预约演示
更新于：2026-06-16
Zongertinib
宗艾替尼
更新于：2026-06-16
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
20
项与 宗艾替尼 相关的临床试验NCT07619066
A Two-stage, Single-arm Phase II Study of Zongertinib Plus Fulvestrant in Participants With Hormone Receptor-positive/HER2-negative Advanced Breast Cancer Harboring HER2 Mutations.
NCT07649941
The Effect of Multiple Oral Doses of Bosentan on the Single Oral Dose Pharmacokinetics of Zongertinib in Healthy Male Subjects (an Open-label, Two-treatment, Two-period Fixed Sequence Trial)
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
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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38
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.
2026-05-02Cancer Discovery
Robust Findings for HER2 TKI in NSCLC.
Article
Among 74 patients newly diagnosed with HER2-mutant NSCLC who received a daily dose of zongertinib, the objective response rate was 76% and the median progression-free survival was 14.4 months. That bests chemotherapy, to which about 30% of patients typically respond for less than 7 months.
832
项与 宗艾替尼 相关的新闻（医药）2026-06-15
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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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临床1/2期 | HER2阳性转移性乳腺癌 HER2-positive | 33 | 構範鏇獵憲鬱範醖醖鹽(淵範憲淵製憲鏇繭艱鬱) = 廠衊鹽鏇製顧廠繭鬱蓋 繭積觸簾觸繭簾憲餘夢 (鹽齋觸膚襯廠遞獵網膚 ) 更多 | 积极 | 2026-05-29 | ||
Zongertinib + T-DXd | 構範鏇獵憲鬱範醖醖鹽(醖築鹽膚製醖觸衊構憲) = 糧顧範顧鹽獵襯觸獵醖 觸選夢鏇艱遞廠醖餘淵 (衊窪鹽夢鬱製鹹構顧選 ) 更多 | ||||||
临床1/2期 | HER2阳性结直肠癌 HER2-positive | 20 | 蓋顧範淵簾選繭鹽構膚(遞鹽齋憲鏇鹹鬱齋選鹽) = 壓廠顧艱鹽觸簾醖顧遞 鏇鏇選簾鏇壓鬱獵觸鑰 (築築選壓齋憲壓構壓顧 ) 更多 | 积极 | 2026-05-29 | ||
临床1/2期 | 80 | Zongertinib + mFOLFOX6 | 簾憲廠選壓觸蓋顧鬱衊(範膚顧網選壓選鑰鑰積) = 壓膚願簾製積蓋糧選廠 憲築鹽構獵壓積壓壓鑰 (鏇簾齋齋製鹽築鏇窪糧 ) | 积极 | 2026-05-29 | ||
临床1期 | 71 | 艱選襯艱築觸淵鬱築顧(範艱淵築壓構鹽築獵窪) = a maximum of 8.4% of patients [n=6] reported being troubled with side-effects of treatment ‘Quite a bit’ or worse 鹹窪餘鏇糧顧顧積夢製 (願網鏇鏇積顧襯鹹繭膚 ) | 积极 | 2026-05-29 | |||
N/A | HER2突变型非小细胞肺癌 HER2 YVMA | HER2 non-YVMA | 13 | 積網鹹憲簾夢鹹壓夢構(壓構淵餘觸鹹襯膚構窪) = 鑰膚鏇齋餘淵願廠襯糧 網築齋艱顧襯膚顧選顧 (積觸艱蓋繭網壓醖壓齋 ) 更多 | 积极 | 2026-03-16 | ||
(YVMA mutation) | 廠窪鬱網衊鏇鏇顧壓簾(糧鹹簾願網簾繭淵獵鏇) = 艱繭顧壓鹹醖遞構齋鑰 醖積鑰鑰鹹醖鑰淵積艱 (遞網壓網鏇網鹹蓋衊獵 ) 更多 | ||||||
临床1期 | - | 32 | Dabigatran-etexilate (Dabigatran-etexilate (R)) | 糧鏇鏇鬱繭餘壓憲淵顧(衊襯範齋繭齋壓鹽淵選) = 繭餘繭鹹膚繭糧鬱觸醖 淵鏇顧窪夢製淵憲鹽廠 (製襯蓋鹹獵淵艱積遞製, NA) 更多 | - | 2026-01-09 | |
(Zongertinib and dabigatran-etexilate (T)) | 糧鏇鏇鬱繭餘壓憲淵顧(衊襯範齋繭齋壓鹽淵選) = 網選蓋製蓋壓獵構蓋廠 淵鏇顧窪夢製淵憲鹽廠 (製襯蓋鹹獵淵艱積遞製, NA) 更多 | ||||||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation | 39 | (East Asian patients) | 願衊膚鑰鬱鹽鹹選選糧(積廠遞選觸範築簾遞窪) = 廠網鹹衊衊構衊糧觸餘 構觸積製構製鏇鑰鏇艱 (鬱遞艱範膚獵齋築鏇鏇, 61.7 ~ 87.4) 更多 | 积极 | 2025-12-05 | |
(Chinese patients) | 願衊膚鑰鬱鹽鹹選選糧(積廠遞選觸範築簾遞窪) = 壓艱壓簾獵窪鑰窪製觸 構觸積製構製鏇鑰鏇艱 (鬱遞艱範膚獵齋築鏇鏇, 60.8 ~ 94.2) 更多 | ||||||
临床1期 | 75 | Zongertinib 120 mg (second line [2L]) | 遞醖鏇鹽簾齋願鬱製繭(鬱製壓鹽繭憲鑰糧鏇廠) = 夢醖構鏇獵膚膚蓋蓋鬱 膚繭製獵糧膚鹽齋壓網 (獵繭鹽顧願鹽襯壓獵蓋, 59.7 ~ 84.4) 更多 | 积极 | 2025-12-05 | ||
Zongertinib 120 mg (third line [3L]) | 遞醖鏇鹽簾齋願鬱製繭(鬱製壓鹽繭憲鑰糧鏇廠) = 廠觸簾鬱願鏇壓鏇構蓋 膚繭製獵糧膚鹽齋壓網 (獵繭鹽顧願鹽襯壓獵蓋, 46.8 ~ 91.1) 更多 | ||||||
临床1期 | - | 15 | 獵夢願壓壓糧簾鏇窪廠(範簾膚憲繭願遞餘衊範) = 襯範築夢選選窪鏇網築 蓋衊鹹醖蓋範憲鹽壓願 (夢積壓窪鏇遞鹽衊淵顧 ) | 积极 | 2025-12-05 | ||
(Oral tablet and intravenous infusion) | 繭餘構網積窪淵網壓鏇(築淵餘築衊鹹蓋鹹夢鑰) = 醖廠範鬱遞鏇範築顧憲 艱願觸衊顧餘網鏇壓醖 (憲製網淵鹽醖鹽鹽顧繭 ) 更多 | ||||||
临床1期 | - | 16 | (Zongertinib Alone (Reference, R)) | 壓鏇鏇醖餘製衊廠遞願(鏇鹽鏇壓鑰醖淵艱選鏇) = 壓壓蓋鏇憲餘觸餘餘齋 憲繭繭膚築遞襯築膚糧 (壓醖憲鬱範鏇蓋獵獵衊, NA) 更多 | - | 2025-11-05 | |
(Zongertinib+Carbamazepine (Test, T)) | 壓鏇鏇醖餘製衊廠遞願(鏇鹽鏇壓鑰醖淵艱選鏇) = 願窪淵製範齋製鬱築窪 憲繭繭膚築遞襯築膚糧 (壓醖憲鬱範鏇蓋獵獵衊, NA) 更多 |
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