TEZSPIRE
Clinical safety rating
cautionComprehensive clinical and safety monograph for TEZSPIRE (TEZSPIRE).
Comprehensive clinical and safety monograph for TEZSPIRE (TEZSPIRE).
Add-on maintenance treatment of severe asthma in patients aged 12 years and older with an eosinophilic phenotype or oral corticosteroid-dependent asthma
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. |
| Molecular Weight | Approximately 150,000 Da (150 kDa) |
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 | Limited human data; no evidence of teratogenicity in animal studies at supratherapeutic doses, but avoid use unless benefit outweighs risk. |
| 2nd trimester | No specific data; theoretical risk of increased infection due to IL-33 blockade; use only if clearly needed. |
| 3rd trimester | Limited data; no known fetal harm from monoclonal antibodies in late pregnancy; consider potential for infection in neonate. |
Clinical note
Comprehensive clinical and safety monograph for TEZSPIRE (TEZSPIRE).
| Placental transfer | Monoclonal antibodies are actively transported across placenta via FcRn, increasing fetal exposure in second and third trimesters. Likely crosses, similar to other IgG antibodies. |
| Breastfeeding | Tezepelumab is a monoclonal antibody; expected to be excreted in human milk in very low amounts. Likely not systemically absorbed by infant due to gastrointestinal breakdown. Consider benefits of breastfeeding, maternal need for drug, and potential risks to infant (e.g., infection). |
| Lactation Rating | L3 (Moderately Safe) |
| 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. |
| 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). |
■ FDA Black Box Warning
None
| Serious Effects |
History of hypersensitivity reaction to tezepelumab or 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 |
| Food/Dietary | No known food interactions. Tezepelumab-ekko is a monoclonal antibody; food does not affect its absorption or efficacy as it is administered subcutaneously. |
| Clinical Pearls | Tezepelumab-ekko is a first-in-class TSLP inhibitor for add-on maintenance therapy of severe asthma. Monitor for hypersensitivity reactions, including anaphylaxis, and advise patients to seek immediate medical care if symptoms occur. Do not discontinue systemic or inhaled corticosteroids abruptly. Live vaccines should not be administered concurrently. Consider pregnancy registry enrollment for exposed patients. |
| Patient Advice | Tezspire is given as an injection under the skin every 4 weeks by a healthcare provider. · Do not suddenly stop taking other asthma medicines unless instructed by your doctor. · Seek medical help right away if you get a rash, itching, swelling, or trouble breathing after injection. · Tell your doctor if you have a parasitic infection or are taking corticosteroids. · Avoid live vaccines during treatment. |
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