Rocbrutinib Receives Chinese Approval in Relapsed/Refractory MCL

The National Medical Products Administration (NMPA) has given accelerated approval to the fourth-generation Bruton’s tyrosine kinase (BTK) inhibitor rocbrutinib (LP-168) in China as a treatment for patients with relapsed/refractory mantle cell lymphoma (MCL) previously treated with at least 2 prior systemic therapies including BTK inhibitors, according to a news release from the developer, Lupeng Pharamaceutical.¹

The NMPA approval was based on findings from the single-arm phase 2 registration ROCK-1 trial (NCT05716087), which encompassed 41 centers across China and evaluated the efficacy and safety of the agent as a monotherapy in this relapsed/refractory population. At the data cutoff date of June 5, 2025, rocbrutinib produced an objective response rate (ORR) of 63.9%, a complete response (CR) rate of 23.0%, and a median duration of response (DOR) of 16.5 months.

Moreover, in April 2026, rocbrutinib was included in the Chinese Society of Clinical Oncology (CSCO) Guidelines for the Diagnosis and Treatment of Lymphoma, listed as a Category II recommendation for relapsed/refractory disease. The developers noted that its inclusion in the guidelines prior to the approval reflected the recognition by clinical experts of the clinical value of the agent in addressing an unmet need for treatment in relapsed/refractory MCL.

"The successful approval of rocbrutinib is a major milestone in Lupeng Pharmaceutical's development. It will bring a new and effective treatment option to [patients with MCL] who have experienced disease progression after earlier-generation BTK inhibitor therapy,” Tan Fenlai, MD, PhD, co-founder and chief executive officer of Lupeng Pharmaceutical, stated in the release.¹ “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."

In the open-label, single-arm trial, patients were given rocbrutinib at 240 mL orally with water, without food once daily.² Treatment continued in the absence of disease progression, unacceptable toxicity, or other discontinuation criteria met.

Those eligible for enrollment on the study had a confirmed diagnosis of MCL per 2017 revised WHO lymphoma classification criteria; an ECOG performance score of 0 to 2; and adequate hematologic, hepatic, and renal function. Patients who received prior non-covalent BTK inhibition; who received antitumor therapies, investigational treatment, major surgery, severe trauma, or chemotherapy within 4 weeks or 5 half-lives prior to first rocbrutinib dose; and those with central nervous system metastases were among those who were ineligible for trial enrollment.

The primary end point of the study was ORR up to 24 months as assessed by an independent reading committee (IRC). Secondary end points included ORR up to 24 months per investigator assessment, CR rate, progression-free survival, DOR, time to response, and safety.

Safety outcomes revealed no reported atrial fibrillation, flutter events, or other cardiac events. No discontinuations occurred due to adverse effects. Moreover, treatment-related toxicities were relatively low per the developers.

Rocbrutinib previously received breakthrough therapy designation by the Center for Drug Evaluation in May 2024 for patients with relapsed/refractory MCL who received 2 or more prior lines of therapy.

Moreover, a phase 1 trial (NCT06978088) conducted in the US found that rocbrutinib conferred an ORR of 78.3% across a population of patients with CLL who previously received BTK inhibition, with doses ranging from 200 mg to 300 mg. Following the publication of these findings, the developers launched the phase 3 ROCKET-CLL trial (NCT07342478) evaluating rocbrutinib against pirtobrutinib (Jaypirca) for the treatment of relapsed/refractory CLL/SLL.

References

1. Lupeng pharmaceutical’s fourth-generation BTK inhibitor rocbrutinib approved in China for relapsed or refractory mantle cell lymphoma. News release. Lupeng Pharmaceuticals. June 4, 2026. Accessed June 5, 2026. https://tinyurl.com/38s3ar4n
2. A study of rocbrutinib in participants with relapse or refractory mantle cell lymphoma. ClinicalTrials.gov. Updated January 15, 2026. Accessed June 5, 2026. https://tinyurl.com/3us8b2hw