ACT-389949

ACT-389949 is a first-in-class, potent, and selective small molecule agonist of the formyl peptide receptor type 2 (FPR2), also known as the Lipoxin A4 receptor (ALX). It has an EC50 of 3 nM for FPR2/ALX internalization into monocytes. The drug was developed to target inflammatory disorders by enhancing endogenous pro-resolution pathways. In phase 1 clinical studies in healthy subjects, ACT-389949 was well tolerated and demonstrated dose-dependent, long-lasting internalization of FPR2/ALX into leukocytes. However, it caused rapid receptor desensitization and only transient pharmacodynamic responses; biomarker analysis suggested a pro-inflammatory rather than anti-inflammatory effect after dosing. No significant effect on neutrophil recruitment was observed in challenge models. The compound is synthetic organic with a molecular formula C20H18F2N6O3 and has been investigated primarily for its anti-inflammatory potential[1][2][3][5][6].