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epacadostat + pembrolizumab + carboplatin + pemetrexed
- Development stage
- Phase 2
- Lead developer
- Incyte
- Modality
- Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
- Administration
- Oral, Intravenous
01
Overview
This is a combination regimen of **epacadostat**, a selective small molecule inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1); **pembrolizumab**, a monoclonal antibody programmed death-1 (PD-1) immune checkpoint inhibitor; **carboplatin**, a platinum-based DNA crosslinking chemotherapeutic agent; and **pemetrexed**, a multi-targeted antifolate chemotherapeutic agent. This combination was investigated for the treatment of advanced or metastatic non-small cell lung cancer (NSCLC) without actionable mutations. The rationale was to combine tumor immune environment modulation (IDO1 inhibition by epacadostat), checkpoint blockade (pembrolizumab), and cytotoxic chemotherapy (platinum doublet). Clinical trials found this regimen to be generally well tolerated, but the addition of epacadostat did not improve efficacy endpoints compared to pembrolizumab plus chemotherapy, and there were some signals of increased toxicity leading to more frequent dose modification and discontinuation[1][3].
- Other names
- epacadostat plus pembrolizumab plus carboplatin plus pemetrexed
02
Targets
DNAIDO1 (Indoleamine 2,3-dioxygenase 1)PDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)GART (GAR transformylase)
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