预约演示
更新于：2025-06-07
Rilertinib Mesylate
甲磺酸瑞厄替尼
更新于：2025-06-07
概要
基本信息
药物类型 小分子化药 |
别名 Oritinib Mesylate、甲磺酸奥瑞替尼、SH 1028 + [2] |
作用方式 抑制剂 |
作用机制 EGFR19外显子缺失突变抑制剂、EGFR21外显子L858R突变抑制剂 |
非在研适应症 |
原研机构 |
在研机构 |
非在研机构- |
权益机构- |
最高研发阶段批准上市 |
首次获批日期 中国 (2024-06-11), |
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C32H41N7O5S |
InChIKeyIKCINODAIQYCSW-UHFFFAOYSA-N |
CAS号2180164-79-6 |
关联
10
项与 甲磺酸瑞厄替尼 相关的临床试验NCT06080776
A Phase III, Double-blind, Randomised Study of SH-1028 Tablets Versus Placebo as Adjuvant Therapy in Resected Stage II-IIIB Non-Small Cell Lung Cancer With Sensitizing EGFR Mutations
NCT04808648
A Single-center, Open-label, Drug-drug Interaction Study of SH-1028 Tablets in Healthy Subjects
CTR20201904
[14C]SH-1028在中国成年健康男性受试者体内的吸收、代谢和排泄研究
100 项与 甲磺酸瑞厄替尼 相关的临床结果
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100 项与 甲磺酸瑞厄替尼 相关的转化医学
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100 项与 甲磺酸瑞厄替尼 相关的专利（医药）
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7
项与 甲磺酸瑞厄替尼 相关的文献（医药）2023-06-01Investigational new drugs
Drug-drug interaction potential of SH-1028, a third-generation EGFR-TKI: in vitro and clinical trials.
Article
作者: Ding, Jiaxiang ; Liu, Yuanyuan ; Wang, Ying ; Shan, Rongfang ; Wang, Zhiqiang ; Ding, Yuzhou ; Li, Xiaoli ; Zhu, Minhui ; Xu, Yuanyuan ; Zhou, Huan ; Liu, Bingyan ; He, Cuixia ; Xie, Jing ; Liu, Yuyan
SH-1028 is an irreversible third-generation EGFR tyrosine kinase inhibitor (EGFR-TKI) for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC). Considering the possibility of combination therapy in patients with NSCLC, we investigated the drug-drug interaction (DDI) potential of SH-1028 both in vitro and in clinical trials. The in vitro studies were conducted to determine the potential of SH-1028 as a substrate, inducer, or inhibitor of cytochrome P450 (CYP) subtypes. A phase I drug-drug interaction study in healthy volunteers was performed to evaluate the impact of co-administering rifampicin (a strong CYP3A4 inducer) and itraconazole (a strong CYP3A4 inhibitor) on the pharmacokinetics of SH-1028. The in vitro experiments showed that SH-1028 was mainly metabolized by CYP3A4. The activities of CYP1A2, 2B6, 2C19, 2D6 and 3A4 enzymes were slightly inhibited in vitro with SH-1028. SH-1028 has no obvious induction effect on CYP1A2 and CYP2B6 activities, but has potential induction effect on CYP3A4 mRNA expression. However, SH-1028 may not induce or inhibit human CYPs significantly at the clinically expected dose (200 mg). The geometric mean ratios of pharmacokinetic parameters and their corresponding 90% confidence intervals for SH-1028 in combination and alone did not fall within the range of 80-125%. It is speculated that itraconazole and rifampicin affect the metabolism of SH-1028. In the clinical application of SH-1028, special attention should be paid to the interaction between SH-1028 and drugs or foods that affect the activity of CYP3A4. (Clinical trial registration number: CTR20210558).
2023-05-15Cancer
Safety, efficacy, and pharmacokinetics of SH‐1028 in EGFR T790M‐positive advanced non–small cell lung cancer patients: A dose‐escalation phase 1 study
Article
作者: Shi, Xinsheng ; Ma, Pei ; Guo, Renhua ; Zhao, Dongmei ; Shu, Yongqian ; Gao, Wen ; He, Jing
Abstract:
Background:
SH‐1028 is a new third‐generation EGFR tyrosine kinase inhibitors (TKI) to benefit patients with EGFR T790M‐mutated NSCLC. Here, the authors report its clinical safety, preliminary efficacy, and pharmacokinetic (PK) profile for the first time.
Methods:
Patients with EGFR T790M mutation, locally advanced non–small cell lung cancer (NSCLC), or metastatic NSCLC who had progressed after previous EGFR TKI therapy were eligible. Patients received SH‐1028 at five oral dose levels (60 mg, 100 mg, 200 mg, 300 mg, and 400 mg) once daily until disease progression, unacceptable toxicity, or patient withdrawal. The primary end points were the safety, dose‐limiting toxicity (DLT), maximum‐tolerated dose (MTD), and PK profile. Secondary end points included objective response rate (ORR), disease control rate (DCR), progression‐free survival (PFS), etc.
Results:
Data cut off on December 31, 2020, a total of 20 patients were enrolled during the trial, two of three patients in 300 mg cohort experienced a DLT, and no DLT was observed in 240 mg cohort, 240 mg was determined to be the MTD of SH‐1028. A total of 95.0% (19 of 20) of patients reported treatment‐related adverse events (TRAEs), and the incidence of serious adverse events was 20.0% (4 of 20). The ORR and DCR of the 200 mg cohort were 75% (95% confidence interval [CI], 19.41–99.37) and 75.0% (95% CI, 19.41–99.37), respectively. The overall ORR was 40% (95% CI, 19.12–63.95), and DCR was 70.0% (95% CI, 45.72–88.11). According to the PK profile, the dosage regimen for future studies was determined as 200 mg once daily.
Conclusions:
SH‐1028 showed a manageable safety and promising antitumor activity in patients with EGFR T790M mutation at the dose of 200 mg once daily.
Plain language summary:
Lung cancer has a high morbidity and mortality, with an estimated 1.8 million deaths in 2020. Non–small cell lung cancer accounts for approximately 85% of lung cancer.First‐ or second‐generation EGFR TKIs' weak selectivity often led to the occurrence of treatment‐related adverse events, such as interstitial lung disease, rash, diarrhea, etc., along with acquired drug resistance within approximately 1 year.A dose of 200 mg of SH‐1028 once daily showed a preliminary antitumor activity with manageable safety in patients with EGFR T790M mutation.
2023-02-01Xenobiotica; the fate of foreign compounds in biological systems
Development and validation of an LC-MS/MS method for simultaneous determination of SH-1028, an irreversible third-generation EGFR TKI, and two of its metabolites in human plasma: application in clinical pharmacokinetics
Article
作者: Wang, Lu ; Sha, Bijun ; Zhou, Sufeng ; Zhao, Yuqing ; Wang, Zhiqiang ; Shao, Feng ; Chen, Xijing ; Zhang, Xian ; Han, Luwei
SH-1028 is a novel, potent, and highly selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) developed for the treatment of T790M Mutation-positive non-small cell lung cancer (NSCLC). The objective was to develop an LC-MS/MS method for the simultaneous determination of SH-1028 and its metabolites, Imp2 and Imp3, in human plasma.The plasma samples were extracted through protein precipitation with acetonitrile on wet ice conditions. A rapid, sensitive, and specific method was developed and successfully applied to evaluate the pharmacokinetic (PK) properties of SH-1028 in patients with advanced NSCLC following single and multiple doses of SH-1028 (60 mg).After single-dose administration, the Cmax of SH-1028, Imp2, and Imp3 was 11.2, 50.2, and 7.99 ng/mL, respectively. The mean AUC0-24 h was 138, 602, and 76.7 h*ng/mL, respectively. And the terminal half-life time was 19.9, 14.4, and 26.1 h, respectively. After multiple-dose administration, SH-1028 exhibited a slight accumulation, with a mean accumulation ratio (RAUC) of 2.00.The study assessed the PK properties of SH-1028 following single and multiple doses in patients with advanced NSCLC and would provide meaningful information for the further development of SH-1028.
79
项与 甲磺酸瑞厄替尼 相关的新闻（医药）2025-06-06
财报医药出海
2025-06-04
抗体药物偶联物ASCO会议临床3期蛋白降解靶向嵌合体
2025-04-19
·圣和药业
CSCO会议临床3期
100 项与 甲磺酸瑞厄替尼 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 |
|---|---|---|---|
| EGFR 外显子 19 缺失突变型非小细胞肺癌 | 中国 | 2024-09-03 | |
| EGFR外显子21替代突变非小细胞肺癌 | 中国 | 2024-09-03 | |
| EGFR-T790M 突变非小细胞肺癌 | 中国 | 2024-06-11 |
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 | 中国 | 2023-05-11 | |
| EGFR突变的非小细胞肺癌 | 临床3期 | 中国 | 2020-03-25 | |
| EGFR阳性非小细胞肺癌 | 临床3期 | - | 2020-01-31 | |
| 局部晚期非小细胞肺癌 | 临床3期 | - | 2020-01-31 | |
| 转移性非小细胞肺癌 | 临床2期 | - | 2019-03-01 | |
| EGFR 突变实体瘤 | 临床1期 | 中国 | 2018-11-09 | |
| 局部晚期恶性实体瘤 | 临床1期 | 中国 | 2018-09-13 |
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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3期 | 245 | Rilertinib 200 mg | 壓糧糧窪餘網餘簾糧糧(獵顧衊製壓糧壓鑰廠齋) = 憲鏇餘鹹襯蓋獵遞憲齋 蓋鹹醖製膚壓選衊齋窪 (齋網廠艱鬱鹹製鹹獵齋, 15.2 ~ 22.3) 更多 | 积极 | 2024-09-08 | ||
Gefitinib 250 mg | 壓糧糧窪餘網餘簾糧糧(獵顧衊製壓糧壓鑰廠齋) = 遞壓願醖艱鹽製醖鬱獵 蓋鹹醖製膚壓選衊齋窪 (齋網廠艱鬱鹹製鹹獵齋, 7.1 ~ 12.6) 更多 | ||||||
临床3期 | 227 | 齋餘夢獵餘糧製鏇範獵(簾遞構憲廠膚夢鏇繭醖) = 鬱構蓋觸鏇膚蓋繭鏇衊 簾鹽壓壓淵願製齋鹽壓 (蓋願選衊餘鑰範積蓋觸 ) 达到 | 积极 | 2024-06-17 | |||
吉非替尼 | 齋餘夢獵餘糧製鏇範獵(簾遞構憲廠膚夢鏇繭醖) = 憲艱積願蓋構範鹹遞顧 簾鹽壓壓淵願製齋鹽壓 (蓋願選衊餘鑰範積蓋觸 ) 达到 | ||||||
临床2期 | 286 | (dose verification study) | 襯艱獵淵顧鹽積餘憲觸(獵遞廠遞齋窪範壓窪顧) = 鏇夢築膚鑰觸顧淵積鑰 齋鏇窪艱糧獵齋製壓鏇 (餘鏇構壓鏇糧製膚膚繭, 42.4 ~ 68.8) 更多 | 积极 | 2022-07-04 | ||
(second-line registration study) | 襯艱獵淵顧鹽積餘憲觸(獵遞廠遞齋窪範壓窪顧) = 醖夢鹽鑰築構鑰襯淵顧 齋鏇窪艱糧獵齋製壓鏇 (餘鏇構壓鏇糧製膚膚繭, 53.7 ~ 66.8) 更多 | ||||||
临床2期 | 227 | 網齋鏇網顧夢範製網鏇(膚構繭淵壓齋簾憲衊鹽) = 顧顧鬱淵製觸餘衊構襯 遞餘鏇淵蓋醖鑰鑰網糧 (窪糧蓋鹽壓鹽鏇夢夢願, 42.4% ~ 68.8%) 更多 | - | 2022-03-30 | |||
临床1期 | EGFR突变的非小细胞肺癌 EGFR T790M Mutation | 20 | 獵糧蓋蓋繭範醖網醖餘(廠觸築鑰範鹽夢顧壓膚) = 3 patients at 300 or 400mg dose, all of DLTs were increased blood creatine phosphokinase 糧積構廠鹽獵鹹顧憲淵 (艱蓋餘齋鏇廠築顧鏇窪 ) 更多 | 积极 | 2021-09-25 | ||
临床1期 | EGFR-T790M 突变非小细胞肺癌 EGFR T790M Mutation | 60 | 襯壓窪夢製膚積廠齋鏇(觸繭鏇淵憲簾遞廠築糧) = 範網遞願願淵鹹範範齋 選顧選憲壓範鑰襯構窪 (鹽顧糧範廠獵鏇衊襯觸, 48.2 ~ 73.8) 更多 | 积极 | 2021-09-08 |
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