REZENOPY
Clinical safety rating: caution
Comprehensive clinical and safety monograph for REZENOPY (REZENOPY).
REZENOPY is a monoclonal antibody that binds to and inhibits the activity of thymic stromal lymphopoietin (TSLP), a cytokine involved in the pathogenesis of asthma. By blocking TSLP, it reduces the release of downstream inflammatory mediators from various cell types.
| Metabolism | REZENOPY is a monoclonal antibody degraded into small peptides and amino acids via general protein catabolism; not metabolized by CYP450 enzymes. |
| Excretion | Renal excretion of unchanged drug accounts for 60% of elimination; biliary/fecal excretion accounts for 30%; the remaining 10% is metabolized. |
| Half-life | Terminal elimination half-life is 18 hours (range 14-22 hours) in adults with normal renal function; clinically relevant for once-daily dosing. |
| Protein binding | Approximately 92% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is 0.5 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral bioavailability is 75% (range 60-85%) under fasting conditions; coadministration with food reduces bioavailability by 20%. |
| Onset of Action | Oral: onset of action occurs within 1-2 hours; intravenous: onset within 5-10 minutes. |
| Duration of Action | Duration of action is approximately 24 hours after oral administration; after IV, effects last 12-18 hours. Clinical monitoring recommended due to interpatient variability. |
100 mg orally twice daily
| Dosage form | SPRAY |
| Renal impairment | eGFR 30-59 mL/min: reduce to 50 mg twice daily; eGFR <30 mL/min: not recommended |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce to 50 mg twice daily; Child-Pugh C: not recommended |
| Pediatric use | Not established; safety and efficacy in patients <18 years have not been studied |
| Geriatric use | No specific dose adjustment required; monitor renal function due to age-related decline |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for REZENOPY (REZENOPY).
| Breastfeeding | Unknown if REZENOPY is excreted in human milk. M/P ratio not established. Caution: risk of infant hypoglycemia. Use only if benefit outweighs risk. |
| Teratogenic Risk | First trimester: Inadequate human data; animal studies show no teratogenicity at clinically relevant doses. Second and third trimesters: No known structural abnormalities; theoretical risk of fetal hypoglycemia due to maternal glucose modulation. |
| Fetal Monitoring |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
["History of hypersensitivity to REZENOPY or any of its excipients"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Do not discontinue systemic or inhaled corticosteroids abruptly","Parasitic (helminth) infection: treat before initiating therapy"] |
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| Maternal: blood glucose levels, hepatic function, renal function. Fetal: ultrasound for growth and anatomy in second trimester; assess for macrosomia if maternal hyperglycemia. |
| Fertility Effects | No human data on fertility. In animal studies, no adverse effects on male or female fertility at exposures up to 10 times the maximum recommended human dose. |