C34-PEG4-Chol

C34-PEG4-Chol (Peptivir-H) is a novel, long-acting, cholesterol-tagged peptide HIV fusion inhibitor. It is composed of a peptide derived from the HR-2 region (amino acid residues 117–150) of the HIV-1 envelope glycoprotein gp41, conjugated to a cholesterol moiety via a four-unit polyethylene glycol (PEG4) spacer. This specific conjugation strategy allows the drug to anchor into the lipid rafts of host cell membranes, significantly increasing its local concentration and antiviral potency compared to its parent compound C34 and the approved fusion inhibitor enfuvirtide. Developed by PeptiPharma in collaboration with Imperial College London, the drug was designed to prevent the formation of the six-helix bundle required for virus-cell membrane fusion. A Phase I first-in-human clinical trial in the United Kingdom was halted after participants experienced grade 3 injection site reactions, although no systemic toxicities were reported.

Brand names

Peptivir-H

Other names

C34 polyethylene glycol 4 cholesterolC-34 polyethylene glycol 4 cholesterolC 34 polyethylene glycol 4 cholesterolC34-PEG4-CholesterolC-34-PEG4-CholesterolC 34-PEG4-Cholesterol