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更新于：2025-02-18
Lenvatinib mesylate
甲磺酸仑伐替尼
更新于：2025-02-18
概要
基本信息
药物类型 小分子化药 |
别名 lenvatinib、lenvatinib mesilate、Lenvatinib mesilate (JAN) + [18] |
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) |
原研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2015-02-13), |
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)、特殊审批 (中国)、孤儿药 (日本)、孤儿药 (澳大利亚)、优先审评 (澳大利亚)、附条件批准 (中国) |
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结构/序列
分子式C22H23ClN4O7S |
InChIKeyHWLFIUUAYLEFCT-UHFFFAOYSA-N |
CAS号857890-39-2 |
关联
622
项与 甲磺酸仑伐替尼 相关的临床试验NCT06669572
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.
NCT05077215
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
NCT05106127
A Phase 2, Open-Label, Safety Lead-In with Long Term Safety Study of EG-007, Added to the Combination of Lenvatinib Plus Pembrolizumab
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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3,626
项与 甲磺酸仑伐替尼 相关的文献（医药）2025-12-31ANNALS OF MEDICINE
Immune infiltration landscape and potential drug-targeted implications for hepatocellular carcinoma with ‘progression/hyper-progression’ recurrence
Article
作者: Qi, Lu-Nan ; Peng, Yu-Chong ; Su, Yue-Xiang ; Xu, Jing-Xuan ; Chen, Yuan-Yuan ; Chen, Zu-Shun ; Huang, Yi-Yue
BACKGROUND AND AIMS:
Hepatocellular carcinoma (HCC) recurrence was previously characterized into four types, and patients with progression/hyper-progression recurrence (type III-IV) have an extremely poor prognosis. However, the immune background of resectable HCC, particularly in patients who experience recurrence, remains underexplored. Therefore, this study aimed to describe the immune landscape of resectable HCC, especially postoperative type III-IV recurrent HCC, and explore potential immune-targeted anti-relapse strategies for treated populations.
METHODS:
The differences in gene expression in patients with recurrent HCC (type I-II (solitary or multi-intrahepatic oligo recurrence) vs. type III-IV) were investigated using bulk sequencing. Multiple immune infiltration methods (single-sample gene set enrichment analysis (GSEA), Microenvironment Cell Populations-counter and ESTIMATE) were used, and patients were divided into four groups to identify four distinct immune subtypes: immune-enrichment/matrix-poor (IE1), immune-enrichment/matrix-rich (IE2), immune intermediate/matrix-rich (ITM) and immune desert/matrix-poor (ID). Co-expression and protein interaction analyses were used to identify characteristic genes in ITM closely associated with type III-IV recurrence, which was matched with drug targets for Huaier granules (HG) and lenvatinib. Virtual docking was used to identify potential therapeutic targets, and the results were verified using single-nuclei RNA sequencing and histological analysis.
RESULTS:
ITM was closely related to type III-IV recurrence and exhibited immunotherapy potential. The potential efficacy of inhibiting CCNA2, VEGFA, CXCL8, PLK2, TIMP1, ITGB2, ALDOA, ANXA5 and CSK in ITM reversal was determined. Molecular docking demonstrated that the proteins of these genes could bind to HG or lenvatinib. The immunohistochemical findings demonstrated differential VEGFA (p < .01) and PLK2 (p < .001) expression in ITM type and ID in type III-IV recurrent HCC.
CONCLUSIONS:
Three primary immunotypes of resectable HCC (IE2, ITM and ID) were identified, and HG and lenvatinib could potentially overcome immune checkpoint blockade (ICB) resistance in ITM patients with HCC, particularly those classified as type III-IV.
2025-12-01CANCER CHEMOTHERAPY AND PHARMACOLOGY
Pharmacokinetic exposure and treatment outcomes of lenvatinib in patients with renal cell carcinoma and differentiated thyroid carcinoma
Article
作者: Steeghs, Neeltje ; Giraud, Eline L ; van Erp, Nielka P ; Walraven, Janneke E W ; de Boer, Jan Paul ; Huitema, Alwin D R ; Zielhuis, Sybrand W J ; Hassan, Esbar ; Meertens, Marinda ; van Thienen, Johannes V ; Desar, Ingrid M E ; Snels, Tiemen T ; Wilgenhof, Sofie
PURPOSE:
After initial approval of lenvatinib for radioiodine-refractory differentiated thyroid cancer (DTC), it has also shown promising outcomes in among others metastatic renal cell carcinoma (mRCC). Given that trial populations typically do not represent routine clinical care populations, questions arise about how applicable trial outcomes are in clinical practice. This study aims to compare the pharmacokinetics (PK), toxicity patterns, and survival data of lenvatinib in a real-world cohort with DTC and mRCC to those observed in pivotal clinical trials.
MATERIALS AND METHODS:
Patients were included when diagnosed with DTC or mRCC, had received current or prior treatment with lenvatinib, and had at least one available lenvatinib plasma concentration measurement. A descriptive comparison was made between the baseline characteristics, PK data, toxicity and survival data in this real-world cohort and those described in the phase III trials.
RESULTS:
Overall, 29 patients with mRCC and 35 patients with DTC were included. For mRCC, median time to treatment discontinuation (mTTD) was shorter than observed in the phase III trial (7.5 versus 11.0 months) with fewer dose-limiting toxicities, likely because 66% of the patients started with a reduced dose. mRCC patients were more pretreated and had a worse performance status than trial participants. This was resembled in overall lower PK exposure in mRCC patients. For DTC, mTTD was longer in our cohort (17.1 versus 13.8 months), with similar toxicity patterns and PK exposure as in the phase III trial.
CONCLUSIONS:
Our data suggests that patient characteristics and outcomes in routine clinical care deviate from clinical trials and show the need for alternative treatment strategies to manage tolerability to lenvatinib.
2025-12-01CANCER CHEMOTHERAPY AND PHARMACOLOGY
Predictive factors for first dose reduction and interruption of lenvatinib after beginning of the standard dose in Japanese patients with thyroid cancer
Article
作者: Sugino, Kiminori ; Suzuki, Akifumi ; Ito, Koichi ; Fujita, Kazuma ; Masaki, Chie ; Nagahama, Mitsuji ; Miura, Masatomo
PURPOSE:
The associations between first dose reduction or interruption by side effects and lenvatinib plasma trough concentration (C0) after administration of a starting dose of 24 mg in 70 Japanese patients with thyroid cancer were evaluated.
METHODS:
Plasma samples were collected each week for 1 month and at the first incidence of side effects leading to dose reduction or interruption after beginning administration of 24 mg lenvatinib.
RESULTS:
The area under the receiver operating characteristic curve was 0.789 at a lenvatinib C0 threshold of 128.25 ng/mL for predicting the first dose reduction or interruption. The median time to the first dose reduction or interruption was 14.0 days in patients with a C0 of ≥ 128.25 ng/mL and 21.0 days in those with a C0 of < 128.25 ng/mL (P = 0.001). At one, two, three and four weeks respectively, the first dose reduction or interruption was associated with body weight (P = 0.034); sex (P = 0.021); sex, age, and lenvatinib C0 of ≥ 128.25 ng/mL (P = 0.025, 0.024, and 0.048, respectively); and age and lenvatinib C0 of ≥ 128.25 ng/mL (each P = 0.004).
CONCLUSIONS:
On day 8 after administration of 24 mg lenvatinib, lenvatinib dose may be adjusted based on the target C0 of 128.25 ng/mL to maintain a high dose intensity during this early phase; however, because persistence of a higher C0 of 128.25 ng/mL causes early dose interruption or reduction, prospective dose reduction based on the next lower target C0 for the maintenance phase may be necessary.
100 项与 甲磺酸仑伐替尼 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 晚期子宫内膜癌 | 欧盟 | 2023-07-25 | |
| 晚期子宫内膜癌 | 冰岛 | 2023-07-25 | |
| 晚期子宫内膜癌 | 列支敦士登 | 2023-07-25 | |
| 晚期子宫内膜癌 | 挪威 | 2023-07-25 | |
| 复发性子宫内膜癌 | 欧盟 | 2023-07-25 | |
| 复发性子宫内膜癌 | 冰岛 | 2023-07-25 | |
| 复发性子宫内膜癌 | 列支敦士登 | 2023-07-25 | |
| 复发性子宫内膜癌 | 挪威 | 2023-07-25 | |
| 胸腺肿瘤 | 日本 | 2021-03-23 | |
| 晚期肾细胞癌 | 欧盟 | 2016-08-25 | |
| 晚期肾细胞癌 | 冰岛 | 2016-08-25 | |
| 晚期肾细胞癌 | 列支敦士登 | 2016-08-25 | |
| 晚期肾细胞癌 | 挪威 | 2016-08-25 | |
| 子宫内膜癌 | 澳大利亚 | 2016-01-28 | |
| 肾细胞癌 | 澳大利亚 | 2016-01-28 | |
| 晚期肝细胞癌 | 欧盟 | 2015-05-28 | |
| 晚期肝细胞癌 | 冰岛 | 2015-05-28 | |
| 晚期肝细胞癌 | 列支敦士登 | 2015-05-28 | |
| 晚期肝细胞癌 | 挪威 | 2015-05-28 | |
| 分化型甲状腺癌 | 欧盟 | 2015-05-28 |
未上市
10 条进展最快的记录, 后查看更多信息
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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 | 2021-10-28 | |
| 食管鳞状细胞癌 | 临床3期 | 美国 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 美国 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 中国 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 中国 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 日本 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 日本 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 阿根廷 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 阿根廷 | 2021-07-28 | |
| 食管鳞状细胞癌 | 临床3期 | 加拿大 | 2021-07-28 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床2期 | 17 | 蓋衊廠築繭鏇廠淵選遞(遞鏇壓網壓鹹製選鹹壓) = 構獵壓夢鬱衊壓鹽淵繭 鏇襯鏇鏇憲壓鹽構醖壓 (製鏇獵襯鏇鏇淵餘窪膚 ) | 积极 | 2025-02-13 | |||
N/A | 19 | 製鏇憲淵糧膚願艱鏇繭(獵顧獵壓淵壓鹹衊餘憲) = There was little correlation between Css and CTCAE Composite Score 遞蓋夢糧範製遞觸鹹構 (顧鏇憲醖壓鬱遞遞鑰鏇 ) 更多 | - | 2025-02-13 | |||
N/A | 转移性肾细胞癌 二线 | 82 | 糧鏇鏇齋鹹餘觸網願簾(鹽壓襯製糧鏇膚製積積) = 蓋鹽憲顧鏇網獵築築範 遞積憲齋窪膚鏇鬱繭築 (簾艱鏇製淵簾觸齋鹹餘 ) 更多 | 积极 | 2025-02-13 | ||
临床2期 | 55 | 壓構鹹淵願鹽鬱積鑰鬱(窪醖選壓鹽憲夢壓獵鏇) = 艱簾壓蓋淵憲餘觸獵艱 夢餘鹽願廠鏇網廠蓋廠 (壓簾醖繭願鹽艱鹹鑰鏇, 31.97 ~ 59.45) 更多 | 积极 | 2025-02-07 | |||
临床3期 | 肾细胞癌 PD-1/PD-L1 | - | Lenvatinib plus Pembrolizumab (LEN + PEM) | 積夢觸構願膚齋鬱廠願(壓廠構襯鹽鹽鬱顧選壓) = 憲鹹窪構窪選艱構鏇觸 淵糧夢醖簾糧襯糧獵觸 (鏇衊觸遞製構鬱選積廠, 0.92 ~ 8.26) 更多 | 积极 | 2025-01-30 | |
Nivolumab plus Ipilimumab (NIVO + IPI) | 積夢觸構願膚齋鬱廠願(壓廠構襯鹽鹽鬱顧選壓) = 積齋窪鏇鬱繭鹹膚廠範 淵糧夢醖簾糧襯糧獵觸 (鏇衊觸遞製構鬱選積廠, 5.60 ~ 10.57) 更多 | ||||||
NEWS 人工标引  | 临床3期 | - | 遞齋簾齋衊選鏇繭壓鬱(顧窪選觸築鬱淵繭築壓) = meeting 蓋簾觸積鏇餘構鹹鬱鑰 (襯簾艱衊糧鑰鹹觸艱鹽 ) 更多 | 不佳 | 2025-01-24 | ||
临床3期 | 880 | 顧淵願夢壓構蓋廠鹹艱(衊襯鏇鹽鬱膚壓衊廠廠) = statistically significant improvement. 鹽構襯築積鹹鹹鑰積簾 (構網衊鹽製願觸製獵遞 ) 达到 更多 | 不佳 | 2025-01-24 | |||
chemotherapy | |||||||
N/A | 晚期胆道癌 一线 | - | 鹹鏇壓艱廠憲範鬱繭餘(願製襯醖選鏇醖遞蓋醖) = All patients experienced adverse events (AEs), addition of lenvatinib does not increase the risk of AEs 範醖遞築醖鹽範網範艱 (顧鏇鹹憲膚鑰淵糧鹹鑰 ) | 积极 | 2025-01-23 | ||
Durvalumab + Gemcitabine-based chemotherapy | |||||||
N/A | 晚期肝细胞癌 alpha-fetoprotein levels | eosinophil count | neutrophil-to-lymphocyte ratio | 30 | Yttrium-90 resin microspheres | 選膚鬱鹹齋繭壓鬱廠鏇(夢憲簾齋願鏇襯壓齋選) = AEs of any grade occurred in 86.7% of patients 選網鬱夢觸壓鏇鹽網艱 (願淵顧餘簾艱願獵築顧 ) 更多 | 积极 | 2025-01-23 | |
临床2期 | 40 | (Cohort A, China: Lenvatinib Monotherapy) | 憲繭糧廠獵廠積簾繭簾(淵製觸構夢積選糧網膚) = 夢選鹽壓窪鏇積鹽積齋 鬱鑰艱廠願齋築壓鹹構 (範蓋壓構艱鑰顧範憲窪, 憲齋鏇觸網壓糧餘觸壓 ~ 鏇觸網廠齋淵夢鹽廠壓) 更多 | - | 2025-01-07 | ||
(Cohort A, Rest of the World: Lenvatinib Monotherapy) | 憲繭糧廠獵廠積簾繭簾(淵製觸構夢積選糧網膚) = 選糧觸淵範遞齋獵廠夢 鬱鑰艱廠願齋築壓鹹構 (範蓋壓構艱鑰顧範憲窪, 獵顧蓋獵鏇獵繭範廠網 ~ 衊醖衊網襯憲觸遞襯艱) 更多 |
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