Vecabrutinib is a potentBTK inhibitor, with IC50s of 4.6 nM and 1.1 nM for WTBTK and C481S BTK, respectively, and also inhibits ITK activity (IC50, 24 nM).
Bruton’s tyrosine kinase (BTK), a member of the Tec family of tyrosine kinases and expressed in B cells, macrophages, and monocytes but not in T cells, plays a crucial role in signaling through the B cell receptor (BCR) and the Fcγ receptor (FcγR) in B cells and myeloid cells, respectively [1]. Vecabrutinib is a potent, noncovalent BTK and ITK (interleukin-2-inducible kinase) inhibitor, with Kd of 0.3 nM and 2.2 nM, respectively. It inhibits WT and C481S BTK with IC50s of 2.9 nM and 4.4 nM, respectively. Vecabrutinib decreases viability of primary CLL cells in the presence of HS5 stromal protection by 5.5%. Vecabrutinib has good oral bioavailability in rat and dog (%F ≥ 40%) and a terminal half-life of 5 to 6 hours and is well tolerated with continuous drug levels.
Chronic Lymphocytic Leukemia
... 展开 >> Small Lymphocytic Lymphoma
Lymphoplasmacytoid Lymphoma
Mantle-Cell Lymphoma
Waldenstrom Macroglobulinemia
Diffuse Large B Cell Lymphoma
Follicular Lymphoma 收起 <<
Phase 1
Phase 2
Recruiting
June 30, 2021
United States, California
... 展开 >>
University of California Irvine Medical Center
Recruiting
Orange, California, United States, 92868-3201
Contact: General Contact 877-827-8839 ucstudy@uci.edu
UC San Diego Moores Cancer Center
Recruiting
San Diego, California, United States, 92093
Contact: Barbara Ivers 858-822-6281 bivers@ucsd.edu
United States, Florida
Moffitt Cancer Center and Research Institute
Recruiting
Tampa, Florida, United States, 33612
Contact: Natalie Miller 813-745-2591 Natalie.Miller@moffitt.org
United States, Massachusetts
Dana-Farber Cancer Institute
Recruiting
Boston, Massachusetts, United States, 02215
Contact: Conner Shaughnessy 617-582-8437 Conner_Shaughnessy@dfci.harvard.edu
United States, New York
Memorial Sloan Kettering Cancer Center
Recruiting
New York, New York, United States, 10065
Contact: Isaac Deonarine 646-888-1319 deonarii@mskcc.org
Weill Cornell Medicine
Recruiting
New York, New York, United States, 10065
Contact: Jessica Harper 646-962-9414 jah2070@med.cornell.edu
United States, Texas
MD Anderson Cancer Center
Recruiting
Houston, Texas, United States, 77030
Contact: Chongjuan Wei 713-792-3530 cwei@mdanderson.org
United States, Washington
Swedish Cancer Institute
Recruiting
Seattle, Washington, United States, 98104
Contact: Ngan Trinh 206-215-2363 Ngan.Trinh@Swedish.org 收起 <<
Chronic Lymphocytic Leukemia
... 展开 >> Small Lymphocytic Lymphoma
Lymphoplasmacytoid Lymphoma
Mantle-Cell Lymphoma
Waldenstrom Macroglobulinemia
Diffuse Large B Cell Lymphoma
Follicular Lymphoma 收起 <<
Phase 1
Phase 2
Recruiting
June 30, 2021
United States, California
... 展开 >>
University of California Irvine Medical Center
Recruiting
Orange, California, United States, 92868-3201
Contact: General Contact 877-827-8839 ucstudy@uci.edu
UC San Diego Moores Cancer Center
Recruiting
San Diego, California, United States, 92093
Contact: Barbara Ivers 858-822-6281 bivers@ucsd.edu
United States, Florida
Moffitt Cancer Center and Research Institute
Recruiting
Tampa, Florida, United States, 33612
Contact: Natalie Miller 813-745-2591 Natalie.Miller@moffitt.org
United States, Massachusetts
Dana-Farber Cancer Institute
Recruiting
Boston, Massachusetts, United States, 02215
Contact: Conner Shaughnessy 617-582-8437 Conner_Shaughnessy@dfci.harvard.edu
United States, New York
Memorial Sloan Kettering Cancer Center
Recruiting
New York, New York, United States, 10065
Contact: Isaac Deonarine 646-888-1319 deonarii@mskcc.org
Weill Cornell Medicine
Recruiting
New York, New York, United States, 10065
Contact: Jessica Harper 646-962-9414 jah2070@med.cornell.edu
United States, Texas
MD Anderson Cancer Center
Recruiting
Houston, Texas, United States, 77030
Contact: Chongjuan Wei 713-792-3530 cwei@mdanderson.org
United States, Washington
Swedish Cancer Institute
Recruiting
Seattle, Washington, United States, 98104
Contact: Ngan Trinh 206-215-2363 Ngan.Trinh@Swedish.org 收起 <<
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