Overview

NCI Definition [1]:
An orally available inhibitor of both monomer and dimer forms of activating mutations of the serine/threonine-protein kinase BRAF (B-raf) protein, including V600 BRAF mutations, non-V600 BRAF mutations, and RAF fusions, with potential antineoplastic activity. Upon administration, BRAF inhibitor BGB-3245 targets and binds to both monomeric and dimeric forms of activating BRAF mutations and fusions. This may result in the inhibition of BRAF-mediated signaling and inhibit proliferation in tumor cells expressing BRAF mutations and fusions. BRAF belongs to the RAF family of serine/threonine protein kinases and plays a role in regulating the mitogen-activated protein kinase (MAPK)/ extracellular signal-regulated kinase (ERK) signaling pathway, which is often dysregulated in human cancers and plays a key role in tumor cell proliferation and survival. BRAF mutations and fusions have been identified in a number of solid tumors and are drivers of cancer growth.

Bgb3245 has been investigated in 1 clinical trial, of which 1 is open and 0 are closed. Of the trial investigating bgb3245, 1 is phase 1 (1 open).

ARAF Mutation, BRAF Codon 600 Missense, and BRAF Fusion are the most frequent biomarker inclusion criteria for bgb3245 clinical trials.

Malignant solid tumor, melanoma, and non-small cell lung carcinoma are the most common diseases being investigated in bgb3245 clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Bgb3245
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating bgb3245 and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
braf monomer/dimer inhibitor bgb-3245, braf inhibitor bgb-3245, bgb 3245, bgb-3245
Drug Target(s) [2]:
ARAF, BRAF, RAF1
NCIT ID [1]:
C173633

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.