预约演示
更新于：2025-06-07
Silevertinib
更新于：2025-06-07
概要
基本信息
药物类型 小分子化药 |
别名 BDTX 1535、BDTX-1535、BDTX1535 |
靶点 |
作用方式 拮抗剂 |
作用机制 EGFR拮抗剂(表皮生长因子受体erbB1拮抗剂) |
在研适应症 |
非在研适应症- |
非在研机构- |
权益机构- |
最高研发阶段临床2期 |
首次获批日期- |
最高研发阶段(中国)- |
特殊审评快速通道 (美国) |
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结构/序列
分子式C30H30ClFN6O2 |
InChIKeyLMOVDLRMIRLIJF-TUVXKDNKSA-N |
CAS号2607829-38-7 |
关联
2
项与 Silevertinib 相关的临床试验NCT06072586
A Phase 0/1 Study of BDTX-1535 in Recurrent High-Grade Glioma (HGG) and Newly Diagnosed Glioblastoma (nGBM) Participants With EGFR Alterations or Fusions Scheduled for Resection to Evaluate Central Nervous System (CNS) Penetration With PK-triggered Expansion Cohort
NCT05256290
A Phase 1/2 Study to Assess BDTX-1535, an Oral EGFR Inhibitor, in Patients With Glioblastoma or Non-Small Cell Lung Cancer
100 项与 Silevertinib 相关的临床结果
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100 项与 Silevertinib 相关的转化医学
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100 项与 Silevertinib 相关的专利（医药）
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3
项与 Silevertinib 相关的文献（医药）2025-06-01BIOORGANIC & MEDICINAL CHEMISTRY
A clinical review on third and fourth generation EGFR tyrosine kinase inhibitors for the treatment of non-small cell lung cancer
Review
作者: Patel, Harun M ; Patil, Chandragouda R ; Gawli, Chandrakant S
"Epidermal growth factor receptor (EGFR)" mutations are pivotal in the pathogenesis of "Non-Small Cell Lung Cancer (NSCLC)," which is associated with high morbidity and mortality rates. The advent of third and fourth-generation EGFR tyrosine kinase inhibitors (TKIs) has significantly advanced the therapeutic landscape for EGFR-mutant NSCLC, particularly in overcoming resistance mutations such as T790M and C797S. This review delves into the current clinical status, efficacy, safety profiles, and regulatory approvals of third-generation EGFR TKIs, including Osimertinib, Lazertinib, Furmonertinib, Aumolertinib, Rezivertinib, Befotertinib, Sunvozertinib. Furthermore, it explores emerging fourth-generation EGFR TKIs designed to address resistance mechanisms beyond those targeted by their predecessors. Notable fourth-generation candidates such as TQB3804, BPI-361175, BDTX-1535, WJ13404, QLH11811, H002, HS-10375, BBT-207, JIN-A02, and HS-10504 are highlighted for their potential to overcome the C797S mutation. The review emphasizes the importance of these advanced inhibitors in enhancing "progression-free survival and overall survival rates". By evaluating the therapeutic potential and limitations of these EGFR TKIs, this review aims to guide future research in the management of EGFR-mutant NSCLC. This acts as guiding beacon for the strategic design and development of third and fourth generation EGFR-TK inhibitors to overcome the drug resistance hurdles in the development of EGFR-TK inhibitors.
2024-11-01Translational Cancer Research
Targeting C797S mutations and beyond in non-small cell lung cancer—a mini-review
Review
作者: Fenchel, Klaus ; Dempke, Wolfram C M
Non-small cell lung cancer (NSCLC) represents over 80% of lung cancer cases and has a high mortality worldwide, however, targeting common epidermal growth-factor receptor (EGFR) alterations (i.e., del19, L858R) has provided a paradigm shift in the treatment of NSCLC. Uncommon EGFR mutations, however, show variable efficacy to EGFR-targeted drugs depending on the molecular alterations within exons 18-21 which underlying biological mechanism are far from being clear. The substitution mutations of G719X in exon 18, L861Q in exon 21, S768I in exon 20, and exon 20 insertions are the most frequent mutations among the uncommon mutations. The development of fourth-generation EGFR-tyrosine kinase inhibitor (TKIs) has gained increased interest as these drugs are able to inhibit resistance mutations (e.g., C797S) often detected in NSCLC patients' resistance to third-generation EGFR TKIs. BDTX-1535 is an orally bioavailable, brain-penetrating, mutation-selective, irreversible EGFR inhibitor with significant antitumour activity in NSCLCs and glioblastomas (phase I/II trials ongoing). It is a fourth-generation EGFR inhibitor that was found to overcome resistance to osimertinib in preclinical models and has shown promising activity in NSCLC patients harbouring C797S mutations. In experimental models BDTX-1535 was found to inhibit all common EGFR mutations and more than 50 of uncommon mutations including T790M, C797S, L718X, E709X, S784F, V834L and A289V, however, exon 20 insertions are inhibited to a much lesser extent. In addition, mutations in the extracellular domain of the EGF receptor (e.g., EGFRvII, III, IV) can be blocked as well. It should be noted that in up to 50% of all NSCLC patients who progress following osimertinib or other EGFR TKI therapy no underlying resistance mechanism can be identified suggesting that non-mutational signal transduction pathways may also be operative, and intratumoural heterogeneity has been found to be a major contributor to resistance and it consists of three main mechanisms: (I) drug-tolerant persister (DTP) cells, (II) chromosomal instability, and (III) extrachromosomal extracellular DNA (ecDNA) (seen in over 50% of NSCLCs) suggesting that novel EGFR TKIs will include many challenges in sufficiently targeting on-target resistance mechanisms. The development of novel drugs that can overcome TKI resistance in NSCLC patients harbouring the C797S mutation and beyond is, therefore, eagerly warranted.
2021-12-01Cancer discovery1区 · 医学
BDTX-1535 Goes after Osimertinib Resistance
1区 · 医学
Article
Abstract:
According to a preclinical report, the investigational tyrosine kinase inhibitor BDTX-1535 may mitigate resistance to osimertinib, the standard of care for EGFR-mutant non–small cell lung cancer. It could also potentially treat central nervous system metastases, having shown preclinical efficacy in glioblastoma.
83
项与 Silevertinib 相关的新闻（医药）2025-06-04
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2025-04-17
临床结果临床1期申请上市ASH会议
2025-03-20
100 项与 Silevertinib 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 |
|---|---|---|---|---|
| 晚期鳞状非小细胞肺癌 | 临床2期 | 美国 | 2022-03-31 | |
| 晚期鳞状非小细胞肺癌 | 临床2期 | 加拿大 | 2022-03-31 | |
| EGFR阳性非小细胞肺癌 | 临床2期 | 美国 | 2022-03-31 | |
| EGFR阳性非小细胞肺癌 | 临床2期 | 加拿大 | 2022-03-31 | |
| 多形性胶质母细胞瘤 | 临床2期 | 美国 | 2022-03-31 | |
| 多形性胶质母细胞瘤 | 临床2期 | 加拿大 | 2022-03-31 | |
| 转移性非小细胞肺癌 | 临床2期 | 美国 | 2022-03-31 | |
| 转移性非小细胞肺癌 | 临床2期 | 加拿大 | 2022-03-31 | |
| 继发性肺恶性肿瘤 | 临床2期 | 美国 | 2022-03-31 | |
| 继发性肺恶性肿瘤 | 临床2期 | 加拿大 | 2022-03-31 |
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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 | 27 | BDTX-1535 200 mg | 網鬱餘夢蓋齋網艱鹽淵(積顧遞構夢遞顧鏇蓋夢) = 夢糧淵艱製齋襯積網醖 顧齋鑰願範鏇觸鑰醖窪 (鬱簾鏇襯窪鹹憲積餘鬱 ) 更多 | 积极 | 2024-09-23 | ||
BDTX-1535 200 mg (either C797S or P-loop alpha-C helix compressing (PACC, a major subset of NCMs)) | 網鬱餘夢蓋齋網艱鹽淵(積顧遞構夢遞顧鏇蓋夢) = 壓鏇網餘選醖醖齋餘蓋 顧齋鑰願範鏇觸鑰醖窪 (鬱簾鏇襯窪鹹憲積餘鬱 ) | ||||||
早期临床1期 | 复发性恶性胶质瘤 EGFR alterations | EGFR fusions | 7 | BDTX-1535 200 mg | 範願築遞選艱鹽衊觸夢(衊構遞鏇願遞選鏇範窪) = No serious adverse events were observed among patients in the Phase 1 component of the study 繭鏇餘醖齋鑰範簾築網 (積窪衊製餘鏇築蓋窪範 ) | 积极 | 2024-05-24 | |
临床1期 | 复发性胶质母细胞瘤 EGFR alterations | EGFRvIII | missense mutations | 54 | BDTX-1535 15mg QD | 蓋餘築願壓膚製鹹淵製(鬱憲獵醖餘獵觸網遞夢) = Gr 3 TRAEs ≥ 10% included rash (19%) reported at 300 or 400 mg QD doses 蓋簾襯齋構蓋鑰蓋餘積 (壓鏇鬱憲鑰遞觸淵獵顧 ) 更多 | 积极 | 2024-05-24 | |
临床1期 | 22 | 壓積鑰淵鑰廠鬱壓範襯(鏇齋範製淵糧齋繭蓋獵) = consistent with the EGFR tyrosine kinase inhibitor (TKIs) class of drugs, including primarily Grade 1 and 2 diarrhea and rash 鏇構膚廠願獵鏇膚鏇範 (遞窪鹹繭構繭簾廠齋願 ) | 积极 | 2023-12-13 | |||
临床1期 | - | 衊餘壓選簾簾餘鬱構襯(築糧鏇鹽蓋鬱窪選艱願) = No patients experienced dose limiting toxicity at 15-200 mg QD doses. One of 15 patients treated at the 300 mg QD dose experienced dose limiting diarrhea and 5 of 12 patients at the 400 mg QD dose experienced dose limiting toxicity (diarrhea, 2 patients; rash, stomatitis, fatigue and decreased appetite, 1 patient each). 繭膚餘選餘鹹鑰憲鹽餘 (範鑰願鏇築窪鏇壓遞獵 ) 更多 | 积极 | 2023-06-27 |
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