News & Events
Lupeng Pharmaceutical, a global leading platform-based emerging biopharmaceutical company focused on developing innovative medicines for the treatment of malignancies and autoimmune diseases based on its proprietary BeyondX® oral drug chemistry platform, recently achieved another significant milestone: the global Phase III head-to-head clinical trial (ROCKET-CLL Study) of its internally developed, first and only dual covalent and non-covalent BTK inhibitor Rocbrutinib (LP-168) for the treatment of relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (R/R CLL/SLL) has been registered on ClinicalTrials.gov (Identifier: NCT07342478). This head-to-head study is designed to compare the efficacy and safety of Rocbrutinib versus the approved non-covalent BTK inhibitor Pirtobrutinib in patients with R/R CLL/SLL who were previously treated with a covalent BTK inhibitor (cBTKi).
The ROCKET-CLL study is a randomized, open-label, multicenter, global Phase III clinical trial planning to enroll approximately 306 eligible adult participants worldwide. Participants will be randomized in a 1:1 ratio to receive either Rocbrutinib (200 mg) orally once daily or Pirtobrutinib (200 mg) orally once daily, administered continuously in 28-day cycles until disease progression, unacceptable toxicity, withdrawal of consent, or other discontinuation criteria are met. Randomization will be stratified by the presence of del(17p)/TP53 mutation, reason for discontinuation of prior cBTKi therapy (toxicity or disease progression), the prior exposure to a BCL-2 inhibitor and the region (United States/China/rest of world).
The primary endpoint of the study is progression-free survival (PFS) as assessed by an Independent Review Committee (IRC) using the iwCLL 2018 criteria for CLL and the Lugano 2014 criteria for SLL. The key secondary efficacy endpoints include overall survival (OS), overall response rate (ORR), duration of response (DOR), time to next treatment (TTNT) and event-free survival (EFS). Additional secondary objectives include characterization of the safety and tolerability of Rocbrutinib relative to Pirtobrutinib. Exploratory objectives include evaluation of patient-reported outcomes and health-related quality of life, as well as biomarker assessments aimed at exploring including mechanisms of response and resistance.
Dr. Fenlai Tan, Co-founder, Chairman and CEO of Lupeng Pharmaceutical, stated: "The initiation of the global head-to-head ROCKET-CLL Phase III study is a significant milestone in the global development of Rocbrutinib. It demonstrates our confidence in Rocbrutinib's unique dual covalent and non-covalent mechanism and significant clinical potential, as well as our commitment to addressing the urgent unmet medical need for patients who have progressed on prior cBTKi therapy. We also believe this study will lay a solid foundation for Rocbrutinib's subsequent entry into first-line treatment for CLL indication research. We look forward to the successful advancement of this study to bring new hope to patients with R/R CLL/SLL worldwide."
About Rocbrutinib
Rocbrutinib (LP-168) is developed through Lupeng Pharmaceutical's proprietary BeyondX® oral medicinal chemistry platform. As the world's first and only dual covalent and non-covalent BTK inhibitor, Rocbrutinib can not only covalently inhibit wild-type BTK, but also non-covalently inhibit C481-mutated BTK. Therefore, it can overcome various drug resistance mutations to the first-, second-, and third-generation BTK inhibitors, such as C481X, T474X, L528W, etc. It has demonstrated excellent safety and efficacy profiles in clinical settings, positioning it as a potential Best-in-Class (BIC) BTK inhibitor. The ongoing clinical development of Rocbrutinib primarily focuses on various mature B-cell malignancies. Notably, for the treatment of relapsed or refractory mantle cell lymphoma (R/R MCL) in patients previously treated with BTK inhibitor, Rocbrutinib has shown outstanding efficacy. A pivotal registrational clinical study has been completed, a New Drug Application (NDA) has been formally accepted, and it has been included in the priority review list in China. Furthermore, in relapsed or refractory non-germinal center B-cell-like diffuse large B-cell lymphoma (R/R non-GCB DLBCL), Rocbrutinib has demonstrated particularly remarkable efficacy. In May 2024, it was granted Breakthrough Therapy Designation (BTD) by the Center for Drug Evaluation (CDE) in China, making it the first BTK inhibitor in China to receive BTD for DLBCL and the only BTK inhibitor globally to have received BTD recognition in DLBCL. The pivotal registrational Phase II clinical study for the R/R non-GCB DLBCL indication has been approved by the CDE and was officially initiated in November 2025 in China. Additionally, the Phase III head-to-head clinical study (PRIME study) comparing Rocbrutinib versus approved covalent BTK inhibitors (Ibrutinib, Acalabrutinib, Zanubrutinib, Orelabrutinib) in R/R MCL has been initiated, and the aforementioned global Phase III head-to-head clinical study (ROCKET-CLL study) comparing Rocbrutinib versus Pirtobrutinib in R/R CLL/SLL is now underway.