更新于：2024-09-13
Fruquintinib
呋喹替尼
更新于：2024-09-13
概要
基本信息
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2018-09-04), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、快速通道 (美国)、优先审评 (中国)、突破性疗法 (中国) |
登录后查看首次获批时间轴
结构
分子式C21H19N3O5 |
InChIKeyBALLNEJQLSTPIO-UHFFFAOYSA-N |
CAS号1194506-26-7 |
关联
159
项与 呋喹替尼 相关的临床试验PD-1 Antibody (Tislelizumab) Combined With VEGFR 1/2/3 Inhibitor (Fruquintinib) for ARID1A-mutated Metastatic pMMR/MSS Colorectal Cancer: an Open-label, Multi-center, Phase II Clinical Trial
A Real-World Study of Neoadjuvant/Conversion Therapy for Locally Advanced or Metastatic Colorectal Cancer With Chemotherapy Combined With Anti-Angiogenic Targeted Agents
A Real-World Study of Neoadjuvant/Conversion Therapy for Locally Advanced or Metastatic Gastric Cancer With Chemotherapy Combined With Immune Checkpoint Inhibitors and Anti-Angiogenic Targeted Agents
100 项与 呋喹替尼 相关的临床结果
登录后查看更多信息
100 项与 呋喹替尼 相关的转化医学
登录后查看更多信息
100 项与 呋喹替尼 相关的专利（医药）
登录后查看更多信息
100
项与 呋喹替尼 相关的文献（医药）2024-02-01Pharmacological research
Properties of FDA-approved small molecule protein kinase inhibitors: A 2024 update
Review
作者: Roskoski, Robert
Owing to the dysregulation of protein kinase activity in many diseases including cancer, this enzyme family has become one of the most important drug targets in the 21st century. There are 80 FDA-approved therapeutic agents that target about two dozen different protein kinases and seven of these drugs were approved in 2023. Of the approved drugs, thirteen target protein-serine/threonine protein kinases, four are directed against dual specificity protein kinases (MEK1/2), twenty block nonreceptor protein-tyrosine kinases, and 43 inhibit receptor protein-tyrosine kinases. The data indicate that 69 of these drugs are prescribed for the treatment of neoplasms. Six drugs (abrocitinib, baricitinib, deucravacitinib, ritlecitinib, tofacitinib, upadacitinib) are used for the treatment of inflammatory diseases (atopic dermatitis, rheumatoid arthritis, psoriasis, alopecia areata, and ulcerative colitis). Of the 80 approved drugs, nearly two dozen are used in the treatment of multiple diseases. The following seven drugs received FDA approval in 2023: capivasertib (HER2-positive breast cancer), fruquintinib (metastatic colorectal cancer), momelotinib (myelofibrosis), pirtobrutinib (mantle cell lymphoma, chronic lymphocytic leukemia, small lymphocytic lymphoma), quizartinib (Flt3-mutant acute myelogenous leukemia), repotrectinib (ROS1-positive lung cancer), and ritlecitinib (alopecia areata). All of the FDA-approved drugs are orally effective with the exception of netarsudil, temsirolimus, and trilaciclib. This review summarizes the physicochemical properties of all 80 FDA-approved small molecule protein kinase inhibitors including the molecular weight, number of hydrogen bond donors/acceptors, polar surface area, potency, solubility, lipophilic efficiency, and ligand efficiency.
2024-02-01Immunotherapy
Toripalimab and Fruquintinib Therapy for Colorectal Cancer after Failed Multiline Chemotherapies: A Case Report
Article
作者: Kong, Ling-Zhijie ; Li, Kaichun ; Zheng, Ying
The options for treating metastatic colorectal cancer are limited after failure of second-line chemotherapy. In this case report, we present the outcome of a 59-year-old male patient who underwent radical resection for rectal cancer in November 2018 and hepatectomy for liver metastasis in January 2021. His metastatic rectal cancer presented a remarkable response to the combination of fruquintinib and toripalimab after the failure of multiline chemotherapies. The patient achieved partial response within 3 months and clinical complete response of pulmonary masses within 12 months. As of now, the patient maintains a good quality of life, and the progression-free survival has been more than 17 months. In conclusion, the combination of fruquintinib and PD-1 inhibitors can improve the prognosis of metastatic colorectal cancer.
2023-12-01Journal of gastrointestinal oncology
Efficacy, safety, and predictors of fruquintinib plus anti-programmed death receptor-1 (PD-1) antibody in refractory microsatellite stable metastatic colorectal cancer in a real-world setting: a retrospective cohort study
Article
作者: Zeng, Yidong ; Yang, Xiaolin ; Zhou, Huijun ; Liu, Wu ; Guo, Geyang ; Yin, Xianli ; Liu, Zhenyang ; Qu, Xiaozhou ; Jagielski, Mateusz
Background:
Patients with microsatellite stable (MSS) advanced colorectal cancer (CRC) have few alternatives for salvage therapy and a large unmet clinical need. Preclinical studies demonstrate that fruquintinib combined with anti-programmed death protein 1 (PD-1) has a synergistic anti-tumor effect. But a few phase 2 clinical studies show inconsistent efficacy of this combination therapy in CRC. The aim of this study was to investigate the efficacy, safety, and predictors of fruquintinib plus PD-1 antibodies in refractory MSS metastatic CRC (mCRC) in a real-world setting.
Methods:
We performed a retrospective single-center analysis to assess the outcomes of patients with MSS mCRC who were treated with fruquintinib plus anti-PD-1 antibodies subsequent to the failure of standard therapies at the Hunan Cancer Hospital. The overall survival (OS), progression-free survival (PFS), objective response rate (ORR), disease control rate (DCR), and toxicity were reviewed and evaluated. The primary endpoint was OS. The impact on OS and PFS was examined using the Cox regression model.
Results:
Between 1 January 2019 and 30 June 2022, we enrolled 70 eligible patients. The median follow-up was 17.2 months (range, 5.3-32.9 months). The median OS (mOS) and median PFS (mPFS) were 19.48 and 5.5 months respectively. The ORR was 11.43% and the DCR was 84.29%. Multivariate Cox regression analysis reveals liver metastasis (LM) without local treatment was a risk factor for OS [hazard ratio (HR) =5.31, P=0.0184], whereas that with local treatment (HR =2.19, P=0.263) was not. The most common adverse events were hand-foot syndrome (37.14%), hypertension (34.29%), mucositis oral (32.86%). No serious adverse effects or adverse effect-related deaths were reported. There were no instances of severe adverse effects or deaths related to adverse effects reported.
Conclusions:
Our study indicates that the combination of fruquintinib and anti-PD-1 antibodies can improve the OS and PFS with a tolerable toxicity profile for Chinese patients with refractory MSS mCRC. LM without local therapy is a negative prognostic factor for OS, but those with local treatment can significantly prolong survival. We require additional well-structured, prospective, and extensive studies to confirm and validate these findings.
100 项与 呋喹替尼 相关的药物交易
登录后查看更多信息
研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
登录
| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 转移性结直肠癌 | 中国 | 2018-09-04 |
未上市
10 条进展最快的记录, 后查看更多信息
登录
| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 晚期子宫内膜癌 | 申请上市 | 中国 | 2024-03-29 | |
| 胃食管交界处腺癌 | 申请上市 | 中国 | 2023-04-18 | |
| 胃癌 | 申请上市 | 中国 | 2023-04-18 | |
| 肾细胞癌 | 临床3期 | 中国 | 2022-10-14 | |
| 结肠转移性腺癌 | 临床3期 | 美国 | 2020-08-12 | |
| 结肠转移性腺癌 | 临床3期 | 日本 | 2020-08-12 | |
| 结肠转移性腺癌 | 临床3期 | 澳大利亚 | 2020-08-12 | |
| 结肠转移性腺癌 | 临床3期 | 奥地利 | 2020-08-12 | |
| 结肠转移性腺癌 | 临床3期 | 比利时 | 2020-08-12 | |
| 结肠转移性腺癌 | 临床3期 | 捷克 | 2020-08-12 |
登录后查看更多信息
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 | 转移性结直肠癌 二线 | 35 | 鹹齋衊鏇製糧鹹鑰鑰簾(壓襯衊艱繭獵廠遞遞鑰) = 憲糧襯蓋獵鏇築繭構憲 簾餘製構夢鹹醖選獵窪 (廠醖夢餘築繭獵鏇鹹網 ) 更多 | 积极 | 2024-09-16 | ||
临床2期 | 局部晚期直肠癌 新辅助 | 23 | Fruquintinib+toripalimab | 憲糧廠餘餘簾淵壓築膚(廠艱醖鏇觸構願顧衊醖) = 構鬱願廠壓壓艱餘遞襯 廠窪憲範齋衊鏇鏇糧鬱 (製鑰淵壓膚獵構廠鬱鏇, 13.8% ~ 61.2%) 更多 | 积极 | 2024-09-16 | |
临床3期 | 703 | 構網網膚鹽醖糧壓簾選(齋簾選網夢積襯鬱繭壓) = 鑰選壓醖願廠願顧遞繭 遞鏇願夢範壓繭選艱獵 (積鹹蓋選齋醖憲繭製繭 ) | 不佳 | 2024-09-16 | |||
Placebo plus Paclitaxel | 構網網膚鹽醖糧壓簾選(齋簾選網夢積襯鬱繭壓) = 蓋顧願願糧願顧糧壓淵 遞鏇願夢範壓繭選艱獵 (積鹹蓋選齋醖憲繭製繭 ) | ||||||
临床3期 | 461 | Fruquintinib + best supportive care | 願蓋鏇憲襯鑰遞憲餘淵(膚夢繭選憲願廠積鬱淵) = 獵鑰膚鹹襯築簾遞願遞 壓鏇獵願憲憲獵鹹網繭 (襯繭廠網製鹹鬱網齋網 ) 更多 | 积极 | 2024-09-16 | ||
Placebo + best supportive care | 願蓋鏇憲襯鑰遞憲餘淵(膚夢繭選憲願廠積鬱淵) = 鏇糧選夢艱遞齋衊選鏇 壓鏇獵願憲憲獵鹹網繭 (襯繭廠網製鹹鬱網齋網 ) 更多 | ||||||
N/A | - | Fruquintinib + Best Supportive Care | 鏇膚範艱獵鏇遞憲範選(醖壓鹽齋獵醖構鏇壓鏇) = 14% for pts aged <55, 15% for pts aged 55−64, 12% for pts aged 65−74 觸窪積遞築積淵願衊鏇 (顧鬱衊觸鑰壓鏇淵蓋鑰 ) 更多 | - | 2024-09-16 | ||
Placebo + Best Supportive Care | |||||||
临床3期 | 351 | 鏇遞網夢醖觸憲簾繭構(廠製鏇膚襯鏇觸鏇衊範) = 59 (16.8%) experienced fruquintinib-induced hypertension. 23 (6.6%) experienced grade 3 or more fruquintinib-induced hypertension. No patient permanently discontinued due to hypertension. 鹹糧廠觸簾網獵繭觸醖 (積艱選顧願鏇構繭簾構 ) | 积极 | 2024-09-16 | |||
临床1/2期 | 胃食管交界处癌 一线 | 维持 | - | 鬱構膚壓壓壓鏇網鏇鹽(蓋鬱觸構構膚繭網齋齋) = 夢憲膚願糧醖積網觸齋 衊憲鹹憲壓淵製廠齋築 (網憲鹹憲憲糧衊齋衊齋 ) 更多 | - | 2024-09-16 | ||
临床3期 | 703 | Fruquintinib plus paclitaxel (F+PTX) | 觸夢蓋衊鬱顧餘鏇憲憲(壓獵艱糧壓蓋積艱襯衊) = 簾窪選遞繭襯壓築鹹夢 廠積憲範製築顧衊夢鏇 (遞鑰膚膚糧鹽顧蓋網壓, 66.4 ~ 93.4) 更多 | 积极 | 2024-09-16 | ||
Placebo plus paclitaxel (PBO+PTX) | 觸夢蓋衊鬱顧餘鏇憲憲(壓獵艱糧壓蓋積艱襯衊) = 獵艱遞鬱鑰顧艱獵觸網 廠積憲範製築顧衊夢鏇 (遞鑰膚膚糧鹽顧蓋網壓, 28.3 ~ 57.8) 更多 | ||||||
临床2期 | 32 | Fruquintinib 5mg | 願夢遞鑰艱窪構鏇築遞(夢夢齋範窪廠網繭衊糧) = 積鑰獵選鹽築構膚遞餘 選遞網醖顧齋蓋簾獵鹽 (齋醖衊願蓋壓廠繭選壓 ) 更多 | 积极 | 2024-09-14 | ||
临床2期 | 一线 | 维持 PD-L1 TPS | TMB | MSS | 38 | 艱製築衊選廠夢積壓襯(構製膚構餘網鏇夢廠顧) = 願襯願鹹鹽範襯願網鑰 簾蓋膚夢壓衊願衊願網 (夢艱觸蓋廠觸窪夢繭蓋, 9.69 ~ NA) 更多 | 积极 | 2024-09-14 |
登录后查看更多信息
转化医学
使用我们的转化医学数据加速您的研究。
登录
或
药物交易
使用我们的药物交易数据加速您的研究。
登录
或
核心专利
使用我们的核心专利数据促进您的研究。
登录
或
临床分析
紧跟全球注册中心的最新临床试验。
登录
或
批准
利用最新的监管批准信息加速您的研究。
登录
或
特殊审评
只需点击几下即可了解关键药物信息。
登录
或
来和芽仔聊天吧
立即开始免费试用!
智慧芽新药情报库是智慧芽专为生命科学人士构建的基于AI的创新药情报平台，助您全方位提升您的研发与决策效率。
立即开始数据试用!
智慧芽新药库数据也通过智慧芽数据服务平台，以API或者数据包形式对外开放，助您更加充分利用智慧芽新药情报信息。
生物序列数据库
生物药研发创新
免费使用
化学结构数据库
小分子化药研发创新
免费使用