China-based Lepu Biopharma has presented Phase II data showing CD20 antibody-drug conjugate (ADC) MRG001 combined with BTK inhibitor orelabrutinib achieved 75% objective response rate (ORR) — including 25% complete responses (CR) — in 16 evaluable patients with relapsed or refractory diffuse large B-cell lymphoma (r/r DLBCL). The combination demonstrated 93.8% disease control rate (DCR), with 100% response in patients previously treated with CD3/CD20 bispecific antibodies (BsAb) and 87.5% response in the triple-class exposed population, including those with bulky lesions exceeding 7.5 centimetres. The safety profile remained manageable without dose-limiting toxicities, supporting a potential registration pathway for this chemotherapy-resistant B-cell malignancy.

MRG001 utilises a valine-citrulline linker conjugating a chimeric anti-CD20 antibody to a MMAE payload, with a mechanism complementary to orelabrutinib's B-cell receptor signalling inhibition without interfering with natural killer cell-mediated antibody-dependent cellular cytotoxicity (ADCC). DLBCL affects approximately 190,000 new patients annually in China, with the global market projected to exceed USD 11.5 billion by 2034.

According to PharmCube's NextBiopharm® database, Lepu's ADC pipeline covers 9 different targets. Click here to request a free trial for NextBiopharm®.