TEZSPIRE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEZSPIRE (TEZSPIRE).
Tezspire (tezepelumab-ekko) is a human monoclonal antibody that binds to thymic stromal lymphopoietin (TSLP), a key epithelial cytokine involved in the initiation and persistence of airway inflammation. By blocking TSLP, tezepelumab reduces the release of pro-inflammatory cytokines and prevents downstream inflammatory responses.
| Metabolism | Tezepelumab is a monoclonal antibody; it is degraded into small peptides and amino acids via general protein catabolic pathways. No significant hepatic metabolism or CYP450 involvement. |
| Excretion | Tezepelumab is a monoclonal antibody. Clearance occurs via intracellular catabolism. No significant renal or fecal elimination of intact drug. Excretion pathways are not defined by percentage. |
| Half-life | Terminal half-life approximately 26 days, supporting subcutaneous dosing every 4 weeks. |
| Protein binding | Tezepelumab binds specifically to thymic stromal lymphopoietin (TSLP). Non-specific protein binding is negligible; not bound to plasma proteins. |
| Volume of Distribution | Estimated central volume of distribution ~3.9 L (approx. 0.056 L/kg for a 70 kg adult), consistent with limited extravascular distribution. |
| Bioavailability | Subcutaneous: Absolute bioavailability not determined; estimated 80-90% based on population pharmacokinetics. |
| Onset of Action | Subcutaneous: Reduction in exacerbation rate observed as early as 2 weeks, maximal effect by 4-8 weeks. |
| Duration of Action | Duration of action reflects dosing interval of 4 weeks. Clinical effect persists throughout the dosing interval; sustained suppression of exacerbations over long-term treatment. |
210 mg subcutaneously every 4 weeks.
| Dosage form | SOLUTION |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²). |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Not approved for pediatric patients; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment recommended; 210 mg subcutaneously every 4 weeks based on limited data in patients aged 65 years and older. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEZSPIRE (TEZSPIRE).
| Breastfeeding | It is unknown whether tezepelumab-ekko is excreted in human milk. Human IgG is present in breast milk, but the amount of monoclonal antibody transfer via breast milk is generally limited. The M/P ratio is not available. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for tezepelumab and any potential adverse effects on the breastfed child from the drug or from the underlying maternal condition. |
| Teratogenic Risk | Tezepelumab-ekko is a human monoclonal antibody. IgG antibodies are known to cross the placental barrier increasingly as pregnancy progresses, with the largest amount transferred during the third trimester. There are no adequate and well-controlled studies in pregnant women. Based on animal studies, no evidence of fetal harm was observed in cynomolgus monkeys administered intravenous doses up to 100 mg/kg/week (approximately 42 times the maximum recommended human dose) during organogenesis. However, because animal reproduction studies are not always predictive of human response, tezepelumab should be used during pregnancy only if clearly needed. |
■ FDA Black Box Warning
None
| Serious Effects |
["History of hypersensitivity to tezepelumab or any of its excipients"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis have been reported","May increase risk of helminth infections; treat pre-existing helminth infection before initiation","No data on patients with hepatic or renal impairment"] |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond standard prenatal care. Monitor for signs of infection and hypersensitivity reactions during treatment. If used during pregnancy, consider monitoring fetal growth and development as part of routine obstetric care. |
| Fertility Effects | No human data on the effect of tezepelumab-ekko on fertility. In animal studies, no adverse effects on male or female fertility were observed in cynomolgus monkeys at intravenous doses up to 100 mg/kg/week (approximately 42 times the maximum recommended human dose). |