甲磺酸仑伐替尼(Lenvatinib mesylate) - 药物靶点：FGFR1 x FGFR2 x FGFR3 x FGFR4 x PDGFRα x RET x VEGFR1 x VEGFR2 x VEGFR3 x c-Kit_在研适应症：晚期子宫内膜癌，复发性子宫内膜癌，胸腺肿瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

lenvatinib、lenvatinib mesilate、Lenvatinib mesilate (JAN)

+ [10]

靶点

FGFR1 x FGFR2 x FGFR3 x FGFR4 x PDGFRα x RET x VEGFR1 x VEGFR2 x VEGFR3 x c-Kit

作用机制

FGFR1拮抗剂(成纤维细胞生长因子受体-1拮抗剂)、FGFR2拮抗剂(成纤维细胞生长因子受体-2拮抗剂)、FGFR3拮抗剂(成纤维细胞生长因子受体-3拮抗剂)

治疗领域

肿瘤消化系统疾病内分泌与代谢疾病+ [10]

在研适应症

晚期子宫内膜癌复发性子宫内膜癌胸腺肿瘤+ [74]

非在研适应症

晚期胃癌晚期非小细胞肺癌甲状腺未分化癌+ [26]

原研机构

Eisai Co., Ltd.

在研机构

Eisai Co., Ltd.

Merck Sharp & Dohme Corp.

Eisai, Inc.

+ [6]

非在研机构

Merck & Co., Inc.

江苏康宁杰瑞生物制药有限公司

最高研发阶段批准上市

首次获批日期

美国 (2015-02-13),

甲状腺癌

最高研发阶段(中国)批准上市

特殊审评突破性疗法 (美国)、加速批准 (美国)、孤儿药 (美国)、优先审评 (中国)、附条件批准 (中国)、孤儿药 (日本)、孤儿药 (澳大利亚)、优先审评 (澳大利亚)、特殊审批 (中国)

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结构

分子式C22H23ClN4O7S

InChIKeyHWLFIUUAYLEFCT-UHFFFAOYSA-N

CAS号857890-39-2

关联

631

项与甲磺酸仑伐替尼相关的临床试验

NCT05077215 / Not yet recruiting临床3期

A Phase 3, Randomized, Open-Label, Active-Controlled, Superiority Trial of EG007, Added to the Combination of Lenvatinib Plus Pembrolizumab Vs. Lenvatinib Plus Pembrolizumab in Patients with Advanced Endometrial Cancer

This is a Phase 3, multicenter, randomized, open-label trial to evaluate whether EG-007 plus Len+Pem is superior to Len+Pem alone in patients with advanced endometrial cancer (Stage III or IV). This trial will be preceded by a safety lead-in study with up to 28 patients (the safety lead-in is a separate, free-standing protocol).
Approximately 450 patients will be randomized equally (1:1) to receive EG-007 plus Len+Pem or Len+Pem alone. The randomization will be stratified by the following stratification factors:
* Diagnosis Classification (advanced Stage III/IV vs. recurrent endometrial cancer)
* ECOG score at baseline (0 vs 1)
* Geographic region (Asia vs ROW)

开始日期2025-12-01

申办/合作机构

Evergreen Therapeutics, Inc

NCT05106127 / Not yet recruiting临床2期

A Phase 2, Open-Label, Safety Lead-In with Long Term Safety Study of EG-007, Added to the Combination of Lenvatinib Plus Pembrolizumab

This is a Phase 2 trial Safety Lead-in trial conducted in 3 cohorts of patients.
A safety lead-in study of the impact of adding the Repurposed Drugs a third agent will be conducted prior to opening enrollment into the compassionate use study. All patients enrolled in the safety lead-in study may continue long-term treatment under this protocol without interruption of dosing.

开始日期2025-08-01

申办/合作机构

Evergreen Therapeutics, Inc

NCT06669572 / Not yet recruiting临床2期IIT

A Phase II, Multi-center, Single Arm Trial of Lenvatinib Plus Pembrolizumab in Patients With Unresectable Locally Advanced and/or Metastatic Anorectal Squamous Cell Carcinoma (ASCC) After Progression on First Line Chemotherapy.

The purpose of this study is to gather information on the safety and effectiveness of lenvatinib combined with pembrolizumab in anal/rectal cancer that has spread to other parts of the body and will not respond to standard care.

开始日期2025-01-13

申办/合作机构

The University of Chicago

100 项与甲磺酸仑伐替尼相关的临床结果

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100 项与甲磺酸仑伐替尼相关的转化医学

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100 项与甲磺酸仑伐替尼相关的专利（医药）

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2,467

项与甲磺酸仑伐替尼相关的文献（医药）

2025-03-01·Annals of Hepatology

Camrelizumab combined with transcatheter arterial chemoembolization and sorafenib or lenvatinib for unresectable hepatocellular carcinoma: A multicenter, retrospective study

Article

作者: Li, Han ; Wang, Fei ; Su, Ke ; Liu, Yu ; Wang, Pan ; Xu, Ke ; Chi, Hao ; Jiang, Xiumei

INTRODUCTION AND OBJECTIVES:

We initiated this study to explore the efficacy of camrelizumab combined with transcatheter arterial chemoembolization (TACE) plus sorafenib or lenvatinib versus TACE plus sorafenib or Lenvatinib for unresectable hepatocellular carcinoma (HCC).

MATERIALS AND METHODS:

From June 2019 to November 2022, 127 advanced HCC patients were retrospectively analyzed in this study. This consisted of 44 patients that received camrelizumab plus TACE plus sorafenib or lenvatinib (triple therapy group) and 83 patients that received TACE plus sorafenib or lenvatinib (double treatment group). The overall survival (OS), progression-free survival (PFS), objective response rate (ORR), and disease control rate (DCR) were compared between the two patient groups.

RESULTS:

Our findings demonstrated that patients received the triple therapy exhibited superior median OS (15.8 vs. 10.3 months, P=0.0011) and median PFS (7.2 vs. 5.2 months, P=0.019) compared to the double treatment group. In addition, the triple therapy group exhibited better 6-month (93.5% vs. 66.3%), 12-month (67.2% vs. 36.3%), and 24-month (17.2% vs. 7.6%) survival rates than the double treatment group. However, the ORR (43.2% vs. 28.9%, P = 0.106) and DCR (93.2% vs. 81.9%, P = 0.084) of the two groups were similar. Subgroup analysis showed that compared with the double treatment group, the triple therapy group had a better mOS for HCC with HBV (15.8 vs. 9.6 months, P = 0.0015) and tumor diameter ≥ 5cm (15.3 vs. 9.6 months, P = 0.00055).

CONCLUSIONS:

Camrelizumab plus TACE and sorafenib or lenvatinib may be a promising treatment approach for the clinical management of unresectable HCC patients.

2025-02-01·BIOMATERIALS

A versatile nanoplatform carrying cascade Pt nanozymes remodeling tumor microenvironment for amplified sonodynamic/chemo therapy of thyroid cancer

Article

作者: Jiao, Lianying ; Wang, Yufeng ; Sun, Lei ; Zhou, Qi ; Zhang, Yujie ; Wang, Dan ; Ma, Wenqi ; Zhang, Yuanyuan ; Jiang, Jue ; Li, Runqing ; Zhang, Mingzhen

Thyroid cancer is increasing globally, with anaplastic thyroid carcinoma (ATC) being the most aggressive type and having a poor prognosis. Current clinical treatments for thyroid cancer present numerous challenges, including invasiveness and the necessity of lifelong medication. Furthermore, a significant portion of patients with ATC experience cancer recurrence and metastasis. To overcome this dilemma, we developed a pH-responsive biomimetic nanocarrier (CLP@HP-A) through the incorporation of Chlorin e6 (Ce6) and Lenvatinib (Len) within hollow polydopamine nanoparticles (HP) that were further modified with platinum nanoparticles (Pt), enabling synergistic chemotherapy and sonodynamic therapy. The CLP@HP-A nanocarriers exhibited specific binding with galectin-3 receptors, facilitating their internalization through receptor-mediated endocytosis for targeted drug delivery. Upon exposure to ultrasound (US) irradiation, Ce6 rapidly generated reactive oxygen species (ROS) to induce significant oxidative stress and trigger apoptosis in tumor cells. Additionally, Pt not only alleviated tumor hypoxia by catalyzing the conversion of H₂O₂ to oxygen (O₂) but also augmented intracellular ROS levels through the production of hydroxyl radicals (•OH), thereby enhancing the efficacy of sonodynamic therapy. Moreover, Len demonstrated a potent cytotoxic effect on thyroid cancer cells through the induction of apoptosis. Transcriptomics analysis findings additionally corroborated that CLP@HP-A effectively triggered cancer cell apoptosis, thereby serving as a crucial mechanism for its cytotoxic effects. In conclusion, the integration of sonodynamic/chemo combination therapy with targeted drug delivery systems offers a novel approach to the management of malignant tumors.

2025-01-01·CLINICAL ONCOLOGY

Real World Outcomes in Patients With Recurrent, Advanced, or Metastatic Endometrial Cancer Treated With Lenvatinib Plus Pembrolizumab

Article

作者: Stewart, A. ; Eminowicz, G. ; Counsell, N. ; Counsell, N ; Tookman, Laura ; Browne, R ; Pawsey, A. ; Eminowicz, G ; Ramessur, A ; Senthivel, N. ; Usman, Sadaf ; Tookman, L. ; Stewart, A ; Counsell, Nicholas ; Patel, A ; Eminowicz, Gemma ; Miller, R ; Mahalingam, P. ; Senthivel, N ; Mahalingam, Preethika ; Usman, S ; Mahalingam, P ; Turnbull, E ; Browne, Riona ; Miller, Rowan ; Ramessur, Anisha ; Nicum, S. ; Usman, S. ; Tookman, L ; Nicum, Shibani ; Pawsey, Alexander ; Turnbull, Emily ; Miller, R. ; Patel, A. ; Ramessur, A. ; Stewart, Alexandra ; Turnbull, E. ; Pawsey, A ; Nicum, S ; Browne, R. ; Patel, Apini ; Senthivel, Nishanthi

AIMS:

Patients with endometrial cancer who progress following first line therapy have improved survival outcomes with pembrolizumab and lenvatinib (pem/len) compared with standard of care chemotherapy, as demonstrated in KEYNOTE-775. This was in a group of trial patients with good performance status and excluded those with carcinosarcoma histology. In KEYNOTE-775 pem/len was associated with significant toxicity, leading to dose reductions, treatment cessation, and patient morbidity. We set out to assess the tolerability, toxicity and outcomes following pem/len for patients with recurrent, advanced or metastatic endometrial cancer in a real-world setting.

MATERIALS AND METHODS:

UK centres treating patients with pem/len for advanced endometrial cancer within the compassionate access programme were approached. Retrospective data were analysed for those treated between May 2022 and June 2023. Data on patient demographics, treatment, toxicity and outcomes were extracted from medical records. Toxicity and tolerability were compared in those over and under the age of 70.

RESULTS:

Seven centres returned data for 70 patients. Median age of patients was 68.5 years (range 45-85) with a performance status of 0-1 in 77.1% and of 2 in 22.9%. Histological subtypes included serous (34.3%), endometrioid (32.9%), carcinosarcoma (14.3%), clear cell (7.1%), mixed (2.9%) and other (8.6%). Grade ≥3 toxicity was reported in 55.7% with any-grade toxicity observed in 85.7%. In those aged ≥70 years (n = 30) the rate of grade ≥3 toxicity was 60.0%. Rates of dose reduction of lenvatinib were 64.3%, and toxicity-related treatment interruption was 45.7%. The 6-month progression-free and overall survival rates were 54.0% (95%CI: 39.0-66.8) and 70.1% (95%CI:56.5-80.1) respectively.

CONCLUSION:

This real-world, observational study of pem/len showed comparable tolerability, toxicity, and outcomes to previously reported clinical trial data. Our cohort included patients with a poorer PS and a broader range of histological subtypes including carcinosarcoma.

797

项与甲磺酸仑伐替尼相关的新闻（医药）

2024-11-15

·Pharma CMC

刚刚，石药集团前三季度业绩公布！营收226.86亿

今日（11月15日），石药集团公布2024年前三季度业绩，报告期内，收入为人民币226.86亿元，较去年同期下跌4.9%。主要受到成药业务收入下跌的影响，股东应占基本溢利39.99亿元，较去年同期下跌15.2%，股东应占溢利较去年同期下跌15.9%至人民币37.78亿元。据公告披露，石药集团成药业务收入为人民币186.70亿元，同比下降3.5%，以下为按主要治疗领域的销售情况：神经系统治疗领域于第三季度的收入较去年同季下跌15.8%，然而，与去年同期（前三季度）相比，本期该领域的收入取得整体增长4.5%。恩必普（®丁苯酞软胶囊、丁苯酞氯化钠注射液）主要因医院在严格控制医疗费用的环境下，对在医院用量排名靠前的药品实施较严格的管控，使其本年第三季度销售有较大幅度的下跌。另一方面，明复乐®（注射用重组人TNK组织型纤溶酶原激活剂）用于治疗急性缺血性卒中患者的新适应症于年初获得上市批准后，于本期取得理想的销售收入。抗肿瘤治疗领域于第三季度和本期的收入分别较去年同季和同期下跌31.2%和17.6%。下跌主要由于津优力（®聚乙二醇化重组人粒细胞刺激因子注射液）及多美素（®盐酸多柔比星脂质体注射液）两款产品的价格于京津冀「3+N」联盟药品集中采购中分别下调了约58%和23%。新产品方面，多恩益（®盐酸伊立替康脂质体注射液）、多恩达（®盐酸米托蒽醌脂质体注射液）及戈瑞特（®甲磺酸仑伐替尼胶囊）的销售于期内仍保持较高增长。心血管治疗领域于第三季度和本期的收入分别较去年同季和同期下跌26.7%和11.1%。下跌主要由于玄宁®（马来酸左氨氯地平片及分散片）并没有在2023年的国家第八批集中采购中中选，使其在严格执行集采政策的医院的销售受到较大冲击，尤其本年第二季度及第三季度的跌幅较为显着。另外，恩存®（硫酸氢氯吡格雷片）及意舒宁®（硝苯地平控释片）于期内的销售保持增长。呼吸系统治疗领域于第三季度和本期的收入分别较去年同季和同期下跌35.1%和18.8%。期内琦效（®盐酸阿比多尔片）的销售收入因市场需求减少而有较大幅度的下跌。另外，受惠于有效的推广策略及强劲的市场需求，伊络达®（乙磺酸尼达尼布软胶囊）及诺一安®（孟鲁司特钠片╱咀嚼片）的销售收入于期内保持理想增长。消化代谢治疗领域于第三季度的收入较去年同季下跌11.2%，然而，与去年同期相比，本期该领域的收入大幅增长30.7%。其中，欧倍妥®（艾司奥美拉唑镁肠溶胶囊）及得必欣®（奥美拉唑肠溶胶囊╱片╱注射剂）受惠于有效的推广策略及市场需求，增长尤其显着。 2024年前三季度，石药集团研发费用为人民币38.80亿元，较去年同期增加5.5%，约占成药业务收入20.8%。目前逾60个重点在研药物已进入临床或申报阶段，其中6个已递交上市申请，24个产品（30个适应症）处于注册临床阶段。自年初至今，于中国有2款创新药（新增适应症）、1款生物类似药、1款特殊制剂获批上市，及在研药物获得34项临床试验批件，7款仿制药获得药品注册批件；于北美地区有3款在研创新药物获得临床试验批准，1项快速通道资格认定。临床管线概览：

财报带量采购临床3期申请上市孤儿药

2024-11-14

·ioncology

国际视角丨肝癌一线免疫治疗进展后何去何从？

点击蓝字关注我们编者按免疫治疗已改变了不可切除肝细胞癌（HCC）的治疗格局。目前，阿替利珠单抗联合贝伐珠单抗（atezo-bev）和度伐利尤单抗联合tremelimumab在许多国家已获得监管部门的批准，作为HCC患者的一线治疗选择。此外，也有数据支持其他免疫治疗组合的使用，如纳武利尤单抗联合伊匹木单抗（nivo-ipi）、卡瑞利珠单抗联合瑞戈非尼和信迪利单抗联合贝伐珠单抗生物类似药。但是，对于在一线免疫治疗后疾病仍出现进展的HCC患者而言，如何确定最佳后续治疗方案成为了一个治疗难题和亟待满足的临床需求。当前国际指南普遍倾向于推荐在免疫治疗后采多激酶抑制剂（MKI）药物（诸如索拉非尼或仑伐替尼），这一建议主要基于以下几点考量：这些药物在一线治疗中的疗效与安全性已得到证实；这些药物具有广泛的可用性；同时，其作用机制也被认为是合理的。然而，需要注意的是，在此特定情境下，这些推荐尚缺乏直接基于确凿证据的支持。因此，香港中文大学威尔斯亲王医院临床肿瘤科的Landon L.Chan博士、加州大学旧金山分校Helen Diller家庭综合癌症中心的Robin K Kelley博士、香港中文大学香港癌症研究所邵逸夫爵士癌症中心转化肿瘤学国家重点实验室的Stephen L. Chan博士回顾了近日发布的前瞻性和回顾性研究数据，总结出了一套在晚期HCC患者一线免疫治疗后出现疾病进展后的治疗方法。从左到右依次为：Dr. Landon L.Chan、Dr. Robin Katie Kelley、Stephen L. Chan 一、免疫治疗进展后应用MKI的前瞻性研究数据 1.卡博替尼最近一项在亚洲进行的多中心Ⅱ期研究证明了卡博替尼在免疫治疗失败后患者中的疗效和安全性，这是该领域的第一项前瞻性证据。该研究纳入了47例接受过1种或多种前期免疫治疗的患者。总体中位无进展生存期（mPFS）为4.1个月，中位总生存期（mOS）为9.9个月。当仅限于二线治疗环境时，卡博替尼的mPFS为4.3个月，mOS为14.3个月。值得注意的是，这些数值与索拉非尼和仑伐替尼在二线环境中的真实世界疗效相当，mPFS在3~6个月之间，mOS在12~18个月之间。安全性特征与以往研究相似，最常见的不良反应包括手足皮肤反应、疲劳和腹泻。尽管如此，3级或更高级别的毒性反应并不常见，最常见的3级或更高级别的毒性反应是血小板减少症。 2.瑞戈非尼在2024年美国临床肿瘤学会胃肠道肿瘤研讨会（ASCO GI）上，另一种MKI药物瑞戈非尼被评估作为一线阿替利珠单抗联合贝伐珠单抗治疗后疾病进展的不可切除HCC患者的二线治疗方案。该研究是在韩国进行的一项前瞻性Ⅱ期临床研究，共入组40例患者，所有患者先前均接受过至少2个周期的阿替利珠单抗联合贝伐珠单抗治疗。在疗效方面，患者的mPFS为3.5个月，mOS为9.7个月，ORR为10%，疾病控制率（DCR）为82.5%。在安全性方面，高级别治疗相关不良事件（TRAEs）不常见，最常见的3~4级TRAEs包括血小板减少症（5.0%）、手足皮肤反应（2.5%）和疲劳（2.5%）。 3.瑞戈非尼联合帕博利珠单抗在2024年ASCO年会上，瑞戈非尼联合帕博利珠单抗被评估为另一种治疗一线免疫治疗失败后疾病进展的晚期HCC患者的治疗选择。在这项国际Ⅱ期研究中，共入组了95例患者，其中先前接受过阿替利珠单抗联合贝伐珠单抗治疗的患者组成队列1（68例），先前接受过其他免疫治疗的患者组成队列2（27例）。在68例先前接受阿特珠单抗联合贝伐珠单抗治疗后疾病进展并接受瑞戈非尼联合帕博利珠单抗联合治疗的患者中，mPFS为2.8个月，ORR为5.9%。在其余27例一线接受其他免疫治疗的患者中，mPFS为4.2个月，ORR为11.1%。由于随访时间相对较短（中位7.1个月），两个队列均未达到mOS。两队列中分别有37%和3%的患者观察到3级或4级药物相关治疗期不良事件，1例患者因治疗发生5级事件（心脏骤停）。对治疗无应答患者的相关性生物标志物分析显示，瑞戈非尼联合帕博利珠单抗降低了巨噬细胞水平和血管生成标志物，但未激活T细胞、减少调节性T细胞或改变非应答者中T细胞耗竭标志。二、免疫治疗进展后继续应用免疫治疗的获益上述3项研究为基于免疫治疗的方案后MKI在HCC治疗中的应用提供了初步前瞻性证据，尽管帕博利珠单抗是免疫治疗基石，但是与瑞戈非尼联合使用似乎并未比单独使用MKI带来更多获益。此外，回顾性队列研究表明，在一线免疫治疗失败后，将抗CTLA-4药物添加到抗PD-L1/抗PD-1抑制中可能具有潜在益处。在10例先前接受阿替利珠单抗联合贝伐珠单抗治疗后接受纳武利尤单抗联合伊匹木单抗联合治疗的患者中，3例（30%）患者观察到确认的客观缓解。在另一项纳入32例先前接受抗PD-L1/抗PD-1治疗随后接受纳武利尤单抗联合伊匹木单抗联合治疗的小规模研究中，ORR为22%（7/32）。因此，在一线免疫治疗进展后继续免疫治疗是否有益仍不明确。一项正在进行的Ⅲ期试验（IMbrave251；NCT04770896）也试图回答这个问题，方法是将在使用阿替利珠单抗联合贝伐珠单抗治疗后疾病进展的患者随机分配接受阿替利珠单抗联合仑伐替尼或索拉非尼治疗，或仅接受仑伐替尼或索拉非尼单药治疗。三、免疫治疗后寡进展应用放疗及其他局部区域治疗的获益寡进展是指经系统治疗后残留病灶有限或仅有少量病灶（通常为3~5个）开始进展。该现象在肺癌、结直肠癌和前列腺癌中常见，但在HCC中描述较少。考虑到潜在的第二原发肿瘤可能因肝脏损伤的基础场效应和转移时的基因组差异而出现，所以对寡进展进行治疗可能在HCC中特别有益，这提示不同疾病克隆对免疫治疗的反应可能不同，为部分患者进行局部治疗提供了理论依据。最近的一项回顾性研究报道了54例对免疫治疗有初步持久反应并随后进展的晚期HCC患者的进展模式。其中，2/3的患者在接受免疫治疗后出现寡进展。对于出现寡进展的患者，又有2/3的患者接受了某种形式的局部区域治疗。接受局部区域治疗的患者mOS长于未接受局部区域治疗的患者（46.2 vs. 22.2个月）。综上所述，3项前瞻性Ⅱ期临床研究探索了在免疫治疗进展后应用MKI方案的疗效，并取得了初步成果。此外，新兴的回顾性研究还表明，对于寡进展患者，加用抗CTLA-4或局部区域治疗可能有益。因此，在总结上述最新证据的基础上，研究者总结出了在晚期HCC患者一线免疫治疗后出现疾病进展后的治疗方法（图1），以供大家参考。图.1 晚期HCC患者免疫治疗进展后的拟治疗方法四、前瞻性数据仍缺乏，多学科诊疗是关键当前关于一线免疫治疗失败后不可切除HCC的治疗决策，前瞻性数据仍然有限，但各方向上的证据正在涌现，如改用二线MKI、替代基于免疫治疗的方案（如抗CTLA-4联合方案）以及为寡进展添加局部区域治疗。多项Ⅱ期研究正在进行中，以测试一线免疫治疗失败后这些策略的有效性（表1）。但是，当前由于前瞻性数据仍然稀缺，多学科诊疗仍然是确定每例患者最佳治疗的关键。当然，我们也非常需要生物标志物研究，包括肿瘤微环境分析以及原发性和获得性基因组异质性分析，以便为HCC患者在日益增多的治疗选择中，精准选择最有效的治疗策略。表1. 免疫治疗进展后系统治疗的在研研究参考资料： https://dailynews-ascopubs-org.libproxy1.nus.edu.sg/do/systemic-therapy-hepatocellular-carcinoma-s-next-after-immunotherapy （来源：肿瘤瞭望消化时讯）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。

ASCO会议免疫疗法临床结果

2024-11-14

·BioPharmaDive

Merck, facing threat to Keytruda, buys into new kind of cancer immunotherapy

Merck & Co. has bought into the kind of drug that has emerged as a top threat to its dominant cancer immunotherapy Keytruda.The company said Thursday it agreed to pay privately-held LaNova Medicines $588 million in cash for worldwide rights to a cancer therapy called LM-299,which is currently in Phase 1 testing in China. LaNova, which is based in Shanghai, could receive up to $2.7 billion in additional payments should the drug hit various development and sales milestones across multiple indications.The deal makes Merck the latest company to acquire a type of dual-pronged cancer immunotherapy thats fast become a top target of drugmakers. These so-called bispecific therapies simultaneously home in on the proteins PD-1 and VEGF, which help tumors grow and evade detection from the immune system.This year, one such drug, ivonescimab, from China-based Akeso and development partner Summit Therapeutics, bested Mercks Keytruda in a late-stage trial in lung cancer the first time thats happened since Keytrudas arrival a decade ago. Though the results came with notable limitations and are unlikely to support a U.S. approval, since then, an array of drugmakers have either acquiredPD-1 and VEGF-targeting bispecifics or built new companiesaround them. Just yesterday, BioNTech agreed to pay $800 million to buy biotech Biotheus, giving it a PD-1 and VEGF drug the companies have been co-developing.Merck has a particularly vested interest in the progress of PD-1 and VEGF bispecifics. Keytruda is the worlds most widely used cancer immunotherapy, having earned 40 approvals since its first in 2014. The drug accounted for $25 billion of Mercks $60 billion in revenue last year, when it officially became the worlds best-selling medicine.But there is still room for improvement, as the majority of people dont durably respond to Keytruda and other drugs like it. Keytruda will also lose patent protection in the U.S. in 2028, after which Merck will be pressed to replace lost revenues.Merck, for its part, has been leaning on a pipeline of drugs for cancer, heart and immune diseases to cover some of those anticipated losses, as well as a formulation of Keytruda administered via subcutaneous injection instead of intravenously. Its also been pairing Keytruda with medicines that target VEGF or related pathways. One such combination, with Eisais Lenvima, is approved for a few tumor types, though it failed to extend survival in a late-stage trial in lung cancer. The company has made a substantial investment in that pathway, said Merck research chief Dean Li, referring to VEGF, on a conference call with analysts last month. Li, at the time, pointed out some key unknowns in Summit and Akesos data, such as whether ivonescimab will prolong survival and how the drug will perform when compared to the Keytruda-chemotherapy regimen thats now standard treatment for most lung cancer cases. I think its really important for all of us to watch carefully, and we are watching carefully, he told analysts. That Merck quickly turned to acquire an ivonescimab-like drug suggests it was either looking for an insurance policy or now has greater conviction on Akeso and Summits results, wrote Evercore ISI analyst Umer Raffat in a Thursday note to investors.Should ivonescimab pan out, for example, the deal will have created the most direct path for Merck to hold on to a very large chunk of the Keytruda franchise, Raffat wrote. Though LaNovas drug is well behind many others in development, among them ivonescimab, Merck will very likely progress very rapidly.However you look at it, this is incredibly savvy [business development] for a very reasonable price, Raffat added.In its statement, Merck said LM-299 has a differentiated molecular design than others in development, consisting of an anti-VEGF antibody fused to two PD-1-targeting antibodies. '

免疫疗法上市批准临床1期并购抗体药物偶联物

100 项与甲磺酸仑伐替尼相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D09920	甲磺酸仑伐替尼	L01XE	DB09078

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
晚期子宫内膜癌	欧盟	Eisai GmbH	2023-07-25
晚期子宫内膜癌	冰岛	Eisai GmbH	2023-07-25
晚期子宫内膜癌	列支敦士登	Eisai GmbH	2023-07-25
晚期子宫内膜癌	挪威	Eisai GmbH	2023-07-25
复发性子宫内膜癌	欧盟	Eisai GmbH	2023-07-25
复发性子宫内膜癌	冰岛	Eisai GmbH	2023-07-25
复发性子宫内膜癌	列支敦士登	Eisai GmbH	2023-07-25
复发性子宫内膜癌	挪威	Eisai GmbH	2023-07-25
胸腺肿瘤	日本	Eisai Co., Ltd.	2021-03-23
晚期肾细胞癌	欧盟	Eisai GmbH	2016-08-25
晚期肾细胞癌	冰岛	Eisai GmbH	2016-08-25
晚期肾细胞癌	列支敦士登	Eisai GmbH	2016-08-25
晚期肾细胞癌	挪威	Eisai GmbH	2016-08-25
子宫内膜癌	澳大利亚	Eisai Co., Ltd.	2016-01-28
肾细胞癌	澳大利亚	Eisai Co., Ltd.	2016-01-28
晚期肝细胞癌	欧盟	Eisai GmbH	2015-05-28
晚期肝细胞癌	冰岛	Eisai GmbH	2015-05-28
晚期肝细胞癌	列支敦士登	Eisai GmbH	2015-05-28
晚期肝细胞癌	挪威	Eisai GmbH	2015-05-28
分化型甲状腺癌	欧盟	Eisai GmbH	2015-05-28

未上市

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适应症	最高研发状态	国家/地区	公司	日期
晚期非小细胞肺癌	临床3期	中国	江苏康宁杰瑞生物制药有限公司	2021-10-28
食管鳞状细胞癌	临床3期	美国	Eisai, Inc.	2021-07-28
食管鳞状细胞癌	临床3期	美国	Merck Sharp & Dohme Corp.	2021-07-28
食管鳞状细胞癌	临床3期	中国	Merck Sharp & Dohme Corp.	2021-07-28
食管鳞状细胞癌	临床3期	中国	Eisai, Inc.	2021-07-28
食管鳞状细胞癌	临床3期	日本	Eisai, Inc.	2021-07-28
食管鳞状细胞癌	临床3期	日本	Merck Sharp & Dohme Corp.	2021-07-28
食管鳞状细胞癌	临床3期	阿根廷	Eisai, Inc.	2021-07-28
食管鳞状细胞癌	临床3期	阿根廷	Merck Sharp & Dohme Corp.	2021-07-28
食管鳞状细胞癌	临床3期	加拿大	Eisai, Inc.	2021-07-28

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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


NCT05523323 (CTgov)	临床3期	复发性头颈部鳞状细胞癌	112	pembrolizumab+Lenvatinib (Pembrolizumab + Lenvatinib)	蓋製網築糧糧觸願鏇選(選艱壓廠繭壓鏇鏇構鑰) = 廠艱網憲顧鑰淵憲積襯壓廠醖糧鹹餘夢觸顧構 (觸糧齋鏇顧範艱鹽網餘, 夢積衊構夢顧齋積鬱餘 ~ 齋襯餘鏇壓製顧鹽觸壓) 更多	-	2024-10-18
				Placebo+pembrolizumab (Pembrolizumab + Placebo)	蓋製網築糧糧觸願鏇選(選艱壓廠繭壓鏇鏇構鑰) = 襯憲廠遞衊蓋構範窪憲壓廠醖糧鹹餘夢觸顧構 (觸糧齋鏇顧範艱鹽網餘, 醖齋鹹襯鹽膚鹽壓願顧 ~ 鑰積醖網製夢夢繭窪廠) 更多
NCT04865289 (MK-7902-001 \| LEAP-001 \| ENGOT-en9, CTgov)	临床3期	复发性子宫内膜癌	130	pembrolizumab+Lenvatinib (Lenvatinib + Pembrolizumab)	遞壓簾鏇鏇網鏇餘醖壓(蓋膚網壓憲襯構鹹網築) = 壓襯糧獵網膚鬱積鹽選遞簾醖襯夢構顧夢築襯 (膚鏇鬱衊醖鏇願網廠願, 壓憲鬱繭鑰觸艱鑰鬱餘 ~ 糧構選鹽窪鏇蓋鑰襯觸) 更多	-	2024-10-18
				Carboplatin+Paclitaxel (Paclitaxel + Carboplatin)	遞壓簾鏇鏇網鏇餘醖壓(蓋膚網壓憲襯構鹹網築) = 鏇顧憲遞遞廠製願範簾遞簾醖襯夢構顧夢築襯 (膚鏇鬱衊醖鏇願網廠願, 膚製築範積夢鏇壓鑰鹹 ~ 鬱網膚蓋觸觸餘簾窪憲) 更多
NCT03884101 (MK-7902-001 \| ENGOT-en9/LEAP-001 \| LEAP-001 \| ENGOT-en9, CTgov)	临床3期	复发性子宫内膜癌	842	pembrolizumab+Lenvatinib (Lenvatinib + Pembrolizumab)	簾夢積鏇鹹壓觸襯構顧(廠築繭糧網網製構齋觸) = 醖顧鑰糧鏇廠願遞衊衊廠齋壓鑰網鏇窪蓋鑰鹽 (積憲網獵鹽願齋觸遞鏇, 艱蓋齋構廠製淵構繭憲 ~ 夢願膚夢襯構願艱構襯) 更多	-	2024-10-16
				Carboplatin+Paclitaxel (Paclitaxel + Carboplatin)	簾夢積鏇鹹壓觸襯構顧(廠築繭糧網網製構齋觸) = 憲觸艱鹹鹽鹽簾餘衊網廠齋壓鑰網鏇窪蓋鑰鹽 (積憲網獵鹽願齋觸遞鏇, 醖鑰鏇糧觸積遞壓選鹽 ~ 構築築鹽網夢醖鏇鬱選) 更多
NCT03776136 (LEAP-004 \| E7080-G000-225 \| 7902-004 \| MK-7902-004, CTgov)	临床2期	黑色素瘤	103	Pembrolizumab+Lenvatinib	淵獵繭簾鹽餘鬱網淵繭(餘遞鏇糧憲繭獵繭蓋遞) = 窪壓鑰積構選網網蓋築蓋願積繭築積蓋鏇淵壓 (鏇憲範鹹築襯餘顧壓遞, 鹹網齋遞艱選觸窪願製 ~ 窪憲憲窪壓膚鹽壓鬱簾) 更多	-	2024-10-09
NCT04716933 (MK-7902-006 \| E7080-G000-315 \| LEAP-006, CTgov)	临床3期	转移性非鳞状非小细胞肺癌	201	Carboplatin+Cisplatin+pembrolizumab+Pemetrexed+Lenvatinib (Pemetrexed+Platinum Chemotherapy+Pembrolizumab+Lenvatinib)	獵蓋網遞鬱鹹觸窪顧鏇(膚衊醖蓋膚壓糧憲鹽遞) = 觸衊淵齋鏇餘齋繭鹽餘餘餘壓製築築鹽襯鹹選 (餘獵鑰廠鬱襯製廠憲齋, 鏇鑰淵蓋鑰範艱壓選簾 ~ 積鹽範鹽鑰獵壓網蓋廠) 更多	-	2024-10-04
				Placebo matching lenvatinib+Carboplatin+Cisplatin+pembrolizumab+Pemetrexed (Pemetrexed+Platinum Chemotherapy+Pembrolizumab+Placebo)	獵蓋網遞鬱鹹觸窪顧鏇(膚衊醖蓋膚壓糧憲鹽遞) = 餘範壓餘襯鏇簾選膚襯餘餘壓製築築鹽襯鹹選 (餘獵鑰廠鬱襯製廠憲齋, 鏇廠獵鑰齋鑰積網鑰觸 ~ 網衊觸淵簾襯範鹹廠遞) 更多
NCT04763408 (STELLAR, ESMO2024) 人工标引	临床4期	肝细胞癌一线	242	Lenvatinib	衊糧襯憲積艱製衊艱餘(構醖鬱簾鹹觸遞艱鹽顧) = 餘鑰鏇觸糧衊蓋夢糧構鏇鹽鹹蓋遞壓鹽齋鬱衊 (襯壓選鏇觸願艱膚憲築 ) 更多	积极	2024-09-16
				Sorafenib	衊糧襯憲積艱製衊艱餘(構醖鬱簾鹹觸遞艱鹽顧) = 鑰網顧築繭夢窪餘夢蓋鏇鹽鹹蓋遞壓鹽齋鬱衊 (襯壓選鏇觸願艱膚憲築 ) 更多
NCT05042336 (BRHCC, ESMO2024) 人工标引	临床1/2期	肝细胞癌	54	TACE combined with Lenvatinib and Camrelizumab (All cohort)	夢築鏇蓋積鏇壓餘憲膚(鏇網積齋壓鬱夢顧觸齋) = 夢壓構蓋醖選蓋築鏇鬱觸醖鑰築構夢衊壓遞齋 (鹽願顧遞衊網範鑰蓋觸 ) 更多	积极	2024-09-16
				TACE combined with Lenvatinib and Camrelizumab (Phase Ib)	夢築鏇蓋積鏇壓餘憲膚(鏇網積齋壓鬱夢顧觸齋) = 範憲鹽積淵鏇鹹鹹壓顧觸醖鑰築構夢衊壓遞齋 (鹽願顧遞衊網範鑰蓋觸 ) 更多
ESMO2024 人工标引	N/A	肝细胞癌一线	1,361	Lenvatinib (LEN)	選淵製範觸構鹹鬱網膚(選願夢艱夢艱餘鏇齋遞) = 衊築襯蓋蓋蓋積夢鬱夢製夢壓鹽獵顧積選糧構 (範遞壓獵糧夢鏇齋選遞, 8.3 ~ 10.8) 更多	积极	2024-09-16
				Sorafenib (SOR)	選淵製範觸構鹹鬱網膚(選願夢艱夢艱餘鏇齋遞) = 窪製觸襯網蓋壓醖願艱製夢壓鹽獵顧積選糧構 (範遞壓獵糧夢鏇齋選遞, 6.4 ~ 9.3) 更多
NCT04745988 (EPOC2001 \| LEAP-015, ESMO2024) 人工标引	临床2期	胃食管交界处腺癌辅助 \| 新辅助	32	Lenvatinib+pembrolizumab+FLOT	膚齋網顧鑰廠繭鏇構獵(鏇膚齋餘築糧築願觸憲) = 齋範顧齋繭糧觸構鏇鬱鏇醖願獵鬱壓鹹顧製選 (築鏇廠網遞構製齋鬱選, 34 ~ 60) 达到更多	积极	2024-09-16
ESMO2024	N/A	肝细胞癌二线	137	Lenvatinib	艱觸顧憲觸積襯窪淵窪(蓋繭廠廠鹽廠淵鑰顧夢) = 顧衊築夢獵鹽蓋繭淵範齋壓願廠醖鹹蓋廠夢齋 (艱衊夢餘鏇襯觸膚鏇積 ) 更多	积极	2024-09-16
				Sorafenib	艱觸顧憲觸積襯窪淵窪(蓋繭廠廠鹽廠淵鑰顧夢) = 鏇壓築窪遞糧網壓構壓齋壓願廠醖鹹蓋廠夢齋 (艱衊夢餘鏇襯觸膚鏇積 ) 更多