ONO-4059 (analog)

The product is the analog of ONO-4059, ONO-4059 is a highly potent and selective Btk inhibitor with an IC50 in the sub-nM range. IC50 value: sub-nM range [2]Target: Btkin vitro: ONO-4059 ( analog ) is a selective, once-daily, oral inhibitor of BTK, which has been shown to play a role in the survival and proliferation of malignant B-cells. ONO-4059 (analog) shows a favourable safety profile along with promising efficacy in this difficult-to-treat patient population. [1]in vivo: ONO-4059 (analog) has demonstrated anti-tumour activity in several pre-clinical models.[1] ONO-4059 (analog) potently and dose-dependently reverse clinical arthritis and prevented bone damage in the CIA model.[2]

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Btk

Research Areas >> Cancer

[1]. Simon Rule,A Phase I Study Of The Oral Btk Inhibitor ONO-4059 In Patients With Relapsed/Refractory B-Cell Lymphoma. November 15, 2013; Blood: 122 (21)

[2]. Toshio Yoshizawa, et al. Development of a Bruton's Tyrosine Kinase (Btk) Inhibitor, ONO-4059: Efficacy in a Collagen Induced Arthritis (CIA) Model Indicates Potential Treatment for Rheumatoid Arthritis (RA). Washington, DC November 9-14, 2012.

[3]. Yamamoto, et al. Preparation of purinone derivatives as selective Btk inhibitors. From PCT Int. Appl. (2011), WO 2011152351 A1 20111208.

Acalabrutinib | GDC-0853 | Evobrutinib | AVL-292 | (±)-Zanubrutinib | ONO-4059 | BMX-IN-1 | GDC-0834 | SNS-062 | RN486 | LFM-A13 | Vecabrutinib | CGI-1746 | BMS-986195 | CNX-774