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) |