Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells ( IC50 =5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease [1].
In Vivo, Icotrokinra (0.03-10 mg/kg; p.o.; once daily for 7 days) acetate reduces the colon weight-to-length ratio and alleviates weight loss in rats with TNBS-induced colitis[1]. Icotrokinra (1-30 mg/kg; p.o.; twice daily for 3 days) acetate prevents IL-23-induced upregulation of IL-17A and IL-22 in a rat skin inflammation model at doses greater than 10 mg/kg[1].
References:
[1]. Fourie AM, et al., JNJ-77242113, a highly potent, selective peptide targeting the IL-23 receptor, provides robust IL-23 pathway inhibition upon oral dosing in rats and humans. Sci Rep. 2024 Jul 30;14(1):17515.
In Vivo, Icotrokinra (0.03-10 mg/kg; p.o.; once daily for 7 days) acetate reduces the colon weight-to-length ratio and alleviates weight loss in rats with TNBS-induced colitis[1]. Icotrokinra (1-30 mg/kg; p.o.; twice daily for 3 days) acetate prevents IL-23-induced upregulation of IL-17A and IL-22 in a rat skin inflammation model at doses greater than 10 mg/kg[1].
References:
[1]. Fourie AM, et al., JNJ-77242113, a highly potent, selective peptide targeting the IL-23 receptor, provides robust IL-23 pathway inhibition upon oral dosing in rats and humans. Sci Rep. 2024 Jul 30;14(1):17515.