Lupeng Pharmaceuticals Launches China's First Homegrown Fourth-Generation BTK Inhibitor Rocbrutinib (Luokeda®) for Relapsed/Refractory Mantle Cell Lymphoma

On June 4, 2026, Lupeng Pharmaceutical announced its self-developed Class 1 innovative drug, Luqueda^®(Rocbrutinib Tablets, Rocbrutinib, Development Code: LP-168)Officially approved by the National Medical Products Administration (NMPA) for marketing, indicated for the treatment of adult patients with relapsed or refractory mantle cell lymphoma (MCL) who have previously received at least two systemic therapies, including a BTK inhibitor.

Figure 1. Conditional Approval Granted by the National Medical Products Administration for the Marketing of Lobutinib Tablets

AsThe world’s first and currently only fourth-generation Bruton’s tyrosine kinase (BTK) inhibitor with both covalent and non-covalent mechanisms,As the first “domestically developed original BTK inhibitor” approved for this indication, the launch of lobrutinib marks a major breakthrough in China’s efforts to overcome resistance to BTK inhibitors, providing a novel treatment option for patients with relapsed or refractory MCL.

Mantle Cell Lymphoma (MCL) is a B-cell non-Hodgkin lymphoma (NHL) characterized by both aggressive and indolent features, accounting for approximately 3%–10% of adult NHL cases. Although earlier generations of Bruton’s tyrosine kinase (BTK) inhibitors have significantly improved treatment outcomes for patients with MCL, drug resistance remains a core bottleneck limiting long-term survival. This is particularly evident in patients who have previously failed covalent BTK inhibitor therapy, for whom subsequent effective treatment options are limited.

Lukeda^®(Lobrutinib Tablets) asFourth-generation covalent and non-covalent dual-mechanism BTK inhibitor,Overcoming the limitation of drug resistance associated with traditional covalent BTK inhibitors, its core advantage lies in a unique “covalent + non-covalent” intelligent switching design: it irreversibly inhibits wild-type BTK via covalent binding, while reversibly binding to mutant BTK (such as C481S) through non-covalent interactions. This approach not only effectively overcomes the C481 mutation but also inhibits various other BTK mutations, including T474 and L528. Furthermore, due toHigher target selectivity,Loebtinib exhibits minimal inhibition of off-targets such as TEC, ITK, and EGFR, significantly reducing off-target-related toxicities. This innovative design opens up a new therapeutic pathway for patients who have failed BTK inhibitor therapy, providing clinicians with a superior treatment option that combines “high efficacy in overcoming resistance” with “excellent safety.”

Figure 2. Schematic illustration of loxoprofen (purple) and previous-generation BTK inhibitors (blue) binding to two distinct pockets of the target protein, respectively.

This approval was based on a pivotal, open-label, single-arm, Phase II registration clinical trial conducted across multiple centers in China.（ROCK-1）positive outcomes. Study data showed that among 61 evaluable subjects with previously treated relapsed or refractory mantle cell lymphoma (MCL) (median of 3 prior lines of therapy, all having received covalent BTK inhibitor treatment):The objective response rate (ORR) was 63.9%, with a complete response rate (CR) of 23.0%; the median progression-free survival (PFS) was 7.39 months, and the median duration of response (mDOR) reached 16.46 months.

In terms of safety, Lu Keda benefits from its good tolerability due to its high selectivity.^®(Lobutinib Tablets) demonstrated an excellent safety profile: no atrial fibrillation/atrial flutter events of any grade were reported, and the incidence of Grade ≥3 bleeding adverse reactions was only 1.6%, significantly reducing treatment-related cardiovascular and bleeding risks. There were no treatment-related permanent discontinuations or deaths during the study, indicating good overall tolerability.

Furthermore, data from another Phase I clinical study, LP-168-CN101 (NCT04880187), demonstrated that Ludake^®(Lobutinib Tablets) also demonstrate best-in-class potential: an ORR of 89.3% and a CRR of 57.1%; at a median follow-up of 21.2 months, the 18-month PFS rate was 74.3%.

Lukeda^®(The approval of lobrutinib tablets) fills the gap in later-line treatment after prior BTK inhibitor therapy, providing more evidence-based options for patients experiencing disease progression on covalent BTK inhibitors. In April 2026, Lukeda^®(Lobutinib Tablets) have been officially included in the "Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Lymphoma 2026" as a second-line treatment recommendation for relapsed/refractory MCL.

Figure 3. Addition of lobrutinib to the CSCO Guidelines for the Diagnosis and Treatment of Lymphoma (2026) as a Recommended Salvage Therapy for R/R MCL

In addition to the approved indication for mantle cell lymphoma, Lukeda^®(Lobrutinib tablets) are also undergoing clinical studies in multiple B-cell lymphoma indications, including chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), marginal zone lymphoma (MZL), and diffuse large B-cell lymphoma (DLBCL). Notably, the indication for relapsed or refractory (R/R) non-germinal center B-cell-like (non-GCB) DLBCL has been granted Breakthrough Therapy Designation by the Center for Drug Evaluation (CDE), making it the first Bruton’s tyrosine kinase (BTK) inhibitor in China to receive such recognition. In the future, Lukeda^®(Lobrutinib Tablets) are expected to bring therapeutic hope to a broader range of patients with hematologic malignancies.

Lupeng Pharmaceutical, founded in Guangzhou in 2018 by Dr. Tan Fenlai and Dr. Chen Yi, is an innovative pharmaceutical company focused on the fields of oncology and autoimmune diseases. The company leverages its independently developed BeyondX^®Oral Small-Molecule Drug Platform: Building a Robust Pipeline of Innovative Therapeutics, with Core Product LP-168 (Lobutinib) Approved for Marketing by the National Medical Products Administration (NMPA) under the Brand Name Lukeda^®; LP-108 (Letocra) has entered the pivotal registration study phase for market approval. Multiple products are being developed through global multi-center clinical trials, with the aim of building a multinational innovative pharmaceutical company with global competitiveness.