Risankizumab

Risankizumab (BI 655066) is a humanised IgG monoclonal antibody, targeting IL-23 p19 subunit (Kd <10 pM) and inhibiting IL-17 production induced by human IL-23 in mouse splenocytes (IC50 = 2 pM). Risankizumab can be used to research immunological and inflammatory disorders such as psoriasis vulgaris, psoriatic arthritis, generalized pustular psoriasis and erythrodermic psoriasis[1][2][3].

Signaling Pathways >> Immunology/Inflammation >> Interleukin Related

Research Areas >> Inflammation/Immunology

IL-23:<10 pM (Kd)

Risankizumab (BI 655066) has a high affinity for human and cynomolgus IL23 with Kds <10 pM[3]. Risankizumab (BI 655066) inhibits endogenous (THP-1 cell generated) human IL23-induced and recombinant cynomolgus IL23-induced IL17 production with IC50s of 2 pM and 17 pM, respectively[3].

Risankizumab (BI 655066) (1 mg/kg; i.p.; single dosage) inhibits IL23-induced mice ear swelling and cytokine production[3]. Animal Model: Mice (injected with BI 655066, 1 h later injected recombinant human IL23 into the skin of the mouse ear for 4 days)[3] Dosage: 1 mg/kg Administration: i.p.; single dosage Result: Significantly inhibited IL23-induced ear swelling and cytokine production. Animal Model: Cynomolgus monkeys[3] Dosage: 1.0 mg/kg Administration: i.v. or s.c. Result: Pharmacokinetic Parameters of Risankizumab (BI 655066) in cynomolgus monkeys[1]. IV (1 mg/kg) SC (1 mg/kg) AUCinf (μg·day/mL) 202 ± 33.5 142 ± 33.3 CL (mL/day/kg) 5.18 ± 0.8 / Vd, ss (mL/kg) 88.3 ± 3.12 / t1/2 (h) 12.2 ± 2.28/ 9.15 ± 1.87 Cmax (μg/mL) / 10.1 ± 3.14 Tmax (day) / 2.11 ± 1.84 F (%) / 70.4 ± 16.5

[1]. McKeage K, Duggan S. Risankizumab: First Global Approval. Drugs. 2019 Jun;79(8):893-900.

[2]. Andrea Chiricozzi, et al. Risankizumab for the treatment of moderate to severe psoriasis. Expert Opinion on Biological Therapy. Volume 19, 2019 - Issue 1

[3]. Singh S, et al. Selective targeting of the IL23 pathway: Generation and characterization of a novel high-affinity humanized anti-IL23A antibody. MAbs. 2015;7(4):778-91.