title: ABT-199 (venetoclax) and BCL-2 inhibitors in clinical development.
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.
authors.affiliation: Department of Oncology, The Henan Province People's Hospital, Zhengzhou, China.
authors.forename: Shundong
authors.initials: S
authors.lastname: Cang
authors.affiliation: Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla, New York, 10595, USA.
authors.forename: Chaitanya
authors.initials: C
authors.lastname: Iragavarapu
authors.affiliation: Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla, New York, 10595, USA.
authors.forename: John
authors.initials: J
authors.lastname: Savooji
authors.affiliation: Henan Cancer Hospital and the Affiliated Cancer Hospital of Zhengzhou University, Zhengzhou, China.
authors.forename: Yongping
authors.initials: Y
authors.lastname: Song
authors.affiliation: Henan Cancer Hospital and the Affiliated Cancer Hospital of Zhengzhou University, Zhengzhou, China. delong_liu@nymc.edu.
authors.forename: Delong
authors.initials: D
authors.lastname: Liu
mesh_terms: D000077329:Agammaglobulinaemia Tyrosine Kinase; D000970:Antineoplastic Agents / Q000494:pharmacology* / Q000627:therapeutic use; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007945:Leukemia, Lymphoid / Q000188:drug therapy* / Q000378:metabolism; D019869:Phosphatidylinositol 3-Kinases / Q000378:metabolism; D011505:Protein-Tyrosine Kinases / Q000187:drug effects*; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors / Q000378:metabolism*; D013449:Sulfonamides / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000970:Antineoplastic Agents; C000595707:BCL2 protein, human; D019086:Bridged Bicyclo Compounds, Heterocyclic; D019253:Proto-Oncogene Proteins c-bcl-2; D013449:Sulfonamides; D019869:Phosphatidylinositol 3-Kinases; D011505:Protein-Tyrosine Kinases; D000077329:Agammaglobulinaemia Tyrosine Kinase; C579720:venetoclax