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更新于：2026-01-29

Tivozanib

替沃扎尼

更新于：2026-01-29

概要

基本信息

药物类型

小分子化药

别名

FOTIVDA、Tivopath、tivozanib hydrochloride monohydrate

+ [11]

靶点

PDGFRβ x VEGFR1 x VEGFR2 x VEGFR3 x c-Kit

作用方式

抑制剂、拮抗剂

作用机制

PDGFRβ抑制剂(血小板衍生生长因子受体β抑制剂)、VEGFR1拮抗剂(血管内皮细胞生长因子受体1拮抗剂)、VEGFR2拮抗剂(血管内皮细胞生长因子受体2拮抗剂)

治疗领域

肿瘤泌尿生殖系统疾病心血管疾病+ [5]

在研适应症

肾细胞癌晚期肾细胞癌湿性年龄相关性黄斑变性+ [4]

非在研适应症

晚期乳腺癌晚期肝细胞癌晚期恶性实体瘤+ [16]

原研机构

Kyowa Kirin Co., Ltd.

在研机构

AVEO Pharmaceuticals, Inc.Kyowa Hakko Kirin Pharma, Inc.

Kyowa Kirin Co., Ltd.

+ [1]

非在研机构

Astellas Pharma, Inc.

Novartis AG

权益机构

NiKang Therapeutics, Inc.

AstraZeneca PLC

Recordati UK Ltd.

+ [6]

最高研发阶段批准上市

首次获批日期

欧盟 (2017-08-24),

晚期肾细胞癌

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C22H22Cl2N4O6

InChIKeyRQXMKRRBJITKRN-UHFFFAOYSA-N

CAS号682745-41-1

关联

项与替沃扎尼相关的临床试验

NCT07218692

/ Not yet recruiting临床2期IIT

A Phase 2 Study of RP2 With Tivozanib in Patients With Metastatic Renal Carcinoma After Progression to Immunotherapy

This phase II trial tests the effect of RP2 and tivozanib in treating patients with renal cell cancer that has spread from where it first started (primary site) to other places in the body (metastatic) and that is growing, spreading, or getting worse (progressive) after receiving immunotherapy with immune checkpoint inhibitors (ICIs). RP2 is a herpes simplex virus (a viral infection commonly known as the "cold sore virus") that has been changed to infect and destroy tumor cells and to activate (turn on) the human immune system to attack the tumor cells. Tivozanib hydrochloride blocks certain proteins, which may help keep tumor cells from growing. It may also prevent the growth of new blood vessels that tumors need to grow. Tivozanib hydrochloride is a type of tyrosine kinase inhibitor and a type of antiangiogenesis agent. Giving RP2 and tivozanib may be safe, tolerable, and/or effective in treating patients with metastatic renal cell cancer that has progressed after receiving immunotherapy with ICIs.

开始日期2026-08-11

申办/合作机构

City of Hope National Medical Center

[+1]

NCT06661720

/ Recruiting临床3期IIT

Short TeRm Intensified Pembrolizumab (KEytruda) and Tivozanib for High-Risk Renal Cell Carcinoma - STRIKE

This phase III trial compares the effect of adding tivozanib to standard therapy pembrolizumab versus pembrolizumab alone for the treatment of patients with high-risk renal cell carcinoma (RCC). Immunotherapy with monoclonal antibodies, such as pembrolizumab, may help the body's immune system attack the cancer, and may interfere with the ability of tumor cells to grow and spread. Tivozanib is in a class of medications called kinase inhibitors. It works by blocking the action of the abnormal protein that signals tumor cells to multiply. This helps stop the spread of tumor cells. Giving pembrolizumab and tivozanib together may work better than pembrolizumab alone in treating patients with RCC.

开始日期2025-03-14

申办/合作机构

Alliance for Clinical Trials in Oncology

NCT06116890

/ Active, not recruiting临床2期

A Phase 2, Multicenter, Randomized, Double-Masked, Parallel Group Study to Assess the Efficacy and Safety of KHK4951, a Vascular Endothelial Growth Factor Receptor Inhibitor, in Patients With Neovascular Age-Related Macular Degeneration

The purpose of this study is to evaluate efficacy and safety of KHK4951 eye drops in patients with nAMD.

开始日期2024-01-31

申办/合作机构

Kyowa Kirin Co., Ltd.

100 项与替沃扎尼相关的临床结果

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100 项与替沃扎尼相关的转化医学

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100 项与替沃扎尼相关的专利（医药）

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319

项与替沃扎尼相关的文献（医药）

2026-02-15·RAPID COMMUNICATIONS IN MASS SPECTROMETRY

Identification and Structural Characterization of Degradation Products of Tivozanib Using LC‐Q‐TOF‐MS/MS and NMR: An In Silico Approach for Degradation and Toxicity Prediction

Article

作者: Khemchandani, Rahul ; Harini, Dharipally ; Shaikh, Nadeem ; Samanthula, Gananadhamu ; Chaganti, Sowmya ; Mouli, H. M. Chandra

ABSTRACT:

Rationale:

The present study investigated the degradation behaviour of tivozanib (TVZ), a potent tyrosine kinase inhibitor, under various stress conditions, including hydrolytic (acid, base, and neutral), oxidative, thermal, and photolytic (UV and visible light) conditions. The resulting degradation products (DPs) were characterized by LC‐Q‐TOF‐MS/MS and NMR. Additionally, in silico toxicity assessment and mutagenicity studies were accomplished by using DEREK Nexus and SARAH Nexus for TVZ and its DPs.

Methods:

The in silico degradation profile of TVZ was predicted using Zeneth software. Separation of the DPs was executed by RP‐HPLC with gradient elution mode using Shim‐pack Solar C18 column (250 × 4.6 mm, 5 μm). The mobile phase consists of solvent A as 10 mM ammonium acetate buffer (pH 3.8) and solvent B as a mixture of acetonitrile:methanol (70%:30% v/v). Structural characterization was performed for TVZ and its DPs using LC‐Q‐TOF‐MS/MS and NMR spectroscopy.

Results:

TVZ was sensitive to hydrolytic (acid, base, and neutral), oxidative, and photolytic (UV light) degradation conditions, wherein seven DPs were observed and separated by RP‐HPLC. A plausible degradation pathway of TVZ was proposed based on mass spectrometry data. The preparative HPLC was used to isolate DP‐III, DP‐IV, and DP‐VI, and the structures were confirmed by NMR spectroscopy. Furthermore, the 2D NMR data helped to differentiate the chemical structure of DP‐IV, which had the same molecular mass as TVZ.

Conclusion:

Forced degradation studies were conducted in accordance with ICH Q1A (R2) and Q1B guidelines. Totally, seven DPs were observed in various stress conditions. DP‐IV, a structural isomer of TVZ, was detected in basic hydrolytic conditions. The developed RP‐HPLC method was validated following the ICH Q2(R1). This study helps in the stability testing and routine quality control analysis during the formulation development of TVZ.

2026-01-27·Blood Advances

Cabozantinib and thromboembolism in patients with cancer: a systematic review, meta-analysis, and retrospective study

Review

作者: Bendapudi, Pavan K. ; Khorana, Alok A. ; Grover, Steven P. ; Kasthuri, Raj S. ; Eswaran, Harish ; Kasthuri, Rohan R. ; van Es, Nick

Abstract:

Antiangiogenic agents, including vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors (TKIs), represent an important class of treatments for a range of solid tumors. However, concerns have arisen over potential associations between antiangiogenic agents and thromboembolic events. We performed a systematic review and meta-analysis of randomized controlled trials (RCTs) that compared a frequently used VEGFR TKI, cabozantinib, with placebo or usual care. The primary outcome was the risk of any thromboembolism. Secondary outcomes included the risk of venous thromboembolism (VTE), risk of arterial thromboembolism (ATE) and progression-free survival. 14 RCTs were included with a combined total of 4204 patients, of whom 212 (5%) developed thromboembolism. Cabozantinib was associated with a significantly increased risk of any thromboembolism (risk ratio [RR], 2.41; 95% confidence interval [CI], 1.72-3.39) driven by VTE (RR, 3.21; 95% CI, 1.86-5.55) but not ATE (RR, 1.31; 95% CI, 0.76-2.26). To account for between-group differences in time on treatment, progression-free survival–adjusted analyses were conducted, with cabozantinib remaining associated with a significantly increased risk of any thromboembolism (RR, 1.47; 95% CI, 1.02-2.12) and VTE (RR, 1.92; 95% CI, 1.08-3.43) but not ATE (RR, 0.76; 95% CI, 0.41-1.40). In a retrospective single health care system cohort study of 295 patients treated with cabozantinib, a thromboembolism rate of 180 per 1000 patient-years on treatment was observed, with most events occurring in the first 3 months after initiation. Together these data demonstrate that cabozantinib is associated with a significantly increased risk of VTE in patients with cancer.

2025-12-01·ACTA PHARMACOLOGICA SINICA

Receptor tyrosine kinase inhibitor tivozanib regulates cell state plasticity and restores MITF dependency in BRAF wild-type melanoma

Article

作者: Guo, Wei ; Chen, Yi-Nan ; Zheng, Yang ; Chen, Xiang-Yu ; Ma, Xu-Hui ; Zhang, Yan-Jie ; Yang, Jie ; Lei, Ming ; Jiang, Min ; Zeng, Han-Lin ; Liu, Rui-Xin ; Zheng, Sheng-Nan ; Hao, Mei-Ling ; Ma, Yan-Ni

While combination BRAF/MEK inhibition has improved survival in BRAF^V600 mutant melanoma, targeted therapies for BRAF^WT melanoma remain limited. Microphthalmia transcription factor (MITF), a lineage-specific transcription factor that regulates melanocyte proliferation and melanin synthesis, represents a promising melanoma-specific drug target. In this study, we evaluated TT-012, a recently identified MITF dimerization specific inhibitor, and surprisingly found that most BRAF^WT melanoma lines were resistant to TT-012 due to low MITF transcriptional activity and reduced dependency on MITF for proliferation. High-throughput drug screen identified tivozanib, an FDA-approved drug targeting VEGFR and other receptor tyrosine kinases (RTKs), which sensitized cells to TT-012. Mechanistically, tivozanib induced cell state transition from MITF^low to MITF^high state via VEGFR2 inhibition followed by NF-κB pathway activation, restoring MITF transcriptional activity and growth dependency. The combination of tivozanib and TT-012 synergistically inhibited melanoma growth both in vitro and in vivo, underscoring its potential as a novel therapeutic strategy for BRAF^WT melanoma.

项与替沃扎尼相关的新闻（医药）

2026-01-23

·巨花健康咨询服务

替沃扎尼：解锁晚期肾癌的靶向+免疫联合治疗新可能

原研药替沃扎尼（暂译，商品名Fotivda®）是由日本协和麒麟率先研发的口服、强效、高选择性血管内皮生长因子受体（VEGFR）酪氨酸激酶抑制剂，核心作用为阻断肿瘤血管生成，凭借高选择性、低脱靶效应的优势，成为晚期肾细胞癌（RCC）的重要治疗选择，且与免疫药物联合时展现出显著的协同抗肿瘤效果，目前已在欧盟、美国正式获批上市，其不良反应风险显著低于索拉非尼等传统靶向药。分子一、作用机制替沃扎尼可精准、强力抑制驱动肿瘤血管生成的VEGFR-1、VEGFR-2、VEGFR-3，半数抑制浓度（IC50）分别为0.21 nM、0.16 nM和0.24 nM，能有效阻断VEGF配体诱导的VEGFR活化，切断肿瘤“营养供应”，延缓肿瘤生长与扩散；同时其对c-Kit、PDGFR、FGFR等脱靶靶点抑制作用较弱，理论上大幅降低了非必要副作用的发生风险。与PD-1抑制剂纳武利尤单抗联用时，二者形成**“抗血管生成+激活免疫”**的协同机制：替沃扎尼缩小肿瘤的同时改善肿瘤微环境，纳武利尤单抗则阻断PD-1/PD-L1通路，解除癌细胞对免疫系统的抑制，让T细胞重新具备攻击癌细胞的能力，实现1+1>2的抗肿瘤效果。二、核心药代与临床特点 1. 药代动力学优异：半衰期约4.7天，允许每日一次的便捷给药方案；口服后中位10小时达血浆药物浓度峰值，连续服药第14天达血药稳态，稳态积累比6~7倍；进食高脂餐对药物吸收（AUC/Cmax）无临床显著差异，可空腹或随餐服用。 2. 代谢途径明确：主要通过CYP3A4酶代谢，血浆中90%组分为原形药，蛋白结合率≥99%，轻至重度肾功能损伤患者药动学无显著差异。 3. 高选择性优势：相比索拉非尼、舒尼替尼等早期多靶点TKI，替沃扎尼作用更集中于VEGFR家族，最大化抗血管生成疗效的同时，减少了因脱靶效应引发的严重副作用。三、临床核心疗效数据替沃扎尼的疗效经多项国际多中心临床试验验证，涵盖单药治疗及联合免疫治疗方案，均展现出优于传统治疗的临床获益，核心试验数据如下：（一）单药治疗：TIVO-1与TIVO-3试验（获批核心依据）替沃扎尼单药均以一线靶向药索拉非尼为头对头对照，分别成为欧盟、美国的获批依据，核心数据如下： 1. TIVO-1试验（欧盟一线获批依据）：用于晚期肾细胞癌治疗，替沃扎尼与索拉非尼疗效相似，不良反应发生风险显著更低，成为欧盟晚期RCC的一线治疗选择。 2. TIVO-3试验（FDA三线/四线获批依据）：针对经2-3线系统治疗失败的复发/难治性晚期肾细胞癌患者，盲法独立评估显示，替沃扎尼组中位无进展生存期（PFS）5.6个月（索拉非尼组3.9个月）、客观缓解率（ORR）18%（索拉非尼组8%），疾病进展/死亡风险降低26%（HR=0.73，95%CI=0.56,0.95，P=0.016），中位总生存期（OS）16.4个月（索拉非尼组19.2个月）。（二）联合治疗：VOLCANO-1Ⅲ期试验（一线治疗新突破）替沃扎尼联合纳武利尤单抗的一线治疗数据，来自国际多中心、随机对照Ⅲ期VOLCANO-1试验，也是目前晚期RCC一线治疗的重要循证依据： 1. 试验设计：纳入621例未经治疗的晚期肾细胞癌患者（含透明细胞癌和非透明细胞癌亚型），分为两组：联合治疗组予替沃扎尼1.34mg每日一次口服+纳武利尤单抗240mg每2周一次静脉输注；对照组予传统一线标准治疗舒尼替尼50mg每日一次口服（4周为一周期）。 2. 核心疗效数据：联合治疗组ORR达45.3%（完全缓解CR率5.1%），显著高于对照组的29.1%（CR率1.7%）；联合治疗组中位PFS为15.2个月，显著长于对照组的10.8个月（HR=0.68，P<0.001），意味着更多患者能实现肿瘤缩小，且肿瘤进展时间大幅延后。 3. 安全性：联合治疗的不良反应以1-2级为主，3级及以上不良反应发生率与舒尼替尼对照组相似（38% vs 41%），未增加严重不良反应风险。四、获批适应症替沃扎尼针对晚期肾细胞癌的适应症在欧盟、美国获批范围不同，具体如下： 1. 欧盟批准：用于晚期肾细胞癌（RCC）的一线治疗； 2. 美国FDA批准：用于复发性/难治性晚期成人肾细胞癌的三线、四线治疗（适用于经至少一种非替沃扎尼/索拉非尼的VEGFR抑制剂治疗失败的患者）。五、临床服用剂量 1. 单药常规剂量：口服1.34mg，每日一次（qd），推荐剂量范围为0.67~1.3mg/日； 2. 联合用药剂量：与纳武利尤单抗联用时，替沃扎尼仍采用1.34mg每日一次口服的剂量，纳武利尤单抗为240mg每2周一次静脉输注； 3. 药代相关：服药后中位10小时达血浆药物浓度峰值，连续服药第14天达到血药稳态，进食高脂餐对药物吸收无临床显著差异，无需刻意调整饮食时间。六、副作用及处理方式替沃扎尼无基因毒性，推荐剂量下心脏安全性良好，副作用多与剂量相关，且单药不良反应发生率低于索拉非尼，联合纳武利尤单抗时不良反应以1-2级为主。结合非临床研究、单药及联合治疗的临床数据，核心副作用及对应处理方式如下： 1. 生殖毒性（重点关注）表现：动物实验显示，替沃扎尼达到一定剂量时，会导致雄性生殖器官异常、雌雄大鼠不孕，还会增加雌鼠胚胎死亡率；处理：育龄期男女治疗期间及停药后需严格采取避孕措施，暂不推荐孕妇及哺乳期女性使用。 2. 肝、肾功能相关副作用肝脏相关表现：中度肝损伤患者（总胆红素1.5~3.0倍正常值）药物暴露量增加62%，严重肝损伤患者相关研究尚未开展；处理：中度肝损伤者治疗期间密切监测肝功能（转氨酶、胆红素），严重肝损伤者禁用，肝功能异常时遵医嘱减量或停药。肾脏相关表现：轻至重度肾功能损伤（CLcr=15~89mL·min-1）患者药动学无显著差异，终末期肾病患者的药物影响尚未明确；处理：轻、中、重度肾损伤者无需调整剂量，终末期肾病患者需在医生指导下使用，定期监测肾功能。 3. VEGFR抑制剂共性副作用表现：高血压、蛋白尿、手足综合征、乏力等，发生率显著低于索拉非尼，联合治疗时该类副作用以1-2级为主；处理：高血压及时用降压药控制，蛋白尿监测尿蛋白定量并予护肾治疗，手足综合征局部外用保湿剂/抗炎药膏，症状严重时遵医嘱减量或暂停用药。 4. 心脏与血液系统表现：推荐剂量下无QTc间期显著延长（无>20ms的均值增加），无骨髓抑制等血液系统异常，联合治疗也未增加该类不良反应风险；处理：无需常规监测心电图及血常规，出现心悸、胸闷时及时就医排查。老挝卢修斯七、购买参考 1. 上市地区：替沃扎尼目前已在欧盟、美国正式获批，国内暂未获批上市； 2. 原研药相关：原研药由日本协和麒麟/美国EUSA生物制药研发，可通过跨境医疗渠道、海外正规药房购买，需药房购买，需凭肿瘤科医生处方开具，优先选择有资质的跨境医药平台，避免假冒产品； 3. 仿制药选择：可选择老挝卢修斯等海外合规仿制药，支持海外邮寄，能在保证疗效的同时兼顾经济性，大幅减轻患者的治疗负担。如有相关需求可添加二维码联系我们将尽心为您服务免责声明：以上内容整理于drugs及网络，仅作信息交流之目的，而非提供医疗建议。文中观点不代表公司立场，亦不代表本公司支持或反对文中观点。本文不构成任何治疗方案的推荐。本公众号内容仅供医学药学专业人士阅读参考，具体用药请咨询主治医师。本公众号仅提供信息展示服务，如需专业治疗方案，请前往正规医院接受诊疗。

2026-01-14

·PRNewswire

AVEO Oncology, an LG Chem company, Announces First Patient Dosed in Front-Line AML Combination Study of Ficlatuzumab

– Collaboration with Blood Cancer United® in its Beat AML® Master Clinical Trial – – AVEO's ficlatuzumab compound to be studied in combination with azacitidine and venetoclax in patients with AML in a Phase 1b/2 clinical trial – – First patient dosed into the Phase 1b/2 clinical trial – BOSTON, Jan. 14, 2026 /PRNewswire/ -- AVEO Oncology, an LG Chem company, (AVEO) announced today that the first patient has been successfully dosed in a Phase 1b/2 clinical trial evaluating ficlatuzumab in combination with azacitidine and venetoclax in patients that are 60 years of age or older with untreated acute myeloid leukemia (AML) through a Master Clinical Trial Collaboration Agreement with Blood Cancer United®, formerly the Leukemia & Lymphoma Society. As part of this strategic collaboration with Blood Cancer United, a global nonprofit focused on blood cancer patient support, research, and advocacy, Blood Cancer United will be sponsoring the clinical trial as a sub-study in their Beat AML® Master Clinical Trial, the first collaborative precision medicine clinical trial in a blood cancer, which tests multiple therapies in multiple study arms simultaneously. The Phase 1b/2 clinical trial is designed to evaluate the safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy of the combination as a potential treatment for AML. Ficlatuzumab is AVEO's investigational humanized IgG1 monoclonal antibody that is designed to bind to the hepatocyte growth factor (HGF) ligand and prevent it from signaling via the c-Met receptor. Early phase clinical trials evaluating ficlatuzumab in combination with cytarabine in AML reported a favorable safety profile with promising clinical activity, supporting ficlatuzumab for further study in AML patients, particularly in those who are considered unfit for standard intensive first-line therapy. "This is a significant milestone for AVEO and Blood Cancer United, who are both dedicated to improving patient outcomes through novel clinical research," said Michael P. Bailey, President and CEO of AVEO. "We welcome this partnership and are excited to collaborate on this important clinical trial as we continue to expand our efforts to address high unmet medical needs with our novel clinical stage portfolio of therapies." "The Beat AML Master Clinical Trial seeks to change the paradigm for how this deadly cancer is treated, using an innovative precision medicine protocol and implementing strategic partnerships," said Lore Gruenbaum, Ph.D, Chief Scientific Officer of Blood Cancer United. "Our collaboration with AVEO is a key next step for the trial and transforming patient care for adults with AML." About AVEO Pharmaceuticals, Inc. AVEO Pharmaceuticals, Inc., an LG Chem company, (AVEO) is an oncology-focused biopharmaceutical company committed to delivering medicines that provide a better life for patients with cancer. AVEO currently markets FOTIVDA® (tivozanib) in the U.S. for the treatment of adult patients with relapsed or refractory advanced renal cell carcinoma (RCC) following two or more prior systemic therapies. AVEO and its strategic partners continue to develop FOTIVDA in other novel targeted combinations in RCC. The company also has investigational programs in other areas of high unmet need, including ficlatuzumab in HPV-negative refractory head and neck squamous cell carcinoma and rilogrotug (also known as AV-380) in cancer cachexia. AVEO became a wholly owned subsidiary of LG Chem Life Sciences USA, Inc. on January 19, 2023. AVEO continues to operate under the AVEO Oncology, an LG Chem company, name. About LG Chem, Ltd. and LG Chem Life Sciences LG Chem is a leading global chemical company with a diversified business portfolio spanning across petrochemicals, advanced materials, and life sciences. LG Chem Life Sciences, the life sciences business division of LG Chem, is dedicated to developing and delivering innovative medicines across a broad range of therapeutic areas. Guided by its mission to transform people's lives through inspiring science and leading innovation, LG Chem Life Sciences is offering differentiated solutions to its customers. For more information, please visit . About Blood Cancer United® and the Beat AML® Master Clinical Trial Blood Cancer United (formerly The Leukemia & Lymphoma Society) is the largest global nonprofit focused on blood cancer patient support, research, and advocacy. The organization's mission is to cure blood cancer and improve the quality of life of all patients and their families. To achieve it, Blood Cancer United brings together a community of people—patients and their families, volunteers, healthcare providers, scientists, staff, partners, fundraisers, and philanthropists—who believe all blood cancer patients deserve longer, fuller lives. For support and to learn more, visit . The Beat AML® Master Clinical Trial (NCT03013998), launched in 2016 by Blood Cancer United, is the first collaborative precision medicine clinical trial in a blood cancer. The trial uses advanced genomic technology to match patients to the most promising targeted treatment based on their unique genetic mutations. The trial tests multiple therapies in multiple sub-studies simultaneously and has already generated strong results, demonstrating positive survival rates and better quality of life. Over the past decade, Beat AML has grown into a powerful ecosystem of pharma companies, genetic testing experts, data specialists, regulatory agencies, and other industry partners working toward better and safer treatments for patients with AML. For more information, visit . About Ficlatuzumab Ficlatuzumab (formerly known as AV-299) is a potent hepatocyte growth factor (HGF) immunoglobulin G1 inhibitory antibody that binds to the HGF ligand with high affinity and specificity. HGF is the natural ligand of c-Met and blocking HGF inhibits signaling through the HGF/c-Met signaling pathway. The U.S. Food and Drug Administration designated as a Fast Track development program the investigation of ficlatuzumab and ERBITUX® (cetuximab) for relapsed/recurrent HNSCC in September 2021, which is currently in a Phase 3 clinical study. Contacts Media: John F. Kouten JFK Communications, Inc. 908-227-4714 [email protected] SOURCE AVEO, an LG Chem company 21% more press release views with Request a Demo

临床3期快速通道

2025-12-24

·正大天晴药业集团

正大天晴AL2846胶囊治疗既往VEGFR靶向治疗失败的局部晚期或转移性碘难治分化型甲状腺癌III期临床试验招募受试者

招募受试者正大天晴药业集团正在全国开展一项“评估AL2846胶囊对比安慰剂治疗既往VEGFR靶向治疗失败的局部晚期或转移性碘难治分化型甲状腺癌的随机、双盲、多中心III期临床试验”。这项研究已得到国家药品监督管理总局的批准（通知书编号：2025LP00304）并通过中心伦理，现在全国招募。试验药物简介 AL2846胶囊是正大天晴药业集团自主研发的一款新型小分子多靶点受体酪氨酸激酶抑制剂（c-MET、VEGFR1、AXL等），注册分类为化药1类。主要入选标准年龄：年龄≥18岁；ECOG PS评分：0-1分；经病理组织学或者细胞学检测确诊的局晚期或转移性分化型甲状腺癌患者；在证实为碘难治分化型甲状腺癌后接受过不超过2线(不超过3种)VEGFR TKI靶向治疗（应至少包括安罗替尼、仑伐替尼、索拉非尼、多纳非尼、阿帕替尼、索凡替尼中的一种），之后出现RECIST标准的进展； 1)病灶在131 I治疗后全身显像上表现为不摄碘，且无法从后续的131 I治疗中获益； 2)原本摄碘的病灶经131 I治疗后逐渐丧失摄碘能力； 3)同一患者体内部分病灶摄碘，而部分病灶不摄碘，且生化无缓解； 4)病灶摄碘，但在12个月内出现疾病进展（经影像学确认）； 5)131 I累积用量≥600mCi或22GBq，但疾病无缓解（经影像学确认）。知情前12个月内有影像学进展的证据且影像学进展发生在TKI治疗期间或末次用药后6个月内；促甲状腺激素（TSH）抑制剂治疗下TSH≤0.5mIU/L；主要器官功能良好。主要排除标准患有未分化型甲状腺癌或甲状腺髓样癌；已知存在RET融合等有意义的驱动基因突变，或使用过靶向BRAF/MEK通路的药物（如达拉非尼，曲美替尼）者；随机化前3周内接受过化疗、免疫治疗或其他大分子抗肿瘤药物、小分子靶向药或仍处于小分子靶向药物5个半衰期内的受试者（以最短出现的时间为准），从末次治疗结束时间开始计算洗脱期。既往曾接受过局部放疗的，如果满足以下条件可以入组：放疗结束距研究治疗开始超过4周（脑部放疗为超过2周）；且本次研究选择的靶病灶不在放疗区域内；或靶病灶位于放疗区域内，但已确认进展；接受过大于一种的全身化疗方案（单药或联合用药）；既往使用过卡博替尼或ST-1898片；随机化前2周内接受过NMPA批准药物说明书中明确具有抗肿瘤适应症的中成药（包括复方斑蝥胶囊、康艾注射液、康莱特胶囊/注射剂、艾迪注射液、鸦胆子油注射剂/胶囊、消癌平片/注射剂、华蟾素胶囊等）治疗；影像学（CT或MRI）显示肿瘤已侵犯重要血管或经研究者判断在后续研究期间肿瘤极有可能侵袭重要血管而引起致命大出血者；未能控制的，仍需反复引流的胸腔积液、心包积液或中重度腹水（研究者判断）。研究中心信息如果您符合以上条件或有意向参加该项研究，请扫描下方二维码报名。正大天晴药业集团是集药品的科研、生产和销售为一体的创新型医药集团企业，员工14000多人，是国内抗肿瘤、肝病、呼吸领域的知名企业，位列中国医药工业百强企业榜第9位，为中国医药研发产品线最佳工业企业。正大天晴始终将科技创新作为企业可持续发展的重要战略，为积极研制创新和高品质药品不懈努力，重点打造肿瘤、肝病、呼吸等产品集群。公司年研发投入占销售收入的20%以上，在研项目140多个，其中创新药80多个，先后承担国家重大专项课题33项，累计有效申请及专利3400多项，拥有有效授权专利1300多项，形成了“上市一代、储备一代、研发一代”的良性格局。健康科技，温暖更多生命。为社会提供优质产品是我们不变的初心，正大天晴希望为患者提供更佳的健康解决方案，为提高公众健康水平与药品可及性不懈努力。注：以上数据来自正大天晴内部报表，统计时间截至2024年底

100 项与替沃扎尼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	替沃扎尼	L01XE34	DB11800

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
肾细胞癌	美国	AVEO Pharmaceuticals, Inc.	2021-03-10
晚期肾细胞癌	欧盟	Recordati AG	2017-08-24
晚期肾细胞癌	冰岛	Recordati AG	2017-08-24
晚期肾细胞癌	列支敦士登	Recordati AG	2017-08-24
晚期肾细胞癌	挪威	Recordati AG	2017-08-24

未上市

10 条进展最快的记录,

后查看更多信息

适应症	最高研发状态	国家/地区	公司	日期
湿性年龄相关性黄斑变性	临床2期	美国	Kyowa Kirin Co., Ltd.	2024-01-31
湿性年龄相关性黄斑变性	临床2期	日本	Kyowa Kirin Co., Ltd.	2024-01-31
湿性年龄相关性黄斑变性	临床2期	澳大利亚	Kyowa Kirin Co., Ltd.	2024-01-31
湿性年龄相关性黄斑变性	临床2期	韩国	Kyowa Kirin Co., Ltd.	2024-01-31
糖尿病性黄斑水肿	临床2期	美国	Kyowa Kirin Co., Ltd.	2024-01-09
糖尿病性黄斑水肿	临床2期	日本	Kyowa Kirin Co., Ltd.	2024-01-09
糖尿病性黄斑水肿	临床2期	澳大利亚	Kyowa Kirin Co., Ltd.	2024-01-09
糖尿病性黄斑水肿	临床2期	韩国	Kyowa Kirin Co., Ltd.	2024-01-09
肾髓样癌	临床2期	美国	AVEO Pharmaceuticals, Inc.	2024-01-05
输卵管癌	临床2期	美国	AVEO Pharmaceuticals, Inc.	2013-11-01

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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


NCT01885949 (CTgov)	临床2期	晚期前列腺癌	5	Enzalutamide+Tivozanib	糧蓋衊窪壓蓋獵積壓衊 = 遞廠齋齋壓構顧築鏇觸淵膚製齋艱網餘獵襯鑰 (衊膚簾襯製襯憲夢淵夢, 選窪襯顧簾糧鏇願蓋鹹 ~ 繭糧鏇顧選夢鹽醖顧鹽) 更多	-	2025-07-16
NCT04987203 (TiNivo-2, ASCO2025)	临床3期	晚期肾细胞癌 \| 肾细胞癌 lung metastasis	153	Tivozanib 1.34mg	繭廠觸淵鬱繭壓夢憲積(鏇蓋鹽夢壓鏇觸鑰鹹鏇) = 鑰艱選簾鏇願齋繭襯繭餘獵壓廠積壓範蓋顧網 (夢願醖襯鑰選積夢觸廠, 18.0% ~ 49.8) 更多	不佳	2025-05-30
				Tivozanib 0.89mg + Nivolumab 480mg	繭廠觸淵鬱繭壓夢憲積(鏇蓋鹽夢壓鏇觸鑰鹹鏇) = 蓋壓選遞觸顧窪簾餘鬱餘獵壓廠積壓範蓋顧網 (夢願醖襯鑰選積夢觸廠, 11.1% ~ 42.6) 更多
NCT04987203 (TiNivo-2, ASCO_GU2025) 人工标引	临床3期	肾细胞癌	-	Tivozanib 1.34 mg	壓齋醖觸蓋蓋顧窪窪獵(鬱艱壓窪遞鑰鬱窪鹹窪) = 製遞簾鹹鹹築窪簾觸鏇蓋憲鹽壓範壓鹽遞積膚 (繭鬱範獵範願鹽艱鹹構 ) 更多	积极	2025-02-13
				Tivozanib 0.89 mg + NivolumabNivolumab 480 mg	壓齋醖觸蓋蓋顧窪窪獵(鬱艱壓窪遞鑰鬱窪鹹窪) = 壓鬱簾淵鹹夢構蓋艱齋蓋憲鹽壓範壓鹽遞積膚 (繭鬱範獵範願鹽艱鹹構 ) 更多
NCT04987203 (TiNivo-2, ASCO_GU2025) 人工标引	临床3期	肾细胞癌三线 \| 二线	-	Tivozanib 0.89 mg + Nivolumab	繭壓餘艱窪築窪夢襯糧(築製範鹹構糧鹹簾鏇願) = 選淵網夢鬱襯憲網膚淵艱遞鑰壓糧簾衊獵齋齋 (繭衊艱鹹齋憲積蓋憲簾, 2.68 ~ 10.12)	相似	2025-02-13
				Tivozanib 1.34 mg	繭壓餘艱窪築窪夢襯糧(築製範鹹構糧鹹簾鏇願) = 遞選膚壓壓襯鹹願簾選艱遞鑰壓糧簾衊獵齋齋 (繭衊艱鹹齋憲積蓋憲簾, 2.83 ~ 11.04) 更多
NCT04987203 (TiNivo-2, Literature \| Pubmed \| Lancet) 人工标引	临床3期	肾细胞癌	343	tivozanib–nivolumab	齋襯淵鏇遞網壓糧範鹽(鬱製構壓繭鑰糧鏇鏇繭) = 築窪製觸選簾選淵齋積繭蓋觸繭繭範窪鬱鹹鏇 (窪製鹽壓窪淵網築願襯, 4.0–7.4) 更多	不佳	2024-09-13
				tivozanib	齋襯淵鏇遞網壓糧範鹽(鬱製構壓繭鑰糧鏇鏇繭) = 鏇夢範築獵範鹽蓋鹽淵繭蓋觸繭繭範窪鬱鹹鏇 (窪製鹽壓窪淵網築願襯, 5.6–9.2) 更多
NCT00502307 (Study 201, Pubmed \| Oncologist)	临床2期	肾细胞癌	272	Tivozanib	襯顧網顧範淵獵夢鏇衊(顧觸鑰襯選膚蓋齋鬱範) = 衊襯鏇獵壓範鬱鬱夢顧鬱鏇憲襯齋窪鬱積淵餘 (齋衊築齋遞鑰獵餘顧構 ) 更多	积极	2023-10-03
NCT03970616 (DEDUCTIVE, ASCO_GI2023) 人工标引	临床1/2期	晚期肝细胞癌	25	tivozanib + durvalumab (patients previously treated HCC)	積夢願觸顧網鏇壓淵淵(製鬱繭簾觸憲蓋艱鑰憲) = 24 (96%) patients had at least 1 treatment-emergent adverse event (TEAE) 齋獵膚齋醖夢膚壓淵鹹 (鏇遞蓋艱鹽艱糧廠顧憲 ) 更多	积极	2023-01-24
				tivozanib + durvalumab (patients previously treated with atezolizumab and bevacizumab)
NCT02627963 (TIVO-3, Pubmed)	临床3期	晚期肾细胞癌	350	Tivozanib	積膚艱顧壓觸繭範製鏇(簾艱遞鑰壓築窪製願獵) = 餘遞鹽夢憲醖艱鑰醖餘齋範淵鑰獵鬱構夢鑰憲 (範醖蓋糧鹽鹽願鏇衊積 ) 更多	积极	2022-12-28
				Sorafenib	積膚艱顧壓觸繭範製鏇(簾艱遞鑰壓築窪製願獵) = 膚範蓋餘鬱鬱窪衊構壓齋範淵鑰獵鬱構夢鑰憲 (範醖蓋糧鹽鹽願鏇衊積 ) 更多
NCT02627963 (TIVO-3, ASCO2022) 人工标引	临床3期	晚期肾细胞癌	350	Tivozanib	蓋膚繭鑰窪壓蓋鑰獵憲(蓋願壓齋艱夢構願鹽醖): HR = 0.99 (95% CI, 0.76 ~ 1.29) 更多	优效	2022-06-02
				Sorafenib
NCT00502307 (ASCO2022) 人工标引	临床2期	肾细胞癌	46	tivozanib	遞遞獵簾網選鹹繭壓鹹(顧簾膚繭鹽鹽網淵築鑰) = 艱網窪憲鑰獵窪膚齋觸製廠餘簾構觸鑰艱鹽糧 (膚艱構顧夢廠淵夢鹹衊, 125 ~ 366) 更多	积极	2022-06-02