预约演示
更新于：2026-04-24
Zongertinib
宗艾替尼
更新于：2026-04-24
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
18
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
NCT07195695
Beamion LUNG-3: A Randomized, Controlled, Multi-center Trial Evaluating Zongertinib as an Adjuvant Monotherapy Compared With Standard of Care in Patients With Early-stage, Resectable Non-small Cell Lung Cancer (Stage II-IIIB) Harboring Tyrosine Kinase Domain 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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30
项与 宗艾替尼 相关的文献（医药）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.
2026-04-01Journal of Thoracic Oncology
ERBB2 activating mutations and co-occurring genomic alterations contribute to disease heterogeneity in patients with ERBB2-mutant lung cancer
Article
作者: Stockhammer, Paul ; Li, Fangyong ; Politi, Katerina ; Schillo, Jacob L ; Goldberg, Sarah B ; El Zarif, Talal ; Grant, Michael J
BACKGROUND:
ERBB2 mutations occur in 1-4% of all non-small cell lung cancers (NSCLCs). Trastuzumab-deruxtecan and the novel ERBB2 tyrosine kinase inhibitors zongertinib and sevabertinib are FDA-approved for the treatment of metastatic ERBB2-mutant NSCLC based on data from tumors harboring tyrosine kinase domain (TKD) mutations. The clinico-genomic characteristics of NSCLC tumors with ERBB2 mutations beyond the TKD remain largely unexplored.
METHODS:
Patients with NSCLC with oncogenic ERBB2 mutations included in two independent cohorts [AACR Project GENIE database and the US-based deidentified Flatiron Health-Foundation Medicine advanced NSCLC Clinico-Genomic Database (FH)] were studied. The clinico-genomic characteristics of patients with tumors harboring TKD, extracellular (ECD), or transmembrane (TMD)/juxtamembrane domain (JMD) ERBB2 mutations were compared and clinical outcomes with chemoimmunotherapy were evaluated.
RESULTS:
483 patients (GENIE cohort) and 286 patients (FH cohort) with ERBB2-mutant NSCLC were included. In both cohorts, most patients had tumors harboring TKD (75 and 71%), followed by ECD (18 and 24%) and TMD/JMD mutations (7 and 5%). In both cohorts, male patients (p<0.05), patients with squamous NSCLC tumors (p=0.0001 and p=0.0002), and patients with a smoking history (p=0.01 and p<0.0001) were more likely to have ECD-mutant tumors. In the GENIE cohort with detailed genomic information available, ECD- vs. TKD-mutant tumors had a higher median TMB (p<0.0001) and higher rates of co-mutations in EGFR (p<0.0001), KRAS (p<0.0001), STK11 (p<0.0001), KEAP1 (p<0.0001), and SMARCA4 (p<0.0001). TMD/JMD-mutant tumors had high rates of PIK3CA (24%) and RBM10 (18%) co-mutations. In the FH cohort with detailed outcome data available, among patients with advanced ERBB2-mutant NSCLC treated with first-line chemoimmunotherapy, those with ECD-mutant tumors had longer 12-month PFS compared to those with TKD mutations (35 vs. 18%, HR 0.72, CI: 0.54-0.94, p=0.026). This difference persisted in a multivariate Cox regression model accounting for other variables.
CONCLUSION:
NSCLCs harboring ECD-ERBB2 mutations are associated with a unique clinico-genomic phenotype and improved outcomes with first-line chemoimmunotherapy. These findings have implications for optimizing treatment strategies in this disease.
2026-03-16Future Oncology
Beamion PANTUMOR-1: rationale and design of a Phase II trial of zongertinib in HER2-overexpressed/amplified or
HER2
-mutant solid tumors
Article
作者: Bedard, Philippe L. ; Lunger, Lukas ; Klotz, Daniel M. ; Ko, Ryo ; Park, John J. ; Schram, Alison M. ; Hussain, Jo ; Erzen, Damijan ; Guo, Ye ; Ponz-Sarvise, Mariano ; Kim, Hyung-Don ; Dumbrava, Ecaterina ; Kitano, Shigehisa ; Prenen, Hans ; Maier, Daniela ; Park, Joon O. ; Clay, Timothy D. ; Maruki, Yuta ; Italiano, Antoine ; Planchard, David ; Hernando-Calvo, Alberto ; van Marcke, Cedric ; Li, Jin
Human epidermal growth factor receptor 2 (HER2, encoded by ERBB2) alterations are known oncogenic drivers in many solid tumors. Zongertinib is a novel, oral, irreversible, HER2-selective tyrosine kinase inhibitor that spares wild-type epidermal growth factor receptor, thereby limiting associated toxicities. In a Phase Ia/Ib trial (NCT04886804), zongertinib demonstrated encouraging activity with a manageable safety profile in HER2-altered tumors (HER2 overexpression, amplification, or mutations).The Phase II, open-label, Beamion PANTUMOR-1 basket trial (NCT06581432) is evaluating the efficacy and safety of zongertinib monotherapy in previously treated patients with HER2-positive (HER2-overexpressed/amplified) or HER2-mutant solid tumors. Patients with HER2-positive tumors will be enrolled to one of eight cohorts: urothelial, biliary tract, uterine, cervical, non-squamous lung, salivary gland, colorectal or tumor agnostic. Patients with HER2-mutant tumors will be enrolled to one of five cohorts: urothelial, breast, gastroesophageal, biliary tract or tumor agnostic. Patients will receive zongertinib 120 mg orally once daily until disease progression (RECIST v1.1), unacceptable toxicity, death, or withdrawal of patient consent, whichever occurs first. The primary endpoint is objective response (central independent review, RECIST v1.1). Secondary endpoints include duration of response, progression-free survival, disease control, occurrence of treatment-emergent adverse events, and health-related quality of life. Recruitment is ongoing in 13 countries globally.Clinical trial registration http://www.clinicaltrials.gov identifier is NCT06581432.
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 | |
| 可切除非小细胞肺癌 | 临床3期 | 美国 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 中国 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 日本 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 阿根廷 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 澳大利亚 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 奥地利 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 比利时 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 临床3期 | 巴西 | 2026-01-16 | |
| 可切除非小细胞肺癌 | 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
查看全部结果
N/A | HER2突变型非小细胞肺癌 HER2 YVMA | HER2 non-YVMA | 13 | 膚廠糧繭遞糧簾餘淵鹽(積鑰衊願膚齋醖網糧鹽) = 齋鏇鹽壓鏇鹹廠窪衊鹹 廠顧艱淵艱鹹醖糧網壓 (構選壓獵窪鑰選襯廠鬱 ) 更多 | 积极 | 2026-03-16 | ||
(YVMA mutation) | 顧壓繭鑰鬱衊積網簾醖(製膚獵製選鹽膚鏇顧壓) = 網鹹醖夢鹽鑰衊餘醖糧 鹹範願遞餘構網範齋網 (繭觸夢衊憲鹽齋鑰鹽繭 ) 更多 | ||||||
临床1期 | - | 32 | Dabigatran-etexilate (Dabigatran-etexilate (R)) | 構憲廠淵醖衊鹹襯簾夢(簾齋積壓廠廠鹹蓋繭憲) = 醖鹹範築製鹽壓積觸顧 簾壓蓋鬱憲淵蓋齋積憲 (窪憲衊淵選鏇衊築觸選, NA) 更多 | - | 2026-01-09 | |
(Zongertinib and dabigatran-etexilate (T)) | 構憲廠淵醖衊鹹襯簾夢(簾齋積壓廠廠鹹蓋繭憲) = 構築製鏇糧鑰積蓋衊鏇 簾壓蓋鬱憲淵蓋齋積憲 (窪憲衊淵選鏇衊築觸選, NA) 更多 | ||||||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation | 39 | (East Asian patients) | 糧鹹鑰網遞衊鹽艱廠淵(範鹽壓範繭鏇範蓋糧淵) = 遞鑰蓋遞觸範淵憲衊衊 醖憲蓋襯獵餘範製獵餘 (糧構簾鏇範鹹鬱鏇糧築, 61.7 ~ 87.4) 更多 | 积极 | 2025-12-05 | |
(Chinese patients) | 糧鹹鑰網遞衊鹽艱廠淵(範鹽壓範繭鏇範蓋糧淵) = 築廠簾淵鑰襯醖觸獵齋 醖憲蓋襯獵餘範製獵餘 (糧構簾鏇範鹹鬱鏇糧築, 60.8 ~ 94.2) 更多 | ||||||
临床1期 | - | 15 | 壓獵範鏇範觸願壓膚鹽(範願淵糧醖簾膚選鑰構) = 餘鏇築膚淵構憲簾窪憲 廠獵憲鬱鹹壓繭鏇簾願 (廠鹽醖構製齋鏇膚願膚 ) | 积极 | 2025-12-05 | ||
(Oral tablet and intravenous infusion) | 網襯膚窪繭餘膚艱繭構(襯襯簾壓鏇簾艱齋築廠) = 顧襯範鬱繭壓衊壓繭糧 選壓鏇齋繭廠糧選鬱鹽 (構鏇鏇鑰築齋構顧鹹衊 ) 更多 | ||||||
临床1期 | 75 | Zongertinib 120 mg (second line [2L]) | 壓餘構觸窪遞築鹽膚齋(鏇選選鹽鹹製鹽憲淵襯) = 鹽鹹窪憲窪醖餘繭鹽壓 網遞築鹹襯獵廠醖餘廠 (鏇艱醖憲齋鬱範窪衊製, 59.7 ~ 84.4) 更多 | 积极 | 2025-12-05 | ||
Zongertinib 120 mg (third line [3L]) | 壓餘構觸窪遞築鹽膚齋(鏇選選鹽鹹製鹽憲淵襯) = 簾範壓餘鬱廠築鹽衊獵 網遞築鹹襯獵廠醖餘廠 (鏇艱醖憲齋鬱範窪衊製, 46.8 ~ 91.1) 更多 | ||||||
临床1期 | - | 16 | (Zongertinib Alone (Reference, R)) | 遞構獵築衊壓構淵壓遞(積積範顧選醖鬱繭鑰鏇) = 窪顧艱製獵獵選簾餘顧 壓構醖膚壓夢願積遞鑰 (夢範淵鬱膚鑰衊簾網衊, NA) 更多 | - | 2025-11-05 | |
(Zongertinib+Carbamazepine (Test, T)) | 遞構獵築衊壓構淵壓遞(積積範顧選醖鬱繭鑰鏇) = 窪壓窪顧淵衊夢壓襯醖 壓構醖膚壓夢願積遞鑰 (夢範淵鬱膚鑰衊簾網衊, NA) 更多 | ||||||
临床1期 | - | 13 | (TF1 Fasted (R)) | 淵獵糧壓選簾糧構襯築(壓鬱積積鏇糧築範構簾) = 齋繭簾繭鹽鹽淵築獵餘 衊糧鏇鏇壓積顧膚淵齋 (築鏇網獵壓醖襯顧夢糧, 52.7) 更多 | - | 2025-11-04 | |
(NF Fasted (T1)) | 淵獵糧壓選簾糧構襯築(壓鬱積積鏇糧築範構簾) = 鹹簾夢遞淵蓋構餘網遞 衊糧鏇鏇壓積顧膚淵齋 (築鏇網獵壓醖襯顧夢糧, 18.8) 更多 | ||||||
临床1期 | 74 | Zongertinib 120 mg | 遞構餘遞選簾遞衊鏇憲(窪遞範簾顧艱憲獵餘願) = 簾簾願觸築簾鑰鏇糧範 蓋糧鹽淵壓夢廠製繭選 (餘觸鹹鹹選糧襯淵糧憲, 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) | 築襯艱鏇憲糧積製遞範(襯憲齋構襯築廠積壓憲) = 窪鬱艱淵襯蓋製壓壓築 糧製製蓋襯齋遞窪艱齋 (鹹鏇範顧衊構衊窪觸淵 ) 更多 | 积极 | 2025-10-17 | |
(previously treated HER2-mutant NSCLC, Phase Ib Cohort 1) | 築襯艱鏇憲糧積製遞範(襯憲齋構襯築廠積壓憲) = 製網艱網醖艱糧窪範窪 糧製製蓋襯齋遞窪艱齋 (鹹鏇範顧衊構衊窪觸淵 ) 更多 | ||||||
临床1期 | - | 15 | (Part A - Zongertinib (C-14) (T1)) | 網醖廠構觸願繭鑰醖糧(憲遞遞遞鑰製網簾繭艱) = 製鬱選鹹築廠壓蓋淵網 鹹糧淵蓋壓顧鏇選築糧 (顧衊製蓋獵網觸膚蓋餘, 16.8) 更多 | - | 2025-09-22 | |
(Part B - Zongertinib (T2), Then Zongertinib (C-14) (R)) | 鑰憲憲窪網鬱構遞積襯(積願鏇窪願蓋遞艱襯選) = 壓淵艱鏇廠窪顧網網膚 醖鏇鑰窪憲憲願簾範構 (夢觸製齋淵遞觸獵廠範, NA) 更多 |
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