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INCB001158 + epacadostat + pembrolizumab

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

Overview

INCB001158 + epacadostat + pembrolizumab is an investigational combination therapy for advanced/metastatic solid tumors. - **INCB001158** is a small molecule **arginase inhibitor** designed to attenuate immune suppression within the tumor microenvironment, thereby enhancing antitumor immune response. - **Epacadostat** is a potent, selective **indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor**, intended to shift the tumor microenvironment toward immune stimulation by reducing tryptophan metabolism. - **Pembrolizumab** is a monoclonal antibody targeting **programmed cell death protein 1 (PD-1)**, functioning as a checkpoint inhibitor to potentiate T-cell-mediated antitumor immunity. The combination aims to synergistically block immune suppression through both arginase and IDO1 enzymatic pathways and restore T cell activity via PD-1 blockade. Primary indications under investigation have included advanced/metastatic solid tumors such as colorectal, stomach, esophageal, head and neck, small cell lung, kidney, bladder cancer, and mesothelioma[1][5][7].

Other names
INCB01158INCB-01158INCB 01158ECHO-202/KEYNOTE-037 (combination trial code)ECHO-207/KEYNOTE-723 (related combination study)
02

Targets

IDO1 (Indoleamine 2,3-dioxygenase 1)ARG1 (Arginase 1)PDCD1 (Programmed cell death protein 1 receptor)

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