NCI Drug Dictionary

The NCI Drug Dictionary contains technical definitions and synonyms for drugs/agents used to treat patients with cancer or conditions related to cancer. Each drug entry includes links to check for clinical trials listed in NCI's List of Cancer Clinical Trials.

An orally bioavailable selective multikinase inhibitor of mutant forms, fusions and rearrangements involving the proto-oncogene receptor tyrosine kinase rearranged during transfection (RET) as well as the serine/threonine-protein kinase B-raf (BRAF), with potential antineoplastic activity. Upon oral administration,agerafenib selectively and potently binds to and targets various RET- and BRAF-containing mutants, fusions and rearrangements. This results in inhibition of cell growth in tumors cells that exhibit increased RET and BRAF activity. RET overexpression, activating mutations, and fusions result in the upregulation and/or overactivation of RET tyrosine kinase activity in various cancer cell types; dysregulation of RET activity plays a key role in the development and progression of these cancers. BRAF, a member of the raf family of serine/threonine protein kinases, plays a role in the regulation of MAP kinase/ERK signaling pathways, which may be constitutively activated in certain cancer cells with activating BRAF gene mutations. Check for active clinical trials using this agent. (NCI Thesaurus)

Code name:AC 013773
RXDX 105