Bruton's tyrosine kinase (Btk) is a member of the Tec family of cytoplasmic protein tyrosine kinases (PTK). BTK enzyme is encoded by the BTK gene. It is expressed in the cells of all hematopoietic lineages except for T and plasma cells. The protein kinase BTK is implicated in the development, differentiation, and activation of B cells through its role in the BCR and TLR signaling cascades. Clinical evidence indicates loss-of-function mutations in BTK result in X-linked agammaglobulinemia and cancers. Thus BTK has emerged as a novel anticancer target for the treatment of B-cell lymphomas and leukemias.
Currently, marketed anti-BTK drug is Imbruvica (ibrutinib). It is indicated for the treatment of graft versus host disease, hematological malignancies, and Non-Hodgkin’s lymphoma.
Pipeline activity of BTK inhibitors is quite dynamic. Several BTK inhibitors candidates more than 20 are in late stage clinical trials and are expected to achieve the regulatory approval in the near future which includes GDC-0834, GDC-0834, RN486, TP-4207, PCI-45261, BGB-3111, PCI 45292, ABBV-105, PRN1008, HCI-1401, EBI-1367, EBI-1266, SNS-062, RG7845, and GDC-0853. Preclinical and early clinical results indicate that these inhibitors are useful for the treatment of lymphomas and leukemias. The companies which are involved in the development of BTK inhibitors are Gilead, Roche, AbbVie, J&J, Eli Lilly, AstraZeneca, and Biogen.
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