CYLTEZO
Clinical safety rating
cautionComprehensive clinical and safety monograph for CYLTEZO (CYLTEZO).
Comprehensive clinical and safety monograph for CYLTEZO (CYLTEZO).
Rheumatoid arthritis (moderate to severe active disease)Juvenile idiopathic arthritis (polyarticular, 2 years and older)Psoriatic arthritisAnkylosing spondylitisAdult Crohn's disease (moderate to severe, anti-TNF naïve)Ulcerative colitis (moderate to severe in adults)Plaque psoriasis (moderate to severe chronic, adult)Hidradenitis suppurativa (moderate to severe, adult)Uveitis (non-infectious intermediate, posterior, and panuveitis in adults and pediatrics)
Adalimumab is a recombinant human monoclonal antibody that binds to tumor necrosis factor-alpha (TNFα) and blocks its interaction with p55 and p75 cell surface TNF receptors. It also modulates biological responses induced or regulated by TNFα, including adhesion molecules, chemotaxis, and matrix metalloproteinases.
| Metabolism | Adalimumab is a monoclonal antibody; it is degraded by proteolytic enzymes into small peptides and amino acids. No specific metabolic pathways or CYP450 enzymes involved. |
| Excretion | Primarily eliminated via intracellular catabolism; no significant renal or biliary elimination of intact adalimumab. |
| Half-life | Approximately 14 days (range 10–20 days) following subcutaneous administration; supports every-other-week dosing. |
| Protein binding | Adalimumab binds specifically to soluble and membrane-bound TNF-alpha; does not bind to other serum proteins; binding to specific target is high affinity but no general protein binding data reported. |
| Volume of Distribution | Approximately 4.7–6.0 L (0.07–0.09 L/kg for a 70 kg adult); indicates distribution primarily within the vascular and interstitial spaces. |
| Bioavailability | Subcutaneous: 64% (absolute bioavailability). |
| Onset of Action | Subcutaneous: Clinical response may be observed within 1–2 weeks, with maximal effect typically by 12 weeks. |
| Duration of Action | Duration of therapeutic effect is approximately 14 days, corresponding to the dosing interval; sustained suppression of inflammatory markers for 2–3 weeks after single dose. |
| Molecular Weight | 147600 |
Adalimumab 40 mg subcutaneously every other week, with or without methotrexate, for rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and plaque psoriasis. For ulcerative colitis and hidradenitis suppurativa, day 1: 160 mg (four 40 mg injections in one day or two 40 mg injections per day for two days), day 15: 80 mg, then 40 mg every other week starting day 29. For uveitis, 40 mg every other week.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment. |
| Liver impairment | No dose adjustment recommended. Not studied in patients with hepatic impairment. |
| Pediatric use | For juvenile idiopathic arthritis (2 years and older): 10-30 mg subcutaneously every other week (10 mg if <15 kg, 20 mg if 15-30 kg, 40 mg if ≥30 kg). For pediatric plaque psoriasis (4 years and older): weight-based dosing with maximum 40 mg starting dose, then 0.8 mg/kg up to 40 mg every other week. For pediatric hidradenitis suppurativa (12 years and older): 40 mg every other week. |
| Geriatric use | No specific dose adjustment. Use with caution due to increased risk of infections. Monitor renal and hepatic function. |
| 1st trimester | Limited data; avoid unless benefit outweighs risk. Active transplacental transfer increases after 16 weeks. |
| 2nd trimester | Active transplacental transfer; may cause fetal B-cell depletion. Use only if clearly needed. |
| 3rd trimester | Significant transplacental transfer; may cause neonatal immunosuppression. Avoid live vaccines in infants for 6 months. |
Clinical note
Comprehensive clinical and safety monograph for CYLTEZO (CYLTEZO).
| Placental transfer | Active transplacental transfer via FcRn receptors; minimal in first trimester, increases after 16 weeks, highest in third trimester. |
| Breastfeeding | Present in breastmilk in low amounts; not expected to cause adverse effects in term infants. Use with caution in preterm or immunocompromised infants. |
| Lactation Rating | L3 |
| Teratogenic Risk | CYLTEZO (adalimumab-adaz) is a TNF-alpha inhibitor. Human data on teratogenicity are limited; however, large cohort studies do not indicate a significant increase in major birth defects. Theoretical risk of harm to the fetus due to TNF inhibition; however, placental transfer is minimal during first trimester but increases in second and third trimester. There is evidence of increased risk of infections in neonates exposed in utero during later pregnancy. Therefore, use is not recommended in the third trimester unless clearly needed. |
| Fetal Monitoring | Monitor maternal liver function tests, complete blood count, and signs of infection. For neonates exposed in utero, monitor for infections, particularly during the first 3 months of life. No specific fetal monitoring is required but consider ultrasound if growth restriction is suspected. |
| Fertility Effects | TNF-alpha inhibitors do not appear to negatively impact fertility. Some studies suggest they may improve fertility in women with inflammatory conditions like rheumatoid arthritis by controlling disease activity. No specific effects on male fertility are reported. |
■ FDA Black Box Warning
Serious infections: Increased risk of serious infections leading to hospitalization or death, including tuberculosis (TB), bacterial sepsis, invasive fungal infections (such as histoplasmosis), and infections due to opportunistic pathogens. Discontinue if serious infection develops. Test for latent TB prior to initiation; treat latent TB before use. Lymphoma and other malignancies: Malignancies, some fatal, have been reported in children and adolescents treated with TNF blockers, including adalimumab. Hepatosplenic T-cell lymphoma (HSTCL) has occurred in adolescent and young adults with inflammatory bowel disease treated with TNF blockers.
| Serious Effects |
Known hypersensitivity to adalimumab or any excipientActive tuberculosis or other severe infections
| Precautions | Serious infections (including TB, invasive fungal infections, and other opportunistic infections), Malignancies (including lymphoma and HSTCL), Hepatitis B reactivation in chronic carriers, Demyelinating disease (new onset or exacerbation), Cytopenias (including pancytopenia and aplastic anemia), Congestive heart failure (worsening or new onset), Lupus-like syndrome, Serious allergic reactions (including anaphylaxis), Immunizations: Avoid live vaccines during therapy |
| Food/Dietary | No significant food interactions reported. Avoid alcohol if liver function is compromised. |
| Clinical Pearls | CYLTEZO (adalimumab-adbm) is a TNF-alpha inhibitor biosimilar to Humira. Subcutaneous injection sites should be rotated; do not inject into tender, bruised, or scarred skin. Live vaccines are contraindicated during therapy. Screen for latent TB and hepatitis B prior to initiation. Monitor for signs of infection, especially in elderly patients. Consider temporary discontinuation if serious infection occurs. May increase risk of lymphoma and other malignancies. Not recommended in patients with moderate to severe heart failure. |
| Patient Advice | Cyltezo is a biosimilar of Humira and works by reducing inflammation. · Inject the medication subcutaneously as directed; rotate injection sites. · Do not receive live vaccines (e.g., MMR, chickenpox, nasal flu) while on Cyltezo. · Contact your doctor immediately if you have signs of infection (fever, cough, painful urination). · Seek medical attention for symptoms of allergic reaction (hives, difficulty breathing, swelling). · Inform your doctor if you have a history of TB, hepatitis B, heart failure, or cancer. · Store Cyltezo in the refrigerator; do not freeze. Protect from light. |
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