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. 2017 Dec 22;9(4):5459–5472. doi: 10.18632/oncotarget.23616

Table 5. Other molecular targeted therapies for brain metastasis in non-small lung cancer.

Drug (trade names) Molecular targets Targeted mutated sites in NSCLC Status Treatment strategies for BM in NSCLC Mechanisms of drug resistance
Dabrafenib (Tafinlar) в-Raf BRAF V600E/K-mutant FDA approved Combination with trametinib (BRAF V600-positive) Overexpression of PDGFRB, NRAS mutation
Vemurafenib (Zelboraf) в-Raf BRAF V600E/K-mutant FDA approved Combination of dabrafenib and trametinib Overexpression of PDGFRB, second NRAS mutation
Cabozantinib (Cabometyx) c-Met, VEGFR-2, AXL, RET RET fusion-positive FDA granted orphan drug status Combination with everolimus None reported
Bevacizumab (Avastin) VEGF-A VEGF positive FDA approved Combination with carboplatin/paclitaxel VEGF-D, VEGF-C
Ramucirumab (Cyramza) VEGFR-2 VEGFR positive FDA approved Combination with carboplatin/paclitaxel VEGFR-2 mutant
Nivolumab (Opdivo) PD-1 BRAF mutant FDA approved Combination with ipilimumab No reports
Pembrolizumab (Keytruda) PD-1 PD-L1 overexpression, no mutations in EGFR or in ALK FDA approved Pembrolizumab No reports
Atezolizumab (Tecentriq) PD-L1 Cytotoxic T-cells FDA approved Atezolizumab No reports
Ipilimumab (Yervoy) CTLA-4 Cytotoxic T lymphocytes FDA approved Combination with carboplatin No reports

NSCLC, non-small cell lung cancer; BM, brain metastases; VEGFR-2, vascular endothelial growth factor receptor 2; VEGF: vascular endothelial growth factor; PD-1, programmed cell death protein 1; PD-L1, Programmed death-ligand 1; EGFR: epidermal growth factor receptor; ALK, anaplastic lymphoma kinase; CTLA-4, cytotoxic T-lymphocyte-associated protein 4.