Guangzhou Lupeng/Newave Pharmaceutical Inc. Enrolled the First Patient in the Global Phase 3 ROCKET-CLL Trial Evaluating Rocbrutinib (LP-168) vs. Pirtobrutinib in R/R CLL/SLL

Head-to-Head Study Highlights Rocbrutinib as the World's First Fourth-Generation Dual Covalent and Non-Covalent BTK Inhibitor Designed to Overcome Resistance Mutations

GUANGZHOU, China and SAN FRANCISCO, May 21, 2026 /PRNewswire/ -- Lupeng Pharmaceutical Ltd, a global clinical-stage biopharmaceutical company, announced the enrollment of the first patient in its global Phase 3 ROCKET-CLL trial (NCT07342478). Newave Pharmaceutical Inc. (hereinafter referred to as "Newave") and Guangzhou Lupeng Pharmaceutical Co., Ltd. (hereinafter referred to as "Guangzhou Lupeng") are both wholly-owned subsidiaries of Lupeng Pharmaceutical Ltd.

This head-to-head study evaluates the efficacy and safety of rocbrutinib (LP-168), a novel oral fourth-generation BTK inhibitor, against pirtobrutinib in patients with relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (R/R CLL/SLL) who have received prior therapy with a covalent BTK inhibitor (cBTKi). Existing BTK inhibitors face resistance challenges, underscoring the need for next-generation therapies that can overcome resistance.

The first study site of the ROCKET-CLL Phase 3 trial (LP-168-US-CLL301; NCT07342478) was activated on April 28, 2026, at OptumCare Cancer Care Center in Las Vegas, Nevada, under the leadership of Dr. Russell Gollard. On May 20, 2026, Dr. Gollard and his team enrolled the first patient, marking a key milestone in the global development of rocbrutinib (LP-168), an investigational BTK inhibitor being evaluated in patients with relapsed or refractory chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) who have progressed after prior covalent BTK inhibitor therapy.

ROCKET-CLL is a randomized, open-label, multicenter Phase 3 study expected to enroll approximately 306 adult patients worldwide. The study is co-led by Drs. Jennifer Woyach at Ohio State University and John Byrd at the University of Pittsburgh Medical Center, with participation by leading academic centers in the US, EU, China, and Australia.

Participants are randomized 1:1 to receive once-daily oral rocbrutinib (200 mg) or pirtobrutinib (200 mg). The primary endpoint is progression-free survival (PFS), and secondary endpoints include overall survival (OS, key secondary endpoint), overall response rate (ORR), and duration of response (DOR), time to next treatment (TTNT), event-free survival (EFS), safety and tolerability. Exploratory endpoints include patient-reported outcomes, health-related quality of life, and biomarker analyses to further characterize treatment response and resistance mechanisms.

Enrollment is expected to be completed by early Q4 2027, with an interim analysis planned for 2029.

"ROCKET-CLL marks an important step in validating rocbrutinib's differentiated dual covalent and non-covalent mechanism," said Jennifer Woyach, MD, Bertha Bouroncle MD and Andrew Pereny Chair of Medicine at The Ohio State University  College of Medicine. "Based on clinical findings from the US Phase 1 study, among CLL patients previously treated with cBTKi and/or ncBTKi, patients treated at dose levels of 200 mg/day or higher, the overall response rate was 78.3%, with an estimated median progression-free survival of 28.1 months for doses of at least 100 mg/daily" ^[1].

About Rocbrutinib (LP-168)

Rocbrutinib (LP-168) is a novel, orally available, highly selective fourth-generation Bruton's tyrosine kinase (BTK) inhibitor developed on Lupeng's proprietary BeyondX platform. It is engineered to combine covalent (irreversible) and non-covalent (reversible) binding, enabling inhibition of both wild-type and C481-mutant BTK and overcoming multiple resistance mutations, including C481X, T474X, and L528W. This differentiated mechanism positions rocbrutinib as a potential best-in-class BTK inhibitor in the post-BTKi setting. Rocbrutinib has demonstrated a favorable safety profile and durable clinical responses across multiple B-cell malignancies.

In China, rocbrutinib's New Drug Application (NDA) for relapsed or refractory mantle cell lymphoma (R/R MCL) has been accepted and is under Priority Review by the Center for Drug Evaluation (CDE) of the National Medical Products Administration (NMPA). Additionally, rocbrutinib has received Breakthrough Therapy Designation (BTD) in China for 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, making it the first BTK inhibitor in China—and the only one globally—to receive such designation in this indication.

About Lupeng Pharmaceutical Ltd

Newave Pharmaceutical Inc. (hereinafter referred to as "Newave") and Guangzhou Lupeng Pharmaceutical Co., Ltd. (hereinafter referred to as "Guangzhou Lupeng") are both wholly-owned subsidiaries of Lupeng Pharmaceutical Ltd. Lupeng Pharmaceutical Ltd is a global clinical-stage biopharmaceutical company dedicated to discovering and developing next-generation therapies for hematological malignancies and autoimmune diseases. Leveraging its proprietary BeyondX medicinal chemistry platform, the company is advancing a robust pipeline targeting clinically validated pathways, including BTK, Bcl-2, and Bcl-xL. With a strong commitment to innovation and global development, Lupeng aims to deliver transformative therapies that address unmet medical needs worldwide.

For more information, please visit www.lupengbio.com.

Forward-Looking Statements

This press release contains forward-looking statements, including those regarding clinical development timelines, regulatory progress, and the potential therapeutic benefits of rocbrutinib. These statements are subject to risks and uncertainties that could cause actual results to differ materially.

Reference:

1. Updates of R/R CLL with prior exposure to Bruton's tyrosine kinase (BTK) inhibitor and/or bcl-2 inhibitor in the Phase 1 trial of LP-168 (rocbrutinib), a novel COVALENT and non-COVALENT BTK inhibitor. ASH 2025. abs25-2620

SOURCE Lupeng Pharmaceutical Ltd