IA-14069 is an orally active TNF-α inhibitor for studies related to rheumatoid arthritis.
IA-14069 potently inhibits both TNF-α-induced cytotoxicity (IC50 < 0.7 μM), which directly binds to TNF-α and TNF-α-triggered signaling (p-IκBα and NF-κB p65) activities. The therapeutic and preventive anti-RA effects of IA-14069 were demonstrated in TNF-α-TG and CIA models. IA-14069 and MTX had synergistic effects in the CIA therapeutic model. According to pharmacokinetic analysis, IA-14069 showed significant bioavailability. In addition, no in vivo toxicity was observed even under treatment with an excessive amount of IA-14069[1].
[1] Sung-Dong Park. “THU0047 IA-14069, A NOVEL SMALL-MOLECULE INHIBITOR DIRECT-TARGETING TUMOR NECROSIS FACTOR-α, ATTENUATES COLLAGEN INDUCED ARTHRITIS.” Annals of the Rheumatic Diseases 78 1 (2019): 291–291.
