Role of ErbB family receptor tyrosine kinases in intrahepatic cholangiocarcinoma

Table 2 Selected anti-cancer agents targeting ErbB family receptors

Agent	Class/Type	Target	Route of administration	Development stage	Ref.
Trastuzumab (Herceptin)	Recombinant humanized mAb	Extracellular domain of ErbB2	Intravenous infusion	Approved (ErbB2-positive breast cancer)	[150-152]
Pertuzumab (Omnitarg, 2C4)	Recombinant humanized mAb	Dimerization domain of ErbB2	Intravenous infusion	Phase II/III	[151,153,154]
Cetuximab (Erbitux, C225)	Recombinant human/mouse chimeric mAb	Extracellular domain of EGFR	Intravenous infusion	Approved (EGFR-positive metastatic colorectal cancer and squamous cell carcinoma head and neck cancer)	[151,155-157]
Panitumumab (ABX-EGF, Vectibix)	Fully human mAb	Extracellular domain of EGFR	Intravenous infusion	Approved (EGFR-positive metastatic colorectal cancer)	[157-159]
Matuzumab (EMI-72000)	Recombinant humanized mAb	Extracellular domain of EGFR	Intravenous infusion	Phase I/II	[157,159,160]
MDX-447	Humanized bispecific mAb	Extracellular domain of EGFR and high affinity IgG receptor CD64	Intravenous infusion	Phase I/II	[157,161]
Gefitinib (Iressa)	Anilinoquinazoline/Reversible TKI	EGFR tyrosine kinase	Oral	Limited approval (NSCLC)	[157,162-164]
Erlotinib (Tarceva)	Anilinoquinazoline/Reversible TKI	EGFR tyrosine kinase	Oral	Approved (NSCLC and pancreatic cancer)	[153,155,157,165,166]
Lapatinib (Tykerb, GW572016)	Thiazolylquinazoline/Reversible TKI	EGFR and ErbB2 tyrosine kinases	Oral	Approved (ErbB2-positive advanced metastatic breast cancer)	[157,166-169]
PKI-166	Pyrrolopyrimidine/Reversible TKI	EGFR and ErbB2 tyrosine kinases	Oral	Phase I	[153,155,157,166,170]
BMS-599626	Pyrrolotriazine/Reversible TKI	EGFR and ErbB2 tyrosine kinases	Oral	Phase I	[171,172]
EKB-569 (Pelitinib)	Cyanoquinoline/Irreversible TKI	EGFR tyrosine kinase	Oral	Phase I/II	[157,166,173]
BIBW-2992	Anilinoquinazoline/Irreversible TKI	EGFR and ErbB2 tyrosine kinases	Oral	Phase I/II	[168,174]
CI-1033 (Canertinib)	Anilinoquinazoline/Irreversible TKI	Pan-ErbB tyrosine kinases	Oral	Phase I/II	[153,157,164,168]
HKI-272	Cyanoquinoline/Irreversible TKI	Pan-ErbB tyrosine kinases	Oral	Phase I/II	[153,164,168,175]

mAb: Monoclonal antibody; TKI: Tyrosine kinase inhibitor; EGFR: Epidermal growth factor receptor; NSCLC: Non-small cell lung cancer.