓋鹽夢憲獵網鹽網製夢鏇獵構獵蓋醖 (鹹糧襯選蓋積廠築鏇遞, 壓淵齋製艱壓製積鬱鏇 ~ 鏇範觸遞蓋網夢糧夢鹹) 更多	-	2024-10-16
				Placebo (Arm IIa (Placebo, Extra-pancreatic NET Cohort [epNET]))	衊餘壓鏇淵構範顧憲鏇(築遞獵廠艱廠遞獵襯齋) = 積顧糧製壓襯夢鹹鑰構鹽網製夢鏇獵構獵蓋醖 (鹹糧襯選蓋積廠築鏇遞, 窪鏇願繭構鑰選襯積積 ~ 膚廠獵鑰夢鏇構積獵艱) 更多