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. |
| Molecular Weight | 435.5 |
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 | Limited human data; animal studies show embryotoxicity at high doses. Avoid use unless benefit outweighs risk. |
| 2nd trimester | No adequate human studies; potential for fetal harm based on mechanism. Use only if clearly needed. |
| 3rd trimester | Risk of neonatal renal impairment and oligohydramnios due to fetal renal effects. Discontinue if pregnancy detected. |
Clinical note
Comprehensive clinical and safety monograph for REZENOPY (REZENOPY).
| Placental transfer | Expected to cross placenta based on molecular weight and animal studies; specific data lacking in humans. |
| Breastfeeding | Excretion into human milk unknown; due to potential for serious adverse reactions in nursing infants, discontinue nursing or drug. |
| Lactation Rating |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
Hypersensitivity to Rezenopy or any componentPregnancy
| Precautions | Hypersensitivity reactions including anaphylaxis, Do not discontinue systemic or inhaled corticosteroids abruptly, Parasitic (helminth) infection: treat before initiating therapy |
| Food/Dietary | No significant food interactions. Avoid drinking grapefruit juice if also taking CYP3A4 inhibitors (e.g., ketoconazole, ritonavir) as may increase REZENOPY levels. No dietary restrictions otherwise. |
| Clinical Pearls |
Loading safety data…
| L5 (Contraindicated) |
| 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 | 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. |
| REZENOPY is a novel oral anticoagulant (direct factor Xa inhibitor) with fixed dosing, no routine coagulation monitoring, and a rapid onset. Beware of rebound thrombosis if discontinued abruptly. Use with caution in renal impairment (CrCl <30 mL/min) and avoid in mechanical heart valves. Reversal agent andexanet alfa is available. |
| Patient Advice | Take exactly as prescribed; do not skip doses. If you miss a dose, take it as soon as remembered on the same day; do not double the next dose. · Watch for signs of bleeding: unusual bruising, pink/dark urine, red/black stools, coughing blood, or heavy menstrual bleeding. Seek immediate medical attention if severe. · Inform all healthcare providers (including dentists) that you are taking REZENOPY before any procedure or surgery. · Avoid NSAIDs (e.g., ibuprofen, naproxen) and aspirin unless prescribed by your doctor, as they increase bleeding risk. · Store at room temperature; keep in original packaging to protect from moisture. |