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更新于：2025-02-14
Limertinib
利厄替尼
更新于：2025-02-14
概要
基本信息
药物类型 小分子化药 |
别名 ASK120067、奥壹新 |
作用机制 EGFR T790M抑制剂(表皮生长因子受体T790M抑制剂) |
非在研适应症- |
原研机构 |
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2025-01-14), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构/序列
分子式C29H32ClN7O2 |
InChIKeyQHPVTCLSVVUPOF-UHFFFAOYSA-N |
CAS号1934259-00-3 |
关联
11
项与 利厄替尼 相关的临床试验CTR20220697
评价 ASKC202 片或联合ASK120067片在晚期实体瘤患者中的安全性、耐受性、药代动力学特征及初步有效性的开放、多中心、I 期临床试验
NCT05631678
An Open-lable, Two- Period, Single-sequence, Self-controlled Study to Evaluate the Effect of Oral Rifampicin or Itraconazole on the Pharmacokinetics of ASK120067 Tablets
CTR20221327
开放、两周期、单序列、自身对照研究设计，评价口服利福平或伊曲康唑对ASK120067片药代动力学的影响
100 项与 利厄替尼 相关的临床结果
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100 项与 利厄替尼 相关的转化医学
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100 项与 利厄替尼 相关的专利（医药）
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11
项与 利厄替尼 相关的文献（医药）2024-05-27JACS Au
AM-DMF-SCP: Integrated Single-Cell Proteomics Analysis on an Active Matrix Digital Microfluidic Chip
Article
作者: Feng, Fang ; Zhou, Hu ; Chen, Hongxu ; Xie, Hua ; Chen, Yimin ; Jin, Kai ; Wang, Yuqiu ; Hu, Siyi ; Pan, Zilu ; Yang, Zhicheng ; Ma, Hanbin ; Shi, Mude ; Liu, Qian
Single-cell proteomics offers unparalleled insights into cellular diversity and molecular mechanisms, enabling a deeper understanding of complex biological processes at the individual cell level. Here, we develop an integrated sample processing on an active-matrix digital microfluidic chip for single-cell proteomics (AM-DMF-SCP). Employing the AM-DMF-SCP approach and data-independent acquisition (DIA), we identify an average of 2258 protein groups in single HeLa cells within 15 min of the liquid chromatography gradient. We performed comparative analyses of three tumor cell lines: HeLa, A549, and HepG2, and machine learning was utilized to identify the unique features of these cell lines. Applying the AM-DMF-SCP to characterize the proteomes of a third-generation EGFR inhibitor, ASK120067-resistant cells (67R) and their parental NCI-H1975 cells, we observed a potential correlation between elevated VIM expression and 67R resistance, which is consistent with the findings from bulk sample analyses. These results suggest that AM-DMF-SCP is an automated, robust, and sensitive platform for single-cell proteomics and demonstrate the potential for providing valuable insights into cellular mechanisms.
2023-10-01Clinical pharmacology in drug development
Effect of Food on the Pharmacokinetics of Limertinib (ASK120067) and its Main Metabolite in Healthy Chinese Volunteers.
Article
作者: Jiang, Bo ; Guo, Haifang ; Chen, Wenjun ; Ruan, Zourong ; Lou, Honggang ; Yang, Dandan ; Jiang, Qianqian
Limertinib (ASK120067) is a newly developed third-generation epidermal growth factor receptor tyrosine kinase inhibitor. This phase I, open-label, 2-period crossover study was conducted to evaluate the effect of food on the pharmacokinetics (PK) of limertinib and its active metabolite CCB4580030 in Chinese healthy volunteers (HVs). HVs were randomly assigned (1:1) to receive a single dose of limertinib (160 mg) under the fasted state in period 1 and fed condition in period 2, or vice versa. Twenty-four HVs were enrolled, and 20 HVs completed both study periods. PK were assessed before dosing and ≤72 hours after dosing. PK parameters were analyzed by a noncompartmental method. Limertinib was absorbed faster in the fasted state compared with the fed state. The geometric mean ratios (fed/fast) of maximum concentration, area under the plasma concentration-time curve from time 0 to the last quantifiable concentration, and area under the plasma concentration-time curve from time 0 to infinity for ASK120067 were 145.5%, 145.4%, and 141.9%, respectively. Geometric mean ratios of the PK parameters of CCB4580030 were >125.00% and 90% confidence intervals were outside the preset bioequivalent range. Safety profiles were similar in both prandial states, and limertinib was well tolerated. Food reduced the rate and increased the extent of limertinib absorption following oral administration. Whether limertinib can be administered regardless of prandial state in patients warrants further investigation of efficacy and safety.
2023-09-02Expert opinion on drug metabolism & toxicology
Phase 1 study to evaluate the effects of rifampin or itraconazole on the pharmacokinetics of limertinib (ASK120067), a novel mutant-selective inhibitor of the epidermal growth factor receptor in healthy Chinese subjects
Article
作者: Yang, Yuanxun ; Zhao, Yu ; Huang, Lei ; Liu, Ming ; Cao, Bei ; Li, Juan ; Ma, Tingting ; Lin, Hui ; Guo, Haifang ; Geng, Yan
BACKGROUND:
Limertinib is a novel mutant-selective and irreversible inhibitor of the epidermal growth factor receptor under development. A phase 1 open, two-period, single-sequence, self-controlled, two-part study was initiated to characterize the effects of a strong CYP3A4 inducer (rifampin) or inhibitor (itraconazole) on the pharmacokinetics of limertinib.
RESEARCH DESIGN AND METHODS:
Twenty-four healthy subjects in each part received a single dose of limertinib alone (160 mg, Part A; 80 mg, Part B) and with multiple doses of rifampin 600 mg once daily (Part A) or itraconazole 200 mg twice daily (Part B).
RESULTS:
Coadministration of rifampin decreased exposure (area under the plasma concentration-time curve from time 0 to infinity, AUC0-inf) of limertinib and its active metabolite CCB4580030 by 87.86% (geometric least-squares mean [GLSM] ratio, 12.14%; 90% confidence interval [CI], 9.89-14.92) and 66.82% (GLSM ratio, 33.18%; 90% CI, 27.72-39.72), respectively. Coadministration of itraconazole increased the AUC0-inf of limertinib by 289.8% (GLSM ratio, 389.8%; 90% CI, 334.07-454.82), but decreased that of CCB4580030 by 35.96% (GLSM ratio, 64.04%; 90% CI, 50.78-80.77).
CONCLUSIONS:
Our study demonstrates that the concomitant use of limertinib with strong CYP3A inducers or inhibitors is not recommended. A single dose of limertinib, administered with or without rifampin or itraconazole, is generally safe and well tolerated in healthy Chinese subjects.
CLINICAL TRIAL REGISTRATION:
www.clinicaltrials.gov identifier is NCT05631678.
100 项与 利厄替尼 相关的药物交易
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外链
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| - | - | - |
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 |
|---|---|---|---|
| EGFR-T790M 突变非小细胞肺癌 | 中国 | 2025-01-14 |
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 |
|---|---|---|---|---|
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 申请上市 | 中国 | 2024-08-13 | |
| EGFR外显子21替代突变非小细胞肺癌 | 申请上市 | 中国 | 2024-08-13 | |
| EGFR阳性非小细胞肺癌 | 临床3期 | 中国 | 2019-10-30 | |
| EGFR阳性非小细胞肺癌 | 临床3期 | 中国 | 2019-10-30 | |
| EGFR阳性非小细胞肺癌 | 临床3期 | 中国 | 2019-10-30 | |
| 转移性非小细胞肺癌 | 临床3期 | 中国 | 2019-07-23 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2018-01-03 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2018-01-03 | |
| 局部晚期非小细胞肺癌 | 临床2期 | 中国 | 2018-01-03 | |
| MET基因扩增非小细胞肺癌 | 临床申请批准 | 中国 | 2023-11-20 |
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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2期 | EGFR突变的非小细胞肺癌 EGFR T790M Mutation | 301 | 膚鏇構獵鏇鹽鹹壓窪齋(糧築構選夢艱醖鏇選構) = 餘壓積鏇鑰選構鹹觸餘 襯範製遞獵積積簾製鬱 (製淵顧糧廠夢醖鹹憲鹽, 63.2 ~ 74.0) 更多 | 积极 | 2022-06-02 | ||
(CNS metastases) | 膚鏇構獵鏇鹽鹹壓窪齋(糧築構選夢艱醖鏇選構) = 壓夢壓鏇獵遞艱蓋獵顧 襯範製遞獵積積簾製鬱 (製淵顧糧廠夢醖鹹憲鹽, 54.4 ~ 74.0) 更多 |
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