News & Events
On May 7th, 2025, the National Medical Products Administration (NMPA) in China granted approval for a pivotal Phase II registration clinical study to investigate the use of Rocbrutinib monotherapy in treating relapsed/refractory non-germinal center B-cell-like diffuse large B-cell lymphoma (R/R non-GCB DLBCL).
Rocbrutinib is the fourth-generation Bruton’s Tyrosine Kinase (BTK) inhibitor. It can covalently bind to and inhibit the activity of wild-type (WT) BTK and non-covalently bind to and inhibit the activity of C481 mutated BTK. Therefore, it not only overcomes drug resistance associated with the first, second, and third generations of BTK inhibitors but also demonstrates significantly improved potency, selectivity, and pharmacokinetics (PK). It is anticipated to become a best-in-class BTK inhibitor.
In addition, clinical studies of Rocbrutinib for the treatment of various B-cell lymphomas, including mantle cell lymphoma (MCL), chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), and marginal zone lymphoma (MZL), are also ongoing.
Given its outstanding efficacy and safety profile compared to other therapies for R/R non-GCB DLBCL, Rocbrutinib was designated as a Breakthrough Therapy Designation (BTD) by the Center for Drug Evaluation (CDE) in May 2024. This makes it the first BTK inhibitor in China and the only BTK inhibitor globally to receive BTD for DLBCL.
Diffuse large B-cell lymphoma (DLBCL) is the most common type of non-Hodgkin lymphoma (NHL), accounting for approximately 30–40% of NHL cases. In 2022, China recorded about 40,000 new DLBCL cases, a number comparable to that in the U.S., but with a significantly higher mortality rate. Based on cell-of-origin, DLBCL can be classified into germinal center B-cell-like (GCB) or non-germinal center B-cell-like (non-GCB) types, with the latter comprising approximately 60–70% of cases. DLBCL is an aggressive, highly heterogeneous, rapidly progressive B-cell malignancy characterized by a short survival period and extremely poor prognosis. Non-GCB DLBCL has a worse prognosis than GCB DLBCL.
Approximately 40% of DLBCL patients experience relapsed or refractory disease after first-line therapy. Treatment options become increasingly limited, and therapeutic efficacy diminishes with each subsequent line of treatment. Therefore, there is an urgent need for novel therapies with distinct mechanisms for this group of patients. Studies have indicated that non-GCB DLBCL is driven by aberrant activation of B-cell receptor (BCR) and NF-κB signaling pathways, which promote tumor proliferation. This provides a theoretical foundation for targeting Bruton’s tyrosine kinase (BTK), a key molecule in the BCR pathway, for the treatment of non-GCB DLBCL.