SPH-5030(SPH-5030) - 药物靶点：HER2_在研适应症：HER2阳性胆道肿瘤，HER2阳性结直肠癌，晚期恶性实体瘤_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

HER2

作用机制

HER2拮抗剂(受体蛋白酪氨酸激酶 erbB-2拮抗剂)

治疗领域

肿瘤消化系统疾病

在研适应症

HER2阳性胆道肿瘤HER2阳性结直肠癌晚期恶性实体瘤+ [1]

非在研适应症-

原研机构-

在研机构

上海医药集团股份有限公司本溪北方药业有限公司

非在研机构-

最高研发阶段临床2期

首次获批日期-

最高研发阶段(中国)临床2期

特殊审评-

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关联

6

项与 SPH-5030 相关的临床试验

NCT06434597 / Recruiting临床2期

A Multicenter, Open, Single-arm Phase II Clinical Study to Evaluate the Efficacy and Safety of SPH5030 Tablets in Subjects With Her2-positive/Mutated Biliary Tract OR Colorectal Cancer.

To evaluate the efficacy and safety of SPH5030 tablets in subjects with Her2-positive/mutated biliary tract OR colorectal cancer.

开始日期2024-07-17

申办/合作机构

上海医药集团股份有限公司

CTR20241487 / Recruiting临床2期

一项评价SPH5030片在HER2阳性/突变胆道和结直肠癌患者中有效性和安全性的多中心、开放性、单臂II期研究。

评价SPH5030片单药治疗HER2阳性/突变晚期胆道癌和结直肠癌患者的客观缓解率。

开始日期2024-07-11

申办/合作机构

上海医药集团股份有限公司

[+1]

NCT06372223 / Completed临床1期

A Single-center, Randomized, Open, Single-dose, Two-cycle, Two-sequence Crossover Food Effect Study of SPH5030 Tablets in Healthy Chinese Adult Subjects.

The purpose of this study is to evaluate the food effect of SPH5030 tablets in healthy Chinese adult subjects.

开始日期2024-03-04

申办/合作机构

上海医药集团股份有限公司

100 项与 SPH-5030 相关的临床结果

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100 项与 SPH-5030 相关的转化医学

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100 项与 SPH-5030 相关的专利（医药）

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2

项与 SPH-5030 相关的文献（医药）

2024-10-01·European Journal of Medicinal Chemistry

Unraveling the future: Innovative design strategies and emerging challenges in HER2-targeted tyrosine kinase inhibitors for cancer therapy

Review

作者: Chen, Ruixian ; Zheng, Sixiang ; Wang, Ting ; Long, Fangyi ; Tan, Lun ; Zhang, Lele ; Li, Lintao

Human epidermal growth factor receptor 2 (HER2) is a transmembrane receptor-like protein with tyrosine kinase activity that plays a vital role in processes such as cell proliferation, differentiation, and angiogenesis. The degree of malignancy of different cancers, notably breast cancer, is strongly associated with HER2 amplification, overexpression, and mutation. Currently, widely used clinical HER2 tyrosine kinase inhibitors (TKIs), such as lapatinib and neratinib, have several drawbacks, including susceptibility to drug resistance caused by HER2 mutations and adverse effects from insufficient HER2 selectivity. To address these issues, it is essential to create innovative HER2 TKIs with enhanced safety, effectiveness against mutations, and high selectivity. Typically, SPH5030 has advanced to phase I clinical trials for its strong suppression of four HER2 mutations. This review discusses the latest research progress in HER2 TKIs, with a focus on the structural optimization process and structure-activity relationship analysis. In particular, this study highlights promising design strategies to address these challenges, providing insightful information and inspiration for future development in this field.

2022-04-14·Journal of Medicinal Chemistry1区 · 医学

Discovery of SPH5030, a Selective, Potent, and Irreversible Tyrosine Kinase Inhibitor for HER2-Amplified and HER2-Mutant Cancer Treatment

1区 · 医学

Article

作者: Ke, Ying ; Hong, Yuan ; Chen, Na ; Qian, Hai ; Wang, Qian ; Tu, Yuanxiang ; Xu, Jia ; Jin, Kaijun ; Gong, Wanchun ; Wang, Xuenan ; Zuo, Hongjian ; Zhang, Jing ; Duan, Lingjun ; Zhang, Zhihui ; Xia, Guangxin ; Li, Di

Small-molecule irreversible tyrosine kinase inhibitors as high potent agents have led to improvements in disease-free and overall survival in patients with HER2-amplified cancer. The approved irreversible HER2 inhibitors, neratinib and pyrotinib, both lack HER2 selectivity, leading to off-target adverse events in patients. The development of HER2 mutation during treatment also hampers the progress of the treatment. We used a molecular hybridization strategy for structural optimizations, in conjunction with in vitro and in vivo drug-like property screening, to obtain a clinical candidate SPH5030. Overall, SPH5030 showed excellent activities against four frequent kinds of HER2 mutants and high relative HER2 selectivity compared with neratinib and pyrotinib, good pharmacokinetic characteristics with desirable bioavailabilities, and significant in vivo antitumor efficacy in xenograft mouse models, especially in a HER2 mutation A775_G776insYVMA xenograft mouse model with its potency much higher than those of neratinib and pyrotinib.

100 项与 SPH-5030 相关的药物交易

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研发状态

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
HER2阳性胆道肿瘤	临床2期	中国	上海医药集团股份有限公司	2024-07-11
HER2阳性结直肠癌	临床2期	中国	上海医药集团股份有限公司	2024-07-11
晚期恶性实体瘤	临床1期	中国	上海医药集团股份有限公司	2024-03-04
HER2阳性实体瘤	临床1期	中国	上海医药集团股份有限公司	2021-12-28
HER2阳性实体瘤	临床1期	中国	本溪北方药业有限公司	2021-12-28

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临床结果

适应症

分期

评价

查看全部结果

研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05245058 (Phase 1a study of SPH5030, ASCO2024)	临床1期	HER2阳性实体瘤 HER2 positive	30	SPH5030 50mg	(淵鬱網構鏇夢淵遞製構) = 20.0%, 0% ≥ G3 選衊顧衊遞願衊遞鑰網 (築鑰醖願積築繭艱衊獵 ) 更多	积极	2024-05-24
				SPH5030 100mg