- Injection, solution 45 mg per 0.5 mL
- Injection, solution 90 mg/mL
Human immunoglobulin G1 (IgG1) kappa monoclonal antibody that binds with high affinity and specificity to the p40 protein subunit used by both the interleukin (IL)–12 and IL-23 cytokines.
T max was 13.5 days and 7 days after a single subcutaneous administration of 45 and 90 mg, respectively. Steady state is reached by wk 28.
The mean Vd during the terminal phase following a single IV administration ranged from 56.1 to 82.1 mL/kg. Following subcutaneous administration of 45 and 90 mg, it was 161 and 179 mL/kg, respectively.
Expected to be degraded via catabolic pathways in the same manner as endogenous IgG.
The mean systemic Cl following a single IV administration ranged from 1.9 to 2.22 mL/day/kg. The mean half-life ranged from 14.9 to 45.6 days following IV and subcutaneous administration.
Special PopulationsRenal Function Impairment
No pharmacokinetic data are available.Hepatic Function Impairment
No pharmacokinetic data are available.Elderly
There were no apparent changes in pharmacokinetic parameters (Cl and Vd) in subjects older than 65 y.Weight
When given the same dose, subjects weighing more than 100 kg had lower median serum concentrations compared with those subjects weighing 100 kg or less.
Indications and Usage
For the treatment of adults (18 y and older) with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.
None well documented.
Dosage and AdministrationAdults 100 kg or less
Subcutaneously 45 mg initially and 4 wk later, followed by 45 mg every 12 wk.More than 100 kg
Subcutaneously 90 mg initially and 4 wk later, followed by 90 mg every 12 wk. 45 mg was also shown to be efficacious; however, 90 mg resulted in greater efficacy in subjects more than 100 kg.
- Administer by subcutaneous injection. Do not shake.
- The needle cover on the prefilled syringe contains dry natural rubber (a derivative of latex). The needle cover should not be handled by persons sensitive to latex.
- Administer each injection at a different anatomic location (such as upper arms, gluteal regions, thighs, or any quadrant of abdomen) than the previous injection, and not into areas where the skin is tender, bruised, erythematous, or indurated.
- Visually inspect for particulate matter and discoloration; do not use if discolored or cloudy or if other particulate matter is present.
- The safety and efficacy of ustekinumab have not been evaluated beyond 2 y.
Store refrigerated between 36° and 46°F. Do not freeze. Keep in original carton to protect from light until time of use.
Drug InteractionsCYP substrates (eg, cyclosporine, warfarin)
Upon initiating ustekinumab therapy in patients receiving CYP-450 substrates, particularly drugs with a narrow therapeutic index, monitor clinical effects (eg, warfarin) or drug concentrations (eg, cyclosporine) and adjust the dose of the drug as needed.Vaccines
It is not known whether patients receiving ustekinumab will be vulnerable to dissemination of infection. Do not administer live vaccines to patients receiving ustekinumab. Do not administer Bacillus Calmette-Guérin (BCG) vaccines to patients receiving ustekinumab or for 1 y prior to initiation or 1 y following discontinuation of treatment. Use with caution in administering live vaccines to household contacts of patients receiving ustekinumab because of risk for viral shedding from the household contact and transmission to the patient. Non-live vaccination given during ustekinumab therapy may not elicit an immune response sufficient to prevent disease.
Headache (5%); fatigue (3%); dizziness (2%); depression (1%).
Nasopharyngitis (8%); pharyngolaryngeal pain (2%).
Hypersensitivity reactions (including rash, urticaria), serious allergic reactions (including angioedema, dyspnea, hypotension), (postmarketing).
Injection-site erythema (2%).
Back pain (2%); myalgia (1%).
Upper respiratory tract infection (5%).
Infections (61%); malignancies.
Evaluate patients for tuberculosis (TB) infection prior to initiating treatment. Closely monitor for development of signs or symptoms of active TB infection during and after treatment.
Category B .
IgG is excreted in human milk, so it is expected that ustekinumab will be present in human milk.
Safety and efficacy not established.
Serious allergic reactions, including angioedema and possible anaphylaxis, have been reported postmarketing.
Ustekinumab may decrease the protective effect of allergy immunotherapy and may increase the risk of an allergic reaction to a dose of allergen immunotherapy. Use with caution in patients receiving or who have received allergy immunotherapy, particularly for anaphylaxis.
Psoriatic patients should receive all age-appropriate immunizations prior to the start of treatment.
Antibodies to ustekinumab may develop. Presence of ustekinumab in the serum can interfere with the detection of these antibodies.
May increase the risk of infections and reactivation of latent infections. Serious bacterial, fungal, and viral infections were observed in patients receiving ustekinumab. Ustekinumab should not be given to patients with any clinically important active infection. Individuals genetically deficient in IL-12/IL-23 are particularly vulnerable to disseminated infections from mycobacteria (including nontuberculous, environmental mycobacteria), Salmonella (including nontyphi strains), and BCG vaccinations.
Because many immunosuppressants have the potential to increase the risk of malignancies, use with caution in patients at high risk of malignancy or with a history of malignancy.
Reversible posterior leukoencephalopathy syndrome
May occur during treatment. If suspected, discontinue ustekinumab and administer appropriate treatment.
Evaluate patients for TB infection prior to initiating treatment; do not administer to patients with active TB.
No data available.
- Instruct patients to read the Medication Guide before starting therapy and each time the prescription is refilled.
- Inform patients that the ability of their immune system to fight infection may be lowered. Instruct patients of the importance of communicating any history of infections and to notify their health care provider if they develop any symptoms of infection.
- Counsel patients about the risk of malignancies while receiving ustekinumab.
- Advise patients to seek immediate medical attention if they experience any symptoms of serious allergic reactions.
Copyright © 2009 Wolters Kluwer Health.