Abstract
With the advent of new agents targeting CD20, Bruton’s tyrosine kinase, and phosphoinositol-3 kinase for chronic lymphoid leukemia (CLL), more treatment options exist than ever before. B-cell lymphoma-2 (BCL-2) plays a major role in cellular apoptosis and is a druggable target. Small molecule inhibitors of BCL-2 are in active clinical studies. ABT-199 (venetoclax, RG7601, GDC-0199) has been granted breakthrough designation by FDA for relapsed or refractory CLL with 17p deletion. In this review, we summarized the latest clinical development of ABT-199/venetoclax and other novel agents targeting the BCL-2 proteins.
Highlights
Tyrosine kinase inhibitors have ushered cancer treatment to the era of targeted therapy [1,2,3,4,5,6,7]
It has been well documented that B-cell lymphoma-2 (BCL-2) plays a major role in cellular apoptosis and is a druggable target
This review focused on the current clinical development of a highly effective class of small molecule BCL-2 inhibitors, including ABT-199/venetoclax
Summary
Tyrosine kinase inhibitors have ushered cancer treatment to the era of targeted therapy [1,2,3,4,5,6,7]. The first trial to evaluate ABT-263/navitoclax studied two different dosing schedules in 55 patients with relapsed/refractory (R/R) lymphoid malignancies [59]. Another phase I trial evaluated intermittent and continuous dosing in 29 patients with relapsed/refractory CLL [60]. ABT-199 was studied in combinations with tyrosine kinase inhibitors (TKIs), including imatinib, nilotinib, dasatinib, or ponatinib, in cells from six patients with blast-crisis chronic myeloid leukemia (CML) [70].
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