Trade Names:Stelara- 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 mg and 90 mg, respectively.
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 mg and 90 mg, it was 161 mL/kg 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.
No pharmacokinetic data are available in patients with renal impairment.Hepatic Function Impairment
No pharmacokinetic data are available in patients with hepatic impairment.Elderly
There were no apparent changes in pharmacokinetic parameters (Cl and Vd) in subjects older than 65 years of age.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.
For the treatment of adults (18 years of age and older) with moderate to severe plaque psoriasis who are candidates for phototherapy or systemic therapy.
AdultsWeighing 100 kg (220 lb) or less
Subcutaneously 45 mg initially and 4 weeks later, followed by 45 mg every 12 weeks.Weighing more than 100 kg (220 lb)
Subcutaneously 90 mg initially and 4 weeks later, followed by 90 mg every 12 weeks. 45 mg was also shown to be efficacious; however, 90 mg resulted in greater efficacy in these subjects.
Store refrigerated at 36° to 46°F. Do not freeze or shake. Keep in original carton to protect from light until time of use.
It is not known whether patients receiving ustekinumab will be vulnerable to dissemination of infection. Do not administer BCG vaccines to patients receiving ustekinumab or for 1 yr prior to initiation or 1 yr following discontinuation of treatment.CYP substrates
The role for ustekinumab in regulation of CYP-450 isozymes has not been determined. 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.Immunosuppressive agents, phototherapy
The safety of coadministration of ustekinumab with immunosuppressive agents or phototherapy has not been evaluated.Live 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. 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.Nonlive vaccinations
The immune response to the vaccination may not be sufficient to prevent the disease.
None well documented.
Headache (5%); fatigue (3%); dizziness (2%); depression (1%).
Nasopharyngitis (8%); pharyngolaryngeal pain (2%).
Injection-site erythema (2%).
Back pain (2%); myalgia (1%).
Upper respiratory tract infection (5%).
Closely monitor for development of signs or symptoms of 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.
Psoriatic patients should receive all age-appropriate immunizations prior to the start of treatment.
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 for malignancy or history of malignancy.
May occur during treatment. If suspected, discontinue ustekinumab and administer appropriate treatment.
Evaluate patients for tuberculosis infection prior to initiating treatment; do not administer to patients with active tuberculosis.
No data available.
Copyright © 2009 Wolters Kluwer Health.