News & Events

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).

On February 24, Guangzhou Lupeng Pharmaceuticals Co., Ltd. (hereinafter referred to as "Lupeng Pharmaceuticals") and Hansoh Pharmaceutical Group Co., Ltd. (hereinafter referred to as "Hansoh Pharmaceutical", 03692.HK)’s collaborative drug, a Class 1 small molecule Bruton's tyrosine kinase inhibitor (BTKi) LP-168 (HS-10561 capsule), was granted regulatory approval by the National Medical Products Administration (NMPA) in China for clinical trials for chronic spontaneous urticaria treatment. This marks the first clinical milestone achieved since the strategic collaboration between Lupeng Pharmaceuticals and Hansoh Pharmaceutical was established.

The 66th ASH Annual Meeting took place on December 7th, 2024, in San Diego, California, USA. At this event, posters highlighting the latest updates on Rocbrutinib (LP-168), a novel covalent and non-covalent new generation BTK inhibitor were presented. The presentations included both clinical and non-clinical study results from China and the United States. Some presentations represented continuation of the clinical research initially introduced at the last ASH Annual Meeting. For comprehensive insights, the complete abstracts and corresponding links are provided as follows: