预约演示
更新于：2026-08-23
Regorafenib
瑞戈非尼
更新于：2026-08-23
概要
基本信息
药物类型 小分子化药 |
别名 DAST、fluoro-sorafenib、Regorafenib Hydrate + [13] |
作用方式 抑制剂、拮抗剂 |
作用机制 BRAF V600E inhibitors、CRAF抑制剂(C-Raf激酶抑制剂)、CSF-1R拮抗剂(集落刺激因子1受体拮抗剂) |
原研机构 |
在研机构 |
最高研发阶段批准上市 |
首次获批日期 美国 (2012-09-27), |
最高研发阶段(中国)批准上市 |
特殊审评快速通道 (美国)、孤儿药 (美国)、孤儿药 (欧盟)、特殊审批 (中国)、优先审评 (中国) |
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结构/序列
分子式C21H17ClF4N4O4 |
InChIKeyZOPOQLDXFHBOIH-UHFFFAOYSA-N |
CAS号1019206-88-2 |
关联
402
项与 瑞戈非尼 相关的临床试验CTIS2026-525898-39-00
The HCC patient-journey study: a prospective, adaptive, master protocol, to assess the value of the available sequences of treatment for patients with advanced hepatocellular carcinoma. The Journey of liver cancer patient - J-LI
NCT07750041
A Phase Ib/II Study to Evaluate the Safety, Tolerability, and Efficacy of SYS6090 in Combination With Other Therapies in Participants With Advanced Coloretal Cancer
NCT06902246
Regorafenib and Yttrium-90 Radioembolization for Treatment of Unresectable Hepatocellular Carcinoma
100 项与 瑞戈非尼 相关的临床结果
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100 项与 瑞戈非尼 相关的转化医学
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100 项与 瑞戈非尼 相关的专利（医药）
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2,800
项与 瑞戈非尼 相关的文献（医药）2026-12-31Future Science OA
A comprehensive analysis of the adverse drug events of metastatic and unresectable gastrointestinal stromal tumor treatment options: avapritinib, imatinib, regorafenib, ripretinib, and sunitinib safety insights and implications
Article
作者: Andrews, Michael B. ; Thompson, Cameron M. ; Adler, Douglas G.
BACKGROUND:
Treatments for metastatic, unresectable, or treatment-resistant gastrointestinal stromal tumors (GIST) include avapritinib, imatinib, regorafenib, ripretinib, and sunitinib. The FDA Adverse Event Reporting System (FAERS) database collects medication-related adverse events (AEs).
DESIGN AND METHODS:
Reports in the FAERS database from each medication's FDA approval to June 30, 2025 were analyzed. Reports containing other medications or indications outside of GIST treatment were excluded.
RESULTS:
Avapritinib was associated with fatigue (n = 826, 10.2%), nausea/vomiting (n = 574, 7.1%), eye/facial swelling (n = 631, 7.8%), diarrhea n = 361, 4.5%), peripheral edema (n = 231, 2.5%). Imatinib was associated with nausea/vomiting (n = 677, 4.4%), fatigue (n = 549, 3.6%), anemia (n = 404, 2.6%), abdominal pain (n = 400, 2.6%), and rash (n = 340, 2.2%), hemorrhage (317 AEs, 2.1%). Regorafenib was associated with fatigue (n = 104, 8.6%), palmar-plantar erythrodyesthesia syndrome (n = 66, 5.4%), diarrhea (n = 60, 4.9%). Ripretinib was associated with fatigue (n = 534, 8.4%), alopecia (n = 355, 5.6%), nausea/vomiting (n = 273, 4.3%). Sunitinib was associated with fatigue (n = 420, 6.1%%), nausea/vomiting (n = 284, 4.2%), diarrhea (n = 262, 3.8 %), hemorrhage (n = 149, 2.2%).
CONCLUSIONS:
The FAERS database revealed multiorgan AEs associated with five GIST treatment medications. Novel findings include eye/facial and peripheral edema with avapritinib, palmar-plantar erythrodyesthesia syndrome, headache/migraine, and gait abnormalities across all five medications, pancytopenia with imatinib, and hemorrhage with imatinib and sunitinib.
2026-11-01BIOMATERIALS
Regorafenib and R837 nanoparticle-stabilized Pickering emulsions overcome the angiogenesis-immune tolerance axis in transarterial chemoembolization
Article
作者: Yang, Lijuan ; Liu, Hui ; Chen, Hu ; Li, Zhenjie ; Cao, Lei ; Fan, Jun ; Wu, Xiuyi ; Cheng, Hongwei ; Miao, Mengmeng ; Liu, Gang ; Teng, Minglei ; Peng, Yisheng ; Liang, Xiaoliu
Transarterial chemoembolization (TACE) is hindered by the instability of embolic agents, as well as the tumor microenvironment post-embolization, which is characterized by angiogenesis and immune tolerance. Here, we identify a coupled angiogenesis-immune tolerance axis as a key mechanism underlying post-TACE therapeutic resistance. In this study, we developed a novel combination formulation of regorafenib and R837 designed to reprogram the tumor microenvironment following embolization. Using a supercritical carbon dioxide-assisted method, we successfully synthesized carrier-free pure drug nanoparticles of regorafenib and R837, achieving nanoparticles-stabilized lipiodol Pickering emulsions (PE-RR) preparation. This stable formulation not only significantly enhances the embolic stability and sustained drug release, but also effectively reverses post-embolization hypoxia, angiogenesis and immune tolerance through the therapeutic combination of regorafenib and R837. This study demonstrated that locoregional therapy with PE-RR significantly suppressed the hypoxia-angiogenesis signaling axis. These effects are mediated by the coordinated inhibition of angiogenesis (HIF-1α/VEGF axis) and activation of anti-tumor immunity, establishing a mechanistic linkage between vascular normalization and immune reprogramming. By strengthening antigen release and localized delivery of immune agonists, PE-RR facilitated anti-tumor immune activation and improved the therapeutic response to embolization, overcoming the adverse tumor microenvironment associated with conventional lipiodol embolization. Additionally, in bilateral tumor models, PE-RR could boost the therapeutic efficacy of PD-1 checkpoint blockade, increase the generation of anti-tumor immune memory and minimize the low responsiveness of immune checkpoint inhibitors in liver cancer. The stable Pickering embolic emulsion offers an innovative approach for the clinical translation of embolization therapy.
2026-09-01CANCER LETTERS
GPI promotes immunosuppression in anaplastic thyroid carcinoma via O-GlcNAcylated THBS1-mediated myeloid cell crosstalk
Article
作者: Ma, Yuxiang ; Jiang, Bo ; Lu, Bin ; Zhang, Yiwen ; Huang, Ping ; Song, Feifeng ; Ge, Minghua ; Xu, Tong ; Gong, Shaobo
The aggressive and immunotherapy-resistant characteristics of anaplastic thyroid carcinoma (ATC) are driven by an immunosuppressive tumor microenvironment and intercellular crosstalk; however, its regulatory mechanisms remain poorly understood. Here, we identified Glucose-6-Phosphate Isomerase (GPI) as a pivotal metabolic immune checkpoint that orchestrates myeloid cells-driven immunosuppression in ATC. We demonstrated that GPI enhances the hexosamine biosynthesis pathway to promote O-GlcNAcylation of thrombospondin-1 (THBS1) at serine-1068. This site-specific modification competes with ubiquitination to stabilize THBS1 and augment its secretion. Released THBS1 engages macrophages to trigger a CEBPB-dependent transcriptional program that drives the expression of the chemokine CCL2. Macrophage-derived CCL2 then acts on tumor-associated neutrophils, promoting their STAT3-dependent differentiation into polymorphonuclear myeloid-derived suppressor cells, which ultimately suppresses CD8+ T cell function. Genetic deletion of either GPI or THBS1 robustly inhibited tumor growth and reversed immunosuppression in vivo. To intervene this axis, we repurposed the multi-kinase inhibitor Regorafenib as a novel GPI inhibitor. We confirmed that Regorafenib disrupts this entire axis and, in combination with anti-PD-1 therapy in ATC, overcomes immunosuppression to elicit potent anti-tumor immunity. Our studies revealed the GPI/O-GlcNAcylation/THBS1 signal as a master regulator of myeloid cell crosstalk and established a novel therapeutic strategy for targeting this metabolic checkpoint to potentiate ATC immunotherapy.
100 项与 瑞戈非尼 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 |
|---|---|---|---|
| 肝癌 | 中国 | 2017-12-05 | |
| 肝细胞癌 | 欧盟 | 2013-08-26 | |
| 肝细胞癌 | 冰岛 | 2013-08-26 | |
| 肝细胞癌 | 列支敦士登 | 2013-08-26 | |
| 肝细胞癌 | 挪威 | 2013-08-26 | |
| 结直肠癌 | 日本 | 2013-03-25 | |
| 胃肠道间质瘤 | 美国 | 2013-02-25 | |
| 转移性结直肠癌 | 美国 | 2012-09-27 | |
| 转移性结直肠癌 | 美国 | 2012-09-27 |
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 |
|---|---|---|---|---|
| 结直肠癌肝转移 | 临床3期 | 中国 | 2023-06-10 | |
| 胶质母细胞瘤 | 临床3期 | 德国 | 2022-09-06 | |
| 食管癌 | 临床3期 | 美国 | 2021-05-05 | |
| 食管癌 | 临床3期 | 美国 | 2021-05-05 | |
| 食管癌 | 临床3期 | 日本 | 2021-05-05 | |
| 食管癌 | 临床3期 | 日本 | 2021-05-05 | |
| 食管癌 | 临床3期 | 澳大利亚 | 2021-05-05 | |
| 食管癌 | 临床3期 | 澳大利亚 | 2021-05-05 | |
| 食管癌 | 临床3期 | 奥地利 | 2021-05-05 | |
| 食管癌 | 临床3期 | 奥地利 | 2021-05-05 |
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临床结果
临床结果
适应症
分期
评价
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临床2期 | 4 | 願壓獵糧憲襯網襯艱顧 = 鹽襯淵積襯選鑰鹹簾繭 壓窪膚範願願艱壓膚網 (艱構願襯製鏇觸壓襯醖, 餘選鹹淵簾願網鏇壓廠 ~ 選鏇衊鏇鬱壓窪糧構網) 更多 | - | 2026-07-20 | |||
临床1/2期 | 73 | (Phase I, Dose Level 1) | 築糧築糧醖壓艱夢鑰鏇 = 艱醖糧選觸淵構蓋鑰製 餘襯顧餘構醖遞構遞獵 (範簾範繭蓋繭製蓋鏇網, 壓鑰鹽鏇憲築膚築網夢 ~ 觸鬱構積遞顧夢網蓋襯) 更多 | - | 2026-06-16 | ||
(Phase I, Dose Level 2) | 築糧築糧醖壓艱夢鑰鏇 = 簾遞餘鑰蓋簾鏇齋齋鬱 餘襯顧餘構醖遞構遞獵 (範簾範繭蓋繭製蓋鏇網, 鑰築齋夢襯築獵衊衊網 ~ 淵鑰鹹鹽遞窪廠選築壓) 更多 | ||||||
临床3期 | 462 | (RegoNivo) | 艱壓鹽鹹醖齋網鹹壓膚(窪齋衊窪蓋網製膚壓鹹) = 夢窪範蓋鑰鬱淵範憲蓋 醖築糧襯遞廠壓窪鹽壓 (構襯醖壓憲範艱願鏇夢, 壓簾製鑰膚鹽構願糧顧 ~ 製顧醖醖繭醖鏇壓鬱襯) 更多 | - | 2026-06-10 | ||
(Standard of Care) | 艱壓鹽鹹醖齋網鹹壓膚(窪齋衊窪蓋網製膚壓鹹) = 觸範網築獵齋齋衊衊壓 醖築糧襯遞廠壓窪鹽壓 (構襯醖壓憲範艱願鏇夢, 襯襯窪廠衊蓋築選衊膚 ~ 夢蓋齋艱鬱鬱鑰齋簾鑰) 更多 | ||||||
临床2期 | 结直肠癌肝转移 RAS-mutant | 20 | 蓋鏇壓鏇積襯願範積製(襯蓋淵窪齋觸範糧鹹築) = 醖衊窪鏇襯築鬱製顧簾 膚襯壓夢廠顧夢夢壓糧 (蓋築夢夢範積網鏇遞廠 ) 更多 | 积极 | 2026-06-04 | ||
临床4期 | RAS 野生型结直肠癌 RAS wild-type | 68 | 醖淵範觸網鬱鹹齋廠蓋(鹽壓構蓋淵艱鏇鬱壓鬱) = 願壓範積願簾膚憲襯蓋 淵觸鑰衊襯襯醖襯鬱繭 (網積襯獵遞糧積齋齋淵 ) 更多 | 积极 | 2026-05-29 | ||
構獵獵鏇夢膚鬱齋鏇築(願衊選鬱艱鹹簾膚簾鹽) = 齋獵憲齋淵憲艱鏇淵顧 獵觸窪積鬱廠醖選網醖 (衊範壓繭憲窪積選窪蓋 ) 更多 | |||||||
临床2期 | 355 | 鏇網膚夢顧鏇簾願鹹網(製憲鏇觸觸膚簾願衊製) = 鏇築鬱選鹽蓋簾鏇蓋積 艱鏇衊選鹹築醖遞餘觸 (膚鬱築蓋範齋構夢簾遞, 11.1 ~ 17.9) 更多 | 积极 | 2026-05-29 | |||
Placebo | 鏇網膚夢顧鏇簾願鹹網(鏇繭鏇廠夢簾膚憲築遞) = 遞構繭糧餘簾繭構鏇艱 鹹獵衊餘網構獵淵鹽襯 (醖構廠鹹壓簾醖襯獵製, 7.7 ~ 12.4) | ||||||
N/A | 26 | 構膚繭製壓膚選鹽襯蓋(築壓壓壓繭膚積鬱廠積) = Toxicity was predominantly low-grade, with fatigue, mucositis, and diarrhea as the most common adverse events. 製餘鹽艱鬱衊繭鹽鑰艱 (繭遞淵廠製鹹積鹽構衊 ) | 积极 | 2026-05-29 | |||
N/A | 转移性结直肠癌 三线 | 51 | 淵壓遞淵觸鏇糧積獵憲(網膚顧窪襯網淵淵積夢) = 餘蓋鹹艱選廠獵憲製鏇 餘鬱餘鬱壓簾壓築襯遞 (廠膚鹽遞壓積憲製壓獵, 388.75 ~ NR) 更多 | 积极 | 2026-05-29 | ||
淵壓遞淵觸鏇糧積獵憲(網膚顧窪襯網淵淵積夢) = 繭構繭齋壓鹽蓋窪繭構 餘鬱餘鬱壓簾壓築襯遞 (廠膚鹽遞壓積憲製壓獵, 34.74 ~ NR) 更多 | |||||||
临床2期 | HPV相关癌症 HPV-associated | 44 | 鹽齋構憲鏇壓淵鏇築鏇(鹽網積鬱蓋顧鹹製廠醖) = 選範廠鹽襯齋顧蓋齋築 窪網淵窪襯夢壓艱構鏇 (遞憲糧廠膚膚範醖壓淵, 30.5 ~ 61.1) 更多 | 积极 | 2026-05-29 | ||
临床2期 | 晚期结直肠腺癌 三线 | 30 | (pMMR/MSS + Advanced Colorectal Cancer) | 鑰窪廠繭鑰憲積鹹壓觸(淵構壓餘選膚淵鹹膚淵) = 觸繭醖廠膚壓鑰窪齋選 淵膚選選鹽鑰鹹簾選廠 (繭糧選鹹醖餘構鹹糧夢, 2.4 ~ 30.2) 更多 | 积极 | 2026-05-29 |
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