Drug intelligence / Profile preview

INCB001158 + pembrolizumab

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

Overview

INCB001158 + pembrolizumab is an investigational combination therapy for advanced or metastatic solid tumors. INCB001158 is an orally bioavailable small-molecule inhibitor of both arginase isoforms (Arg1/Arg2), designed to reverse T-cell immunosuppression in the tumor microenvironment and enhance antitumor immune responses. Pembrolizumab is a monoclonal antibody targeting programmed death protein 1 (PD-1), functioning as an immune checkpoint inhibitor to promote T-cell mediated antitumor activity. The combination aims to synergistically improve immune-mediated tumor control by simultaneously blocking arginase-mediated immunosuppression and PD-1–mediated inhibition of T cells. Clinical studies have evaluated this combination in various advanced/metastatic solid tumors, including non-small cell lung cancer, melanoma, urothelial carcinoma, colorectal cancer (MSI/MSS), gastric cancer, head and neck squamous cell carcinoma, and mesothelioma[1][2][3][4].

02

Targets

ARG2 (Arginase 2)PDCD1 (Programmed cell death protein 1 receptor)ARG1 (Arginase 1)

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