On December 23, 2013 BeiGene reported that it has enrolled first patient in a phase I study of BGB-283 in patients with B-RAF or K-RAS mutations. BGB-283 is an investigational, oral, selective, potent second generation inhibitor of B-RAF, making it a targeted therapeutic candidate to potentially treat and bring benefit to patients with cancers that harbour BRAF mutations and/or aberrations in the RAS-MAPK (mitogen-activated protein kinase) pathway (Press release BeiGene, DEC 23, 2013, View Source [SID:1234500417]).
BGB-283 is part of BeiGene’s two-asset strategic collaboration with Merck. Established earlier this year, the goal of the partnership is to leverage Merck’s global oncology development and commercialization expertise. The phase I multi-centre, open-label, dose escalation clinical trial of BGB-283 is designed to assess the safety, tolerability and pharmacokinetic properties of BGB-283 as a single agent. The study is expected to only enroll subjects who have B-RAF or K-RAS mutations. Key objectives in the study include determining maximum tolerated dose, pharmacokinetics, pharmacodynamics and preliminary anti-tumour activity of BGB-283. Disease-specific expansion cohorts will be enrolled at the maximally tolerated or biologically relevant dose.
The mitogen-activated protein kinase (MAPK) pathway comprises several key signalling components that play critical roles in tumourigenesis. Alteration of the RAS-MAPK pathway has frequently been reported in human cancer as a result of abnormal activation of receptor tyrosine kinases or gain-of-function mutations mainly in the RAS or RAF genes. Activating mutations of the RAS family genes (H-RAS, K-RAS, and N-RAS) comprise up to 30 per cent of all human cancers. B-RAF mutations also have been reported in seven to eight per cent of all human cancers. Accordingly, components of this pathway are important therapeutic targets for cancer treatment.

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