Lupeng Pharmaceutical's Fourth-Generation BTK Inhibitor Rocbrutinib Approved in China for Relapsed or Refractory Mantle Cell Lymphoma

GUANGZHOU, China, June 4, 2026 /PRNewswire/ -- Lupeng Pharmaceutical today announced that the National Medical Products Administration (NMPA) has granted accelerated approval to 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.

Rocbrutinib, independently developed by Lupeng Pharmaceutical, is the fourth-generation BTK inhibitor with dual covalent (irreversible) and non-covalent (reversible) mechanism. The approval of rocbrutinib will provide a new breakthrough treatment option for R/R MCL patients following failure of earlier-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. It will bring a new and effective treatment option to MCL patients who have experienced disease progression after earlier-generation BTK inhibitor therapy. Furthermore, it demonstrates Lupeng's global leadership in advancing BTK-targeted innovation. Going forward, we will continue to advance clinical studies of rocbrutinib in other indications such as diffuse large B-cell lymphoma (DLBCL) and chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), to help more patients with various hematologic malignancies."

Dr. Chen Yi, co-founder and CSO of the company, said, "The market launch of rocbrutinib is a successful example of Lupeng's 'innovation methodology,' proving that the company's unique 'Beyond the Rule of 5' , BeyondX Oral MedChem Platform , can efficiently develop next-generation, globally best-in-class small molecule targeted drugs featuring novel mechanisms of action."

The NMPA approval of rocbrutinib for the treatment of R/R MCL is primarily based on positive results from a nationwide, multi-center, open-label, single-arm Phase II registration clinical trial (the ROCK-1 study)^[1-2], led by Professor Zhu Jun and Professor Song Yuqin from Peking University Cancer Hospital. Forty-one centers across China participated in the study, which was designed 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 June 5, 2025, clinical trial data showed an objective response rate (ORR) of 63.9%, a complete response rate (CR) of 23%, and a median duration of response (mDOR) of 16.5 months. All enrolled patients had previously received at least a covalent BTK inhibitor; more than one-third of them had received two or more cBTK inhibitors. Baseline characteristics of the patient group were generally difficult to treat and had poor prognosis. In terms of safety, no atrial fibrillation/flutter or other cardiac events occurred, and no patient permanently discontinued treatment due to adverse events. The incidence of BTK inhibitor–associated toxicity was relatively low.

In April 2026, rocbrutinib was included for the first time in the Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Lymphoma , where it was listed as a Category II recommendation for the treatment of R/R MCL. Its inclusion in the guidelines prior to formal NMPA approval reflects the recognition by leading clinical experts of rocbrutinib's innovative mechanism and promising clinical value in addressing the significant unmet need in R/R MCL.

Professor Weiping Liu of Peking University Cancer Hospital noted that, based on key evidence from clinical studies, rocbrutinib has become an important recommended treatment option for MCL and provides support for standardized clinical practice. Professor Jun Ma of Harbin Institute of Hematology & Oncology further emphasized that patients with R/R MCL have long lacked effective standard treatment options, representing a major challenge in clinical practice. As the first fourth-generation BTK inhibitor to reach the marketing application stage, rocbrutinib's dual covalent and non-covalent mechanism enables it to target C481-site and other resistance mutations such as T474I and L528W, providing a scientific basis for overcoming acquired resistance.

The recommendation provides authoritative and standardized clinical guidance for physicians and offers a new treatment opportunity for patients with R/R MCL.

More importantly, rocbrutinib's anti-tumor activity is not limited to MCL; it has demonstrated positive therapeutic potential in various B-cell malignancies, including DLBCL, CLL/SLL and Marginal zone lymphoma (MZL). The guidelines also include a note indicating rocbrutinib's efficacy as monotherapy or in combination therapy for patients with R/R DLBCL.

Based on preliminary study results in adult patients with non-GCB DLBCL who had received at least two prior lines of treatment, rocbrutinib was granted Breakthrough Therapy Designation (BTD) by the Center for Drug Evaluation (CDE) in May 2024. The corresponding pivotal Phase II registration study (ROCK-2) had already been initiated by the end of 2025.

Results from a Phase I study conducted in the United States showed that rocbrutinib achieved an ORR of 78.3% at doses of 200–300 mg/day in CLL patients previously treated with BTK inhibitors, with an estimated median progression-free survival (PFS) of 28.1 months in the 100–300 mg/day dose range^[3]. In January 2026, the global Phase III head-to-head clinical trial comparing rocbrutinib with the third-generation non-covalent BTK inhibitor pirtobrutinib for the treatment of R/R CLL/SLL (the ROCKET-CLL study, NCT07342478) was launched, marking a new stage in rocbrutinib's global development.

About Lupeng Pharmaceutical

Lupeng Pharmaceutical is a clinical-stage company dedicated to the discovery and development of innovative medicines for the treatment of hematological malignancies and autoimmune diseases. In pursuit of cutting-edge science, we are mainly focusing on clinically validated targets such as BTK, Bcl-2 and Bcl-xL and promoting international and domestic multi-center clinical development and commercialization.

Our investigational drugs LP-168 (rocbrutinib), LP-108 (lacutoclax) and LP-118 have demonstrated promising efficacy with a favorable safety profile, positioning them as potential Best-in-Class (BIC) medicines.  Rocbrutinib was already granted accelerated approval for relapsed or refractory mantle cell lymphoma (R/R MCL) by the National Medical Products Administration (NMPA) in China and was included in the Lymphoid Diagnosis and Treatment Guidelines of Chinese Society of Clinical Oncology (CSCO) 2026. Lacutoclax have been granted regulatory approval by CDE for pivotal registration trials.

At Lupeng Pharmaceutical, we are committed to building a multinational pharmaceutical company and delivering innovative medicines to address unmet medical needs for the improvements of patient's lives.

SOURCE Lupeng Pharmaceutical Ltd