Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM[1][2]. Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-beta activity[3][4]. Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects[5].
