| Compound |
Structure |
Mechanism of Action |
Currently FDA approved indications |
Stage of Development in bladder cancer |
| Cetuximab (C225/Erbitux) |
Human/mouse chimeric moAb |
inhibits erbB1 |
H & N, mCRC |
Phase II |
| Panitumumab (ABX-EGF/Vectibix) |
Human moAb |
inhibits erbB1 |
mCRC |
Preclinical |
| Nimotuzumab (Theracim) |
Humanized moAb |
inhibits erbB1 |
(being evaluated in various cancers including esophageal cancer, NSCLC, pancreatic cancer) |
none |
| Matuzumab (EMD 7200) |
Humanized moAb |
inhibits erbB1 |
(being evaluated in NSCLC, EGC, ovarian cancer) |
none |
| Zalutumumab |
Human moAb |
inhibits erbB1 |
(being evaluated in H & N, CRC, NSCLC) |
none |
| Gefitinib (Iressa) |
TKI |
inhibits erbB1 |
NSCLC |
Phase II, Phase III |
| Erlotinib (Tarceva) |
TKI |
inhibits erbB1 |
NSCLC |
Phase II |
| Lapatinib (Tykerb) |
MTKI |
inhibits erbB1, erbB2 |
BRC |
Preclinical |
| Vandetanib (Caprelsa) |
MTKI |
inhibits erbB1, VEGFR-2, VEGFR-3, and RET |
MTC |
none |
| AEE788 |
MTKI |
inhibits erbB1, erbB2, VEGFR-2 |
(being evaluated in GBM) |
none |
| AC 480 (BMS-599626) |
MTKI |
inhibits erbB1, erbB2 |
(being evaluated in BRC, GBM) |
none |
| AZD 8931 |
MTKI |
inhibits erbB1, erbB2, erbB3 |
(being evaluated in BRC, gastric cancer, other solid malignancies) |
none |
| DAB389EGF |
chimeric protein |
conjugated toxin protein targeting erbB1 |
none |
Preclinical |
| miR-133 |
microRNA |
promotes EGFR mRNA degradation/blocks EGFR translation |
none |
Preclinical |
| LRIG1 cDNA |
cDNA |
protein product inhibits erbB1 |
none |
Preclinical |
Acronyms
TKI: tyrosine kinase inhibitor; MTKI: multitargeted kinase inhibitor; moAb: monoclonal antibody; H & N: head and neck cancer; CRC: colorectal cancer; mCRC: metastatic
colorectal cancer; NSCLC: non-small cell lung cancer; BRC: breast cancer; MTC: medullary thyroid cancer