News & Events

Lupeng Pharmaceutical, a global leading platform-based emerging biopharmaceutical company focused on developing innovative medicines for the treatment of malignancies and autoimmune diseases based on its proprietary BeyondX® oral drug chemistry platform, recently achieved another significant milestone: the global Phase III head-to-head clinical trial (ROCKET-CLL Study) of its internally developed, first and only dual covalent and non-covalent BTK inhibitor Rocbrutinib (LP-168) for the treatment of relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (R/R CLL/SLL) has been registered on ClinicalTrials.gov (Identifier: NCT07342478). This head-to-head study is designed to compare the efficacy and safety of Rocbrutinib versus the approved non-covalent BTK inhibitor Pirtobrutinib in patients with R/R CLL/SLL who were previously treated with a covalent BTK inhibitor (cBTKi).

The American Society of Hematology (ASH) Annual Meeting and Exposition is one of the largest academic conferences in the field of hematology, showcasing the most cutting-edge research advancements and the latest drug development data from around the world. The 67th ASH Annual Meeting was held from December 6–9, 2025, in Orlando, Florida, USA. At this conference, updates on clinical studies for Rocbrutinib (LP-168) and LP-118 were presented as types of oral presentation, abstract and poster.

Rocbrutinib is a 4th generation Bruton’s tyrosine kinase inhibitors (BTKi) with high selectivity, excellent bioavailability and a unique dual (covalent and non-covalent) binding activity. It can target wild type (WT) BTK irreversibly (covalent binding), C481 mutant BTK (C481S, C481F and C481R) reversibly (non-covalent binding), and other non-C481 mutations such as the gatekeeper mutation T474I irreversibly. Therefore, it can inhibit the activity of both wild-type (WT) as well as mutant BTK.

On May 28, 2025, the New Drug Application (NDA) for Rocbrutinib, the 4th generation Bruton's tyrosine kinase (BTK) inhibitor, independently developed by Lupeng Pharmaceutical, was formally accepted by the Center for Drug Evaluation (CDE) in China for the treatment of relapsed or refractory mantle cell lymphoma (R/R MCL) in adult patients who have previously received other BTK inhibitor therapies. If approved, Rocbrutinib is expected to become China’s first domestically developed BTK inhibitor used to treat this disease.

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).