Loading...
Loading...
Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Stelara
Generic Name
Ustekinumab
Active Ingredient
UstekinumabCategory
Interleukin-12 Antagonist [EPC]
Variants
3
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Stelara, you must consult a qualified healthcare professional.
Detailed information about Stelara
Ustekinumab is a human monoclonal antibody and interleukin-12/23 antagonist used to treat chronic inflammatory conditions, including plaque psoriasis, psoriatic arthritis, Crohn's disease, and ulcerative colitis.
The dosage of Ustekinumab is highly individualized based on the patient's weight and the specific condition being treated. For Plaque Psoriasis and Psoriatic Arthritis, the standard adult dose for individuals weighing 100 kg (220 lbs) or less is 45 mg administered subcutaneously initially, followed by a 45 mg dose 4 weeks later, and then every 12 weeks thereafter. For adults weighing more than 100 kg, the dose is increased to 90 mg on the same schedule.
For Crohn’s Disease and Ulcerative Colitis, the treatment begins with a one-time intravenous (IV) induction dose based on body weight to quickly reach therapeutic levels. For patients weighing up to 55 kg, the IV dose is 260 mg; for those between 55 kg and 85 kg, it is 390 mg; and for those over 85 kg, it is 520 mg. Eight weeks after this initial IV infusion, patients transition to a subcutaneous maintenance dose of 90 mg every 8 weeks.
Ustekinumab is FDA-approved for the treatment of moderate-to-severe plaque psoriasis in pediatric patients aged 6 years and older. The dosage is based on body weight:
The schedule follows the adult pattern: an initial dose, a second dose 4 weeks later, and then maintenance doses every 12 weeks. Use in children for other conditions, such as Crohn's disease, has not been established as safe or effective by the FDA as of 2024.
There are no specific dosage adjustments provided in the manufacturer's labeling for patients with renal (kidney) impairment. Because Ustekinumab is a large protein cleared through catabolism rather than renal filtration, kidney function is not expected to significantly impact its clearance. However, clinical studies in this population are limited.
Similarly, no dosage adjustments are recommended for patients with hepatic (liver) impairment. As the drug is not metabolized by the liver's CYP450 system, liver dysfunction is unlikely to alter the drug's levels significantly. Nevertheless, patients with severe liver disease should be monitored closely for overall health stability.
Clinical studies did not identify significant differences in safety or efficacy between patients aged 65 and older and younger patients. However, because the risk of infection is generally higher in the elderly, healthcare providers usually exercise caution when prescribing biologics to this population.
Ustekinumab is administered by injection. The initial IV dose for IBD must be performed by a healthcare professional in a clinical setting. Maintenance subcutaneous injections may be self-administered by the patient or a caregiver after proper training.
If you miss a dose, contact your healthcare provider for instructions. Generally, the dose should be taken as soon as remembered, and the subsequent schedule should be adjusted accordingly. Do not 'double up' on doses to make up for a missed one, as this increases the risk of side effects.
In the event of an overdose, patients should be monitored for signs or symptoms of adverse reactions, particularly infections. There is no specific antidote for Ustekinumab. Seek emergency medical attention or contact a Poison Control Center immediately if an excessive amount is administered.
> Important: Follow your healthcare provider's dosing instructions exactly. Do not adjust your dose or frequency without explicit medical guidance, as this may lead to a loss of response to the medication.
Side effects occurring in more than 10% of patients are generally mild but require monitoring. The most frequently reported include:
Before starting Ustekinumab, it is critical to understand that this medication alters the way your immune system functions. While this is necessary to treat your condition, it also means your body may not respond to infections as effectively as it normally would. You must inform your doctor if you have any current infections, even minor ones like an open sore or a cold, before receiving a dose. Patients with a history of chronic or recurring infections must be monitored with extreme care.
No FDA black box warnings for Ustekinumab. However, the FDA requires a comprehensive Medication Guide to be provided to every patient, detailing the risks of serious infections and potential for malignancy.
Conditions where Ustekinumab must NEVER be used include:
These are conditions requiring a careful risk-benefit analysis by a medical professional:
Ustekinumab is classified as a drug that should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Data from the PIANO (Pregnancy in IBD and Neonatal Outcomes) registry suggests that monoclonal antibodies like Ustekinumab do not appear to increase the risk of major birth defects or miscarriages. However, it is known that human IgG antibodies cross the placental barrier, especially during the second and third trimesters. This means the infant may have detectable levels of Ustekinumab in their blood at birth. This is particularly important for the infant's vaccination schedule; live vaccines should generally be avoided in infants exposed to Ustekinumab in utero for at least 6 months after birth.
Limited data indicate that Ustekinumab is excreted in human breast milk in very small amounts. Because Ustekinumab is a large protein molecule, it is likely to be degraded in the infant's digestive tract, meaning very little of the drug is expected to be absorbed into the infant's bloodstream. Most experts consider breastfeeding to be generally compatible with Ustekinumab therapy, but the decision should be made in consultation with a pediatrician, weighing the benefits of breastfeeding against any potential (though likely low) risk to the nursing child.
Ustekinumab is a fully human IgG1κ monoclonal antibody that binds with high affinity and specificity to the p40 protein subunit of the human cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23). These cytokines are involved in inflammatory and immune responses, such as natural killer cell activation and CD4+ T-cell differentiation and activation. By binding to the p40 subunit, Ustekinumab inhibits the bioactivity of human IL-12 and IL-23 by preventing these cytokines from binding to their IL-12Rβ1 receptor protein expressed on the surface of immune cells. This blockage disrupts the signaling pathways that lead to the production of pro-inflammatory cytokines like IFN-γ and IL-17, which are key drivers in the pathogenesis of psoriasis and inflammatory bowel disease.
The pharmacodynamic effect of Ustekinumab is characterized by a significant decrease in the expression of mRNA for its target cytokines in the skin and intestinal tissues. In patients with psoriasis, treatment leads to a reduction in epidermal hyperplasia (thickening of the skin) and inflammatory cell infiltration. The onset of action is gradual; while some patients see improvement within 2 weeks, the peak clinical effect is typically observed between weeks 12 and 24. Because of its long half-life, the anti-inflammatory effects persist for several weeks even after a dose is missed.
Common questions about Stelara
Ustekinumab is a prescription biologic medication used to treat several chronic inflammatory conditions caused by an overactive immune system. It is FDA-approved for adults and children 6 and older with moderate-to-severe plaque psoriasis, as well as adults with psoriatic arthritis. Additionally, it is used for adults with moderate-to-severe Crohn's disease and ulcerative colitis who have not responded to other treatments. By blocking specific inflammatory proteins called IL-12 and IL-23, it helps reduce skin lesions, joint pain, and gut inflammation. Your doctor will determine if this specific mechanism is appropriate for your diagnosis.
The most frequently reported side effects of Ustekinumab include nasopharyngitis (the common cold), upper respiratory tract infections, headaches, and fatigue. Some patients also experience redness, itching, or pain at the site of the injection. Because the drug affects the immune system, minor infections may occur more easily than usual. Most of these common side effects are mild and do not require stopping the medication. However, you should always keep your healthcare provider informed of any new or worsening symptoms you experience during treatment.
There is no known direct chemical interaction between alcohol and Ustekinumab. However, alcohol can sometimes worsen the symptoms of the conditions Ustekinumab treats, such as psoriasis or inflammatory bowel disease. Heavy alcohol use can also impact liver health and overall immune function, which may complicate your treatment plan. It is generally advised to consume alcohol only in moderation while on biologic therapy. Always discuss your lifestyle habits with your doctor to ensure they do not interfere with your recovery.
Ustekinumab should be used during pregnancy only if the potential benefits outweigh the potential risks to the fetus. Current research, including data from pregnancy registries, has not shown a clear link between Ustekinumab and an increased risk of birth defects or pregnancy complications. However, because the drug can cross the placenta, the baby may have a temporarily weakened immune system after birth. It is vital to inform your obstetrician and gastroenterologist or dermatologist if you are pregnant or planning to become pregnant. They will help you weigh the risks of the medication against the risks of an untreated disease flare.
The time it takes to see results from Ustekinumab varies depending on the condition being treated and the individual patient. For plaque psoriasis, many patients begin to see skin improvement within the first 2 to 4 weeks, with maximum results often appearing around week 12 to 24. For Crohn's disease and ulcerative colitis, some patients notice a reduction in symptoms within a few weeks of the initial IV infusion, though it may take several months to achieve full clinical remission. Patience is key, and you should continue your scheduled doses even if you do not see immediate changes. Discuss your progress with your doctor at each follow-up appointment.
While stopping Ustekinumab suddenly does not cause a physical withdrawal syndrome, it is highly likely that your symptoms will return. Because Ustekinumab has a very long half-life, the drug stays in your system for several weeks, meaning the 'rebound' of symptoms may be delayed but significant. Stopping and restarting biologics can also increase the risk of your body developing antibodies against the drug, which may make it less effective in the future. You should never stop your treatment without first consulting your healthcare provider. They will help you decide the best course of action if you need to pause therapy for surgery or due to an infection.
If you miss a dose of Ustekinumab, you should contact your healthcare provider as soon as possible for guidance on when to take the next injection. Generally, you should take the missed dose as soon as you remember and then adjust your subsequent dosing schedule based on that new date. Do not take two doses at once to make up for a missed one, as this can increase the risk of side effects. Maintaining a consistent schedule is important for keeping the drug at therapeutic levels in your blood. Setting a calendar reminder or using a medication tracking app can help you stay on schedule.
Weight gain is not listed as a common side effect of Ustekinumab in clinical trials. However, some patients with Crohn's disease or ulcerative colitis may gain weight as their condition improves because their body is better able to absorb nutrients and they are no longer experiencing chronic inflammation. Conversely, some patients may experience weight changes due to other medications they may be taking concurrently, such as corticosteroids. If you notice significant or rapid changes in your weight, you should discuss them with your doctor. They can help determine if the change is related to your treatment or another underlying factor.
Ustekinumab can interact with other medications, particularly those that also suppress the immune system. Combining it with other biologics or strong immunosuppressants like cyclosporine can significantly increase your risk of serious infections. It may also indirectly affect how your liver processes drugs like warfarin or certain heart medications by changing the level of inflammation in your body. You must provide your doctor with a complete list of all prescriptions, over-the-counter drugs, and herbal supplements you are taking. Your doctor will monitor you for potential interactions and may adjust your other dosages if necessary.
As of 2024, there are no 'generic' versions of Ustekinumab because it is a complex biologic drug. However, 'biosimilars' are becoming available. A biosimilar is a biological product that is highly similar to and has no clinically meaningful differences from an existing FDA-approved biologic. Several biosimilars for Ustekinumab have been developed and approved by regulatory agencies (such as Wezlana, approved by the FDA in late 2023). These biosimilars may offer a more cost-effective option for patients. Your doctor or pharmacist can tell you if a biosimilar is an appropriate and available option for your specific treatment plan.
Other drugs with the same active ingredient (Ustekinumab)
> Warning: Stop taking Ustekinumab and call your doctor immediately if you experience any of these serious symptoms.
Long-term use of Ustekinumab (multi-year therapy) requires ongoing vigilance for malignancies (cancers). While the overall risk appears low in clinical data, the theoretical risk of lymphoma or other cancers exists whenever the immune system is modulated over long periods. Additionally, some patients may develop 'anti-drug antibodies,' where the immune system begins to recognize Ustekinumab as a foreign substance and neutralizes it, leading to a gradual loss of the drug's effectiveness over several years.
As of 2024, Ustekinumab does not carry a specific FDA Black Box Warning. However, it does carry significant 'Warnings and Precautions' regarding serious infections and malignancies that are treated with the same level of clinical importance as a boxed warning in practice.
Report any unusual symptoms or changes in your health to your healthcare provider immediately. Regular follow-up appointments are essential to ensure the medication remains safe and effective for you.
Your healthcare provider will require regular monitoring to ensure the drug is not causing silent harm. This typically includes:
Ustekinumab is not known to significantly impair the ability to drive or operate heavy machinery. However, if you experience side effects like dizziness or fatigue after an injection, you should wait until these symptoms subside before performing tasks that require alertness.
There is no known direct interaction between Ustekinumab and alcohol. However, alcohol can exacerbate certain conditions like psoriasis or Crohn's disease and may put additional strain on the liver. Discuss your alcohol consumption habits with your doctor.
Stopping Ustekinumab suddenly does not typically cause a 'withdrawal syndrome' like corticosteroids do. However, the symptoms of your underlying condition (psoriasis, Crohn's, etc.) are likely to return, sometimes more severely, once the drug levels in your blood drop. If you need to stop the medication due to an upcoming surgery or a serious infection, your doctor will provide a specific plan for when to restart.
> Important: Discuss all your medical conditions, including any history of cancer, TB, or recent vaccinations, with your healthcare provider before starting Ustekinumab.
There are no known specific food interactions with Ustekinumab. It can be taken regardless of meal timing because it is administered via injection and bypasses the digestive system. However, for patients with Crohn's or Ulcerative Colitis, maintaining a diet recommended by a gastroenterologist is essential for managing the underlying disease.
Ustekinumab does not typically interfere with standard laboratory tests like glucose or cholesterol panels. However, it may affect the results of certain specialized immune system tests. For example, if you are being tested for TB using an Interferon-Gamma Release Assay (IGRA), the results could potentially be influenced by the drug’s effect on cytokine levels, though this is rare.
For each major interaction, the mechanism usually involves either an additive effect on the immune system (pharmacodynamic interaction) or a change in the liver's metabolic capacity due to reduced systemic inflammation. The clinical consequence is often an increased risk of infection or a change in the effectiveness of other medications.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking, including over-the-counter pain relievers and vitamins.
There is no known cross-sensitivity between Ustekinumab and other classes of biologics, such as TNF-alpha inhibitors (e.g., Infliximab). However, patients who have had a reaction to other human monoclonal antibodies should be monitored closely, as the manufacturing processes and certain stabilizing proteins may be similar.
> Important: Your healthcare provider will evaluate your complete medical history, including any past allergic reactions and exposure to infectious diseases, before determining if Ustekinumab is safe for you.
Ustekinumab is approved for the treatment of moderate-to-severe plaque psoriasis in children and adolescents aged 6 years and older. Clinical trials (such as the CADMUS study) demonstrated that the safety profile in children is similar to that in adults. However, the long-term effects on growth and development are still being monitored. It is not currently approved for pediatric use in Crohn's disease or psoriatic arthritis, as the necessary clinical trials for these specific age groups and conditions are still ongoing or awaiting further data.
In clinical trials, approximately 5-6% of participants were aged 65 or older. While no overall differences in efficacy were observed, the incidence of serious infections was higher in the geriatric population in general. Older adults often have reduced physiological reserve and may be taking multiple other medications (polypharmacy), which increases the risk of complications. Healthcare providers typically start with the standard dose but maintain a higher level of vigilance for signs of infection or skin cancer.
As Ustekinumab is a monoclonal antibody, it is not filtered by the kidneys. Therefore, no dosage adjustment is required for patients with mild, moderate, or severe renal impairment. It is also not expected to be cleared by dialysis due to its large molecular size. However, patients with kidney disease should be monitored for fluid balance, especially during the initial IV induction phase.
Ustekinumab has not been specifically studied in patients with hepatic impairment. However, since the liver is not the primary route of elimination for monoclonal antibodies (which are cleared via cellular catabolism), liver dysfunction is not expected to affect the drug's concentration. No dose adjustments based on Child-Pugh scores are currently recommended.
> Important: Special populations require individualized medical assessment. Always inform your specialist if you are planning to become pregnant or if you are managing other chronic health conditions.
| Parameter | Value |
|---|---|
| Bioavailability | 57% (Subcutaneous) |
| Protein Binding | Not applicable (Monoclonal Antibody) |
| Half-life | 15 to 45 days (Mean ~3 weeks) |
| Tmax | 7 to 13.5 days (SC administration) |
| Metabolism | Intracellular catabolism to peptides/amino acids |
| Excretion | Not characterized; likely non-renal |
Ustekinumab is produced by a continuous mammalian cell culture process (Sp2/0 cells). It has a molecular weight of approximately 148,074 Daltons. It consists of two heavy chains and two light chains linked by disulfide bonds. The solution is clear to slightly opalescent and colorless to light yellow, with a pH of approximately 6.0.
Ustekinumab is classified as an Interleukin-12 and Interleukin-23 Antagonist. It is distinct from TNF-alpha inhibitors (like Etanercept) and IL-17 inhibitors (like Secukinumab). By targeting the 'upstream' p40 subunit, it provides a unique therapeutic profile that can be effective even in patients who have failed other classes of biologic therapy.