Drug intelligence / Profile preview

INCB057643 + pembrolizumab + epacadostat

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

Overview

This is a **combination therapy** consisting of three agents under investigation for advanced malignancies, particularly solid tumors and certain hematological cancers: - **INCB057643** is an orally available, small molecule bromodomain and extra-terminal (BET) protein inhibitor. BET proteins, such as BRD4, regulate gene expression involved in cancer cell proliferation and immune modulation. INCB057643 demonstrates anti-tumor and immunomodulatory effects, especially in preclinical models of pancreatic cancer, by altering tumor microenvironment and immune cell populations. - **Pembrolizumab** is a monoclonal antibody acting as a programmed cell death protein 1 (PD-1) immune checkpoint inhibitor. It blocks the PD-1 receptor on T cells, preventing tumor-induced immune suppression and thereby promoting anti-tumor T cell activity. - **Epacadostat** is a selective small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme responsible for tryptophan catabolism that suppresses T-cell mediated immune response in the tumor microenvironment. Inhibition of IDO1 aims to reverse immune suppression and enhance efficacy of immunotherapies. This triple-drug combination is investigational and being evaluated for **advanced solid tumors** and potentially other malignancies in early-phase clinical trials.

02

Targets

PDCD1 (Programmed cell death protein 1 receptor)IDO1 (Indoleamine 2,3-dioxygenase 1)BRD4 (Bromodomain-containing protein 4)

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