Drug intelligence / Profile preview

pembrolizumab + epacadostat + platinum-based chemotherapy

Development stage
Unknown
Lead developer
Merck
Modality
Nucleic Acid-Directed Small Molecules → Small Molecules, Monoclonal Antibodies → Antibody-Based Therapeutics, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
Administration
Intravenous (pembrolizumab/chemotherapy), Oral (epacadostat)
01

Overview

This is a combination regimen composed of **pembrolizumab** (an anti-PD-1 monoclonal antibody), **epacadostat** (an oral, selective inhibitor of indoleamine 2,3-dioxygenase 1 [IDO1]), and **platinum-based chemotherapy** (which may include agents such as cisplatin, carboplatin, and pemetrexed, or carboplatin with paclitaxel; the specific platinum agent is selected based on tumor type). - **Pembrolizumab** blocks the programmed death-1 (PD-1) pathway and reactivates T-cell antitumor immune responses. - **Epacadostat** inhibits IDO1, blocking tryptophan metabolism to kynurenine, a pathway mediating immune suppression in the tumor microenvironment. - **Platinum-based chemotherapy** damages DNA, inducing apoptosis in dividing cancer cells. The rationale for the combination is to simultaneously target cancer cells (chemotherapy), inhibit a key immunosuppressive pathway (IDO1), and unleash T-cell-mediated antitumor immunity via checkpoint inhibition. This combination has been investigated primarily as a first-line treatment in patients with advanced or metastatic non-small cell lung cancer (NSCLC), and in other solid tumors, with the aim of improving response rates beyond immunotherapy or chemotherapy alone[1][2][4].

Brand names
Keytruda + epacadostat + platinum-based chemotherapy
Other names
pembrolizumab + epacadostat + platinum-based chemotherapy
02

Targets

PDCD1 (Programmed cell death protein 1 receptor)

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