Compound Targets Study Phase Monotherapy or Combination (C) Tumor Type
EGFR Inhibitors
Erlotinib EGFR TKI a.) FDA a.) Monotherapy a.) NSCLC [5]
b.) FDA b.)C:Gemcitabine b.) Pancreatic cancer [5]
c.) III c.)C:Gemcitabine c.) Pancreatic cancer [75]
Gefitinib EGFR TKI a.) FDA* a.) Monotherapy a.) NSCLC [5]
b.) III b.)C:Cisplatin and Docetaxel b.) NSCLC [76,77]
     
Lapatinib EGFR, HER2 TKI a.) FDA a.)C: apecitabine a.)HER2+ breast cancer [5]
b.) III b.) C: Paclitaxel b.)HER2+ metastatic breast cancer [50]
Afatinib EGFR, HER2 TKI a.) FDA a.) Monotherapy a.) NSCLC [5]
b.) III b.) Monotherapy b.) HNSCC (NCT01427478)
Dacomitinib EGFR TKI (pan- HER inhibitor) a.) II a.) C: Cetuximab a.) HNSCC [49]
b.) III b.) C: Gefitinib b.) NSCLC (NCT01774721)
Cetuximab EGFR MAb a.) FDA a.) C: Cytotoxic or radiation therapies a.) CRC, head and neck cancer [5]
b.) II/III b.) C: Platinum –based chemotherapy b.) NSCLC [86]
Panitumumab EGFR MAb a.) FDA a.) Monotherapy a.) CRC [5]
b.) III b.) C: FOLFOX regimen b.) Metastatic CRC (NCT00364013)
Matuzumab EGFR MAb II C: Pemetrexed NSCLC (NCT00111839)
Zalutumumab EGFR MAb III C: Radiotherapy HNSCC (NCT00496652)
c-Met Inhibitors
Tivantinib c-Met TKI a.) I a.) C: Sorafenib a.) HCC [83]
b.) II b.) C: Erlotinib b.) NSCLC [84]
c.) III c.) Monotherapy c.) NSCLC, HCC (NCT01755767)
Cabozantinib c-Met/multi-kinase TKI a.) FDA a.) Monotherapy a.) Medullary thyroid cancer [28]
b.) II b.) Monotherapy b.) CRPC [80]
c.) III c.) C: Prednisone c.) CRPC (NCT01605227)
Foretinib c-Met/multi-kinase TKI II Monotherapy Renal papillary cell carcinoma [87]
Crizotinib c-Met, ALK, ROS1 TKI a.) FDA a.) Monotherapy a.) ALK+ NSCLC [28]
b.) II b.) Monotherapy b.) Hematologic and metastatic cancers, and solid tumors (NCT02034981)
MetMAb c-Met MAb a.) II a.) C: Erlotinib a.) NSCLC [79,85]
b.) III b.) C: mFOLFOX6 b.) HER2 negative(-) and c-Met+ adenocarcinoma of the stomach or GEJ (NCT01662869)
Rilotumumab HGF (c-Met ligand) MAb III Monotherapy c-Met+ gastric or GEJ adenocarcinoma (NCT01697072)
Table 1: Inhibitors of EGFR/c-Met and their clinical status. Abbreviations: NSCLC: Non-small Cell Lung Cancer; HNSCC: Head and Neck Squamous Cell Carcinoma; CRPC: Castration-Resistant Prostate Cancer; CRC: Colorectal Cancer; HCC: Hepatocellular Carcinoma; GEJ: Gastroesophageal Junction; TKI: Tyrosine Kinase Inhibitor; MAb: Monoclonal antibody. *FDA approval was withdrawn in the USA