2. Academic Validation
  3. HZ-A-005, a potent, selective, and covalent Bruton's tyrosine kinase inhibitor in preclinical development

HZ-A-005, a potent, selective, and covalent Bruton's tyrosine kinase inhibitor in preclinical development

  • Bioorg Chem. 2020 Dec;105:104377. doi: 10.1016/j.bioorg.2020.104377.
Wenhai Huang 1,  Shu Wang 1,  Zhimin Zhang 1,  Chixiao Zhang 1,  Shenxin Zeng 1,  Meihao Liang 1,  Zhengrong Shen 2,  Xingguo Liu 3
Affiliations

Affiliations

  • 1 Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Hangzhou Medical College, Hangzhou 310013, China.
  • 2 Key Laboratory of Neuropsychiatric Drug Research of Zhejiang Province, Hangzhou Medical College, Hangzhou 310013, China. Electronic address: Shenzr@zjams.com.cn.
  • 3 Hangzhou Hertz Pharmaceutical Co., Hangzhou 310018, China. Electronic address: Liuxingguo_hz@hzpharma.com.
PMID: 33091668 DOI: 10.1016/j.bioorg.2020.104377
Abstract

Bruton's tyrosine kinase (Btk), a non-receptor tyrosine kinase, is a member of the Tec kinases family and is essential for B cell receptor (BCR) mediated signaling. Btk inhibitors such as ibrutinib hold a prominent role in the treatment of B cell malignancies. Here we disclose a potent, selective, and covalent Btk Inhibitor, HZ-A-005, currently in preclinical development. HZ-A-005 demonstrated dose-dependent activity in two xenograft models of lymphoma in vivo. It showed highly favourable safety, pharmacokinetic (PK), and pharmacodynamic (PD) profiles in preclinical studies. On the basis of its potency, selectivity, and covalent mode of inhibition, HZ-A-005 reveals the potential to be a promising Btk Inhibitor for a wide range of Cancer indications.

Keywords

Anti-proliferative activity; BTK; HZ-A-005; Preclinical studies; Safety; Stability.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-147784
    BTK抑制剂
    Btk
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