Stelara Ustekinumab Injection

1. Indications and Usage
Plaque Psoriasis (PsO): Treatment of adult and pediatric patients (≥6 years of age) with moderate to severe plaque psoriasis who are candidates for systemic therapy or phototherapy.
Psoriatic Arthritis (PsA): Treatment of adult patients with active PsA, as monotherapy or in combination with methotrexate (MTX).
Crohn’s Disease (CD): Treatment of adult patients with moderately to severely active CD.
Ulcerative Colitis (UC): Treatment of adult patients with moderately to severely active UC.
2. Dosage and Administration
Route of Administration:
PsO & PsA: For Subcutaneous Injection ONLY.
CD & UC: For Intravenous (IV) Induction, followed by Subcutaneous Maintenance.
Recommended Dosage:
Plaque Psoriasis:
≤100 kg: 45 mg at Weeks 0 and 4, then every 12 weeks.
>100 kg: 90 mg at Weeks 0 and 4, then every 12 weeks.
Psoriatic Arthritis: 45 mg at Weeks 0 and 4, then every 12 weeks. (90 mg may be considered for patients >100 kg).
Crohn’s Disease & Ulcerative Colitis:
Induction: Single IV infusion (weight-based dosing, approx. 6 mg/kg).
Maintenance: Subcutaneous injection (90 mg or 180 mg) starting 8 weeks after the IV infusion, then every 8 or 12 weeks.
3. Mechanism of Action
Dual Pathway Inhibition:
Ustekinumab is a human IgG1κ monoclonal antibody that binds specifically to the p40 subunitshared by both IL-12 and IL-23.
Blocking Signaling:
By binding to the p40 subunit, it prevents these cytokines from interacting with their receptors on the cell surface.
Downstream Effect:
IL-12 and IL-23 are key drivers of inflammation. IL-12 drives Th1 responses, while IL-23 is critical for the differentiation and maintenance of Th17 cells. Blocking both pathways modulates the inflammatory cascade responsible for psoriasis and IBD.
4. Safety and Warnings
Infections:
Ustekinumab may increase the risk of infections. Evaluate patients for tuberculosis (TB) prior to initiating therapy.
Malignancy:
No data on long-term safety regarding malignancy.
Hypersensitivity:
Hypersensitivity reactions (e.g., angioedema, urticaria, serum sickness-like reactions) have been reported.
Vaccinations:
Avoid live vaccines during treatment.
5.Adverse Reactions
Most Common (Incidence ≥3% and greater than placebo):
Nasopharyngitis, headache, fatigue, upper respiratory tract infection, and injection site reactions.
6.Drug Interactions
CYP450 Substrates:
Blocking IL-12/23 signaling may normalize CYP450 enzyme activity. Monitor dosage of CYP substrates when starting or stopping ustekinumab.
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Ustekinumab.
Available Strength: 45 mg/0.5 mL, 90 mg/1 mL (prefilled syringes/pens); IV solution for infusion.
Appearance: Clear to slightly opalescent, colorless to pale yellow liquid.
Storage: Store at 2°C to 8°C (36°F to 46°F) in the original carton to protect from light.