napabucasin + pembrolizumab

Napabucasin + pembrolizumab is a combination of a **cancer stemness inhibitor (napabucasin, BBI608)** and a **PD-1 immune checkpoint inhibitor (pembrolizumab, Keytruda)**. Napabucasin inhibits signal transducer and activator of transcription 3 (STAT3), downregulates WNT/β-catenin signaling, and impacts PD-L1 expression, which are pathways involved in tumor immune evasion and resistance to checkpoint inhibitors[3][4][6]. Pembrolizumab acts by blocking PD-1, thereby enhancing T cell-mediated antitumor immunity. This combination is being developed primarily for **metastatic colorectal cancer (mCRC)**, especially in populations poorly responsive to immunotherapy, such as microsatellite stable (MSS) tumors. Clinical trials have demonstrated acceptable safety and preliminary evidence of antitumor activity, particularly in microsatellite instability-high (MSI-H) cohorts, with some activity also reported in MSS cases[1][3][4][6].

Other names

napabucasin plus pembrolizumabnapabucasin and pembrolizumabBBI608 + pembrolizumab