Drug intelligence / Profile preview

RGX-104 + pembrolizumab + carboplatin + pemetrexed

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

Overview

This is a **combination regimen** consisting of: - **RGX-104**: An orally administered small molecule agonist of Liver X Receptor (LXR), which modulates innate immunity via activation of the ApoE gene. RGX-104 depletes myeloid-derived suppressor cells (MDSC), inhibits tumor angiogenesis, and enhances T-cell activation, potentially overcoming resistance to immunotherapy and chemotherapy. - **Pembrolizumab**: A monoclonal antibody that inhibits the programmed death-1 (PD-1) receptor, acting as a checkpoint inhibitor to activate T-cells against tumor cells. - **Carboplatin**: A platinum-based chemotherapeutic agent that induces DNA crosslinking and apoptosis in rapidly dividing cells. - **Pemetrexed**: An antifolate chemotherapeutic agent that inhibits several enzymes necessary for purine and pyrimidine synthesis, thereby blocking DNA and RNA synthesis in tumor cells. This combination is under investigation, particularly for the treatment of advanced or metastatic non-squamous non-small cell lung cancer (NSCLC), including patients who are refractory to checkpoint inhibitors or have PD-L1-negative tumors[4].

02

Targets

LXRB (Liver X receptor beta)GART (GAR transformylase)NR1H3 (Liver X receptor beta)DHFR (Dihydrofolate reductase)DNAPDCD1 (Programmed cell death protein 1 receptor)TS (Thymidylate synthase)

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