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. Author manuscript; available in PMC: 2017 Nov 9.
Published in final edited form as: Expert Opin Emerg Drugs. 2015 Mar 31;20(2):313–329. doi: 10.1517/14728214.2015.1031653

Figure 1. Currently applied and emerging investigated drugs in head and neck squamous cell carcinoma.

Figure 1

Current FDA-approved drugs for the treatment of HNSCC include five conventional chemotherapy drugs (cisplatin, methotrexate, 5-flurouracil, bleomycin, docetaxel) and one targeted agent (cetuximab). Emerging investigated drugs in clinical trials including other targeted agents, immunotherapy agents and gene therapy agents are represented here. Briefly, EGFR, VEGFR, c-MET and IGF-1R signals utilize a variety of downstream molecular pathways including the PI3K/Akt/mTOR, STAT and Ras/Raf/MEK/MAPK. Aberrant activation of these pathways are associated with tumor growth and angiogenesis. Agents targeting these pathways include monoclonal antibodies (cetuximab, zalutumumab, panitumumab, nimotuzumab, bevacizumab, ficlatuzumab and figitumumab), tyrosine kinase inhibitors (gefitinib, erlotinib, lapatinib, afatinib, dacomitinib), multikinase inhibitors (sorafenib, sunitinib), downstream inhibitors including Src family kinase inhibitors (dasatinib) and PI3K/Akt/mTOR inhibitors (BKM120, BYL719, everolimus, temsirolimus). Gene therapy includes Adp53/CRAdp53-based gene therapy (Gendicine, H-101, SCH-58500, ONYX-015) and EGFR antisense DNA. Immunotherapy includes non-specific immune stimulators/agents (nivolumab, IRX-2) and vaccine candidates (peptide-based vaccine, DNA vaccine and dendritic cell vaccine).

Akt: Protein kinase B; AREG: Amphiregulin; EREG: Epiregulin; ERK: Extracellular signal-regulated kinase; HB-EGF: Heparin-binding EGF-like growth factor; HER: Human EGFR; HGF: Hepatocyte growth factor; IGF-1R: IGF-1 receptor; MET: Also called c-MET tyrosine kinase or HGF receptor; MEK: MAPK/ERK kinase; mTOR: Mammalian target of rapamycin; NRG: Neuregulin; PI3K: Phosphatidylinositol-3-kinase; Raf: Rapidly accelerated fibrosarcoma kinase; Ras: Rat sarcoma protein; Src: Sarcoma-family kinase; STAT: Signal transducer and activator of transcription; VEGFR: VEGF receptor.