Ibrutinib repurposing : from B-cell malignancies to solid tumors

Ibrutinib (Imbruvica®, also known as PCI-32765) is a first-in-class, irreversible small-molecule inhibitorof Bruton's Tyrosine Kinase (BTK) that binds covalently to cysteine C481 within the ATP-binding pocket. Since BTK is a Tec family non-receptor tyrosine kinase that is specifically required for B-cell antigen receptor (BCR) signaling, ibrutinib was initially developed for the treatment of B-cell malignancies. Currently, it is approved for first-line treatment of chronic lymphocytic leukemia, and for the treatment of mantle-cell lymphoma and Waldenström's macroglobulinemia patients that have received at least one previous therapy