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entospletinib

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https://www.readbyqxmd.com/read/27785737/pharmacokinetics-pharmacodynamics-and-safety-of-entospletinib-a-novel-psyk-inhibitor-following-single-and-multiple-oral-dosing-in-healthy-volunteers
#1
Srini Ramanathan, Julie A Di Paolo, Feng Jin, Lixin Shao, Shringi Sharma, Michelle Robeson, Brian P Kearney
BACKGROUND AND OBJECTIVES: Entospletinib is a selective, reversible, adenosine triphosphate-competitive small-molecule spleen tyrosine kinase (SYK) inhibitor that blocks B cell receptor-mediated signaling and proliferation in B lymphocytes. This study evaluated the safety, pharmacokinetics, and pharmacodynamics of entospletinib in a double-blind, single/multiple ascending dose study in healthy volunteers. METHODS: In sequential cohorts, 120 subjects received entospletinib (25-1200 mg; fasted) as single or twice-daily oral doses for 7 days...
October 26, 2016: Clinical Drug Investigation
https://www.readbyqxmd.com/read/27541051/new-drugs-for-follicular-lymphoma
#2
Marc Sorigue, Josep-Maria Ribera, Cristina Motlló, Juan-Manuel Sancho
Despite the improvement in prognosis since the advent of rituximab, follicular lymphoma is still incurable and remains the cause of death of most afflicted patients. With the expanding knowledge of the pathogenesis of B-cell malignancies, in the last few years a plethora of new therapies acting through a variety of mechanisms have shown promising results. This review attempts to analyze the evidence available on these new drugs, which include new monoclonal antibodies and immunoconjugates, the anti-angiogenic and immunomodulatory agent lenalidomide, the proteasome inhibitor bortezomib, inhibitors of B-cell receptor pathway enzymes, such as ibrutinib, idelalisib, duvelisib and entospletinib, BCL2 inhibitors and checkpoint inhibitors...
October 2016: Leukemia Research
https://www.readbyqxmd.com/read/27247756/targeting-b-cell-receptor-signaling-kinases-in-chronic-lymphocytic-leukemia-the-promise-of-entospletinib
#3
REVIEW
Jeff Sharman, Julie Di Paolo
The B-cell receptor signaling pathway has emerged as an important therapeutic target in chronic lymphocytic leukemia and other B-cell malignancies. Novel agents have been developed targeting the signaling enzymes spleen tyrosine kinase (SYK), Bruton's tyrosine kinase, and phosphoinositide 3-kinase delta. This review discusses the rationale for targeting these enzymes, as well as the preclinical and clinical evidence supporting their role as therapeutic targets, with a particular focus on SYK inhibition with entospletinib...
June 2016: Therapeutic Advances in Hematology
https://www.readbyqxmd.com/read/26968534/phase-2-study-of-idelalisib-and-entospletinib-pneumonitis-limits-combination-therapy-in-relapsed-refractory-cll-and-nhl
#4
Paul M Barr, Gene B Saylors, Stephen E Spurgeon, Bruce D Cheson, Daniel R Greenwald, Susan M O'Brien, Andre K D Liem, Rosemary E Mclntyre, Adarsh Joshi, Esteban Abella-Dominicis, Michael J Hawkins, Anita Reddy, Julie Di Paolo, Hank Lee, Joyce He, Jing Hu, Lyndah K Dreiling, Jonathan W Friedberg
Although agents targeting B-cell receptor signaling have provided practice-changing results in relapsed chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL), they require prolonged administration and provide incomplete responses. Given synergistic preclinical activity with phosphatidylinositol 3-kinase δ and spleen tyrosine kinase inhibition, this phase 2 study evaluated the safety and efficacy of the combination of idelalisib and entospletinib. Eligible patients with relapsed or refractory CLL or NHL underwent intrapatient dose escalation with each agent...
May 19, 2016: Blood
https://www.readbyqxmd.com/read/26773040/diffuse-large-b-cell-lymphoma-patient-derived-xenograft-models-capture-the-molecular-and-biological-heterogeneity-of-the-disease
#5
Bjoern Chapuy, Hongwei Cheng, Akira Watahiki, Matthew D Ducar, Yuxiang Tan, Linfeng Chen, Margaretha G M Roemer, Jing Ouyang, Amanda L Christie, Liye Zhang, Daniel Gusenleitner, Ryan P Abo, Pedro Farinha, Frederike von Bonin, Aaron R Thorner, Heather H Sun, Randy D Gascoyne, Geraldine S Pinkus, Paul van Hummelen, Gerald G Wulf, Jon C Aster, David M Weinstock, Stefano Monti, Scott J Rodig, Yuzhuo Wang, Margaret A Shipp
Diffuse large B-cell lymphoma (DLBCL) is a heterogeneous disease defined by transcriptional classifications, specific signaling and survival pathways, and multiple low-frequency genetic alterations. Preclinical model systems that capture the genetic and functional heterogeneity of DLBCL are urgently needed. Here, we generated and characterized a panel of large B-cell lymphoma (LBCL) patient-derived xenograft (PDX) models, including 8 that reflect the immunophenotypic, transcriptional, genetic, and functional heterogeneity of primary DLBCL and 1 that is a plasmablastic lymphoma...
May 5, 2016: Blood
https://www.readbyqxmd.com/read/25696919/an-open-label-phase-2-trial-of-entospletinib-gs-9973-a-selective-spleen-tyrosine-kinase-inhibitor-in-chronic-lymphocytic-leukemia
#6
MULTICENTER STUDY
Jeff Sharman, Michael Hawkins, Kathryn Kolibaba, Michael Boxer, Leonard Klein, Meihua Wu, Jing Hu, Steve Abella, Chris Yasenchak
Small-molecule inhibitors of kinases involved in B-cell receptor signaling are an important advance in managing lymphoid malignancies. Entospletinib (GS-9973) is an oral, selective inhibitor of spleen tyrosine kinase. This multicenter, phase 2 study enrolled subjects with relapsed or refractory chronic lymphocytic leukemia (CLL; n = 41) or non-Hodgkin lymphoma (n = 145). Participants received 800 mg entospletinib twice daily. We report efficacy outcomes in the CLL cohort (n = 41) and safety outcomes in all cohorts (N = 186)...
April 9, 2015: Blood
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