Halofuginone is a coccidiostat used in veterinary medicine. This synthetic enzyme inhibitor is derived from febrifugine, a quinazoline alkaloid isolated inDichroa febrifuga. As a halogenated quinazoline derivative, Halofuginone contains a fused pair of aromatic rings, benzene and pyrimidine.
The chemical selectively regulates the autoimmune disease-promotive T helper 17 cell development. Halofuginone also controls cell migration, collagen type I synthesis and MMP-2 gene expression to inhibit proliferative tumor activity. In mice, Halofuginone has suppressed tumors and cancerous metastasis by functioning as a high-affinity inhibitor to glutamyl-prolyl tRNA synthetase. This inhibition induces anti-inflammatory and anti-fibrotic effects by means of the amino acid starvation response.
Medicinally, Halofuginone qualifies as an anti-inflammatory, antiprotozoal and anti-angiogenic agent. When fed to animals, it prevents coccidiosis. In studies of osteoarthritis, Halofuginone inhibited TGF-β activity and H-type vessel formation, attenuating the condition.