— Bringing a new treatment option for patients with relapsed or refractory mantle cell lymphoma (R/R MCL)
GuangzhouJune 4, 2026 /PRNewswire/ — Guangzhou Lupeng Pharmaceutical Co., Ltd. today announced that the National Medical Products Administration (NMPA) has approved, through a priority review and approval process, the company’s independently developed Class 1 innovative drug, the covalent and non-covalent fourth-generation Bruton’s tyrosine kinase (BTK) inhibitor, Rocbrutinib tablets (trade name: Lupenda®, generic name: Rocbrutinib, development code: LP-168), for the treatment of adult patients with relapsed or refractory mantle cell lymphoma (R/R MCL) who have received at least two prior systemic therapies (including BTK inhibitors).
As a fourth-generation BTK inhibitor with a dual covalent and non-covalent mechanism of action, the approval of Rocbrutinib will provide a breakthrough new treatment option for mantle cell lymphoma patients facing therapeutic challenges after failure of prior-generation BTK inhibitor therapy.
Dr. Tan Fenlai, co-founder and CEO of Lupeng Pharmaceutical, stated, “The successful approval of Rocbrutinib is a major milestone in Lupeng Pharmaceutical’s development, bringing a novel and effective treatment option for mantle cell lymphoma patients who have developed resistance and progressed after prior-generation BTK inhibitor therapy. This further validates Lupeng Pharmaceutical’s global leadership in deep innovation targeting the BTK pathway. In the future, we will continue to advance clinical research of Rocbrutinib in other indications such as diffuse large B-cell lymphoma (DLBCL), chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), to help more patients with different types of hematologic malignancies.” Dr. Chen Yi, co-founder and CSO of the company, said, “The launch of Rocbrutinib is a successful example of the company’s ‘innovation methodology,’ demonstrating that our proprietary ‘Beyond Five Rules’ medicinal chemistry R&D platform, BeyondX, can efficiently develop best-in-class and novel-mechanism next-generation small molecule targeted drugs.”
The NMPA’s approval of Rocbrutinib for the treatment of relapsed or refractory mantle cell lymphoma is primarily based on positive results from a national multicenter, open-label, single-arm registrational Phase II clinical trial (ROCK-1 study).[1-2] This study, led by Professor Zhu Jun and Professor Song Yuqin from Peking University Cancer Hospital, with participation from 41 centers nationwide, aimed to evaluate the efficacy and safety of Rocbrutinib monotherapy in MCL patients who had relapsed or were refractory after prior treatment with covalent BTK inhibitors. As of the data cutoff date of June 5, 2025, the objective response rate (ORR) was 63.9%, the complete response rate (CR) was 23%, and the median duration of response (mDOR) was 16.5 months. All enrolled patients had received multiple prior lines of therapy and had all been previously treated with covalent BTK inhibitors, with over one-third having received two or more BTK inhibitors. Baseline characteristics indicated that the study population was generally more refractory and had a poor prognosis. In terms of safety, no cardiac events such as atrial fibrillation/flutter were reported, no discontinuations due to adverse reactions occurred, and the incidence of other adverse reactions was relatively low and generally manageable.
In April 2026, Rocbrutinib was first included in the Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Lymphoma (2026 Edition), listed as a Level II recommendation for the treatment of relapsed/refractory mantle cell lymphoma (R/R MCL). Professor Liu Weiping from Peking University Cancer Hospital stated that based on key evidence-based data, Rocbrutinib has been confirmed as an important recommended regimen for MCL, supporting standardized diagnosis and treatment. Professor Ma Jun from the Harbin Institute of Hematology and Oncology pointed out that R/R MCL patients have long lacked effective standard treatment options, which has become a prominent challenge in clinical practice. As the first fourth-generation BTK inhibitor to enter the marketing application stage, Rocbrutinib, with its dual covalent and non-covalent mechanism, can effectively target the C481 site as well as resistance mutations such as T474I and L528W, providing a basis for overcoming acquired resistance. Its inclusion as a Level II recommendation in the CSCO guidelines for R/R MCL treatment offers authoritative and standardized medication guidance for clinical decision-making, bringing new survival opportunities for patients. More importantly, Rocbrutinib’s antitumor activity is not limited to MCL; it has shown positive therapeutic potential in various common B-cell lymphoma subtypes, including DLBCL, CLL/SLL, and MZL. The guidelines also note that Rocbrutinib has demonstrated efficacy as monotherapy or in combination therapy for patients with relapsed/refractory DLBCL.
In May 2024, Rocbrutinib was granted Breakthrough Therapy designation by the Center for Drug Evaluation of the NMPA for the indication of adult patients with relapsed or refractory non-germinal center B-cell-like diffuse large B-cell lymphoma (R/R non-GCB DLBCL) who have received at least two prior lines of therapy. The corresponding pivotal registrational Phase II clinical study (ROCK-2) was initiated in late 2025. Results from a Phase I study conducted in the United States showed that Rocbrutinib achieved an ORR of 78.3% in patients with chronic lymphocytic leukemia (CLL) previously treated with BTK inhibitors, with a median progression-free survival (mPFS) of 28.1 months.[3]
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[1] Song et al. Efficacy and safety of rocbrutinib, the fourth generation bruton’s tyrosine kinase inhibitor,in patients with BTK inhibitor pre-treated relapsed or refractory Mantle Cell Lymphoma: Results from a Phase II rock-1 trial, ASH 2025, 146 (Supplement 1): 886 |
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[2] Song et al. updated efficacy and safety results of rocbrutinib from the phase 2 rock-1 study in patients with relapsed or refractory mantle cell lymphoma and previously treated with btk inhibitor. EHA 2026,1354, PF945 |
About Lupeng Pharmaceutical
Lupeng Pharmaceutical focuses on the research and development of next-generation small molecule targeted innovative drugs for the treatment of malignant tumors and autoimmune diseases, with a particular emphasis on key targets such as BTK, Bcl-2, and Bcl-xL in hematologic malignancies, comprehensively advancing international and domestic multicenter clinical development and commercialization. The company’s core projects, LP-168 (Rocbrutinib), LP-108 (Lacutoclax), and LP-118, are highly competitive in the industry and are expected to become best-in-class products. Among them, Rocbrutinib (trade name Lupenda®) has been approved for marketing by the NMPA and included in the CSCO Guidelines for the Diagnosis and Treatment of Lymphoma 2026. Lacutoclax has also received CDE approval to enter pivotal registrational studies. Since its inception, the company has received continuous investment and support from multiple international and domestic biopharmaceutical venture capital funds. Adhering to the philosophy of “diligence, pragmatism, innovation, and benefiting society,” Lupeng is committed to building a multinational pharmaceutical enterprise integrating R&D, production, and sales, with a high degree of innovation and social responsibility.