The Class 1 innovative drug BCL-2 inhibitor HZ-L105 Tablet, jointly developed by Hangzhou HealZen Therapeutics Co., Ltd. and Guangdong Hongye Pharmaceutical Technology Co., Ltd., has been approved by the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA) to conduct a Phase I clinical trial for the treatment of mature B-cell malignancies.

Venetoclax is the world's first approved highly selective Bcl-2 inhibitor for treating chronic lymphocytic leukemia/small lymphocytic lymphoma and acute myeloid leukemia and has been recommended as a first-line therapy in clinical guidelines. In 2023, the sales of Venetoclax reached $2.288 billion. Additionally, multiple Bcl-2 inhibitors are currently in clinical development. The main indications include Chronic Lymphocytic Leukemia/Small Lymphocytic Lymphoma (CLL/SLL), Mantle Cell Lymphoma (MCL), Non-Hodgkin Lymphoma (NHL), Waldenström's Macroglobulinemia (WM), Acute Myeloid Leukemia (AML), Multiple Myeloma (MM), AL Amyloidosis, Systemic Lupus Erythematosus (SLE), etc.

About the BCL-2 Inhibitor HZ-L105 Tablets

HZ-L105 is a new generation of orally administered, highly efficient, and highly selective Bcl-2 inhibitor designed and optimized through structure-activity relationship studies. It exhibits robust inhibitory activity against Bcl-2 resistant mutations, including G101V, D103Y, D103V, and D103E. Furthermore, compared to Venetoclax, HZ-L105 demonstrates enhanced inhibitory activity in B-NHL tumor cells such as MCL and DLBCL. While maintaining high activity and selectivity, HZ-L105 has improved pharmacokinetic properties, including better oral absorption, higher plasma exposure, and enhanced metabolic stability. It does not significantly inhibit hepatic metabolic enzymes, reducing the risk of drug interactions and making it more suitable for combination therapy.HZ-L105 has demonstrated significant antitumor effects in vitro and in vivo, with good nonclinical safety profiles. HZ-L105 is expected to offer a new and better option for patients with hematological malignancies.