Abstract
Burton’s tyrosine kinase (BTK) is a nonreceptor/cytoplasmic tyrosine kinase that modulates the downstream signaling pathway of B-cell receptor (BCR) [1]. Aberrant BCR signaling including upregulation of tyrosine kinases i.e. Lyn, Syk and Btk is a common feature in lymphoid malignancies such as Chronic Lymphocytic Leukemia (CLL), Mantle Cell Lymphoma (MCL) and other Non-Hodgkin’s Lymphoma (NHL) [2]. Therefore, inhibition of tyrosine kinases is an attractive treatment option in these lymphoid malignancies. Ibrutinib (formerly PCI-32765) is a first-in-human, orally bioavailable small molecule inhibitor of BTK that has shown potent clinical activity in majority of CD20 positive B-cell malignancies. Based on high response rate, tolerability and safety data, Imbruvica/Ibrutinib has recently been approved by Food and Drug Administration (FDA) for the treatment of MCL (in November 2013) and CLL (in February 2014) with at least one prior therapy. It is now under evaluation as front line therapy in other subtypes of NHL and is explored for combination with other drugs.
Highlights
Aberrant B-cell receptor (BCR) signaling including upregulation of tyrosine kinases i.e. Lyn, Syk and Btk is a common feature in lymphoid malignancies such as Chronic Lymphocytic Leukemia (CLL), Mantle Cell Lymphoma (MCL) and other Non-Hodgkin’s Lymphoma (NHL) [2]
Based on high response rate, tolerability and safety data, Imbruvica/Ibrutinib has recently been approved by Food and Drug Administration (FDA) for the treatment of MCL and CLL with at least one prior therapy
Treatment of ibrutinib is under evaluation for other tumors such as Follicular lymphoma (FL), diffuse large B-cell lymphoma (DLBCL), and Multiple myeloma (MM)
Summary
Aberrant BCR signaling including upregulation of tyrosine kinases i.e. Lyn, Syk and Btk is a common feature in lymphoid malignancies such as Chronic Lymphocytic Leukemia (CLL), Mantle Cell Lymphoma (MCL) and other Non-Hodgkin’s Lymphoma (NHL) [2]. Updated results presented in American society of hematology (Ash) meeting 2014 demonstrated the durability of response and sustained single agent activity of ibrutinib in an international multicenter phase II study of refractory MCL [4]. Results from other recent studies supports ibrutinib as first line or second treatment option in refractory cases [6].
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