MK-2206 + trastuzumab + lapatinib

This is an investigational combination therapy consisting of MK-2206 (an allosteric AKT inhibitor), trastuzumab (a monoclonal antibody targeting human epidermal growth factor receptor 2, HER2), and lapatinib (a small molecule dual tyrosine kinase inhibitor targeting HER2 and EGFR). The rationale for combining these agents is to overcome resistance mechanisms in HER2-positive cancers by simultaneously inhibiting upstream HER2 signaling (trastuzumab, lapatinib) and downstream AKT signaling (MK-2206). The combination has been evaluated primarily in HER2-positive breast cancer, especially in patients who developed resistance to standard HER2-targeted therapies[1][3][5][7][9]. MK-2206 is developed by Merck; trastuzumab by Genentech/Roche; lapatinib by GSK. Early-phase clinical trials indicate safety, tolerability, and preliminary anti-tumor activity in advanced HER2+ breast cancer. MK-2206 is not approved, and development was stopped, but the combination remains of significant academic and clinical interest for drug resistance settings in HER2+ cancers.

Brand names

HerceptinTykerb

Other names

trastuzumablapatinib