预约演示
更新于：2026-05-21
Zongertinib
宗艾替尼
更新于：2026-05-21
概要
基本信息
药物类型 小分子化药 |
别名 佐博替尼、宗格替尼、BI 1810631 + [4] |
靶点 |
作用方式 拮抗剂 |
作用机制 HER2拮抗剂(受体蛋白酪氨酸激酶 erbB-2拮抗剂) |
在研适应症 |
非在研适应症- |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 美国 (2025-02-26), |
最高研发阶段(中国)批准上市 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、加速批准 (美国)、优先审评 (中国)、突破性疗法 (中国)、附条件批准 (中国)、孤儿药 (日本)、局长国家优先审评券 (美国)、快速通道 (美国) |
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结构/序列
分子式C29H29N9O2 |
InChIKeyYSGNGFPNTLERCR-UHFFFAOYSA-N |
CAS号2728667-27-2 |
关联
19
项与 宗艾替尼 相关的临床试验CTIS2025-523193-16-00
A study in healthy men to test how bosentan influences the amount of zongertinib in the blood
NCT07486817
Beamion 44: A Randomized, Open-label, Multi-center Phase IIa Platform Trial to Evaluate the Safety and Tolerability of Zongertinib Plus Platinum-based Doublet Chemotherapy With or Without Pembrolizumab (and Potential Other Combinations) in Treatment-naïve Patients With Locally Advanced/Metastatic Non-squamous NSCLC With Activating HER2 Mutations
CTIS2025-524769-26-00
FINACCESS - Finnish National Study for Early Access to Cancer Therapies
100 项与 宗艾替尼 相关的临床结果
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100 项与 宗艾替尼 相关的转化医学
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100 项与 宗艾替尼 相关的专利（医药）
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36
项与 宗艾替尼 相关的文献（医药）2026-06-01LUNG CANCER
First case report of transformation of adenocarcinoma to adenosquamous carcinoma with giant-cell carcinoma harboring HER2 mutation after zongertinib (BI 1810631) resistance
Article
作者: Zhu, Yue ; Xu, Bing-Fei ; Yan, Li-Xu ; Wu, Yi-Long ; Lin, Jia-Xin ; Sun, Yue-Li ; Tu, Hai-Yan ; Yin, Kai
BACKGROUND:
Human epidermal growth factor receptor 2 (HER2) mutations have been identified as a rare molecular subset in non-small cell lung cancer (NSCLC) with poor prognosis and limited treatment options. Zongertinib, an irreversible covalent HER2 inhibitor, demonstrated promising response rates and safety profile in the Beamion LUNG-1 trial, leading to approval for previously treated HER2-mutant NSCLC. Nevertheless, the resistance mechanisms to zongertinib remain largely unexplored despite its established efficacy.
CASE DESCRIPTION:
A 52-year-old female never-smoker was diagnosed with stage IV lung adenocarcinoma in March 2023. Next generation sequencing (NGS) of tumor tissue identified an HER2 exon 20p.Y772_A775dup mutation along with concurrent NF1, RB1, and TP53 mutations, plus increased AKT2 gene copy number. First-line platinum-based chemotherapy combined with immunotherapy was initiated with transient disease stabilization. The patient subsequently achieved a confirmed partial response to zongertinib (240 mg daily) in the Beamion LUNG-1 trial, maintaining clinical benefit for 20 months until symptomatic progression emerged. Repeat biopsy revealed histologic transformation to adenosquamous carcinoma with giant-cell features, with PD-L1 expression switch from undetectable to 80% positivity. The genomic profiling showed persistent original mutations plus newly acquired MAP3K1 mutation, HER2 amplification, and TERT amplification. In the third-line treatment, the patient was enrolled in a clinical trial evaluating BC3195, a novel CDH3-targeted antibody-drug conjugate, and achieved partial response at the time of reporting.
CONCLUSION:
This case is the first to elucidate the putative resistance mechanisms to zongertinib in HER2-mutant lung adenocarcinoma might be transformation of adenosquamous with giant-cell carcinoma and acquired HER2 amplification through integrated histological and molecular analyses. These findings highlight the necessity of post-progression biopsy and genomic profiling to characterize resistance evolution and guide subsequent therapy selection.
2026-05-03Future Oncology
Evaluating zongertinib in the treatment of patients with HER2-mutant non-small cell lung cancer
Review
作者: Kim, Jinyong ; Ahn, Myung-Ju
HER2 mutations define a distinct molecular subset of non-small cell lung cancer (NSCLC) associated with poor outcomes and limited benefit from conventional systemic therapies. Zongertinib is a next-generation, HER2-selective irreversible tyrosine kinase inhibitor (TKI) designed to spare wild-type EGFR and improve tolerability. Zongertinib has demonstrated clinically meaningful systemic and intracranial activity with a manageable safety profile across multiple cohorts in the phase Ia/Ib Beamion LUNG-1 study, including previously treated, treatment-naïve, post-HER2 antibody-drug conjugate (ADC), non-tyrosine kinase domain mutation, and brain metastases populations. This review summarizes the pharmacologic rationale, clinical efficacy, safety, biomarker analyses, and ongoing phase III development of zongertinib in HER2-mutant NSCLC.
2026-05-01BIOMEDICAL CHROMATOGRAPHY
Pharmacokinetics, Bioavailability, and Metabolism of Zongertinib, a Novel HER2‐Selective Tyrosine Kinase Inhibitor, in Rat by Liquid Chromatography Hyphenated With Electrospray Ionization Tandem Mass Spectrometry
Article
作者: Wang, Fang ; Ma, Zheheng ; Chu, Furui ; Sun, Wenfei
ABSTRACT:
Zongertinib, a selective human epidermal growth factor receptor 2 (HER2) tyrosine kinase inhibitor, has been approved by the US Food and Drug Administration for the treatment of non‐small cell lung cancer. This study aimed to develop a sensitive and cost‐effective LC–MS/MS method for quantifying zongertinib in rat plasma. Following protein precipitation with acetonitrile, samples were analyzed on an ACQUITY BEH C
18
column using a gradient of 0.1% formic acid and acetonitrile at 40°C within a 2‐min run time. The assay demonstrated excellent linearity from 1 to 1000 ng/mL (
r
> 0.995). All validation parameters—including precision, accuracy, matrix effect, recovery, and stability—met accepted criteria for bioanalytical quantification. The validated method was successfully applied to a pharmacokinetic study in rats. Additionally, metabolites in rat plasma were investigated using LC‐Orbitrap‐HRMS. Three metabolites were identified and structurally characterized based on accurate mass and fragmentation patterns, revealing metabolic pathways such as oxygenation, demethylation, and epoxide hydrolysis. This is the first report on the method validation for the measurement of zongertinib in biological matrices, which enables clinical development of zongertinib and can be applied for clinical pharmacokinetics and therapeutic drug monitoring in future clinical practice.
100 项与 宗艾替尼 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 |
|---|---|---|---|
| 转移性非鳞状非小细胞肺癌 | 美国 | 2026-02-26 | |
| HER2阳性非鳞状非小细胞肺癌 | 美国 | 2025-08-08 | |
| HER2突变型非小细胞肺癌 | 美国 | 2025-02-26 |
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 | 申请上市 | 加拿大 | 2026-01-01 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 美国 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 中国 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 日本 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 阿根廷 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 澳大利亚 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 奥地利 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 比利时 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 巴西 | 2026-01-16 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 加拿大 | 2026-01-16 |
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临床结果
临床结果
适应症
分期
评价
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N/A | HER2突变型非小细胞肺癌 HER2 YVMA | HER2 non-YVMA | 13 | 網衊簾蓋鹹鹹憲繭憲艱(壓鏇淵壓鹽範願衊衊蓋) = 築蓋醖憲積觸壓鬱廠範 窪遞窪網簾鑰鑰窪製膚 (齋鏇構繭鑰選襯餘鑰鬱 ) 更多 | 积极 | 2026-03-16 | ||
(YVMA mutation) | 夢觸壓衊窪鬱淵襯鏇範(選夢廠鑰蓋壓獵簾築膚) = 鬱餘鏇顧觸壓壓鏇製憲 鏇鹽選蓋夢蓋膚蓋鏇鬱 (廠築餘糧築蓋顧築鑰鏇 ) 更多 | ||||||
临床1期 | - | 32 | Dabigatran-etexilate (Dabigatran-etexilate (R)) | 選衊鹽壓窪齋齋構齋膚(鑰獵繭網鏇網遞襯鏇艱) = 餘願觸廠鑰遞糧遞積願 糧願選遞網襯襯醖餘製 (製壓觸繭餘鑰鏇淵襯淵, NA) 更多 | - | 2026-01-09 | |
(Zongertinib and dabigatran-etexilate (T)) | 選衊鹽壓窪齋齋構齋膚(鑰獵繭網鏇網遞襯鏇艱) = 襯衊範構獵窪廠遞廠廠 糧願選遞網襯襯醖餘製 (製壓觸繭餘鑰鏇淵襯淵, NA) 更多 | ||||||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation | 39 | (East Asian patients) | 膚積夢鏇遞廠繭獵鹹鏇(夢選淵膚襯遞顧鏇範簾) = 繭夢窪繭衊繭選糧簾鏇 廠淵醖遞廠獵鬱繭網構 (顧衊願艱膚選積獵築憲, 61.7 ~ 87.4) 更多 | 积极 | 2025-12-05 | |
(Chinese patients) | 膚積夢鏇遞廠繭獵鹹鏇(夢選淵膚襯遞顧鏇範簾) = 夢獵築鏇鏇糧艱選築醖 廠淵醖遞廠獵鬱繭網構 (顧衊願艱膚選積獵築憲, 60.8 ~ 94.2) 更多 | ||||||
临床1期 | 75 | Zongertinib 120 mg (second line [2L]) | 鹹鑰簾糧願膚築遞構顧(艱糧製鹽醖網簾艱膚廠) = 鹽淵遞廠願窪獵獵鹹願 鹽鑰製餘蓋觸膚衊窪餘 (顧齋艱網艱願窪構範選, 59.7 ~ 84.4) 更多 | 积极 | 2025-12-05 | ||
Zongertinib 120 mg (third line [3L]) | 鹹鑰簾糧願膚築遞構顧(艱糧製鹽醖網簾艱膚廠) = 願廠蓋積範築壓壓顧繭 鹽鑰製餘蓋觸膚衊窪餘 (顧齋艱網艱願窪構範選, 46.8 ~ 91.1) 更多 | ||||||
临床1期 | - | 15 | 積淵選餘餘製壓範夢糧(醖簾糧蓋觸醖遞壓衊壓) = 壓夢壓鹽窪蓋蓋糧壓衊 遞獵壓鑰夢淵膚鏇壓醖 (廠齋鏇鏇糧艱餘顧構淵 ) | 积极 | 2025-12-05 | ||
(Oral tablet and intravenous infusion) | 蓋衊選齋鬱廠鏇鏇餘觸(窪顧憲築範鏇製憲遞餘) = 鑰製膚鹹積廠鏇遞衊醖 鑰積蓋選蓋顧鹹網鏇繭 (獵衊衊願廠築觸齋築鑰 ) 更多 | ||||||
临床1期 | - | 16 | (Zongertinib Alone (Reference, R)) | 艱鬱網鏇廠築壓鑰夢衊(醖襯遞夢鑰鏇鬱襯願夢) = 餘鹽艱鬱鹽廠鹽憲襯襯 夢築鏇築獵觸壓壓蓋餘 (餘觸觸遞夢築顧齋鏇選, NA) 更多 | - | 2025-11-05 | |
(Zongertinib+Carbamazepine (Test, T)) | 艱鬱網鏇廠築壓鑰夢衊(醖襯遞夢鑰鏇鬱襯願夢) = 鏇餘顧窪膚糧遞衊遞蓋 夢築鏇築獵觸壓壓蓋餘 (餘觸觸遞夢築顧齋鏇選, NA) 更多 | ||||||
临床1期 | - | 13 | (TF1 Fasted (R)) | 構餘蓋願鑰選簾願蓋淵(鹽蓋簾襯遞憲鹹遞選鏇) = 獵齋齋築艱構構衊夢糧 積齋膚鑰繭繭鹽網網鹽 (廠壓艱顧壓廠範繭膚醖, 52.7) 更多 | - | 2025-11-04 | |
(NF Fasted (T1)) | 構餘蓋願鑰選簾願蓋淵(鹽蓋簾襯遞憲鹹遞選鏇) = 淵窪遞鹽築簾遞衊壓壓 積齋膚鑰繭繭鹽網網鹽 (廠壓艱顧壓廠範繭膚醖, 18.8) 更多 | ||||||
临床1期 | 74 | Zongertinib 120 mg | 觸窪餘醖獵積網衊獵積(衊憲觸網蓋願膚糧鏇鹽) = 網淵壓繭壓選繭艱蓋蓋 夢鏇簾憲鹹鏇顧膚鏇淵 (遞廠鬱鏇衊築鏇夢製糧, 66 ~ 85) 更多 | 积极 | 2025-10-17 | ||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation | 185 | (HER2 aberration-positive solid tumors, Phase Ia) | 膚獵築餘選鏇製艱構糧(醖膚鏇獵網鹹製繭齋獵) = 夢製鑰艱窪淵憲壓廠製 壓襯鬱鏇壓鹽夢夢選鹹 (獵顧醖選艱壓鏇願獵齋 ) 更多 | 积极 | 2025-10-17 | |
(previously treated HER2-mutant NSCLC, Phase Ib Cohort 1) | 膚獵築餘選鏇製艱構糧(醖膚鏇獵網鹹製繭齋獵) = 糧觸餘餘壓蓋構齋觸鏇 壓襯鬱鏇壓鹽夢夢選鹹 (獵顧醖選艱壓鏇願獵齋 ) 更多 | ||||||
临床1期 | - | 16 | (Zongertinib iCF Fed (Test (T))) | 壓積簾積製醖築顧廠範(窪構糧廠鑰網齋網觸願) = 網繭築廠顧製糧網廠顧 餘鬱觸獵膚鏇壓膚網醖 (選選艱衊網艱築醖製蓋, NA) 更多 | - | 2025-09-22 | |
(Zongertinib iCF Fasted (Reference (R))) | 壓積簾積製醖築顧廠範(窪構糧廠鑰網齋網觸願) = 餘餘齋衊衊衊齋憲繭繭 餘鬱觸獵膚鏇壓膚網醖 (選選艱衊網艱築醖製蓋, NA) 更多 |
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