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Risankizumab

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Risankizumab Basic information

Product Name:
Risankizumab
Synonyms:
  • Immunoglobulin G1, anti-(human interleukin 23 subunit p19) (human-Mus musculus heavy chain), disulfide with human-Mus musculus κ-chain, dimer
  • Risankizumab
  • Research Grade Risankizumab (DHJ63101)
  • Risankizumab (anti-IL-23)
  • Risankizumab rzaa|||SKYRIZI|||ABBV 066|||BI-655066
  • Research Grade Risankizumab
CAS:
1612838-76-2
MW:
0
Mol File:
Mol File
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Risankizumab Chemical Properties

form 
Liquid
color 
Colorless to light yellow
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Risankizumab Usage And Synthesis

Description

Risankizumab is a fully humanized IgG1 monoclonal antibody (mAb) directed against interleukin 23 (IL-23). It gained its first global approval in Japan in March 2019, followed by approval in Canada, the US, and Europe in April 2019. Risankizumab is used to treat plaque psoriasis, psoriatic arthritis, and Crohn's disease. Risankizumab is being investigated for atopic dermatitis.

Uses

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].

in vivo

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 ± 33.5142 ± 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

IC 50

IL-23: <10 pM (Kd)

Mode of action

Risankizumab is an Interleukin-23 Antagonist which is used to treat moderate-to-severe plaque psoriasis. The mechanism of action of risankizumab is as an Interleukin-23 Antagonist. It is generally well tolerated and is associated with a low rate of serum aminotransferase elevations during therapy, but has not been linked to instances of clinically apparent liver injury.

References

[1] McKeage K, Duggan S. Risankizumab: First Global Approval. Drugs. 2019 Jun;79(8):893-900. DOI:10.1007/s40265-019-01136-7
[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. DOI:10.1080/19420862.2015.1032491

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