CYLTEZO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CYLTEZO (CYLTEZO).
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. |
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 | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for CYLTEZO (CYLTEZO).
| Breastfeeding | Adalimumab is excreted in human milk in low amounts; M/P ratio not established for adalimumab-adaz specifically. The molecular weight suggests it is unlikely to be absorbed by the infant in significant amounts. Expert consensus generally considers TNF-alpha inhibitors compatible with breastfeeding, but caution is advised. Monitor infant for potential adverse effects such as increased risk of infections or hypersensitivity. |
| 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. |
■ 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 |
["Severe infection (e.g., sepsis, active TB)","Moderate to severe heart failure (NYHA class III/IV) - relative","Known hypersensitivity to adalimumab or any component"]
| 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"] |
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| 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. |