Ustekinumab Overview

Introduction of Ustekinumab

Ustekinumab (L04AC05) is a humanized IgG1κ monoclonal antibody developed by the biotechnology company Centocor. It was designed to target interleukins IL-12 and IL-23, which are the member of interleukin 12 (IL-12) family cytokines. Ustekinumab acts as a human immunosuppressive drug used to treat psoriasis. With the trade name Stelara, ustekinumab was approved by the U.S. Food and Drug Administration (FDA), Health Canada, and European Medicines Agency for the treatment of plaque psoriasis and psoriatic arthritis in 2009. Besides, the medication was approved by FDA for the treatment of moderate-severe Crohn's disease in September 2016.

Mechanism of Action of Ustekinumab

Interleukin-23 (IL-23) is a pro-inflammatory cytokine composed of an IL12B (IL-12p40) subunit (that is shared with IL12) and the IL23A (IL-23p19) subunit. Il-23 exerts its biological fnction through its functional receptor, which is composed of IL-12R β1 and IL-23R. IL-23 has been demonstrated to be related with IL-23- dependent differentiation and activation of Th-17 cells, IL-17 and IL-22 cytokine production and secretion. This results in synovium and skin inflammation as well as bone remodeling. IL-12 is a heterodimeric cytokine composed of two subunits, IL-12A (p35) and IL-12B (p40). Binding of IL-12 to its receptor, IL-12R, induces the transduction of cellular signal pathway known as JAK-STAT. Both IL-23 and IL-12 are considered as the key cytokines in inflammatory diseases. Ustekinumab is designed to bind specifically to the p40 subunit of IL-12 and IL-23, blocking their interaction with their receptors. This inhibits the downstream Th-17 signaling pathways and interferes with the triggering of inflammatory response, disrupting the proinflammatory pathways in several chronic diseases.

Fig.1 Mechanism of action of Ustekinumab

Table 1. Clinical Projects of Ustekinumab*

Table 2. Approved Drugs of Trastuzumab**

INN (trade name)	Therapeutic area	Dose	Strength	Route	Company	Marketing start	Market
Stelara	Adult patients with moderately to severely active Crohn’s disease	Powder for injection	5mg/1 mL	Intravenous injection	Janssen Biotech Inc.	September 23, 2016
Stelara	Moderate to severe plaque psoriasis	Powder for injection	90mg/1 mL	Subcutaneous injection	Janssen Biotech Inc.	September 25, 2009
Stelara	Crohn’s Disease/ Plaque psoriasis/ Paediatric plaque psoriasis	Powder for injection	5mg/1 mL, 90mg/1 mL	Intravenous/ Subcutaneous infusion	Janssen Biotech Inc.	January, 16, 2009
Stelara	Adults with Psoriatic Arthritis/ Plaque Psoriasis/ Children 12 to 17 years of age with Plaque Psoriasis	Powder for injection	90mg/1 mL	Subcutaneous infusion	Janssen Biotech Inc.	December 12, 2008
Stelara	Adult patients with moderately to severely active Crohn’s disease (CD)	Powder for injection	5 mg/mL	Intravenous infusion	Janssen Biotech Inc.	December 14, 2016
Stelara	Crohn's Disease	Powder for injection	5.0 mg / 1 m	Intravenous infusion	Janssen-Cilag Pty Ltd	January /03/2017

What We Provide

Therapeutic Antibody

Ustekinumab

We provide high-quality Ustekinumab for use in WB, FC, IP, ELISA, Neut, FuncS, IF and most other immunological methods. For lab research use only, not for diagnostic, therapeutic or any in vivo human use.

Reference
* The table was excerpted from the following website
https://clinicaltrials.gov/ct2/results?cond=&term=Ustekinumab

** Information presented in the table were collected from the following websites:
http://search.tga.gov.au/s/search.html?collection=tga-artg&profile=record&meta_i=282906
https://www.accessdata.fda.gov/scripts/cder/daf/index.cfm?event=BasicSearch.process

For research use only. Not intended for any clinical use.