Drug intelligence / Profile preview

MK-0472 + pembrolizumab

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

Overview

MK-0472 + pembrolizumab is an investigational combination therapy being studied for advanced or metastatic solid tumors. MK-0472 is a small molecule inhibitor of SHP2, a protein tyrosine phosphatase that is involved in cell signaling pathways driving tumor cell proliferation. SHP2 inhibition aims to block cancer cell growth and may help overcome resistance to immunotherapies. Pembrolizumab is a monoclonal antibody targeting the programmed cell death 1 (PD-1) receptor, acting as a checkpoint inhibitor that augments immune responses against cancer by preventing tumor-mediated immune evasion. The rationale for combining these agents is to enhance antitumor immunity and inhibit tumor growth via dual targeting: direct oncogenic signaling interruption (SHP2) and immune system activation (PD-1 blockade). MK-0472 is investigational, while pembrolizumab is FDA-approved for multiple cancer types. Primary indications in current trials are advanced/metastatic solid tumors, including breast and genitourinary cancers[1][3][5][6][7][9].

Other names
pembrolizumabMK-0472 + KEYTRUDA
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)PTPN11 (Tyrosine-protein phosphatase non-receptor type 11)

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