Iguratimod

Iguratimod is a disease-modifying antirheumatic drug (DMARD) and COX-2 inhibitor (IC₅₀ = 7.7 µg/ml).¹ It is selective for COX-2 over COX-1 (IC₅₀ = >300 µg/ml) but also inhibits the tautomerase activity of macrophage migration inhibitory factor (MIF; IC₅₀ = 6.81 µM).^1,2 Iguratimod (1-10 µM) inhibits osteoclastogenesis and bone resorption of isolated mouse bone marrow-derived macrophages stimulated with macrophage colony-stimulating factor (M-CSF) and RANKL, as well as prevents bone loss in ovariectomized mice.³ It decreases disease severity in a rat model of collagen-induced arthritis when administered alone or in combination with methotrexate (Item No. 13960).⁴ Iguratimod (12.5 mg/kg) also decreases disease severity in a MOG_35-55 mouse model of experimental autoimmune encephalomyelitis (EAE) when administered in combination with dexamethasone (Item No. 11015).² Formulations containing iguratimod have been used in the treatment of rheumatoid arthritis.

WARNING This product is not for human or veterinary use.

1. Tanaka, K., Kawasaki, H., Kurata, K., et al. T-614, a novel antirheumatic drug, inhibits both the activity and induction of cyclooxygenase-2 (COX-2) in cultured fibroblasts. Jpn. J. Pharmacol. 67(4), 305-314 (1995).

2. Bloom, J., Metz, C., Nalawade, S., et al. Identification of iguratimod as an inhibitor of macrophage migration inhibitory factor (MIF) with steroid-sparing potential. The Journal of Biological Chemisty 291(51), 26502-26514 (2016).

3. Li, C.-H., Ma, Z.-Z., Jian, L.-L., et al. Iguratimod inhibits osteoclastogenesis by modulating the RANKL and TNF-α signaling pathways. Int. Immunopharmacol. 90, 107219 (2021).

4. Du, F., Lü, L., Fu, Q., et al. T-614, a novel immunomodulator, attenuates joint inflammation and articular damage in collagen-induced arthritis. Arthritis Res. Ther. 10(6), R136 (2008).