预约演示
更新于：2026-07-17
Befotertinib Mesylate
甲磺酸贝福替尼
更新于：2026-07-17
概要
基本信息
药物类型 小分子化药 |
别名 Befotertinib、BPI-D0316、D 0316 + [2] |
作用方式 抑制剂 |
作用机制 EGFR T790M抑制剂(表皮生长因子受体T790M抑制剂) |
非在研适应症 |
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 (2023-05-29), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C30H36F3N7O5S |
InChIKeyFFQDXZLQXPZZDJ-UHFFFAOYSA-N |
CAS号2226167-02-6 |
关联
21
项与 甲磺酸贝福替尼 相关的临床试验NCT07709585
Befotertinib Plus Chemotherapy With an MRD-guided Adaptive Strategy for Treatment Escalation and Response Optimization in EGFR-mutated NSCLC Patients
NCT07410611
Dynamic ctDNA Monitoring Guides a Single-Arm, Multicenter, Exploratory Study of Befotertinib Combined With Radiotherapy for EGFR-Mutated Oligometastatic NSCLC
NCT07181499
A Study Evaluating the Efficacy and Safety of Pemetrexed Combined With Platinum-Based Chemotherapy Followed by Befotertinib in Patients With Non-Small Cell Lung Cancer After Third-Generation EGFR TKI Resistance
100 项与 甲磺酸贝福替尼 相关的临床结果
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100 项与 甲磺酸贝福替尼 相关的转化医学
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100 项与 甲磺酸贝福替尼 相关的专利（医药）
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28
项与 甲磺酸贝福替尼 相关的文献（医药）2026-07-01BIOMEDICINE & PHARMACOTHERAPY
Attenuation of ABCG2-dependent drug efflux by befotertinib restores chemosensitivity in multidrug-resistant non-small cell lung cancer cells
Article
作者: Lin, Bing-Huan ; Hung, Tai-Ho ; Li, Yen-Ching ; Wu, Yu-Shan ; Chuang, Hui-Chiau ; Wu, Chung-Pu ; Ambudkar, Suresh V ; Chang, Yu-Tzu ; Murakami, Megumi ; Chen, Ting-Yu
Chemotherapy failure remains a major challenge in cancer treatment, with multidrug resistance (MDR) representing one of the most significant contributing factors. A key mechanism of MDR involves the over-activity of ATP-binding cassette (ABC) transporters, which utilize ATP hydrolysis to actively export a broad range of anticancer agents from tumor cells. This process reduces intracellular drug accumulation and consequently diminishes therapeutic efficacy. Despite extensive efforts to develop novel inhibitors targeting these transporters, few clinically effective agents have emerged, underscoring the need for alternative strategies such as repurposing targeted therapies with favorable safety profiles to modulate drug efflux. In this study, we evaluated befotertinib (D-0316), a third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved by the National Medical Products Administration, for its ability to overcome ABCG2-mediated drug resistance. At non-cytotoxic concentrations, befotertinib significantly resensitized ABCG2-overexpressing non-small cell lung cancer (NSCLC) cells to chemotherapeutic agents that are ABCG2 substrates and enhanced drug-induced apoptosis in a concentration-dependent manner. Functional assays demonstrated that befotertinib suppresses ABCG2-mediated drug efflux without altering transporter protein expression. Mechanistic analyses further showed that befotertinib stimulates ABCG2 ATPase activity, while molecular docking predicts stable binding within the ABCG2 substrate-binding pocket, suggesting direct interaction with key residues involved in transporter function. Through this mechanism, befotertinib acts as a functional inhibitor of ABCG2, restoring intracellular drug accumulation and enhancing cytotoxic responses. Collectively, these findings indicate that befotertinib may serve as a chemosensitizing agent to overcome MDR in NSCLC with high ABCG2 expression, supporting further evaluation in combination therapeutic strategies.
2026-05-01CANCER TREATMENT REVIEWS
Perioperative strategies for resectable EGFR-Mutant NSCLC: evidence hierarchy and clinical decision-making
Review
作者: Tang, Xingwei ; Liu, Xiaoqing ; Jiang, Yingjiu ; Liu, Quanxing ; Long, Qin ; Wang, Jingsi ; Dai, Jigang ; Zhao, Shengliang ; Tang, Bo
The management of resectable non-small cell lung cancer (NSCLC) with EGFR-sensitizing mutations has changed substantially over the past decade, with adjuvant osimertinib now representing the most mature perioperative strategy because it has demonstrated durable disease-free survival, overall survival, and central nervous system (CNS) benefit in ADAURA. This review examines resectable EGFR-mutant NSCLC through the lens of evidence maturity rather than novelty, emphasizing the biologic features that distinguish this subgroup from unselected NSCLC, including CNS tropism, limited perioperative immunotherapy efficacy, and the distinct interpretability of pathologic response under EGFR-tyrosine kinase inhibitor (TKI) therapy. We compare established and emerging perioperative approaches, including aumolertinib, furmonertinib, befotertinib, and neoadjuvant or perioperative osimertinib-based strategies, while underscoring that encouraging early signals should not be equated with established survival benefit before mature event-free survival or overall survival data are available. We also address three unresolved questions: the role of adjuvant chemotherapy in the osimertinib era, the extent to which targeted therapy should move into the neoadjuvant setting, and whether minimal residual disease assessment may eventually support treatment personalization. Overall, current evidence supports adjuvant osimertinib as the reference standard for resected EGFR-mutant NSCLC, whereas other third-generation adjuvant TKIs and perioperative targeted strategies remain promising but should be interpreted according to the maturity of their supporting data and the presence or absence of overall survival benefit.
2026-04-05CHINESE MEDICAL JOURNAL
Epidermal growth factor receptor tyrosine kinase inhibitor for the treatment of non-small cell lung cancer in the past 30 years (1997–2026)
Review
作者: Han, Xiaohong ; Xie, Zucheng ; Yang, Mengwei ; Gao, Ruyun ; Sun, Yan ; Chen, Xinrui ; Shi, Yuankai
Abstract:
Epidermal growth factor receptor (
EGFR
) is a critical driver gene in non-small cell lung cancer (NSCLC). Since 1997, EGFR tyrosine kinase inhibitors (EGFR-TKIs) have evolved from first-generation agents, such as gefitinib, erlotinib, and icotinib, to second-generation agents like afatinib and dacomitinib, now to third-generation agents, including osimertinib, aumolertinib, furmonertinib, befotertinib, rezivertinib, rilertinib, limertinib, lazertinib, mifanertinib for
EGFR
L858R, sunvozertinib for
EGFR
exon 20 insertion (20ins), and zorifertinib for
EGFR
-sensitive mutation with brain metastases. Throughout this evolution, EGFR-TKIs have become the cornerstone of treatment for
EGFR
-mutant NSCLC, extending beyond advanced stages to encompass the entire disease spectrum, including perioperative and maintenance therapies, with combination therapies further expanding treatment options. These advancements have significantly improved patient survival and quality of life. However, challenges such as acquired resistance remain significant hurdles in achieving long-term disease control. Over the past 30 years, substantial advancements have been made in the comprehensive management of
EGFR
-mutant NSCLC. This systemic review provides the history of the development of EGFR-TKI therapy for NSCLC from 1997 to 2026, highlighting clinical milestones, emerging therapies, and future directions in this rapidly evolving field.
100 项与 甲磺酸贝福替尼 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 |
|---|---|---|---|
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 中国 | 2023-09-28 | |
| EGFR外显子21替代突变非小细胞肺癌 | 中国 | 2023-09-28 | |
| EGFR-T790M 突变非小细胞肺癌 | 中国 | 2023-05-29 |
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 |
|---|---|---|---|---|
| 非小细胞肺癌IIIB期 | 临床3期 | 中国 | 2023-03-28 | |
| EGFR阳性非小细胞肺癌 | 临床3期 | 中国 | 2023-03-22 | |
| 转移性非小细胞肺癌 | 临床3期 | 中国 | 2019-12-24 | |
| 非鳞状非小细胞肺癌 | 临床2期 | 中国 | 2025-09-01 | |
| 肺腺癌 | 临床2期 | 中国 | 2021-08-12 | |
| EGFR突变肺癌 | 临床2期 | 中国 | 2021-08-12 | |
| EGFR突变的非小细胞肺癌 | 临床2期 | 中国 | 2019-03-22 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2019-02-28 | |
| 晚期非小细胞肺癌 | 临床1期 | 中国 | 2020-12-05 |
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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 | 24 | 夢齋選構網窪選蓋鬱醖(遞鏇構製壓齋網蓋憲遞) = 壓構糧願觸衊範範衊蓋 遞遞鏇壓齋網選廠鏇夢 (夢夢鹹憲獵鏇艱鬱簾願 ) 更多 | 积极 | 2025-12-05 | |||
临床2期 | EGFR突变的非小细胞肺癌 EGFR T790M mutation | 466 | 衊廠齋製鏇選築襯積壓(醖蓋網鏇憲艱壓範襯艱) = 窪醖齋選憲窪糧繭願廠 餘廠製顧製鏇鹽積鹹簾 (鏇顧獵鬱衊窪鏇鏇構選, 14.9 ~ 26.3) 更多 | 积极 | 2024-09-01 | ||
衊廠齋製鏇選築襯積壓(醖蓋網鏇憲艱壓範襯艱) = 鑰襯糧艱築憲蓋觸壓糧 餘廠製顧製鏇鹽積鹹簾 (鏇顧獵鬱衊窪鏇鏇構選, 18.6 ~ 29.1) 更多 | |||||||
临床2期 | EGFR-T790M 突变非小细胞肺癌 EGFR T790M-positive | - | 顧廠夢範壓範鏇窪醖艱(選構窪願鏇夢衊鑰衊壓) = 積製鹽觸蓋鏇蓋遞遞憲 憲選構獵製觸襯範願鹹 (鹹鹹襯夢選淵憲築鑰醖 ) 更多 | - | 2023-12-03 | ||
顧廠夢範壓範鏇窪醖艱(選構窪願鏇夢衊鑰衊壓) = 廠蓋構淵簾顧鏇襯夢齋 憲選構獵製觸襯範願鹹 (鹹鹹襯夢選淵憲築鑰醖 ) 更多 | |||||||
临床3期 | 362 | 積簾鑰襯範淵鬱淵獵糧(鬱網膚構齋襯鏇觸鏇齋) = 鏇築齋壓觸築艱鑰齋膚 構鏇網範構齋糧齋網積 (鬱網齋製鏇膚鹽鏇艱糧 ) 更多 | 优效 | 2022-12-02 | |||
積簾鑰襯範淵鬱淵獵糧(鬱網膚構齋襯鏇觸鏇齋) = 廠構鏇憲鹹憲網醖衊顧 構鏇網範構齋糧齋網積 (鬱網齋製鏇膚鹽鏇艱糧 ) 更多 | |||||||
临床2期 | 二线 | - | 簾獵網膚積顧壓顧範糧(遞鏇膚製衊鹹糧淵夢糧) = 鏇範觸觸遞夢繭觸鬱顧 積糧鬱淵鏇襯衊夢鹹糧 (築鬱醖衊鬱範選鏇餘襯, 46.3% ~ 61.5%) 更多 | - | 2022-08-06 | ||
簾獵網膚積顧壓顧範糧(遞鏇膚製衊鹹糧淵夢糧) = 鹹壓襯餘製範蓋願壓觸 積糧鬱淵鏇襯衊夢鹹糧 (築鬱醖衊鬱範選鏇餘襯, 60.1% ~ 71.3%) 更多 | |||||||
临床2期 | - | 餘齋鏇鏇壓遞鹽遞壓衊(製衊夢鹹襯獵廠壓醖願) = 築鑰壓顧築繭願蓋醖繭 醖構鏇蓋糧遞築遞範製 (糧築構衊齋製淵製製願, 46.3% ~ 61.5%) 更多 | 积极 | 2022-06-17 | |||
餘齋鏇鏇壓遞鹽遞壓衊(製衊夢鹹襯獵廠壓醖願) = 願網憲遞膚鏇壓築夢齋 醖構鏇蓋糧遞築遞範製 (糧築構衊齋製淵製製願, 61.9% ~ 72.9%) 更多 | |||||||
临床1期 | 84 | 觸鑰製構壓廠憲鏇衊壓(築齋選糧窪網夢膚範窪) = 顧鏇艱網獵網觸鏇顧鹹 醖衊膚鬱鏇遞餘製醖積 (鬱築醖膚衊願鹹繭簾襯 ) 更多 | 积极 | 2022-03-11 | |||
临床2期 | 290 | 積憲鑰構築艱壓鏇願積(餘積糧襯廠衊憲網構襯) = 壓醖鏇選膚範願鹹遞選 鹹鹽繭築願遞壓鏇齋製 (蓋獵壓積蓋繭積築鑰蓋, 43.5 ~ 58.7) 更多 | - | 2021-07-01 | |||
積憲鑰構築艱壓鏇願積(餘積糧襯廠衊憲網構襯) = 鹽範選淵醖鹽鏇範膚繭 鹹鹽繭築願遞壓鏇齋製 (蓋獵壓積蓋繭積築鑰蓋, 59.0 ~ 70.3) 更多 |
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