Table 1.
EGFR inhibitors
Inhibitor | Manufacturer | Class | Specificity | FDA indication and year of approval |
---|---|---|---|---|
Cetuximab C225, Erbitux® |
ImClone Systems | Mouse-human chimeric antibody |
EGFR | EGFR-expressing mCRC in patients refractory to irinotecan-based chemotherapy (2004) Locally or regionally advanced HNSCC in combination with radiotherapy (2006) |
Matuzumab EMD72000 |
EMD Pharmaceuticals | Mouse-human chimeric antibody |
EGFR | Not yet approved |
Nimotuzumab h-R3, TheraCIM® |
YM BioSciences | Human antibody | EGFR | Not yet approved |
Panitumumab ABX-EGF, Vectibix® |
Amgen | Human antibody | EGFR | EGFR-expressing mCRC with progression on or following chemotherapy regimens containing fluoropyrimidine, oxaliplatin, and irinotecan (2006) |
Zalutumumab HuMax-EGFr |
Genmab | Human antibody | EGFR | Not yet approved |
Erlotinib OSI-774, Tarceva® |
Genentech | Anilinoquinazoline- based reversible inhibitor |
EGFR | NSCLC as a monotherapy after failure of at least one prior chemotherapy (2004) Advanced pancreatic cancer in combination with gemcitabine for patients who have not received previous chemotherapy (2005) |
Gefitinib ZD1839, Iressa® |
AstraZeneca | Anilinoquinazoline- based reversible inhibitor |
EGFR | Locally advanced metastatic NSCLC cancer after failure of both platinum- based and docetaxel chemotherapies (2003) |
Vandetanib ZD6474, Zactima® |
AstraZeneca | Anilinoquinazoline- based inhibitor |
EGFR VEGFR2 RET- tyrosine kinase |
NSCLC Submitted for approval in June 2009, but application withdrawn in October 2009 in NSCLC setting with chemotherapy |
Lapatinib GW572016, Tykerb® |
GlaxoSmithKline | Thiazolylquinazoline- based reversible inhibitor |
EGFR HER2 |
Metastatic breast cancer in combination with capecitabine whose tumors overexpress HER2 and have received prior therapy, including an anthracycline, a taxane, and trastuzumab (2006) |
Pelitinib EKB-569 |
Wyeth | Cyanoquinoline-based irreversible inhibitor |
EGFR HER2 |
Not yet approved |
Abbreviations: HNSCC, head and neck squamous cell carcinoma; mCRC, metastatic colorectal cancer; NSCLC, non-small cell lung cancer;