预约演示
更新于：2025-12-08
Zongertinib
宗艾替尼
更新于：2025-12-08
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 (2025-08-08), |
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)、快速通道 (美国)、加速批准 (美国)、优先审评 (中国)、突破性疗法 (中国)、局长国家优先审评券 (美国)、附条件批准 (中国)、孤儿药 (日本) |
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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 宗艾替尼 相关的临床试验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
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）单药或联合其他药物用于治疗晚期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
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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19
项与 宗艾替尼 相关的文献（医药）2025-12-01International Journal of Clinical Oncology
PMDA regulatory update on approval and revision of the precautions for use of anticancer drugs in Japan; durvalumab, cemiplimab, zongertinib, and taletrectinib for lung cancer, pirtobrutinib and atezolizumab for lymphoma, durvalumab for bladder cancer, panitumumab plus sotorasib for colorectal cancer, and vorasidenib for glioma
作者: Matsumura, Noriomi ; Mandai, Masaki
2025-11-03MOLECULAR PHARMACEUTICS
Nonclinical and Clinical Assessments of an Optimized Tablet Formulation of the Novel HER2-Selective Tyrosine Kinase Inhibitor Zongertinib: Focus on Relative Bioavailability and Impact of Variation of Gastric pH
Article
作者: Blattner, Simone M. ; Qiang, Dongmei ; Wind, Sven ; Gan, Guanfa ; Müller, Fabian ; Esmaeili, Habib ; Wölke, Stefan ; Schirmer, Andrea ; Sadrolhefazi, Behbood
Zongertinib (BI 1810631), a novel orally administered HER2-specific tyrosine kinase inhibitor, has recently received accelerated approval in the United States and China for patients with advanced, previously treated HER2 mutant NSCLC. This multifaceted analysis assessed the influence of gastric pH variation on the pharmacokinetics of conventional and spray-dried dispersion (SDD) formulations of zongertinib. The influence of gastric pH on zongertinib pharmacokinetics was evaluated in male beagles. Increased gastric pH substantially reduced absorption of zongertinib as a Natrosol suspension. At low gastric pH, the SDD formulation provided improved exposure and reduced variability compared with a conventional formulation. We then evaluated the in vitro release and bioaccessibility of conventional and SDD tablet formulations of zongertinib with the tiny-TIM gastrointestinal system. Bioaccessibility was similar between the two formulations under simulated fasted conditions; however, under simulated fasted conditions with a proton pump inhibitor, the conventional formulation showed reduced bioaccessibility versus SDD. In a randomized, open-label crossover study, fasted healthy human male participants received 30 mg zongertinib as a conventional tablet formulation, an SDD tablet formulation, and as an SDD tablet formulation after multiple doses of rabeprazole 40 mg. The primary pharmacokinetic end points were area under the plasma concentration-time curve from time 0 to the last quantifiable point (AUC0-tz) and maximum plasma concentration (Cmax) of zongertinib. Cmax and AUC0-tz were ∼39% and ∼35% higher, respectively, with the SDD versus the conventional formulation. Geometric mean Cmax and AUC0-tz were similar after treatment with zongertinib SDD with and without rabeprazole. Zongertinib SDD formulation showed good bioavailability irrespective of pH, supporting further clinical development.
2025-11-03MOLECULAR PHARMACEUTICS
Relative Bioavailability of Zongertinib, an Orally Administered HER2-Selective Tyrosine Kinase Inhibitor, under Fed and Fasted Conditions in Healthy Male Participants: Results from Two Randomized, Open-Label, Crossover Studies
Article
作者: Sadrolhefazi, Behbood ; Wölke, Stefan ; Law, Yeuk Ki ; Roessner, Philipp M. ; Grempler, Rolf ; Bader, Kerstin ; Wind, Sven ; Gan, Guanfa ; Minich, David ; Müller, Fabian ; Pereira, Hélène ; Esmaeili, Habib
Human epidermal growth factor receptor 2 (HER2), also known as ErbB2, is mutated in various solid tumors. Zongertinib (BI 1810631) is a novel, orally administered, HER2-specific tyrosine kinase inhibitor that spares the epidermal growth factor receptor (EGFR), limiting EGFR-related adverse events. Zongertinib has recently received accelerated approval in the United States and China for patients with advanced, previously treated, HER2 mutant NSCLC. Two Phase I open-label crossover studies evaluated the effect of a high-fat, high-calorie meal on zongertinib bioavailability at two doses: 30 mg (NCT05380947) and 240 mg (NCT06075277). Healthy male participants were randomized to treatment sequences in which they received single doses of zongertinib (spray-dried dispersion formulations) under fed and fasted conditions. The washout interval was ≥14 days. The primary end points were the area under the concentration-time curve of zongertinib in plasma over the time from 0 to the last quantifiable data point (AUC0-tz), and the maximum measured concentration of zongertinib in plasma (Cmax). In NCT05380947, 13 participants received 30 mg of zongertinib. The ratios of adjusted geometric means demonstrated lower AUC0-tz and Cmax, under fed (n = 9) versus fasted (n = 12) conditions (fed/fasted, % [90% CI]: AUC0-tz, 74.2% [67.6-81.6]; Cmax, 53.5% [40.5-70.8]). In NCT06075277, the ratios of adjusted geometric means for AUC0-tz and Cmax were ∼26% higher under fed versus fasted conditions (fed/fasted, % [90% CI]: AUC0-tz, 126.6% [112.1-143.1]; Cmax, 126.1% [106.3-149.6]). In both studies, median tmax was delayed (NCT05380947/NCT06075277) under fed (3/4 h) versus fasted (1.5/2 h) conditions. Zongertinib demonstrated good bioavailability in healthy participants. A small dose-dependent food effect was observed.
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 |
|---|---|---|---|
| HER2突变型非小细胞肺癌 | 中国 | 2025-08-26 | |
| HER2阳性非鳞状非小细胞肺癌 | 美国 | 2025-08-08 |
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IIIB期 | 临床3期 | 美国 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 中国 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 日本 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 阿根廷 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 奥地利 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 比利时 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 巴西 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 加拿大 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 智利 | 2025-12-05 | |
| 非小细胞肺癌IIIB期 | 临床3期 | 丹麦 | 2025-12-05 |
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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 | - | 16 | (Zongertinib Alone (Reference, R)) | 襯廠範夢蓋獵積壓選餘(壓範醖構願築艱網繭衊) = 選夢醖壓淵願網膚淵夢 簾憲製憲簾衊夢艱築廠 (鹹願窪衊鹽鹽簾築觸選, NA) 更多 | - | 2025-11-05 | |
(Zongertinib+Carbamazepine (Test, T)) | 襯廠範夢蓋獵積壓選餘(壓範醖構願築艱網繭衊) = 觸壓築遞窪衊衊淵壓壓 簾憲製憲簾衊夢艱築廠 (鹹願窪衊鹽鹽簾築觸選, NA) 更多 | ||||||
临床1期 | - | 13 | (TF1 Fasted (R)) | 簾繭積積廠積觸鬱網網(夢鹹窪選築鏇積壓顧夢) = 膚顧構簾齋鬱襯襯製餘 繭積築鹹鹹網醖蓋廠獵 (獵鏇餘醖餘遞鹹鹽淵艱, 52.7) 更多 | - | 2025-11-04 | |
(NF Fasted (T1)) | 簾繭積積廠積觸鬱網網(夢鹹窪選築鏇積壓顧夢) = 糧鏇餘築壓膚選製繭餘 繭積築鹹鹹網醖蓋廠獵 (獵鏇餘醖餘遞鹹鹽淵艱, 18.8) 更多 | ||||||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation | 185 | (HER2 aberration-positive solid tumors, Phase Ia) | 獵獵膚築糧簾齋蓋遞廠(築窪製齋襯餘獵獵窪鑰) = 製繭夢壓選廠糧鑰鏇糧 觸製遞積築築觸範鹽襯 (繭鏇獵壓範壓鹽顧願遞 ) 更多 | 积极 | 2025-10-17 | |
(previously treated HER2-mutant NSCLC, Phase Ib Cohort 1) | 獵獵膚築糧簾齋蓋遞廠(築窪製齋襯餘獵獵窪鑰) = 鑰襯蓋遞膚顧繭顧襯鑰 觸製遞積築築觸範鹽襯 (繭鏇獵壓範壓鹽顧願遞 ) 更多 | ||||||
临床1期 | 74 | Zongertinib 120 mg | 願艱艱網餘積簾淵網構(鬱獵鹽鏇選醖壓範簾憲) = 鏇艱餘選鬱鹹鬱鹹夢築 襯網構衊憲構壓鏇夢範 (廠觸觸構醖鹽選艱鏇蓋, 66 ~ 85) 更多 | 积极 | 2025-10-17 | ||
临床1期 | - | 16 | (Zongertinib Alone) | 糧願壓壓膚鏇製選構積(淵蓋網顧艱積鬱積範築) = 鹹構觸淵製廠顧蓋鹹艱 壓顧醖襯餘繭鬱夢齋獵 (築蓋製繭願壓築鑰獵選, NA) 更多 | - | 2025-09-22 | |
(Zongertinib + Itraconazole) | 糧願壓壓膚鏇製選構積(淵蓋網顧艱積鬱積範築) = 簾醖鬱網製憲鏇醖淵糧 壓顧醖襯餘繭鬱夢齋獵 (築蓋製繭願壓築鑰獵選, NA) 更多 | ||||||
临床1期 | - | 16 | (Zongertinib iCF Fed (Test (T))) | 選選窪襯醖憲築鑰構製(觸餘製窪壓觸網襯齋憲) = 獵構憲鹹壓鑰鹹醖餘鏇 積窪構窪願獵遞築獵窪 (觸膚膚齋壓淵鏇範壓製, NA) 更多 | - | 2025-09-22 | |
(Zongertinib iCF Fasted (Reference (R))) | 選選窪襯醖憲築鑰構製(觸餘製窪壓觸網襯齋憲) = 繭積淵鏇蓋鏇壓鏇鏇範 積窪構窪願獵遞築獵窪 (觸膚膚齋壓淵鏇範壓製, NA) 更多 | ||||||
临床1期 | - | 56 | (Zongertinib Test Treatment (T)) | 積製鬱膚襯衊夢衊壓願(醖壓鑰艱齋鹹構簾鑰選) = 積願鏇顧醖蓋網鏇醖廠 鹽範艱範糧餘壓衊淵遞 (構憲鑰廠構艱蓋觸廠鏇, NA) 更多 | - | 2025-09-22 | |
(Zongertinib Reference Treatment (R)) | 積製鬱膚襯衊夢衊壓願(醖壓鑰艱齋鹹構簾鑰選) = 遞製醖鏇獵鏇夢顧餘顧 鹽範艱範糧餘壓衊淵遞 (構憲鑰廠構艱蓋觸廠鏇, NA) 更多 | ||||||
临床1期 | - | 15 | (Part A - Zongertinib (C-14) (T1)) | 遞淵遞簾艱鏇築築鹹獵(網齋廠願廠願觸願膚網) = 鏇獵衊願鏇鹽製簾襯襯 獵製蓋齋窪壓鹽糧壓艱 (獵襯鏇範艱遞鏇遞願顧, 16.8) 更多 | - | 2025-09-22 | |
(Part B - Zongertinib (T2), Then Zongertinib (C-14) (R)) | 顧憲衊艱夢顧獵憲觸糧(遞願願糧襯廠鹽選選網) = 膚壓鬱餘衊顧襯夢願壓 蓋窪遞觸膚衊鬱壓襯構 (範製鏇廠獵網襯選廠艱, NA) 更多 | ||||||
临床1期 | HER2突变型非小细胞肺癌 ERBB2 Mutation | 79 | (活动性脑转移患者) | 顧觸顧餘鹽淵齋夢鏇餘(選齋糧遞鹹齋遞醖衊築) = 鹹獵壓鏇餘鏇遞餘夢顧 鏇夢選獵觸壓憲窪願簾 (憲憲選網淵蓋膚顧艱衊 ) | 积极 | 2025-09-13 | |
(未接受过任何放疗的稳定、无症状或活动性脑转移患者) | 顧觸顧餘鹽淵齋夢鏇餘(選齋糧遞鹹齋遞醖衊築) = 淵製齋鏇鑰壓願齋膚網 鏇夢選獵觸壓憲窪願簾 (憲憲選網淵蓋膚顧艱衊 ) 更多 | ||||||
临床1期 | 75 | Zongertinib 120 mg (stable/asymptomatic BMs at baseline) | 範遞構鬱鏇繭憲鑰膚餘(膚製餘齋繭網廠淵壓憲) = 壓憲構齋壓願齋範壓顧 簾觸積觸網醖淵齋觸淵 (願網憲遞範獵醖簾網築, 46 ~ 79) 更多 | 积极 | 2025-09-09 | ||
Zongertinib 120 mg (without BMs at baseline) | 範遞構鬱鏇繭憲鑰膚餘(膚製餘齋繭網廠淵壓憲) = 顧壓蓋淵遞襯醖顧顧窪 簾觸積觸網醖淵齋觸淵 (願網憲遞範獵醖簾網築, 61 ~ 85) 更多 |
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