Drug intelligence / Profile preview

pembrolizumab + imatinib

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

Overview

Pembrolizumab + imatinib is a combination therapy under investigation primarily for the treatment of unresectable or metastatic melanoma with KIT mutations. Pembrolizumab is a monoclonal antibody that targets programmed cell death protein 1 (PD-1), acting as an immune checkpoint inhibitor to enhance T-cell mediated anti-tumor responses. Imatinib is a small molecule tyrosine kinase inhibitor that targets c-KIT and platelet-derived growth factor receptor alpha (PDGFRα), inhibiting oncogenic signaling in tumors with relevant mutations. The rationale for combining these agents stems from evidence suggesting synergistic effects in KIT-mutant melanoma, where imatinib may sensitize tumors to immunotherapy by modulating the tumor microenvironment and enhancing immune cell activity[1][2][3][4][5]. Clinical trials have shown promising responses in some patients resistant to prior immunotherapies.

Other names
pembrolizumab mesylateimatinib mesylate
02

Targets

KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDCD1 (Programmed cell death protein 1 receptor)

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