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pegargiminase + mFOLFOX6
- Development stage
- Discontinued
- Lead developer
- Polaris Pharmaceuticals
- Modality
- Classical Binding Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules, Therapeutic Enzymes → Recombinant Proteins and Enzymes
- Administration
- Intravenous (mFOLFOX6), Intramuscular (pegargiminase/ADI-PEG 20)
01
Overview
**pegargiminase + mFOLFOX6** is an experimental combination therapy comprising pegargiminase (ADI-PEG 20), a pegylated recombinant arginine deiminase enzyme, and the chemotherapy regimen mFOLFOX6, which includes oxaliplatin, leucovorin (folinic acid), and fluorouracil (5-FU). Pegargiminase depletes systemic arginine, interfering with tumor cell metabolism—particularly in arginine-auxotrophic tumors like hepatocellular carcinoma—and alters nucleotide biosynthesis and DNA repair, potentially enhancing cytotoxicity of chemotherapies. mFOLFOX6 exerts cytotoxic effects mainly through DNA crosslinking and inhibition of DNA synthesis. The combination has been investigated for its safety and efficacy in advanced gastrointestinal malignancies, especially hepatocellular carcinoma, in a phase 1 clinical trial, with favorable safety and promising antitumor activity[1]. Developers for pegargiminase include Polaris Pharmaceuticals, and mFOLFOX6 is a standard chemotherapy regimen with no singular commercial developer.
- Other names
- pegargiminase + modified FOLFOX6ADI-PEG 20 + mFOLFOX6pegylated arginine deiminase + mFOLFOX6
02
Targets
DNATS (Thymidylate synthase)
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