The Bruton's Tyrosine Kinase (BTK) Inhibitor ARQ 531 Effectively Inhibits Wild Type and C481S Mutant BTK and Is Superior to Ibrutinib in a Mouse Model of Chronic Lymphocytic Leukemia

被引：7
|
作者：
Reiff, Sean D. [1 ]
Mantel, Rose [1 ]
Smith, Lisa L. [1 ]
McWhorter, Samantha [1 ]
Goettl, Virginia M. [1 ]
Johnson, Amy J. [2 ]
Eathiraj, Sudharsan [3 ]
Abbadessa, Giovanni [3 ]
Schwartz, Brian [3 ]
Byrd, John C. [1 ]
Woyach, Jennifer A. [1 ]
机构：
[1] Ohio State Univ, Div Hematol, Dept Internal Med, Columbus, OH USA
[2] Ohio State Univ, Div Hematol, Columbus, OH USA
[3] ArQule Inc, Burlington, MA USA
来源：
BLOOD | 2016年 / 128卷 / 22期
关键词：
D O I：
10.1182/blood.V128.22.3232.3232
中图分类号：
R5 [内科学];
学科分类号：
1002 ; 100201 ;
摘要：
3232
引用
收藏
页数：4
相关论文
共 50 条
  • [1] ZYBT1, a potent, irreversible Bruton's Tyrosine Kinase (BTK) inhibitor that inhibits the C481S BTK with profound efficacy against arthritis and cancer
    Ghoshdastidar, Krishnarup
    Patel, Hoshang
    Bhayani, Hitesh
    Patel, Ankit
    Thakkar, Kinjal
    Patel, Dinesh
    Sharma, Manoranjan
    Singh, Jaideep
    Mohapatra, Jogeswar
    Chatterjee, Abhijit
    Patel, Dipam
    Bahekar, Rajesh
    Sharma, Rajiv
    Gupta, Lakshmikant
    Patel, Nirmal
    Giri, Poonam
    Srinivas, Nuggehally R.
    Jain, Mukul
    Bandyopadhyay, Debdutta
    Patel, Pankaj R.
    Desai, Ranjit C.
    [J]. PHARMACOLOGY RESEARCH & PERSPECTIVES, 2020, 8 (04):
  • [2] Development of novel, selective, reversible inhibitors equipotent against wild-type and C481S Bruton's tyrosine kinase (BTK)
    Guisot, Nicolas E. S.
    Walker, Victoria
    Best, Stuart A.
    Abet, Valentina
    Chappell, Rose
    Emmerich, Juliette
    Ho, Kelvin
    Kelly, James R.
    Lyons, Kristina
    Muller, Melanie
    Refuerzo, Julienne
    Sargent, Louise
    Talab, Fatima
    Waldron, Madelene
    Bingham, Matilda
    Campbell, Mary-Ann
    Phillips, Caroline
    Armer, Richard
    [J]. CANCER RESEARCH, 2016, 76
  • [3] Development of novel Btk inhibitor, CB988 targering ibrutinib-resistant Btk C481S mutant
    Kawahata, Wataru
    Asami, Tokiko
    Irie, Takayuki
    Iwata, Yasuhiro
    Kiyoi, Takao
    Sawa, Masaaki
    [J]. CANCER RESEARCH, 2017, 77
  • [4] Evaluation of the novel Bruton's tyrosine kinase (BTK) inhibitor GDC-0853 in chronic lymphocytic leukemia (CLL) with wild type or C4815 mutated BTK.
    Reiff, Sean David
    Guinn, Daphne
    Mantel, Rose
    Smith, Lisa
    Cheney, Carolyn
    Johnson, Amy J.
    Byrd, John C.
    Woyach, Jennifer Ann
    [J]. JOURNAL OF CLINICAL ONCOLOGY, 2016, 34 (15)
  • [5] Next-generation Bruton's Tyrosine Kinase (BTK) Inhibitors Potentially Targeting BTK C481S Mutation- Recent Developments and Perspectives
    Das, Debasis
    Wang, Jingbing
    Hong, Jian
    [J]. CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2022, 22 (20) : 1674 - 1691
  • [6] SNS-062 demonstrates efficacy in chronic lymphocytic leukemia in vitro and inhibits C481S mutated Bruton tyrosine kinase
    Fabian, Catherine A.
    Reiff, Sean D.
    Guinn, Daphne
    Neuman, Linda
    Fox, Judith A.
    Wilson, Wendy
    Byrd, John C.
    Woyach, Jennifer A.
    Johnson, Amy J.
    [J]. CANCER RESEARCH, 2017, 77
  • [7] The effect of Bruton ' s tyrosine kinase (BTK) inhibitor in the eosinophilic asthma model of mouse
    Choi, Yeji
    Kim, Seo-Hee
    Shin, Seung Jun
    Park, Hae-Sim
    Shin, Yoo Seob
    [J]. INTERNATIONAL IMMUNOPHARMACOLOGY, 2024, 132
  • [8] Bruton's tyrosine kinase (BTK) function is important to the development and expansion of chronic lymphocytic leukemia (CLL)
    Woyach, Jennifer A.
    Bojnik, Engin
    Ruppert, Amy S.
    Stefanovski, Matthew R.
    Goettl, Virginia M.
    Smucker, Kelly A.
    Smith, Lisa L.
    Dubovsky, Jason A.
    Towns, William H.
    MacMurray, Jessica
    Harrington, Bonnie K.
    Davis, Melanie E.
    Gobessi, Stefania
    Laurenti, Luca
    Chang, Betty Y.
    Buggy, Joseph J.
    Efremov, Dimitar G.
    Byrd, John C.
    Johnson, Amy J.
    [J]. BLOOD, 2014, 123 (08) : 1207 - 1213
  • [9] CB1763, a highly selective, novel non-covalent BTK inhibitor, targeting ibrutinib-resistant BTK C481S mutant
    Asami, Tokiko
    Kawahata, Wataru
    Kashimoto, Shigeki
    Sawa, Masaaki
    [J]. MOLECULAR CANCER THERAPEUTICS, 2018, 17 (01)
  • [10] REDX08608, a Novel, Potent and Selective, Reversible BTK Inhibitor with Efficacy and Equivalent Potency Against Wild-Type and Mutant C481S BTK
    Guisot, Nicolas E. S.
    Best, Stuart A.
    Wright, Victoria
    Thomason, Andrew
    Woyach, Jennifer A.
    Mantel, Rose
    McClanahan, Fabienne
    Abet, Valentina
    Castagna, Diana
    Cousin, Peggy
    Emmerich, Juliette
    Ho, Kelvin
    Kelly, James Russell
    King-Tours, James
    Lyons, Kristina
    Muller, Melanie
    Refuerzo, Julienne
    Sargent, Louise
    Talab, Fatima
    Bingham, Matilda
    Phillips, Caroline
    Armer, Richard
    [J]. BLOOD, 2016, 128 (22)
12345