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

被引:217
|
作者
Cang, Shundong [1 ]
Iragavarapu, Chaitanya [2 ,3 ]
Savooji, John [2 ,3 ]
Song, Yongping [4 ,5 ]
Liu, Delong [4 ,5 ]
机构
[1] Henan Prov Peoples Hosp, Dept Oncol, Zhengzhou 450052, Peoples R China
[2] Westchester Cty Med Ctr, Dept Med, Valhalla, NY 10595 USA
[3] New York Med Coll, Valhalla, NY 10595 USA
[4] Zhengzhou Univ, Henan Canc Hosp, Zhengzhou 450052, Peoples R China
[5] Zhengzhou Univ, Affiliated Canc Hosp, Zhengzhou 450052, Peoples R China
来源
关键词
CHRONIC LYMPHOCYTIC-LEUKEMIA; ACUTE LYMPHOBLASTIC-LEUKEMIA; IN-VIVO EFFICACY; BISPECIFIC ANTI-CD30/CD16A ANTIBODY; ACUTE MYELOID-LEUKEMIA; BH3 MIMETIC ABT-263; FAMILY PROTEINS; CELL-DEATH; HEMATOLOGICAL MALIGNANCIES; NUCLEAR EXPORT;
D O I
10.1186/s13045-015-0224-3
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
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.
引用
收藏
页数:8
相关论文
共 50 条
  • [1] ABT-199 (venetoclax) and BCL-2 inhibitors in clinical development
    Shundong Cang
    Chaitanya Iragavarapu
    John Savooji
    Yongping Song
    Delong Liu
    Journal of Hematology & Oncology, 8
  • [2] Quantitative assessment of BCL-2: BIM complexes as a pharmacodynamic marker for venetoclax (ABT-199)
    Jin, Sha
    Tapang, Paul
    Osterling, Donald J.
    Gao, Wenqing
    Albert, Daniel H.
    Souers, Andrew J.
    Leverson, Joel D.
    Phillips, Darren C.
    Chen, Jun
    CANCER RESEARCH, 2015, 75
  • [3] ABT-199: Taking Dead Aim at BCL-2
    Davids, Matthew S.
    Letai, Anthony
    CANCER CELL, 2013, 23 (02) : 139 - 141
  • [4] Correlative biomarkers of clinical activity of the BCL-2 inhibitor, venetoclax (ABT-199/GDC-0199), in acute myeloid leukemia patients
    Popovic, Relja
    Daver, Naval
    Ruvolo, Vivian
    Chen, Ken
    Wang, Zixing
    Huang, Xin
    Mabry, Mack
    Potluri, Jalaja
    McKeegan, Evelyn
    Konopleva, Marina
    Chyla, Brenda J.
    CANCER RESEARCH, 2016, 76
  • [5] The Role of Lymphatic Transport on the Systemic Bioavailability of the Bcl-2 Protein Family Inhibitors Navitoclax (ABT-263) and ABT-199
    Choo, Edna F.
    Boggs, Jason
    Zhu, Chunqiang
    Lubach, Joseph W.
    Catron, Nathaniel D.
    Jenkins, Gary
    Souers, Andrew J.
    Voorman, Richard
    DRUG METABOLISM AND DISPOSITION, 2014, 42 (02) : 207 - 212
  • [6] The BCL-2 inhibitor ABT-199/venetoclax synergizes with proteasome inhibition via transactivation of the MCL-1 antagonist NOXA
    Weller, Sandra
    Toenniessen, Astrid
    Schaefer, Benjamin
    Beigl, Tobias
    Muenchow, Alina
    Bopple, Kathrin
    Hofmann, Ute
    Gillissen, Bernhard F.
    Aulitzky, Walter E.
    Kopp, Hans-Georg
    Essmann, Frank
    CELL DEATH DISCOVERY, 2022, 8 (01)
  • [7] The BCL-2 inhibitor ABT-199/venetoclax synergizes with proteasome inhibition via transactivation of the MCL-1 antagonist NOXA
    Sandra Weller
    Astrid Toennießen
    Benjamin Schaefer
    Tobias Beigl
    Alina Muenchow
    Kathrin Böpple
    Ute Hofmann
    Bernhard F. Gillissen
    Walter E. Aulitzky
    Hans-Georg Kopp
    Frank Essmann
    Cell Death Discovery, 8
  • [8] Remarkable early clinical activity with the Bcl-2 selective inhibitor ABT-199: Proving the concept.
    Humerickhouse, Rod
    CANCER RESEARCH, 2013, 73 (08)
  • [9] Dexamethasone Synergizes with ABT-199 through the Induction of Bim and Bcl-2 Dependence in Myeloma
    Matulis, Shannon
    Nooka, Ajay K.
    Von Hollen, Hayley
    Kaufman, Jonathan L.
    Lonial, Sagar
    Boise, Lawrence H.
    BLOOD, 2014, 124 (21)
  • [10] The potential of venetoclax (ABT-199) in chronic lymphocytic leukemia
    Itchaki, Gilad
    Brown, Jennifer R.
    THERAPEUTIC ADVANCES IN HEMATOLOGY, 2016, 7 (05) : 270 - 287