Orelabrutinib: First Approval.

Dysregulation of Bruton's tyrosine kinase (BTK) signalling has been linked to various B cell malignancies and autoimmune diseases. Orelabrutinib (®) is an orally administered, potent, irreversible and highly selective BTK-inhibitor being developed by InnoCare Pharma for the treatment of B cell malignancies and autoimmune diseases. In December 2020, orelabrutinib received its first approval in China for the treatment of patients with mantle cell lymphoma (MCL) or chronic lymphocytic leukaemia (CLL)/small lymphocytic lymphoma (SLL), who have received at least one treatment in the past. Clinical development of orelabrutinib for various indications is underway in the USA and China. This article summarizes the milestones in the development of orelabrutinib leading to this first approval.