HER2 therapy. Small molecule HER-2 tyrosine kinase inhibitors

Breast Cancer Research

Table 1 Tyrosine kinase inhibitors that block HER-2 kinase that are in clinical development

Compound	Profile	Reversible or irreversible	Phase of clinical development
Lapatinib	EGFR, HER-2	Reversible	Phase III
CI-1033 (canertinib)	Pan-HER	Irreversible	Phase II
HKI-272	Pan-HER	Irreversible	Phase II
AEE-788	EGFR, HER-2	Reversible	Phase I
BIBW-2992	EGFR, HER-2	Irreversible	Phase I
TAK165	HER-2	Irreversible	Phase I
BMS-599626	Pan-HER	Not reported	Phase I

EGFR, epidermal growth factor receptor; HER, human epidermal growth factor receptor.

ISSN: 1465-542X