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.