Rocbrutinib: First Approval.

Rocbrutinib (; LP-168) is a fourth generation Bruton's tyrosine kinase (BTK) inhibitor with both covalent and non-covalent modes of binding, which allow it to inhibit both wildtype as well as mutant variants of BTK. It is being developed by Lupeng Pharmaceuticals primarily as a treatment for patients with B-cell malignancies. Rocbrutinib received its first approval in June 2026 in China for use in adult patients with mantle cell lymphoma (MCL) that is relapsed or refractory to BTK inhibitors, and who have received ≥ 2 systemic therapies (including BTK inhibitors). This article summarizes the milestones in the development of rocbrutinib leading to its first approval in this indication.