预约演示
更新于：2025-08-05
Zongertinib
宗格替尼
更新于：2025-08-05
概要
基本信息
非在研机构- |
最高研发阶段申请上市 |
首次获批日期- |
最高研发阶段(中国)申请上市 |
特殊审评优先审评 (美国)、突破性疗法 (美国)、快速通道 (美国)、突破性疗法 (中国)、孤儿药 (日本)、优先审评 (中国) |
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结构/序列
分子式C29H29N9O2 |
InChIKeyYSGNGFPNTLERCR-UHFFFAOYSA-N |
CAS号2728667-27-2 |
关联
17
项与 宗格替尼 相关的临床试验NCT06692322
Pharmacokinetics, Safety and Tolerability of Zongertinib Following Oral Administration in Male and Female Participants of Non-childbearing Potential With Different Degrees of Hepatic Impairment (Child-Pugh Classification A and B) Compared With Matched Male and Female Participants of Non-childbearing Potential With Normal Hepatic Function (an Open-label, Non-randomised, Single-dose, Parallel, Individual-matched Design Trial)
CTR20242277
Beamion BCGC-1：一项评价口服zongertinib（BI 1810631）联合德曲妥珠单抗（T-DXd）静脉给药或联合恩美曲妥珠单抗（T-DM1）静脉给药用于治疗晚期HER2+转移性乳腺癌（mBC）和转移性胃癌、食管胃结合部癌或食管腺癌（mGEAC）患者的Ib期剂量递增和II期剂量优化、随机、开放性、多中心临床研究
NCT06581432
Beamion PANTUMOR-1: A Phase II, Multicentre, Multicohort, Open-label Trial to Evaluate the Efficacy and Safety of Oral Zongertinib (BI 1810631) for the Treatment of Selected HER2-mutated or Overexpressed/Amplified Solid Tumours
100 项与 宗格替尼 相关的临床结果
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100 项与 宗格替尼 相关的转化医学
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100 项与 宗格替尼 相关的专利（医药）
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11
项与 宗格替尼 相关的文献（医药）2025-07-28Cureus Journal of Medical Science
Targeted Therapy in HER2 Exon 20-Mutant Non-small Cell Lung Cancer With Leptomeningeal Disease: A Case-Based Approach to Treatment Decision-Making
Article
作者: Elzaafarany, Osama
A rare and clinically challenging case of leptomeningeal disease (LMD) secondary to HER2-mutated non-small cell lung cancer (NSCLC), marked by both exon 20 insertion and gene amplification, is presented. In the absence of LMD-specific therapeutic guidelines for HER2-driven NSCLC, treatment was initiated with trastuzumab deruxtecan (Enhertu), based on extrapolated evidence from clinical trials in systemic NSCLC and HER2-positive breast cancer with central nervous system involvement. The patient, a 69-year-old woman with good performance status, developed LMD following prior systemic therapy and local CNS treatments. MRI and CSF cytology confirmed the diagnosis. Given the lack of approved therapies for HER2-mutant NSCLC with LMD, the treatment strategy was informed by available clinical data and supporting literature on the CNS activity of Enhertu. Other options such as poziotinib and zongertinib were considered but not pursued. This case underscores the urgent need for inclusive clinical trials addressing CNS complications in molecularly defined NSCLC and demonstrates the real-world application of precision oncology beyond trial populations.
2025-06-19NEW ENGLAND JOURNAL OF MEDICINE
Zongertinib in Previously Treated
HER2
-Mutant Non–Small-Cell Lung Cancer
Article
作者: Yoh, Kiyotaka ; Zugazagoitia, Jon ; Sabari, Joshua K. ; Nadal, Ernest ; Eigenbrod-Giese, Sabina ; Wu, Yi-Long ; Heymach, John V. ; Smit, Egbert F. ; Sadrolhefazi, Behbood ; Cho, Byoung Chul ; Ahn, Myung-Ju ; von Wangenheim, Ute ; Planchard, David ; Girard, Nicolas ; Ruiter, Gerrina ; Zhao, Yanqiu ; Tu, Hai-Yan ; Rohrbacher, Maren ; Yamamoto, Noboru
BACKGROUND:
Innovative oral targeted therapies are warranted for patients with human epidermal growth factor receptor 2 (HER2)-mutant non-small-cell lung cancer (NSCLC). Zongertinib is an oral, irreversible, HER2-selective tyrosine kinase inhibitor that has been shown to have efficacy in persons with advanced or metastatic solid tumors with HER2 alterations in a phase 1 study.
METHODS:
We evaluated zongertinib in a multicohort, phase 1a-1b trial involving patients with advanced or metastatic HER2-mutant NSCLC. Here we report the primary analysis of zongertinib in previously treated patients: those with tumors harboring a mutation in the tyrosine kinase domain (cohort 1), those with tumors harboring a mutation in the tyrosine kinase domain previously treated with a HER2-directed antibody-drug conjugate (cohort 5), and those with tumors harboring a non-tyrosine kinase domain mutation (cohort 3). In cohort 1, patients were initially randomly assigned to receive zongertinib at a dose of 120 mg or 240 mg once daily. Patients in cohorts 5 and 3 initially received 240 mg daily. After an interim analysis of data from cohort 1, subsequently recruited patients across all cohorts received zongertinib at a dose of 120 mg. The primary end point was an objective response assessed by blinded independent central review (cohorts 1 and 5) or by investigator review (cohort 3). Secondary end points included the duration of response and progression-free survival.
RESULTS:
In cohort 1, a total of 75 patients received zongertinib at a dose of 120 mg. At the data cutoff (November 29, 2024), 71% of these patients (95% confidence interval [CI], 60 to 80; P<0.001 against a ≤30% benchmark) had a confirmed objective response; the median duration of response was 14.1 months (95% CI, 6.9 to not evaluable), and the median progression-free survival was 12.4 months (95% CI, 8.2 to not evaluable). Grade 3 or higher drug-related adverse events occurred in 13 patients (17%). In cohort 5 (31 patients), 48% of the patients (95% CI, 32 to 65) had a confirmed objective response. Grade 3 or higher drug-related adverse events occurred in 1 patient (3%). In cohort 3 (20 patients), 30% of the patients (95% CI, 15 to 52) had a confirmed objective response. Grade 3 or higher drug-related adverse events occurred in 5 patients (25%). Across all three cohorts, no cases of drug-related interstitial lung disease occurred.
CONCLUSIONS:
Zongertinib showed clinical benefit with mainly low-grade adverse events in patients with previously treated HER2-mutant NSCLC. (Funded by Boehringer Ingelheim; Beamion LUNG-1 ClinicalTrials.gov number, NCT04886804.).
2025-04-10JOURNAL OF CLINICAL ONCOLOGY
HER2-Selective Tyrosine Kinase Inhibitor, Zongertinib (BI 1810631), in Patients With Advanced/Metastatic Solid Tumors With
HER2
Alterations: A Phase Ia Dose-Escalation Study
Article
作者: Serra, Josep ; Yoh, Kiyotaka ; Schröter, Lukas ; Sadrolhefazi, Behbood ; Barve, Minal ; Wu, Yi-Long ; Heymach, John V. ; Berz, David ; Botilde, Yanick ; Yamamoto, Noboru ; Opdam, Frans ; Tu, Hai-Yan
PURPOSE:
Human epidermal growth factor receptor 2 (HER2) alterations occur in many solid cancers, including non–small cell lung cancer (NSCLC). Beamion LUNG-1 (ClinicalTrials.gov identifier:
NCT04886804
) is assessing the safety/efficacy of zongertinib (BI 1810631), a novel HER2-selective tyrosine kinase inhibitor that spares epidermal growth factor receptor, in patients with HER2-altered solid tumors.
MATERIALS AND METHODS:
Beamion LUNG-1 is an ongoing multicenter, multicohort phase Ia/Ib trial. Phase Ia assessed zongertinib administered twice a day (15-150 mg) or once daily (60-360 mg) in pretreated patients with various tumors, including NSCLC. Primary end points were maximum tolerated dose (MTD) and dose-limiting toxicities (DLTs); tumor response was a secondary end point.
RESULTS:
As of May 23, 2024, 105 patients were treated. Two DLTs occurred during the MTD evaluation period; MTD was not reached (NR). The recommended doses for expansion were 120 mg once daily and 240 mg once daily. Treatment-related adverse events (TRAEs; any/grade ≥3) occurred in 82%/10% of patients. The most common TRAEs (any/grade ≥3) included diarrhea (50%/1%), rash (16%/2%), anemia (10%/0%), decreased appetite (10%/1%), and increased alanine transaminase (10%/4%). The confirmed investigator-assessed overall response rate (ORR) across all doses/tumors was 30% (95% CI, 23 to 40); median duration of response was 12.7 months (95% CI, 6.9 to NR). In 54 patients with NSCLC, confirmed ORR was 35% (95% CI, 24 to 49). Activity was observed in patients with A775_G776insYVMA (ORR, 38%) and those who had received previous HER2-directed therapy (ORR, 28%). In patients with NSCLC receiving zongertinib once daily, median progression-free survival was 17.2 months (95% CI, 8.3 to NR).
CONCLUSION:
Zongertinib had a manageable safety profile and demonstrated preliminary antitumor activity in patients with HER2-altered tumors, including those with
HER2
-mutant NSCLC.
157
项与 宗格替尼 相关的新闻（医药）2025-08-02
2025-07-31
100 项与 宗格替尼 相关的药物交易
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研发状态
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| HER2突变型非小细胞肺癌 | 申请上市 | 中国 | 2025-01-15 | |
| 晚期癌症 | 临床2期 | 美国 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 中国 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 日本 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 澳大利亚 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 比利时 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 加拿大 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 法国 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 德国 | 2024-10-11 | |
| 晚期癌症 | 临床2期 | 意大利 | 2024-10-11 |
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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1期 | - | Zongertinib 120 mg | 壓壓醖構憲鑰糧築蓋淵(齋願鑰醖獵鏇艱鏇簾鏇) = 顧願餘壓願醖鑰範構鏇 鏇繭艱願獵蓋簾窪淵衊 (範鏇繭鹽糧構鹹顧顧範, 60 ~ 80) 更多 | 积极 | 2025-06-19 | ||
HER2-directed antibody-drug conjugate | 壓壓醖構憲鑰糧築蓋淵(齋願鑰醖獵鏇艱鏇簾鏇) = 衊網鬱鹹構鹽願鑰築淵 鏇繭艱願獵蓋簾窪淵衊 (範鏇繭鹽糧構鹹顧顧範, 32 ~ 65) | ||||||
临床1期 | HER2 阴性乳腺癌 HER2 | 121 | 鬱範廠顧鏇鬱齋餘廠艱(鹽鬱齋衊簾鹹範窪夢壓) = The MTD was not reached 窪壓廠醖鏇獵艱簾窪鏇 (範鑰襯願襯觸糧艱鹹壓 ) | 积极 | 2025-05-30 | ||
Tucatinib | |||||||
临床1期 | HER2 mutations | - | 鑰繭齋膚鬱鑰蓋願夢窪(獵簾衊網顧齋艱製遞網) = 壓鹽鏇膚憲壓餘構醖艱 廠壓願範襯構鏇選淵窪 (鹹獵餘淵築艱範衊製願 ) 更多 | 积极 | 2025-04-29 | ||
遞憲窪廠觸壓膚襯築選(糧鬱製鏇憲選衊憲遞窪) = 齋膚觸蓋鏇蓋廠選構壓 齋糧製願艱鹹構範艱艱 (夢獵醖選壓觸憲襯襯艱 ) | |||||||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation (Activating) | 126 | (cohort 1; pretreated HER2-mutant NSCLC within the TKD) | 淵窪憲選衊範衊壓齋鏇(製簾淵鏇範醖網選顧糧) = 積糧醖製積夢齋醖齋蓋 構遞鏇製淵鏇蓋築淵憲 (築廠鬱繭蓋顧糧衊選觸, 60 ~ 80) 更多 | 积极 | 2025-04-28 | |
(cohort 3; pretreated HER2-mutant NSCLC with TKD or non-TKD mutations) | 淵窪憲選衊範衊壓齋鏇(製簾淵鏇範醖網選顧糧) = 憲襯齋獵繭壓鑰膚範餘 構遞鏇製淵鏇蓋築淵憲 (築廠鬱繭蓋顧糧衊選觸, 15 ~ 52) 更多 | ||||||
临床1期 | 105 | 夢遞鏇觸夢鏇製膚願願(觸膚鏇遞繭夢膚鏇窪蓋) = MTD was not reached 鹹憲憲觸鏇齋願願繭獵 (構衊餘遞選壓鹹製選壓 ) 更多 | 积极 | 2025-04-10 | |||
临床1期 | 105 | 宗格替尼 | 窪鏇顧繭窪繭艱顧壓範(糧艱願醖艱淵鑰夢淵糧) = Two DLTs occurred during the MTD evaluation period. 夢築範製醖選廠選遞窪 (鏇襯鹽齋廠獵餘齋願構 ) 更多 | 积极 | 2025-03-11 | ||
宗格替尼 (NSCLC) | |||||||
临床1期 | HER2突变型非小细胞肺癌 HER2 | - | (每日120毫克，单次服用) | 網膚觸壓願遞遞膚獵夢(顧鬱艱鬱齋齋觸糧襯窪) = 顧襯顧遞鬱蓋窪鬱夢醖 壓構觸蓋觸淵壓餘齋齋 (顧壓鹽衊構構積範糧繭 ) 更多 | 积极 | 2024-12-10 | |
临床1期 | HER2阳性实体瘤 HER2 Positive | 105 | 壓築簾艱窪衊憲積顧鏇(齋膚網糧廠構鬱願繭艱) = MTD was not reached for BID or QD schedules. 構蓋淵膚餘繭簾艱淵糧 (餘膚糧顧窪鬱鑰構壓願 ) 更多 | 积极 | 2024-12-07 | ||
(Asian pts) | |||||||
临床1期 | HER2阳性实体瘤 HER2 Positive | 83 | Zongertinib BID | 衊衊選壓鹹鹹獵築淵廠(築網齋鑰遞膚廠齋網鹹) = 願鹹範製壓夢繭簾夢鑰 繭積醖憲繭製醖餘顧範 (淵鏇壓鏇蓋鑰壓廠製繭 ) 更多 | 积极 | 2024-09-10 | |
Zongertinib QD | 鹽獵鏇觸鏇餘製繭夢選(廠網壓淵獵衊廠獵鏇鑰) = 鬱壓壓艱鬱窪範蓋築糧 繭夢淵範構齋艱鏇鏇積 (夢鬱願繭醖顧餘範繭膚 ) 更多 | ||||||
临床1期 | 61 | Zongertinib 15/30/60/100/150 mg BID | 鏇遞夢膚願鹽壓製鬱鏇(蓋構艱選艱鹽鑰觸廠糧) = 願築鹹窪齋艱蓋淵願鹹 蓋鑰窪壓廠壓夢餘製觸 (蓋遞淵顧餘衊齋鹹膚網 ) 更多 | 积极 | 2024-05-24 | ||
Zongertinib 60/120/180/240/300/360 mg QD | 鏇遞夢膚願鹽壓製鬱鏇(蓋構艱選艱鹽鑰觸廠糧) = 構顧衊齋積遞願艱廠壓 蓋鑰窪壓廠壓夢餘製觸 (蓋遞淵顧餘衊齋鹹膚網 ) 更多 |
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