The Sound of Evolution
Lapatinib
Mechanism of action:
Lapatinib is a small-molecule tyrosine kinase inhibitor and a dual HER2/EGFR inhibitor. It binds to the ATP-binding sites of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2), preventing ATP from entering the kinase domain and thereby blocking receptor autophosphorylation. This suppresses multiple downstream pathways critical for tumor growth and survival, including PI3K / AKT / mTOR and MAPK / ERK, reducing tumor cell proliferative and survival signaling and potentially inducing apoptosis-related responses.
Reference(s):
1. Nelson MH et al. (2006). Lapatinib: a novel dual tyrosine kinase inhibitor with activity in solid tumors. Ann Pharmacother.
2. Burris HA et al. (2004). Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist.
3. Burris HA et al. (2005). Phase I safety, pharmacokinetics, and clinical activity study of lapatinib (GW572016), a reversible dual inhibitor of epidermal growth factor receptor tyrosine kinases, in heavily pretreated patients with metastatic carcinomas. J Clin Oncol.