Drug intelligence / Profile preview

MK-2206 + trastuzumab

Development stage
Unknown
Lead developer
Merck
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

MK-2206 + trastuzumab is an investigational combination therapy consisting of MK-2206, a selective allosteric inhibitor of AKT (a serine/threonine kinase in the PI3K/AKT pathway), and trastuzumab, a monoclonal antibody targeting the human epidermal growth factor receptor 2 (HER2). This combination is being studied primarily for HER2-positive cancers such as breast and gastric cancer. The rationale for combining these agents is that resistance to trastuzumab can develop through activation of downstream signaling via the PI3K/AKT pathway; thus, inhibiting AKT with MK-2206 may overcome or delay resistance to HER2-targeted therapy. Clinical studies have shown that this combination can be safely administered and has demonstrated clinical activity in patients with HER2+ tumors who have progressed on prior therapies[1][2][3][8].

02

Targets

AKT2 (Rac-beta serine/threonine-protein kinase)AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)ERBB2 (Erb-b2 receptor tyrosine kinase 2)

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