- BGB-283 Phase Ia data demonstrates activity against K-RAS and N-RAS mutations not currently targeted by first generation B-RAF inhibitors -
BEIJING, July 14, 2015 (GLOBE NEWSWIRE) -- BeiGene, Ltd., an innovative oncology company focused on developing targeted and immune-oncology therapeutics, today announced it has dosed the first patient in a Phase Ib clinical trial for BGB-283, a second generation B-RAF inhibitor. This study is designed to determine the efficacy of a once daily oral dosing regimen for BGB-283 in solid tumors that harbor B-RAF mutations and/or aberrations in the RAS-MAPK (mitogen-activated protein kinase) pathway. The study is being conducted across multiple centers in Australia and New Zealand.
The Phase Ib study being undertaken by BeiGene follows the successful completion of a Phase Ia dose escalation study in patients who have B-RAF or K-RAS mutations. In this study, BGB-283 demonstrated a good safety profile along with promising early clinical activity in patients harboring mutations that previously could not be targeted by first generation B-RAF inhibitors.
"We have continued to make great progress across all our clinical development programs," commented John Oyler, the CEO of BeiGene. "BGB-283 is a clinically differentiated B-RAF inhibitor able to hit multiple important mutations in the RAS-MAPK pathway. The data from the Phase Ia dose escalation study gave us confidence to move into a broad Phase Ib study that is designed to demonstrate BGB-283's single agent activity across a wide range of solid tumors."
First generation B-RAF inhibitors including vemurafenib and dabrafenib selectively target mutant B-RAFV600E and have exhibited remarkable clinical activities in melanoma patients with the B-RAFV600E mutation. They are approved for the treatment of patients with B-RAFV600E metastatic melanoma. However, first generation B-RAF inhibitors have limited clinical activity outside of melanoma with B-RAFV600E mutation (1-4). For example, the clinical response among CRC patients with B-RAFV600E mutations is much lower than that observed in melanoma patients.(5) BGB-283 is a second generation B-RAF inhibitor with unique RAF dimer and EGFR inhibiting activity. BGB-283 shows promising antitumor activities in preclinical models for not only cancers with B-RAF V600E mutation but also non-V600E B-RAF mutation and K-RAS/N-RAS mutations.
BeiGene is an innovative oncology R&D company focused on immune-oncology therapeutics. With a team of 170+ scientists and staff, working from their Beijing based R&D facility; BeiGene's pipeline is comprised of novel oral small molecules and monoclonal antibodies for cancer. BeiGene is working to create combination solutions that will have both a meaningful and lasting impact on cancer patients. For more information, please visit our website at www.beigene.com.
1. Sosman JA, Kim KB, Schuchter L, Gonzalez R, Pavlick AC, Weber JS, et al. Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib. New England Journal of Medicine. 2012;366:707-14.
2. Anforth R, Fernandez-Peñas P, Long GV. Cutaneous toxicities of RAF inhibitors. The Lancet Oncology. 2013;14:e11-e8.
3. Anforth RM, Blumetti TCMP, Kefford RF, Sharma R, Scolyer RA, Kossard S, et al. Cutaneous manifestations of dabrafenib (GSK2118436): a selective inhibitor of mutant BRAF in patients with metastatic melanoma. British Journal of Dermatology. 2012;167:1153-60.
4. Chapman PB, Hauschild A, Robert C, Haanen JB, Ascierto P, Larkin J, et al. Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation. New England Journal of Medicine. 2011;364:2507-16.
5. Kopetz S, Desai J, Chan E, Hecht J, O'dwyer P, Lee R, et al. PLX4032 in metastatic colorectal cancer patients with mutant BRAF tumors. J Clin Oncol. 2010;28:3534.
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