The innovative targeted protein degrader HZ-Q1070 capsules developed by Hangzhou HealZen Therapeutics Co., Ltd has been cleared by the United States Food and Drug Administration (FDA) to conduct a Phase I clinical trial for the treatment of relapsed or refractory B-cell lymphoma

B-cell lymphoma (BCM) is a heterogeneous lymphoproliferative disease originating from B-lymphocytes. Common subtypes of BCM in China include diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), marginal zone lymphoma (MZL), chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), mantle cell lymphoma (MCL), primary central nervous system lymphoma (PCNSL), etc.

Bruton's tyrosine kinase (BTK) is mainly expressed in B lymphocytes and plays a crucial role in B-cell proliferation, apoptosis, differentiation, and migration. Currently, multiple covalent BTK inhibitors and one non-covalent BTK inhibitor have been approved for marketing in both domestic and international markets. The approved indications include CLL/SLL, WM, MCL, MZL, FL, PCNSL, etc. However, both covalent and non-covalent BTK inhibitors can cause acquired drug resistance mutations.

BTK protein degraders are bifunctional molecules composed of three parts: protein of interest (POI) ligand, E3 ligase binding ligand, and Linker linking them, which can utilize the ubiquitin-proteasome system (UPS) naturally occurring in the body to degrade pathogenic proteins and achieve the purpose of treating diseases.

This technology has become a new strategy for drug development, enabling continuous degradation of targets through a recycling catalytic mechanism. Compared to traditional small-molecule inhibitors, targeted protein degraders can exert their effects without requiring tight binding to the sites that affect protein activity, which can address the issue of drug resistance encountered by traditional small-molecule inhibitors[1].

About the BTK protein degrader HZ-Q1070 Capsules

HZ-Q1070 is a BTK degrader with novel structure, excellent degradation activity/selectivity and good druggability, which is expected to solve the problem of drug resistance of small molecule BTK inhibitors and become a new therapeutic drug for B-cell lymphoma. It has previously been approved by the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA), China, to conduct a Phase I clinical trial for relapsed or refractory B-cell lymphoma.

About Hangzhou HealZen Therapeutics Co., Ltd

Hangzhou HealZen Therapeutics Co., Ltd is an innovative small-molecule drug development company driven by innovative technology in the clinical stage,  dedicated to addressing unmet clinical needs. The company independently develops targeted protein degradation drugs and an intelligent drug development platform, focusing on drug development in disease areas such as hematological tumors and the central nervous system. The company has established project pipelines with over 10 Class 1 new drugs, of which 6 molecules have entered the clinical research stage, 1 molecule is in clinical phase III, and 1 molecule has been recognized as a breakthrough therapy. In addition, the company has accumulated 4 new drug pipelines for external cooperation, and the drug discovery capability has been widely recognized in the industry.

References：

1. Li, K., Crews, C. M. PROTACs: past, present and future. Chem Soc Rev. 2022, 20;51(12): 5214-5236.