Dosing & Uses
Dosage Forms & 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 and adolescents aged ≥12 years with moderate-to-severe plaque psoriasis who are candidates for phototherapy or systemic therapy
≤100 kg: 45 mg SC at Weeks 0 and 4, then q12weeks thereafter
>100 kg: 90 mg SC at Weeks 0 and 4, then q12weeks thereafter
Psoriatic Arthritis
Indicated for adults with active psoriatic arthritis alone or in combination with methotrexate
45 mg SC at Weeks 0 and 4, then q12weeks thereafter
For patients >100 kg with co-existent moderate-to-severe plaque psoriasis, increase dose to 90 mg SC at Weeks 0 and 4, then q12weeks thereafter
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
Orphan Designations
Primary biliary cirrhosis
Patients with type I DM with residual beta-cell function
Sponsor
- Janssen Biotech, Inc; 200 Great Valley Parkway; Malvern, PA 19355-1307
Dosage Forms & Strengths
injectable solution for SC
- 45mg/0.5mL (prefilled syringe or single-dose vial)
- 90mg/mL (prefilled syringe)
Plaque Psoriasis
Indicated for treatment of adolescents aged ≥12 years with moderate-to-severe plaque psoriasis who are candidates for phototherapy or systemic therapy
<12 years: Safety and efficacy not established
≥12 years
- <60 kg: 0.75 mg/kg SC at Weeks 0 and 4, then q12weeks thereafter
- 60-100 kg: 45 mg SC at at Weeks 0 and 4, then q12weeks thereafter
- >100 kg: 90 mg SC at Weeks 0 and 4, then q12weeks thereafter
- See also Administration
Orphan Designations
Pediatric ulcerative colitis
Pediatric systemic lupus erythematosus (SLE)
Sponsor
- Janssen Biotech, Inc; 1400 McKean Road, Spring House, Pennsylvania 19477
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse 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
Respiratory, thoracic and mediastinal disorders: Interstitial pneumonia, eosinophilic pneumonia and cryptogenic organizing pneumonia
Warnings
Contraindications
Hypersensitivity
Active serious infection
Concomitant live vaccines
Cautions
Use caution in patients genetically deficient in IL-12/IL-23
Reversible posterior leukoencephalopathy syndrome (RPLS) reported (1 case); if RPLS is suspected, administer appropriate therapy and discontinue treatment
Provide age-appropriate immunization prior to initiating therapy
Hypersensitivity reactions reported, including anaphylaxis and angioedema
Infections
- Do not administer treatment to patients with active tuberculosis infection; initiate treatment of latent tuberculosis (TB) prior to administering ustekinumab; closely monitor for signs and symptoms of active tuberculosis during and after treatment
- May increase risk of infections and reactivation of latent infections; serious bacterial, fungal, and viral infections observed with treatment; evaluate for TB infection before initiating drug
- Cases of interstitial pneumonia, eosinophilic pneumonia and cryptogenic organizing pneumonia have been reported; if diagnosis is confirmed, discontinue therapy and institute appropriate treatment
- Other serious infections requiring hospitalization reported include diverticulitis, cellulitis, pneumonia, appendicitis, cholecystitis, sepsis, osteomyelitis, viral infections, and UTIs
- In patients with Crohn’s disease, serious or other clinically significant infections included anal abscess, gastroenteritis, ophthalmic herpes, pneumonia, and listeria meningitis
- Treatment should not be initiated in patients with any clinically important active infection until infection resolves or is adequately treated; consider risks and benefits of treatment prior to initiating therapy in patients with a chronic infection or a history of recurrent infection
- Instruct patients to seek medical advice if signs or symptoms suggestive of infection occur and consider discontinuing therapy for serious or clinically significant infections until infection resolves or is adequately treated
Malignancies
- 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
Drug interactions overview
- Formation of CYP450 enzymes can be altered by increased levels of certain cytokines (eg, IL-1, IL-6, IL-10, TNFα, IFN) during chronic inflammation; ustekinumab (IL-12 and IL-23 antagonist) may normalize the formation of CYP450 enzyme; monitor therapeutic effects (eg, warfarin) or concentration (eg, cyclosporine) with concomitant CYP450 substrates use (especially narrow therapeutic index drugs)
- 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
- Avoid use of live vaccines with ustekinumab
- BCG vaccines should not be given during treatment or for one year prior to initiating treatment or one year following discontinuation of treatment; use caution when administering live vaccines to household contacts of patients receiving treatment due to the potential risk for shedding from the household contact and transmission to patient
Pregnancy & Lactation
Pregnancy
Pregnancy registry (1-877-311-8972) available that monitors pregnancy outcomes in women exposed to ustekinumab during pregnancy
Limited data on ustekinumab use in pregnant women to inform a drug associated risk
In animal reproductive and developmental toxicity studies, no adverse developmental effects were observed after administration of ustekinumab to pregnant monkeys at exposures greater than 100 times the human exposure at the maximum recommended human subcutaneous dose (MRHD)
Lactation
Data are not available on the presence of ustekinumab in human milk, effects on the breastfed infant, or effects on milk production
Developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for ustekinumab and any potential adverse effects on the breastfed child from ustekinumab or from the underlying maternal condition
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
Mechanism of Action
Human IgG1қ monoclonal antibody binds to the p40 protein subunit used by IL-12 and IL-23 cytokines; IL-12 and IL-23 are involved in inflammatory and immune responses (eg, natural killer cell activation, CD4+ T-cell differentiation, and activation)
Absorption
Bioavailability: 57% (SC)
Peak plasma time: 13.5 days (45 mg-dose); 7 days (90 mg-dose)
Distribution
Vd (steady-state): 4.62 L
Metabolism
Ustekinumab is expected to be degraded into small peptides and amino acids via catabolic pathways in the same manner as endogenous IgG
Excretion
Half-life: 14.9 – 45.6 days (SC, psoriasis patients); 19 days (Crohn disease patients)
Clearance: 0.19 L/day
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
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Patient Handout
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
