Emerging BTK Inhibitor Tested in B-Cell Malignancies

Ariela Katz
Published: Thursday, May 18, 2017
Dr Constantine S. Tam

Constantine S. Tam, MBBS

BGB-3111, a second-generation Bruton tyrosine kinase (BTK) inhibitor, is being tested in patients with refractory B-cell lymphoid malignancies in an effort to determine whether the novel oral small molecule is a viable therapeutic option and to better understand its pharmacologic properties. Investigators also are seeking to differentiate BGB-3111 from ibrutinib (Imbruvica), the first and thus far only FDA-approved BTK inhibitor.

The phase I study (NCT02343120) features a dose escalation component followed by an expansion stage in which patients will be assigned to different cohorts based on the histology of their cancer. The trial, which seeks to recruit 235 participants, is open to patients with most B-cell lymphoid malignancies. The study is enrolling patients at The University of Texas MD Anderson Cancer Center in Houston and at centers in Australia, New Zealand, and South Korea.


BGB-3111 is a potent, irreversible, and highly selective BTK inhibitor that blocks the signaling that leads to growth inhibition and cell death in malignant B cells. “The mechanism is the same as ibrutinib, but with less off-target kinase activity,” said Constantine S. Tam, MBBS, MD, a hematologist at the Peter MacCallum Cancer Centre in Melbourne, Australia, in an e-mail interview. Tam is the principal investigator for the trial.

Tam said that investigators are targeting “the diseases known to be sensitive to ibrutinib, such as chronic lymphocytic leukemia [CLL], follicular lymphoma, mantle cell lymphoma, marginal zone lymphoma, Waldenström macroglobulinemia, and activated B-cell like–diffuse large B-cell lymphoma.”

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