The potential of venetoclax (ABT-199) in chronic lymphocytic leukemia-Reference-Cited by-同舟云学术

The potential of venetoclax (ABT-199) in chronic lymphocytic leukemia

Published:2016-07-31 Issue:5 Volume:7 Page:270-287
ISSN:2040-6207
Container-title:Therapeutic Advances in Hematology
language:en
Short-container-title:Therapeutic Advances in Hematology

Author:

Itchaki Gilad¹,Brown Jennifer R.²

Affiliation:

1. Beilinson Hospital, Rabin Medical Center, Petah Tikva, Israel

2. Dana-Farber Cancer Institute, 450 Brookline Avenue, Boston, MA 02215, USA

Abstract

Venetoclax (VEN, ABT-199/GDC-0199) is an orally bioavailable BH3-mimetic that specifically inhibits the anti-apoptotic B-cell lymphoma/leukemia 2 (BCL2) protein. Although BCL2 overexpression is not genetically driven in chronic lymphocytic leukemia (CLL), it is nearly universal and represents a highly important and prevalent mechanism of apoptosis evasion, making it an attractive therapeutic target. This review summarizes the role of BCL2 in CLL pathogenesis, the development path targeting its inhibition prior to VEN, and the preclinical and clinical data regarding the effectiveness and safety of VEN. We further strive to contextualize VEN in the current CLL treatment landscape and discuss potential mechanisms of resistance.

Publisher

SAGE Publications

Subject

Hematology

Link

http://journals.sagepub.com/doi/pdf/10.1177/2040620716655350

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