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更新于：2025-08-31
Ifebemtinib
更新于：2025-08-31
概要
基本信息
药物类型 小分子化药 |
别名 BI 853520、BI-853520、IN 10018 + [2] |
靶点 |
作用方式 抑制剂 |
作用机制 FAK抑制剂(粘着斑蛋白酪氨酸激酶抑制剂) |
在研适应症 |
非在研适应症 |
最高研发阶段临床3期 |
首次获批日期- |
最高研发阶段(中国)临床3期 |
特殊审评快速通道 (美国)、突破性疗法 (中国) |
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结构/序列
分子式C28H28F4N6O4 |
InChIKeyULMMVBPTWVRPSI-UHFFFAOYSA-N |
CAS号1227948-82-4 |
关联
27
项与 Ifebemtinib 相关的临床试验NCT05982522
A Multicenter, Open-Label, Randomized, Phase Ib/II Clinical Trial to Evaluate the Efficacy, Safety, Tolerability, and Pharmacokinetics of IN10018 Combined With Taxane and Anti-PD-1/L1 Monoclonal Antibody in Previously-treated Solid Tumors
NCT06946927
A Phase Ib, Dose Escalation and Expansion Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Efficacy of JMKX001899 in Combination With Other Therapies in Subjects With Locally Advanced or Metastatic Non-Small Cell Lung Cancer With KRAS G12C Mutation.
NCT06708663
Phase IIa Study of HX009+IN10018 in Patients with Advanced Solid Tumours, Including Biliary Tract Malignancies and Malignant Melanoma, Treated with or Without Standard Chemotherapy
100 项与 Ifebemtinib 相关的临床结果
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100 项与 Ifebemtinib 相关的转化医学
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100 项与 Ifebemtinib 相关的专利（医药）
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21
项与 Ifebemtinib 相关的文献（医药）2025-07-17INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
Sensitivity of Pancreatic Cancer Cell Lines to Clinically Approved FAK Inhibitors: Enhanced Cytotoxicity Through Combination with Oncolytic Coxsackievirus B3.
Article
作者: Kurreck, Jens ; Fechner, Henry ; Elsner, Leslie ; Girod, Maxim ; Dieringer, Babette ; Van Linthout, Sophie ; Geisler, Anja
Pancreatic ductal adenocarcinoma (PDAC) is a highly aggressive cancer characterized by a dense desmoplastic stroma and a highly immunosuppressive tumor microenvironment (TME). The focal adhesion kinase (FAK), a non-receptor tyrosine kinase, is considered a critical regulator of various cellular processes involved in cancer development. FAK inhibitors (FAKi) have proven to be promising therapeutics for cancer treatment including for pancreatic cancer. As monotherapy, however, FAKi showed only a modest effect in clinical studies. In this study, we investigated the cytotoxicity of six FAKi (Defactinib, CEP-37440, VS-4718, VS-6062, Ifebemtinib and GSK2256098) used in clinical trials on five pancreatic tumor cell lines. We further examined whether their anti-tumor activity can be enhanced by combination with the oncolytic coxsackievirus B3 (CVB3) strain PD-H. IC50 analyses identified Defactinib and CEP-37440 as the most potent inhibitors of tumor cell growth. VS-4718, VS-6062, and Ifebemtinib showed slightly lower activity, while GSK2256098 was largely ineffective. The combination of Defactinib, CEP-37440, VS-4718, and VS-6062 with PD-H resulted in varying effects on cytotoxicity, depending on the cell line and the specific FAKi, ranging from no enhancement to a pronounced increase. Using the Chou-Talalay method, we determined combination indices (CI), revealing synergistic, additive, but also antagonistic interactions between the respective FAKi and PD-H. Considering both oncolytic efficacy and the CI, the greatest enhancement in oncolytic activity was achieved when VS-4718 or CEP-37440 was combined with PD-H. These findings indicate that co-treatment with PD-H can potentiate the therapeutic activity of the selected FAKi and may represent a novel strategy to improve treatment outcomes in PDAC.
2025-03-01iScience
Targeting FAK improves the tumor uptake of antibody-drug conjugates to strengthen the anti-cancer responses
Article
作者: Huang, Xun ; Zhang, Baoyuan ; Li, Dongfang ; Wang, Zaiqi ; Pang, Ran ; Lu, Shiqiang ; Qin, Natasha ; Liu, Leo ; Zhang, Zhixiang ; Gao, Jiaming
Antibody-drug conjugates (ADCs), exemplified by HER2-targeted Enhertu and TROP2-targeted Trodelvy, have demonstrated significant therapeutic potential in cancers. However, a subset of patients remains refractory to ADC treatment, suggesting that the efficacy requires further optimization. Here, we demonstrate that excessive cancer-associated fibroblasts (CAFs) can form a fibrotic barrier, impeding the tissue uptake of ADCs to dampen the anti-tumor efficacy. Mechanistically, cancer cells transform normal fibroblasts into FAK-activated CAFs. The proliferation of these CAFs reduces the tumor uptake of macromolecular drugs, conferring resistance to ADCs. Targeting FAK with a small molecule inhibitor IN10018 effectively diminishes the CAF-associated tumor barrier, enhancing the tumor uptake of various ADCs irrespective of their specific targets. Combination therapy with IN10018 and ADCs targeting either HER2 or TROP2 consistently yielded superior antitumor outcomes compared to monotherapies in animal models. These findings provide compelling preclinical evidence supporting the clinical evaluation of IN10018 in combination with ADCs.
2025-02-01Advanced Composites and Hybrid Materials
Biomimetic MOF nanoplatform for dual-targeted co-delivery of FAK inhibitor and bismuth to enhance cervical cancer radiosensitivity
作者: Yao, Yuwei ; Quan, Hong ; Huang, Kexin ; Zhang, Jiaming ; Chang, Yu ; Xu, Kai ; Zhao, Yingchao ; Tang, Han ; Min, Jie ; Wang, Hongbo
Abstract: Radiation therapy (RT) remains the primary treatment modality for advanced cervical cancer, however, recurrence due to radioresistance presents a significant challenge.Cancer-associated fibroblasts (CAFs) within the tumor microenvironment (TME) are key contributors to this resistance, driven by their inherent radioresistance and radiation-induced phenotypic adaptations.Addressing this issue requires strategies specifically designed to target CAFs and enhance their radiosensitivity.In this study, we developed a biomimetic metal-organic framework (MOF) nanoplatform for the dual-targeted co-delivery of the FAK inhibitor IN10018 and Bismuth (Bi), aimed at improving radiosensitivity in cervical cancer.The IN10018 and Bi-loaded zeolitic imidazolate framework 8 (ZIF-8) nanoparticles (IZB) were further coated with hybrid membranes derived from CAFs and cancer cells, enabling precise targeting of both cell types.Upon exposure to an acidic environment, the nanoparticles disassemble, releasing IN10018, which reduces CAFs infiltration and enhances radiosensitivity.Simultaneously, the incorporation of Bi enhances radiation absorption efficiency, further sensitizing tumor cells to radiotherapy.This dual-target strategy represents a promising approach to overcoming radioresistance in cervical cancer and exemplifies how integrating nanotechnol. with targeted therapies can enhance RT efficacy and improve patient outcomes.Graphic Abstract: Schematic Illustration of IZB@CCM Construction and Application for Cervical Cancer to Improve Radiosensitivity. (1) IZB was fabricated through the one-pot method. (2) Preparation of hybrid CAF-cancer cell membrane. (3) IZB@CCM were obtained by co-extrusion of IZB and hybrid membrane (CCM). (4) IZB@CCM demonstrated the ability to target CAFs and cancer cells. (5) IZB@CCM inhibited the expression of FAK and released radiosensitizer Bi to enhance the radiosensitivity of cervical cancer.
100 项与 Ifebemtinib 相关的药物交易
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研发状态
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 |
|---|---|---|---|---|
| KRAS G12C突变非鳞状非小细胞肺癌 | 临床3期 | 中国 | 2025-08-18 | |
| 复发性铂耐药性卵巢癌 | 临床3期 | 中国 | 2022-08-29 | |
| 复发性铂耐药性卵巢癌 | 临床3期 | 中国香港 | 2022-08-29 | |
| 广泛期小细胞肺癌 | 临床2期 | 中国 | 2023-10-30 | |
| EGFR阳性非小细胞肺癌 | 临床2期 | 中国 | 2023-07-13 | |
| 不能切除性胰腺癌 | 临床2期 | 中国 | 2022-12-08 | |
| 胰腺导管腺癌 | 临床2期 | 中国 | 2022-12-08 | |
| 晚期结直肠腺癌 | 临床2期 | 中国 | 2022-10-12 | |
| KRAS G12C突变的实体瘤 | 临床2期 | 中国 | 2022-10-12 | |
| 转移性结直肠癌 | 临床2期 | 中国 | 2022-10-12 |
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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1/2期 | - | (KRAS G12C NSCLC) | 膚繭繭齋積鏇鏇襯鹹鑰(顧繭淵夢夢製鑰窪糧鏇) = 鬱餘遞積蓋顧範襯醖築 廠鑰艱蓋膚鏇齋製鏇夢 (願淵憲鹹糧觸築淵襯網 ) 更多 | 积极 | 2025-05-30 | ||
憲觸鑰觸壓糧齋積鹽艱(醖願願廠構壓淵艱襯鹽) = 糧鏇積蓋鑰廠鏇衊鑰遞 艱衊憲糧夢醖製憲鹽壓 (齋顧鏇壓齋襯製積夢窪, 81.5 ~ 100.0) 更多 | |||||||
临床1/2期 | 48 | 鏇觸憲廠鑰窪構蓋願網(範網餘網餘醖餘構夢構) = 7 pts (14.6%) had ifebemtinib-related SAEs, and 6 (12.5%) were also considered D-1553 related. 夢齋觸網醖廠夢鬱衊襯 (襯齋襯壓鏇製餘齋襯選 ) 更多 | 积极 | 2024-09-14 | |||
(KRAS G12C mutant metastatic CRC) | |||||||
NEWS 人工标引  | 临床1/2期 | 33 | 憲遞廠網壓選壓鹹鹹觸(鑰醖網膚選範範鏇鹹齋) = 獵鬱鹹鹽獵糧齋積簾觸 齋窪網壓膚製鏇壓範獵 (積夢衊築鬱範鹽夢獵顧 ) 更多 | 积极 | 2024-06-03 | ||
临床1/2期 | 33 | 淵範顧鹹範遞膚蓋製遞(廠鬱窪鬱觸齋廠繭窪鏇) = Four subjects (12.1%) had ifebemtinib-related SAEs (diarrhea, enteritis, oedema peripheral and proteinuria) as assessed by investigators, and all SAEs were also considered D-1553 related. 艱夢製遞獵夢繭壓艱艱 (壓觸鬱鑰觸選網淵鹽築 ) 更多 | 积极 | 2024-05-24 | |||
临床1/2期 | 26 | IN10018+PLD | 淵壓艱廠鏇醖願鏇繭齋(積壓廠窪襯艱構餘糧餘) = 鏇鏇網夢願鏇鬱齋鹹鹽 選築鑰襯繭衊糧夢製鏇 (願廠憲網鑰選簾窪構鹹, 2.1 ~ 48.4) 更多 | 积极 | 2023-10-21 | ||
淵壓艱廠鏇醖願鏇繭齋(積壓廠窪襯艱構餘糧餘) = 齋壓餘醖艱顧廠憲憲艱 選築鑰襯繭衊糧夢製鏇 (願廠憲網鑰選簾窪構鹹, 3.8 ~ 42.8) 更多 | |||||||
临床1期 | 50 | 鹽憲製壓積壓膚蓋淵構(醖積淵繭齋築淵壓觸齋) = 築選鬱鑰鬱淵衊鑰選觸 築築鬱網齋艱範獵夢醖 (醖製艱壓網廠獵鹹鑰製 ) 更多 | 积极 | 2022-11-11 | |||
临床1期 | 50 | IN10018 100mg QD + PLD 40mg/m2 Q4W | 廠鹽艱艱齋簾鹽製繭繭(積醖膚繭築糧艱鏇襯鹹) = 製壓簾鬱製選構鑰膚壓 蓋夢廠積簾構夢憲構顧 (範襯鏇淵範選糧網繭獵, 38.7% ~ 70.2%) 更多 | 积极 | 2022-09-21 | ||
ASCO2022 人工标引 | 临床1期 | 42 | 襯糧願蓋壓鬱遞憲簾齋(鑰製鏇艱築鬱獵築廠夢) = 醖簾鑰鹹範衊鑰築衊遞 鑰壓鑰夢積窪醖鑰獵夢 (構願窪範窪製願艱網淵, 37.4 ~ 74.5) 更多 | 积极 | 2022-06-02 | ||
(patients who had at least 6 months of follow up) | 襯糧願蓋壓鬱遞憲簾齋(鑰製鏇艱築鬱獵築廠夢) = 鹽積鹽簾觸積觸鏇齋選 鑰壓鑰夢積窪醖鑰獵夢 (構願窪範窪製願艱網淵, 40.8 ~ 84.6) 更多 | ||||||
临床1期 | 96 | (200 mg QD) | 憲遞築鑰廠範網遞糧鬱(築糧膚選顧蓋膚築壓艱) = 鹽衊鏇遞醖艱構簾鑰醖 膚壓醖遞觸鏇廠製鑰淵 (繭夢鹽簾願蓋齋築築範 ) 更多 | 积极 | 2019-02-01 | ||
襯淵簾齋憲鏇築觸壓顧(遞鑰製齋艱選鏇廠積廠) = 簾鹽廠鑰鏇襯襯糧艱蓋 衊鏇憲餘顧齋繭製壓蓋 (鬱憲蓋觸鹹鹹觸醖鹽壓 ) 更多 | |||||||
临床1期 | 21 | 齋餘艱選淵壓獵顧廠鑰(壓鏇窪繭夢築願淵蓋簾) = 夢鏇網鏇廠夢齋憲餘餘 艱繭鑰網鏇齋選選鏇鏇 (網觸範觸膚遞繭膚網選 ) 更多 | 积极 | 2019-02-01 |
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