BMS-986504 + pembrolizumab

BMS-986504 + pembrolizumab is a novel investigational **combination therapy** currently studied primarily for first-line treatment of metastatic non-small cell lung cancer (NSCLC) with homozygous MTAP (methylthioadenosine phosphorylase) deletion. BMS-986504 is a **selective MTA-cooperative inhibitor of PRMT5 (protein arginine methyltransferase 5)**, designed to exploit synthetic lethality in MTAP-deficient cancer cells: when MTAP is deleted, methylthioadenosine (MTA) accumulates and binds PRMT5, enabling BMS-986504 to specifically inhibit PRMT5’s enzymatic activity in tumor cells while sparing healthy ones[1][4][5]. Pembrolizumab is a **humanized monoclonal antibody** that blocks the PD-1 receptor, thereby inhibiting immune checkpoint signaling, unleashing anti-tumor immune responses. The combination aims to maximize both direct tumor cell killing and immune-mediated effects. Collaboratively developed and studied by **Bristol Myers Squibb** and involving Merck’s Keytruda (pembrolizumab), this regimen is currently under phase 2/3 clinical investigation for NSCLC and may be relevant for other solid tumors with MTAP loss[1][3][4][5].

Other names

pembrolizumabPRMT5-MTA inhibitor + pembrolizumab