Rocbrutinib

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 . 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 21% more press release views with Request a Demo

> 2026年5月19日，一项针对复发难治性成熟B细胞肿瘤的新药临床试验悄然启动。广州麓鹏制药有限公司登记了评估口服BTK抑制剂洛布替尼（LP-168片）联合BCL-2抑制剂乐托克拉的Ib/II期研究（登记号：CTR20261866），目标入组92人，目前状态为进行中（尚未招募）。 在现有疗法面临耐药瓶颈的背景下，这一组合疗法的探索为血液肿瘤领域带来了新的变量。 ## 试验启动：关键设计与未满足需求 本次临床试验旨在评估LP-168联合乐托克拉在成熟B细胞肿瘤患者中的**安全性、耐受性、药代动力学及初步疗效**。研究分为Ib期和II期两个阶段：Ib期重点探索剂量与安全性，为后续阶段确定推荐剂量；II期则将初步验证该联合方案的抗肿瘤活性。 试验面向的**复发或难治性患者群体**，正是当前临床治疗中挑战最大的部分，常规治疗后选项有限，生存质量亟待改善。 ## 疾病背景：B细胞肿瘤的治疗困局 成熟B细胞肿瘤是一组起源于成熟B淋巴细胞的血液系统恶性肿瘤，包括弥漫大B细胞淋巴瘤、滤泡性淋巴瘤等多种常见类型。尽管靶向药、化疗等手段不断进步，但耐药与复发仍是拉低患者长期生存率的关键因素。开发能克服耐药、作用机制新颖的药物，成为领域内明确的研发方向。 ## 行业视角：机制创新驱动研发竞赛 LP-168的临床推进并非孤立事件，它置身于一个创新药研发高度活跃的生态中。当前，具有明确作用机制、旨在解决核心临床未满足需求的差异化产品，正成为全球药企竞逐的焦点。 - 在减重与代谢领域，博瑞医药的**BGM0504注射液**作为GLP-1/GIP双靶点激动剂，其III期临床数据不仅显示了显著的减重效果，更在**血压、血脂、骨密度等多重代谢指标**上展现出综合调节潜力，提示其从“减重药”向“代谢综合管理候选者”演变的可能。 - 同样，和铂医药利用**人工智能平台Hu-mAtrIx™** 开发的抗体药物**LET003**，靶向ACVR2A/2B通路，临床前研究显示其与GLP-1药物联用可**显著增强减脂并保护瘦体重**，体现了通过精准靶点选择和分子工程实现“同类最佳”潜力的研发策略。 > 这些案例共同印证了当下的研发逻辑：深厚的科学洞察与前沿技术平台相结合，催生出能直面复杂疾病机制的新一代疗法。 ## LP-168的潜力与未来展望 作为一款口服BTK抑制剂，LP-168联合BCL-2抑制剂的方案，理论上旨在通过双通路抑制协同杀伤肿瘤细胞，可能为克服单药耐药提供新思路。其**口服给药**的便利性，若最终证实有效，有望提升患者治疗体验。 尽管LP-168的临床数据尚待揭晓，但其临床启动本身，已折射出中国本土药企在血液肿瘤这一高技术壁垒领域持续深入的研发布局。从靶点选择到联合用药探索，每一步都指向对患者实际生存获益的追求。 未来，随着Ib/II期试验的推进，该疗法的安全性与初步疗效轮廓将逐渐清晰，为后续确证性研究奠定基础。在创新药研发的马拉松中，每一个扎实的临床节点，都是向终点迈出的关键一步。