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Review
. 2015 Nov 20:8:129.
doi: 10.1186/s13045-015-0224-3.

ABT-199 (venetoclax) and BCL-2 inhibitors in clinical development

Shundong Cang  1 , Chaitanya Iragavarapu  2 , John Savooji  2 , Yongping Song  3 , Delong Liu  4
Affiliations
Review

ABT-199 (venetoclax) and BCL-2 inhibitors in clinical development

Shundong Cang et al. J Hematol Oncol. .

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.

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Figures

Fig. 1
Fig. 1
Structures of BCL-2 family proteins. According to the BH domains, the BCL-2 family proteins can be categorized into three subsets. BH4-containing BCL-2 and related BCL-XL, BCL-w, MCL-1, A1(BFL-1), and Boo are anti-apoptotic proteins. The remaining two subsets (BAX and Bik subgroups) do not have a BH4 domain and are pro-apoptotic proteins
See this image and copyright information in PMC

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