Drug intelligence / Profile preview

epacadostat + pembrolizumab + carboplatin + paclitaxel

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

Overview

Epacadostat + pembrolizumab + carboplatin + paclitaxel is a multi-agent combination therapy evaluated in advanced and metastatic solid tumors, especially non-small cell lung cancer (NSCLC). **Epacadostat** is an oral small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1), an enzyme involved in immunosuppressive tryptophan metabolism. **Pembrolizumab** is a monoclonal antibody targeting programmed death 1 (PD-1), a checkpoint inhibitor that activates anti-tumor immunity. **Carboplatin** is a platinum-based cytotoxic chemotherapy agent, while **paclitaxel** is a microtubule-stabilizing chemotherapeutic. The rationale for this regimen is to inhibit IDO1-mediated immunosuppression, release PD-1 checkpoint-mediated immune inhibition, and induce direct tumor cytotoxicity via chemotherapy. Multiple phase I/II studies have evaluated this combination in NSCLC and other solid tumors. While the regimen demonstrated an acceptable safety profile, clear added efficacy from epacadostat in combination with pembrolizumab and chemotherapy has not been established, and later-phase trials failed to show benefit from adding epacadostat over pembrolizumab plus chemotherapy alone[1][2][3][4].

02

Targets

TUBB (Tubulin (alpha and beta subunits))IDO1 (Indoleamine 2,3-dioxygenase 1)DNAPDCD1 (Programmed cell death protein 1 receptor)

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