Dosing and uses of Stelara (ustekinumab)
Adult dosage forms and strengths
injectable solution for SC
- 45mg/0.5mL (prefilled syringe or single-dose vial)
- 90mg/mL (prefilled syringe)
injectable solution for IV infusion
- 130mg/26mL (5mg/mL) single-dose vial
Plaque Psoriasis
Indicated for the treatment of adults (18 years or older) with moderate-to-severe plaque psoriasis who are candidates for phototherapy or systemic therapy
≤100 kg: 45 mg SC initially, THEN 4 weeks later give 45 mg SC, and THEREAFTER 45 mg SC q12weeks
>100 kg: 90 mg SC initially, THEN 4 weeks later give 90 mg SC, and THEREAFTER 90 mg SC q12weeks
FDA Medication Guide required to be given to patient with each new outpatient prescription and refilL
Psoriatic Arthritis
Indicated for adults with active psoriatic arthritis alone or in combination with methotrexate
45 mg SC initially, THEN 4 weeks later give 45 mg SC, and THEREAFTER 45 mg SC q12 weeks
For patients >100 kg with co-existent moderate-to-severe plaque psoriasis, increase dose to 90 mg SC initially, THEN 4 weeks later, give 90 mg SC, and THEREAFTER 90 mg SC q12 weeks
Crohn Disease
Indication
- Indicated for adults with moderately to severely active Crohn disease who have
- Failed or were intolerant to immunomodulators or corticosteroids, but never failed treatment with a tumor necrosis factor (TNF) blocker OR
- Failed or were intolerant to treatment with ≥1 TNF blockers
Initial weight-based IV dose
- Single IV dose infused over 1 hr (also see maintenance dose below)
- ≤55 kg: 260 mg IV
- >55 kg to 85 kg: 390 mg IV
- >85 kg: 520 mg IV
Maintenance dose
- Begin 90 mg SC 8 weeks after the initial IV infusion, then q8wk thereafter
Dosage modifications
Renal or hepatic impairment: Safety and efficacy not established
Diabetes Mellitus Type 1 (Orphan)
Orphan designation for patients with type I DM with residual beta-cell function
Orphan sponsor
- Johnson & Johnson Pharmaceutical & Development LLC; 902 Route 202 South; Room 1654; Raritan, NJ 08869
Biliary Cirrhosis (Orphan)
Orphan designation of ustekinumab; human monoclonal antibody to interleukin 12p40 for treatment of primary biliary cirrhosis
Orphan sponsor
- Janssen Biotech, Inc; 200 Great Valley Parkway; Malvern, PA 19355-1307
Pediatric dosage forms and strengths
<18 years: Safety and efficacy not established
Stelara (ustekinumab) adverse (side) effects
>10%
Upper respiratory infection
1-10%
Nasopharyngitis
Back pain
Cellulitis
Depression
Diarrhea
Fatigue
Headache
Injection site erythema
Myalgia
Fatigue
Nasal congestion
Urticaria
Rash
Pruritus
Antibody formation
<1% (selected)
Severe infection
Malignancy
Reversible posterior leukoencephalopathy syndrome
Postmarketing Reports
Immune system disorders: Serious hypersensitivity reactions (including anaphylaxis and angioedema), other hypersensitivity reactions (including rash and urticaria)
Skin reactions: Pustular psoriasis, erythrodermic psoriasis
Warnings
Contraindications
Hypersensitivity
Active serious infection
Concomitant live vaccines
- Discontinue at least 15 weeks before live vaccines
- Resume at least 2 weeks later
Cautions
May increase risk of infections and reactivation of latent infections; serious bacterial, fungal, and viral infections observed with treatment; evaluate for TB infection prior to administration
Other serious infections requiring hospitalization reported including diverticulitis, cellulitis, pneumonia, appendicitis, cholecystitis, sepsis, osteomyelitis, viral infections, gastroenteritis, and UTIs
Increased risk of malignancy
Reports of the rapid appearance of multiple cutaneous squamous cell carcinomas in patients with pre-existing risk factors for developing nonmelanoma skin cancer; monitor all patients for nonmelanoma skin cancer
Avoid pregnancy
Provide age-appropriate immunization prior to initiating therapy
Administration of live-virus to household contacts
Hypersensitivity reactions reported, including anaphylaxis and angioedema
Use caution in patients genetically deficient in IL-12/IL-23
Psoriasis studies the safety of ustekinumab in combination with immunosuppressive agents or phototherapy has not been evaluated; in psoriatic arthritis studies, concomitant methotrexate use did not appear to influence the safety or efficacy
May decrease the protective effect of allergen immunotherapy
Reversible posterior leukoencephalopathy syndrome reported (1 case)
Pregnancy and lactation
Pregnancy category: B
Lactation: use caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Stelara (ustekinumab)
Mechanism of action
Fully human monoclonal antibody that antagonizes interleukin-12 and -23
Pharmacokinetics
Bioavailability: 57% (SC)
Peak Plasma Time: 7-13.5 days
Vd (terminal elimination phase): 96-264 mL/kg
Half-Life elimination: 10-126 days
Clearance: 1.62-2.85 mL/day/kg
Administration
SC Preparation
Visually inspect for particulate matter and discoloration
Solution should appear clear, colorless to light yellow and may contain a few small translucent or white particles
Do not use if it is discolored or cloudy, or if other particulate matter is present
Does not contain preservatives; therefore, discard any unused product remaining in the vial and/or syringe
SC Administration
See full prescribing information for how to use prefilled syringe injector
Each injection should be administered at a different anatomic location (eg, upper arms, gluteal regions, thighs, or any quadrant of abdomen) than the previous injection
Do not inject into areas where the skin is tender, bruised, erythematous, or indurated
When using the single-dose vial, a 27-gauge, 0.5-inch needle is recommended
IV Preparation
Must be diluted, prepared and infused by a healthcare professional using aseptic technique
Calculate dose and the number of ustekinumab vials needed based on patient weight (see Adult Dosing)
Each 26 mL vial contains 130 mg of ustekinumaB
Withdraw, and then discard a volume of the 0.9% NaCl from the 250 mL infusion bag equal to the volume ustekinumab to be added (discard 26 mL NaCl for each vial of needed, for 2 vials- discard 52 mL, for 3 vials- discard 78 mL, 4 vials- discard 104 mL)
Withdraw 26 mL from each vial needed and add it to the 250 mL infusion bag
The final volume in the infusion bag should be 250 mL
Gently mix
Visually inspect the diluted solution before infusion
Do not use if visibly opaque particles, discoloration or foreign particles are observed
IV Administration
Infuse the diluted solution over a period of at least 1 hr
Once diluted, the infusion solution may be stored for up to 4 hr prior to infusion
Use only an infusion set with an in-line, sterile, nonpyrogenic, low protein-binding filter (pore size 0.2 micrometer)
Do not infuse concomitantly in the same IV line with other agents
Does not contain preservatives
Each vial is for single use only
Discard any remaining solution
Storage
Vials and prefilled syringes must be refrigerated at 2-8°C (36-46°F)
Store vials upright
Keep the product in the original carton to protect from light until the time of use
Do not freeze
Do not shake
Diluted IV solution
- If necessary, the diluted infusion solution may be stored for up to 4 hr at room temperature up to 25°C (77°F)
- Do not freeze
- Discard any unused portion of the infusion solution
