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Bruton's tyrosine kinase (BTK), a non-receptor tyrosine kinase, plays an important role in B-cell receptor activation.1 BCR activation results in translocation and phosphorylation of BTK. When BTK is inducted it activates phospholipase C and calcium mobilization, which results in downstream events, including proliferation, maturation, differentiation, and survival.2
Understanding the Role of BTK
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BTK Inhibitors
BTK inhibitors block the B-cell receptor signaling cascade, thus slowing or stopping the growth of abnormal and normal B-cells. This table outlines BTK inhibitors both approved by the FDA and in the pipeline.
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BTK+ Cancer Drugs Approved by the FDAa |
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Brand Name (Generic Drug Name) |
Indications |
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Brukinsa (zanubrutinib)1 |
Treatment of adults with MCL after at least 1 previous therapy |
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Treatment of adults with WM |
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Treatment of adults with R/R MZL who have received at least 1 anti–CD20-based regimen |
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Calquence (acalabrutinib)2 |
Treatment of adults with MCL who have received at least 1 prior therapy |
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Treatment of adults with CLL or SLL |
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Imbruvica (ibrutinib)3 |
Treatment of adults with MCL who have received at least 1 prior therapy |
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Treatment of adults with CLL or SLL |
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Treatment of adults with CLL or SLL with 17p deletion |
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Treatment of adults with WM |
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Treatment of adults with MZL who require systemic therapy and have received at least 1 prior anti-CD20-based therapy |
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Treatment of adult and pediatric patients aged ≥1 years with cGVHD unresponsive to ≥1 lines of systemic therapy |
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BTK+ Cancer Drugs in the Pipelineb |
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Brand Name (Generic Drug Name) |
Potential Indications |
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AS-17634 |
Being evaluated for the treatment of patients with CLL and other B-cell malignancies |
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BGB-3111 (zanubrutinib)5 |
Being evaluated for the treatment of patients with R/R CLL and/or SLL |
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Being evaluated in combination with obinutuzumab for the treatment of patients with R/R FL |
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Being evaluated in combination with rituximab for the first-line treatment of patients with MCL |
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Being evaluated in combination with venetoclax for the first-line treatment of patients with CLL and/or SLL. |
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Being evaluated in combination with lenalidomide and with or without rituximab for the treatment of patients with R/R DLBCL |
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Being evaluated in combination with BGB-10188 for the treatment of patients with R/R FL, R/R MCL, or R/R DLBCL |
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Being evaluated in combination with ME-401 for the treatment of patients with R/R CLL and/or SLL or B-cell NHL |
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Being evaluated in combination with BGB-11417 for the treatment of patients with R/R mature B-cell malignancies |
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BGB-166735 |
Being evaluated for the treatment of B-cell malignancies, MZL, FL, NHL, and WM |
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CG-806 (luxeptinib)6
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Being evaluated for the treatment of patients with R/R B-cell malignancies, including CLL and NHL, unresponsive to prior treatments |
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ICP-022 (orelabrutinib)7 |
Being evaluated for the treatment of patients with B-cell malignancies, R/R GCB DLBCL, R/R CLL and/or SLL, R/R MCL, R/R MZL, R/R WM, and R/R CNSL |
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Being evaluated for the first-line treatment of patients with CLL and/or SLL |
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LOXO-305 (pirtobrutinib)8 |
Being evaluated for the treatment of patients with CLL, SLL, MCL, and NHL |
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NX-21279 |
Being evaluated in combination with IKZF for the treatment of patients with B-cell malignancies |
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NX-59489 |
Being evaluated for the treatment of patients with B-cell malignancies unresponsive to prior treatments |
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BTK, Bruton's tyrosine kinase; cGVHD, chronic graft versus host disease; CLL, chronic lymphocytic leukemia; CNSL, central nervous system lymphoma; DLBCL, diffuse large B-cell lymphoma; FL, follicular lymphoma; GCB, germinal center B-cell like; MCL, mantle cell lymphoma; MZL, marginal zone lymphoma; NHL, non-Hodgkin’s lymphoma; R/R, relapsed and/or refreactory; SLL, small lymphocytic lymphoma; WM, Waldenström’s macroglobulinemia.
aAdapted from prescribing information.1-3 b Adapted from manufacturer websites.4-9 |
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