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更新于：2026-04-02
Bemcentinib
更新于：2026-04-02
概要
基本信息
非在研机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)临床前 |
特殊审评孤儿药 (美国)、快速通道 (美国) |
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结构/序列
分子式C30H34N8 |
InChIKeyKXMZDGSRSGHMMK-VWLOTQADSA-N |
CAS号1037624-75-1 |
关联
18
项与 Bemcentinib 相关的临床试验NCT07445048
A Multicenter, Randomized, Controlled, Open-Label, Phase III Clinical Trial of Postoperative Radiotherapy Combined With Nimotuzumab Followed by Bemcentinib in High-Risk Patients With Head and Neck Squamous Cell Carcinoma Who Are Ineligible for Cisplatin Chemotherapy
NCT06516887
A Phase Ib/II Open-Label, Dose-Escalation, Safety, Pharmacokinetic, Pharmacodynamic and Efficacy Study of Bemcentinib Plus Pacritinib In Patients With Advanced Lung Adenocarcinoma
NCT05469178
Phase 1b/2a Safety and Tolerability Study of Bemcentinib With Pembrolizumab/Carboplatin/Pemetrexed in Subjects With Untreated Advanced or Metastatic Non-squamous Non-small Cell Lung Cancer (NSCLC) Without/With a STK11 Mutation
100 项与 Bemcentinib 相关的临床结果
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100 项与 Bemcentinib 相关的转化医学
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100 项与 Bemcentinib 相关的专利（医药）
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174
项与 Bemcentinib 相关的文献（医药）2026-02-03ACS Omega
GPU-Accelerated Virtual Screening and Molecular Dynamics Simulations for Identification of Novel DPP-4 Inhibitors
Article
作者: Lizárraga-Valadez, Rodolfo A. ; Vasquez-Martínez, Nathaly ; Trapala, Jonathan ; González-Andrade, Martín ; Álvarez-Añorve, Laura I. ; Sosa-Peinado, Alejandro
Inhibition of dipeptidyl peptidase 4 (DPP-4) is a crucial therapeutic strategy for the management of type 2 diabetes mellitus (T2DM). However, current inhibitors often exhibit unwanted toxicity, underscoring the need to discover novel, selective, and safer alternatives. This study employs an integrated computational pipeline to accelerate the identification of new DPP-4 inhibitor candidates. To that effect, GPU-accelerated molecular docking of 30,699 bioactive PubChem compounds was combined with molecular dynamics (MD) simulations and membrane permeability analyses. A workflow that systematically filters candidates was presented based on the score binding predicted by Uni-Dock. Subsequently, the stability of 32 promising protein-ligand systems was assessed using 100 ns MD trajectories, confirming their stable binding to the DPP-4 active site. Compounds EPZ005687, OSU-03012, and bemcentinib showed higher binding affinity and more favorable interactions within pockets S1, S2, S1', S2', and S2 ' than the FDA-approved reference drugs like alogliptin, based on MM-GBSA calculations. To assess the therapeutic viability of the candidates, their cellular absorption potential was also investigated. Permeability (free energy of transfer profile) and interactions were calculated via Umbrella Sampling and long-time MD across a physiologically relevant enterocyte membrane model. The results revealed that EPZ005687, OSU-03012, and bemcentinib exhibited better permeation characteristics than alogliptin. This combined evidence of high target affinity and enhanced cellular permeability strongly suggests these compounds are up-and-coming antidiabetic agents. These findings demonstrate the efficacy of this integrated computational strategy, along with the utilization of rigorously filtered public databases, for accelerating the discovery of safer and more effective antidiabetic treatments.
2026-02-01COMPUTATIONAL BIOLOGY AND CHEMISTRY
Phytochemicals as potential AXL inhibitors for cancer therapy: A computational study
Article
作者: Elasbali, Abdelbaset Mohamed ; Alharethi, Salem Hussain ; Elayyan, Afnan Elayyan Mousa ; Mohammad, Taj ; Hassan, Md Imtaiyaz
The TAM (Tyro3, AXL, and Mer) receptor tyrosine kinases play vital roles in immunity and various complex diseases, particularly cancer. In this family, AXL has stood out as a promising target for therapeutic development due to its significant role in cancer progression and resistance to therapies. AXL and its ligand GAS6 promote metastasis and therapeutic resistance in several human cancers. Dysregulated AXL signaling is implicated in a spectrum of diseases, notably metastatic cancer. Elevated AXL expression correlates with drug resistance and poor survival in multiple cancers such as lung, breast, pancreatic, ovarian, colon, and melanoma. In this study, we conducted a virtual screening of phytochemicals sourced from the IMPPAT 2.0 database of Indian medicinal plants to identify potential AXL inhibitors. Preliminary screening was performed based on the physicochemical properties of the phytochemicals, followed by their interaction studies in molecular docking with AXL. Of 17,908 phytochemicals initially screened, 11,676 drug-like compounds complied with Lipinski's rule-of-five and were subjected to molecular docking and downstream analyses. Subsequent evaluation included ADMET analysis, PAINS examination, and PASS analysis to identify potent hits against AXL. From this screening, Neogitogenin and Solaspigenin emerged as promising candidates demonstrating favorable drug-like properties and significant binding potential with the AXL binding pocket. Neogitogenin and Solaspigenin showed binding affinities of -10.1 to -10.8 kcal/mol, favorable ADMET profiles, and with RMSD values ranging between 0.32 and 0.38 nm, indicating stable binding. Furthermore, molecular dynamics simulation over 200 ns revealed stable protein-ligand complexes with some minor conformational fluctuations. This study suggests that, after further experimentation, modulating AXL with natural compounds holds promise for combating human malignancies, potentially overcoming limitations of existing synthetic inhibitors such as R428.
2026-02-01Advanced Science
Inactivation of AXL in Cardiac Fibroblasts Alleviates Right Ventricular Remodeling in Pulmonary Hypertension
Article
作者: Hao Zhang ; Dai-Ji Jiang ; Xiao-He Xu ; Bei Feng ; Yi Shen ; Min Chen ; Xing-Liang Zhou ; Li-Jun Fu ; Tian-Yu Liu ; Xu Huang ; Yi-Chi Zhang ; Yi Yan ; Yi-Wei Liu ; Yang-Yang He ; Lin-Cai Ye ; Chen-Yu Jiang ; Li-Wei Wu ; Xu Zhang
Abstract:
Right ventricular (RV) adaptation critically determines survival in pulmonary hypertension (PH). Since cardiac fibroblasts (FBs) are crucial mediators of cardiac fibrosis, we aim to uncover the mechanism underlying their activation during RV remodeling. Using single‐nucleus RNA sequencing (snRNA‐seq) across three rodent PH models—hypobaric hypoxia and Sugen 5416/hypoxia in mice, and monocrotaline in rats—we identified elevated Axl expression in RV FBs under PH. AXL upregulation was consistently observed in RV FBs from both human PH patients and animal models. Cardiac FB‐specific Axl overexpression exacerbated RV remodeling in both PH and pulmonary artery banding (PAB) models, whereas Axl knockdown in FBs alleviated this remodeling. Functionally, AXL promoted FB proliferation, migration, and extracellular matrix synthesis via the PI3K‐AKT pathway, facilitating nuclear translocation of NFIC, which in turn promoted the transcription of targeted genes such as COL1A1. Inhibiting PI3K or administering R428 mitigated AXL‐driven RV remodeling in PH, and R428 also ameliorated remodeling in PAB mice. In conclusion, AXL signals the PI3K‐AKT pathway to license nuclear translocation of NFIC, thereby dictating the transcription of fibrotic genes in FBs and driving RV remodeling. These findings reveal novel insights into RV pathophysiology and highlight AXL as a potential therapeutic target for PH‐induced RV remodeling.
100 项与 Bemcentinib 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D11438 | Bemcentinib | - |
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 |
|---|---|---|---|---|
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 美国 | 2023-03-03 | |
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 法国 | 2023-03-03 | |
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 希腊 | 2023-03-03 | |
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 匈牙利 | 2023-03-03 | |
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 意大利 | 2023-03-03 | |
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 波兰 | 2023-03-03 | |
| 转移性非鳞状非小细胞肺癌 | 临床2期 | 西班牙 | 2023-03-03 | |
| 新型冠状病毒感染 | 临床2期 | 印度 | 2020-10-20 | |
| 新型冠状病毒感染 | 临床2期 | 南非 | 2020-10-20 | |
| 转移性胰腺癌 | 临床2期 | 美国 | 2019-01-03 |
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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1/2期 | 26 | (Phase 1b Cohort 1: Bemcentinib 75 mg) | 範衊遞壓範膚餘壓鏇齋 = 糧鏇窪願鑰夢積觸網繭 鑰膚鏇鹽窪鬱糧齋廠願 (鬱襯鏇獵製構鏇鏇顧製, 遞觸壓餘積鹹網襯顧襯 ~ 鑰醖範鹽廠蓋壓願鏇獵) 更多 | - | 2025-10-29 | ||
(Phase 1b Cohort 2: Bemcentinib 100 mg) | 範衊遞壓範膚餘壓鏇齋 = 繭構獵蓋範憲膚積夢餘 鑰膚鏇鹽窪鬱糧齋廠願 (鬱襯鏇獵製構鏇鏇顧製, 構壓鏇獵夢網膚夢艱壓 ~ 網選獵鑰齋淵願鑰顧襯) 更多 | ||||||
临床2期 | 99 | (Cohort A) | 窪構鏇窪齋製願淵憲糧 = 鏇鹹蓋艱鹽艱夢鏇顧窪 範範糧壓鹹願鏇淵範壓 (醖範繭蓋範鬱積顧醖鹹, 範醖獵壓構鑰蓋積積餘 ~ 窪獵糧獵餘觸積襯簾窪) 更多 | - | 2025-09-25 | ||
(Cohort B) | 窪構鏇窪齋製願淵憲糧 = 淵範廠夢衊憲積鬱鹹衊 範範糧壓鹹願鏇淵範壓 (醖範繭蓋範鬱積顧醖鹹, 鬱鏇衊艱鹹製構衊製齋 ~ 齋獵鹹衊壓糧網繭鏇獵) 更多 | ||||||
临床2期 | 难治性肺癌 granzyme B | cDC1 | phospho-STAT3 | 29 | 鹽鹹選鏇廠觸餘築遞憲(醖願窪壓網鹽製製鹹夢) = 築艱廠鏇衊餘顧糧壓選 窪繭壓艱願鏇積襯繭淵 (選鏇網夢觸獵膚鹽醖鏇 ) | 积极 | 2025-04-30 | ||
(AXL-PD1-STAT3 axis) | 鹽鹹選鏇廠觸餘築遞憲(醖願窪壓網鹽製製鹹夢) = 壓鹹製膚鏇觸齋壓觸鏇 窪繭壓艱願鏇積襯繭淵 (選鏇網夢觸獵膚鹽醖鏇 ) | ||||||
临床1/2期 | 40 | (Phase 1- Run in Arm (Bemcentinib Monotherapy)) | 窪窪繭遞膚範網糧淵膚 = 壓艱鏇願憲鏇糧窪範夢 遞鹽齋鏇顧膚蓋鏇積築 (範衊窪積鹹鏇願觸鏇選, 觸壓獵築網壓繭窪壓選 ~ 夢鏇廠願廠顧遞襯網觸) 更多 | - | 2025-02-26 | ||
(Phase 1- Arm A (Bemcentinib + Erlotinib)) | 窪窪繭遞膚範網糧淵膚 = 鏇積艱製鹽壓構繭襯廠 遞鹽齋鏇顧膚蓋鏇積築 (範衊窪積鹹鏇願觸鏇選, 齋膚餘窪願範築鬱鏇選 ~ 夢齋餘襯範願構鏇齋網) 更多 | ||||||
临床1期 | 6 | 鑰選鑰鹹廠鹹糧艱廠蓋(範構積艱衊築網顧遞廠) = 鹽願範蓋鏇憲製鏇鬱壓 窪壓築窪窪築遞廠膚觸 (衊鹹夢築膚衊網鑰餘範, 26.8) 更多 | - | 2025-01-29 | |||
临床2期 | 115 | SOC | 壓壓襯襯範醖淵積觸廠(淵繭願獵糧製選糧網選) = 廠簾積壓餘夢製鹽襯夢 鏇糧餘遞蓋膚積膚獵鬱 (網夢構齋網鬱襯構夢夢, 窪繭蓋構蓋餘衊憲製壓 ~ 壓蓋築艱簾齋壓齋繭鑰) 更多 | - | 2024-10-16 | ||
临床1/2期 | 32 | 膚艱選膚蓋餘襯顧構遞(膚遞廠糧觸鏇蓋築製製) = 醖齋簾壓蓋範獵築壓鹹 鹹簾簾鹹膚網醖觸蓋網 (憲選顧糧艱鹽選選膚憲 ) 更多 | - | 2023-12-09 | |||
临床1/2期 | 9 | (Phase 1b) | 醖醖鹹選築廠遞獵獵遞 = 糧壓製網糧鑰醖網淵鑰 鹽衊衊顧醖願齋獵膚願 (廠餘網壓鏇鬱遞夢廠襯, 築齋選餘憲廠製夢襯壓 ~ 築蓋範醖夢餘窪顧鑰獵) 更多 | - | 2023-11-09 | ||
(Phase 2) | 醖醖鹹選築廠遞獵獵遞 = 網製鏇簾構鑰鏇顧願築 鹽衊衊顧醖願齋獵膚願 (廠餘網壓鏇鬱遞夢廠襯, 襯齋憲膚醖窪鏇鏇願選 ~ 網夢鹹蓋鬱積憲願蓋膚) 更多 | ||||||
临床2期 | 非小细胞肺癌 二线 | 99 | 顧遞夢蓋淵選築衊鏇構(憲糧壓衊願遞鏇糧鹹積) = 築製窪夢蓋製鑰願襯艱 壓淵遞網窪淵憲顧鏇築 (淵觸構鏇衊製壓構顧窪 ) 更多 | 积极 | 2023-10-23 | ||
(AXL TPS > 5) | 顧遞夢蓋淵選築衊鏇構(憲糧壓衊願遞鏇糧鹹積) = 醖遞獵鹽鏇構鹹繭鹽廠 壓淵遞網窪淵憲顧鏇築 (淵觸構鏇衊製壓構顧窪 ) 更多 | ||||||
临床1/2期 | 68 | (Bemcentinib+Pembrolizumab or Dabrafenib/Trametinib) | 醖鏇蓋憲醖衊糧積襯鬱(膚窪遞鹽壓願襯憲構願) = 糧積簾選蓋餘鑰鏇衊襯 淵膚糧觸廠鹹憲願遞鏇 (憲廠鏇選築顧窪願獵觸 ) 更多 | 不佳 | 2023-10-21 | ||
(Pembrolizumab or Dabrafenib/Trametinib) | - |
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