更新于：2024-11-08
Shanghai Haihe Pharmaceutical Research & Development Co., Ltd.
更新于：2024-11-08
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[14C]HH2853 在中国健康受试者中的物质平衡研究
评估口服谷美替尼（SCC244 ，一种选择性 MET 抑制剂）在具有MET 14外显子跳变的晚期非小细胞肺癌患者中有效性和安全性的多中心、单臂、开放III期确证性临床研究
一项开放、多中心对比谷美替尼与多西他赛在既往接受免疫治疗和含铂双药化疗后进展的驱动基因阴性且伴有MET 过表达的局部晚期或转移性非小细胞肺癌患者中的随机对照III 期临床研究
100 项与 上海海和药物研究开发股份有限公司 相关的临床结果
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2024-12-01EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Discovery of orally bioavailable phosphonate prodrugs of potent ENPP1 inhibitors for cancer treatment
Article
作者: Jiang, Shujuan ; Zhang, Chaobo ; Xu, Yanxiao ; Liu, Lei ; Tu, Wangyang ; Zhang, Yixiang ; Gao, Shanyun ; Li, Jingjing ; Yu, Bing ; Hou, Yingjie ; Yu, Songda ; Li, Leping
Ectonucleotide pyrophosphatase phosphodiesterase 1 (ENPP1) is the dominant hydrolase of 2',3'-cyclic GMP-AMP (cGAMP). Inhibition of ENPP1 contributes to increased cGAMP concentration and stimulator of interferon gene (STING) activation, with the potential to boost immune response against cancer. ENPP1 is a promising therapeutic target in tumor immunotherapy. To date, orally bioavailable ENPP1 inhibitors with highly potent activity under physiological conditions have been rarely reported. Herein, we report our effort in the design and synthesis of two different series of ENPP1 inhibitors, and in the identification of a highly potent ENPP1 inhibitor 27 (IC50 = 1.2 nM at pH 7.5), which significantly enhanced the cGAMP-mediated STING activity in THP-1 cells. Phosphonate compound 27 has good preclinical pharmacokinetic profiles with low plasma clearance rate in mouse, rat, and dog. It has been developed as bis-POM prodrug 36 which successfully improves the oral bioavailability of 27. In the Pan02 syngeneic mouse model of pancreatic cancer, orally administered 36 showed synergistic effect in combination with radiotherapy.
2024-06-13ACS Medicinal Chemistry Letters
Lead Identification of Novel Naphthyridine Derivatives as Potent SOS1 Inhibitors
Article
作者: Jiang, Shujuan ; Li, Dongsheng ; Xie, Qing ; Liu, Lei ; Sun, Kang ; Yu, Bing ; Zhang, Yixiang ; Tu, Wangyang ; Yang, Maozhi ; Yu, Songda ; Li, Leping ; Cai, Yalei
SOS1, a guanine nucleotide exchange factor (GEF), plays a critical role in catalyzing the conversion of KRAS from its GDP- to GTP-bound form, regardless of KRAS mutation status, and represents a promising new drug target to treat all KRAS-driven tumors.Herein, we employed a scaffold hopping strategy to design, synthesize, and optimize a series of novel binary ring derivatives as SOS1 inhibitors.Among them, compound 10f (HH0043) displayed potent activities in both biochem. and cellular assays and favorable pharmacokinetic profiles.Oral administration of HH0043 resulted in a significant tumor inhibitory effect in a s.c. KRASG12C-mutated NCI-H358 (human lung cancer cell line) xenograft mouse model, and the tumor inhibitory effect of HH0043 was superior to that of BI-3406 at the same dose (total growth inhibition, TGI: 76% vs 49%).On the basis of these results, HH0043, with a novel 1,7-naphthyridine scaffold that is distinct from currently reported SOS1 inhibitors, is nominated as the lead compound for this discovery project.
2024-02-01Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
Characterization of complexes of PF4 and heparins by size-exclusion chromatography coupled with multi-angle light scattering detector
Article
作者: Qiu, Piaopiao ; Zhang, Zhenqing ; Liu, Haiying ; Yi, Lin ; Ouyang, Yilan ; Xue, Yiting ; Tian, He ; Zhao, Jingwen
Heparin-induced thrombocytopenia (HIT) is an immune complication of heparin therapy. Antibodies binding to complexes of platelet factor 4 (PF4) and heparin is the trigger of HIT. A method using size exclusion chromatography with multi-angle laser light scattering detector (SEC-MALS) was developed in this work. The soluble ultra-large complex (ULC) was separated from the small complex (SC) and their molecular weights (MWs) were firstly measured. The complexes of PF4 and three heparins with different MW, including unfractionated heparin (UFH), dalteparin (Daltep) and enoxaparin (Eno) were characterized using this method. The contents and the sizes of ULC increased gradually when heparins were added to PF4 to certain amounts. While, they reduced after more heparins were added. It is the first time to measure the MWs of the biggest ULC of PF4-heparins as millions of Dalton. at the proper ratios of PF4 to heparin (PHR). Meanwhile, those mixtures at those certain PHRs induced the higher expression of CD83 and CD14 markers on dendritic cells (DCs) suggesting that they had stronger immunogenicity and is critical for HIT.
100 项与 上海海和药物研究开发股份有限公司 相关的药物交易
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100 项与 上海海和药物研究开发股份有限公司 相关的转化医学
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