JE-2147

Summary

JE-2147 (also known as AG-1776 or KNI-764) is a peptidomimetic HIV protease inhibitor developed in the late 1990s. It incorporates a allophenylnorstatine-based core structure and demonstrates potent activity against HIV-1 and HIV-2, including some multidrug-resistant strains. It was primarily investigated as a research tool and did not advance to approved clinical use.

Mechanism of Action

Competitive inhibitor of HIV-1 and HIV-2 aspartyl protease; binds the active site of the viral protease, preventing cleavage of Gag and Gag-Pol polyprotein precursors, thereby blocking maturation of infectious viral particles.

Routes of Administration

Goals & Uses

• HIV-2 protease inhibitionAntiviralLow
• HIV-1 protease inhibitionAntiviralModerate
• Research tool for protease resistance studiesResearchModerate
• Activity against drug-resistant HIV strainsAntiviralModerate

Contraindications

• Not established for clinical useGeneralHigh

Adverse Effects

• Unknown human safety profileGeneralUnknown

Drug Interactions

• CYP3A4 substrates/inhibitorsLow

Population Constraints

• General populationGeneralAbsolute

Regulatory Status

• European UnionUnapprovedNo marketing authorization; research use only.
• United StatesUnapprovedResearch compound only; no IND or NDA filed as publicly known.
• United KingdomUnapprovedNo regulatory approval; laboratory research compound.

JE-2147 has not received regulatory approval in any jurisdiction. It remains a research/investigational compound used primarily in laboratory studies of HIV protease inhibition and resistance mechanisms.

Evidence & Sources

No sources recorded yet.