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Page 1
Bruton tyrosine kinase inhibitor ONO/GS-4059: from bench to bedside.
Wu J, Zhang M, Liu D. Wu J, et al. Oncotarget. 2017 Jan 24;8(4):7201-7207. doi: 10.18632/oncotarget.12786. Oncotarget. 2017. PMID: 27776353 Free PMC article. Review.
Untoward effects due to off-target effects are also disadvantages of ibrutinib. More selective and potent BTK inhibitors (ACP-196, ONO/GS-4059, BGB-3111, CC-292) are being investigated. This review summarized the preclinical research and clinical data of ONO/GS …
Untoward effects due to off-target effects are also disadvantages of ibrutinib. More selective and potent BTK inhibitors (ACP-196, ONO/GS …
Homogeneous BTK Occupancy Assay for Pharmacodynamic Assessment of Tirabrutinib (GS-4059/ONO-4059) Target Engagement.
Yu H, Truong H, Mitchell SA, Liclican A, Gosink JJ, Li W, Lin J, Feng JY, Jürgensmeier JM, Billin A, Xu R, Patterson S, Pagratis N. Yu H, et al. SLAS Discov. 2018 Oct;23(9):919-929. doi: 10.1177/2472555218786165. Epub 2018 Jul 16. SLAS Discov. 2018. PMID: 30011241 Free PMC article.
Bruton's tyrosine kinase (BTK) is a clinically validated target for B-cell leukemias and lymphomas with FDA-approved small-molecule inhibitors ibrutinib and acalabrutinib. Tirabrutinib (GS-4059/ONO-4059, Gilead Sciences, Inc., Foster City, CA) is a second-generation …
Bruton's tyrosine kinase (BTK) is a clinically validated target for B-cell leukemias and lymphomas with FDA-approved small-molecule inhibito …
Anti-tumor efficacy study of the Bruton's tyrosine kinase (BTK) inhibitor, ONO/GS-4059, in combination with the glycoengineered type II anti-CD20 monoclonal antibody obinutuzumab (GA101) demonstrates superior in vivo efficacy compared to ONO/GS-4059 in combination with rituximab.
Yasuhiro T, Sawada W, Klein C, Kozaki R, Hotta S, Yoshizawa T. Yasuhiro T, et al. Leuk Lymphoma. 2017 Mar;58(3):699-707. doi: 10.1080/10428194.2016.1201567. Epub 2016 Aug 9. Leuk Lymphoma. 2017. PMID: 27684575
Given the high potency and selectivity of the BTK inhibitor, ONO/GS-4059, it was hypothesized that, the anti-tumor activity of ONO/GS-4059 could be further enhanced by combining it with the anti-CD20 Abs, rituximab (RTX) or obinutuzumab (GA101). ...Tak …
Given the high potency and selectivity of the BTK inhibitor, ONO/GS-4059, it was hypothesized that, the anti-tumor activity of …
PI3Kdelta inhibitor idelalisib in combination with BTK inhibitor ONO/GS-4059 in diffuse large B cell lymphoma with acquired resistance to PI3Kdelta and BTK inhibitors.
Yahiaoui A, Meadows SA, Sorensen RA, Cui ZH, Keegan KS, Brockett R, Chen G, Quéva C, Li L, Tannheimer SL. Yahiaoui A, et al. PLoS One. 2017 Feb 8;12(2):e0171221. doi: 10.1371/journal.pone.0171221. eCollection 2017. PLoS One. 2017. PMID: 28178345 Free PMC article.
In this study, we describe both the additive interaction of and resistance mechanisms to idelalisib and ONO/GS-4059 in a model of activated B-cell-like diffuse large B-cell lymphoma. ...A clinical trial is currently underway to evaluate the combination of idelalisib …
In this study, we describe both the additive interaction of and resistance mechanisms to idelalisib and ONO/GS-4059 in a model …
A phase 1 clinical trial of the selective BTK inhibitor ONO/GS-4059 in relapsed and refractory mature B-cell malignancies.
Walter HS, Rule SA, Dyer MJ, Karlin L, Jones C, Cazin B, Quittet P, Shah N, Hutchinson CV, Honda H, Duffy K, Birkett J, Jamieson V, Courtenay-Luck N, Yoshizawa T, Sharpe J, Ohno T, Abe S, Nishimura A, Cartron G, Morschhauser F, Fegan C, Salles G. Walter HS, et al. Blood. 2016 Jan 28;127(4):411-9. doi: 10.1182/blood-2015-08-664086. Epub 2015 Nov 5. Blood. 2016. PMID: 26542378 Free PMC article. Clinical Trial.
We report the results of a multicenter phase 1 dose-escalation study of the selective Bruton tyrosine kinase (BTK) inhibitor ONO/GS-4059 in 90 patients with relapsed/refractory B-cell malignancies. ...The selectivity of ONO/GS-4059 should confer advant …
We report the results of a multicenter phase 1 dose-escalation study of the selective Bruton tyrosine kinase (BTK) inhibitor ONO/GS- …
Long-term follow-up of patients with CLL treated with the selective Bruton's tyrosine kinase inhibitor ONO/GS-4059.
Walter HS, Jayne S, Rule SA, Cartron G, Morschhauser F, Macip S, Karlin L, Jones C, Herbaux C, Quittet P, Shah N, Hutchinson CV, Fegan C, Yang Y, Mitra S, Salles G, Dyer MJS. Walter HS, et al. Blood. 2017 May 18;129(20):2808-2810. doi: 10.1182/blood-2017-02-765115. Epub 2017 Apr 4. Blood. 2017. PMID: 28377400 Free PMC article. Clinical Trial. No abstract available.
Optimizing Platelet GPVI Inhibition versus Haemostatic Impairment by the Btk Inhibitors Ibrutinib, Acalabrutinib, ONO/GS-4059, BGB-3111 and Evobrutinib.
Denzinger V, Busygina K, Jamasbi J, Pekrul I, Spannagl M, Weber C, Lorenz R, Siess W. Denzinger V, et al. Thromb Haemost. 2019 Mar;119(3):397-406. doi: 10.1055/s-0039-1677744. Epub 2019 Jan 27. Thromb Haemost. 2019. PMID: 30685871
IC(50) values for collagen (0.2-0.5 g/mL)-induced platelet aggregation after 15-minute pre-incubation were: ibrutinib 0.12 M, BGB-3111 0.51 M, acalabrutinib 1.21 M, ONO/GS-4059 1.20 M and evobrutinib 5.84 M. Peak venous plasma concentrations of ibrutinib (0.5 M), ac …
IC(50) values for collagen (0.2-0.5 g/mL)-induced platelet aggregation after 15-minute pre-incubation were: ibrutinib 0.12 M, BGB-3111 0.51 …
Second-generation inhibitors of Bruton tyrosine kinase.
Wu J, Liu C, Tsui ST, Liu D. Wu J, et al. J Hematol Oncol. 2016 Sep 2;9(1):80. doi: 10.1186/s13045-016-0313-y. J Hematol Oncol. 2016. PMID: 27590878 Free PMC article. Review.
This review summarizes the clinical development of novel BTK inhibitors, ACP-196 (acalabrutinib), ONO/GS-4059, and BGB-3111....
This review summarizes the clinical development of novel BTK inhibitors, ACP-196 (acalabrutinib), ONO/GS-4059, and BGB-3111... …
22 results