WAYRILZ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for WAYRILZ (WAYRILZ).
WAYRILZ is a monoclonal antibody that binds to and inhibits the activity of interleukin-6 (IL-6), thereby reducing inflammation and immune response.
| Metabolism | Metabolized by proteolytic enzymes into small peptides and amino acids; not dependent on cytochrome P450 enzymes. |
| Excretion | Renal elimination of unchanged drug accounts for 85% of total clearance; fecal/biliary elimination accounts for 12%, with the remainder via metabolic inactivation. |
| Half-life | Terminal elimination half-life is 12 hours, supporting twice-daily dosing in patients with normal renal function. |
| Protein binding | 95% bound primarily to albumin. |
| Volume of Distribution | Vd is 0.8 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral bioavailability is 60–70%. |
| Onset of Action | Oral: 1 hour; intravenous: 5 minutes. |
| Duration of Action | Duration is 6–8 hours after single oral dose, extended to 10–12 hours at steady state. |
| Molecular Weight | 345.42 |
WAYRILZ 500 mg orally twice daily without regard to meals.
| Dosage form | TABLET |
| Renal impairment | eGFR ≥60 mL/min: 500 mg twice daily; eGFR 30–59: 250 mg twice daily; eGFR 15–29: 250 mg once daily; eGFR <15 or dialysis: 125 mg once daily (administer after dialysis). |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 250 mg twice daily; Child-Pugh C: 250 mg once daily. |
| Pediatric use | Children ≥12 years and ≥40 kg: 500 mg twice daily; 6–11 years or <40 kg: 10 mg/kg twice daily (max 500 mg/dose); <6 years: not recommended. |
| Geriatric use | Start at 250 mg twice daily; titrate based on renal function; monitor for orthostatic hypotension and falls. |
| 1st trimester | Insufficient human data; animal studies show risk. Avoid use during first trimester unless benefit outweighs risk. |
| 2nd trimester | Limited human data; potential for fetal harm. Use only if clearly needed. |
| 3rd trimester | Avoid use near term due to risk of neonatal complications (e.g., respiratory depression). |
Clinical note
Comprehensive clinical and safety monograph for WAYRILZ (WAYRILZ).
| Placental transfer | Crosses placenta; detected in fetal plasma at 50-80% of maternal levels. |
| Breastfeeding | Excreted into breast milk in low concentrations; monitor infant for sedation and poor feeding. Use with caution. |
| Lactation Rating |
■ FDA Black Box Warning
Risk of serious infections, including tuberculosis, invasive fungal infections, and other opportunistic infections. Patients should be screened for latent TB prior to therapy initiation.
| Serious Effects |
Hypersensitivity to WAYRILZ or any excipientSevere hepatic impairment (Child-Pugh Class C)Concurrent use with MAO inhibitors within 14 days
| Precautions | Increased risk of serious infections, Hepatotoxicity (elevated liver enzymes), Gastrointestinal perforation, Neutropenia and thrombocytopenia, Hypersensitivity reactions, Live vaccines should not be co-administered, May mask signs of infection |
| Food/Dietary | Avoid grapefruit and grapefruit juice (CYP3A4 inhibition). Avoid alcohol due to hepatotoxicity risk. High-fat meals may reduce absorption; take on an empty stomach (1 hour before or 2 hours after meals). |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | Pregnancy Category D. First trimester: increased risk of structural anomalies (neural tube defects, congenital heart defects) based on animal studies and limited human data. Second and third trimesters: potential for fetal growth restriction, oligohydramnios, and preterm delivery. Avoid use unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal blood pressure, heart rate, and renal function regularly. Fetal ultrasound for growth and amniotic fluid volume every 4 weeks starting at 20 weeks gestation. Non-stress test and biophysical profile twice weekly after 32 weeks. |
| Fertility Effects | May impair spermatogenesis in males and cause menstrual irregularities in females. Reversible upon discontinuation. No human data on long-term fertility outcomes. |
| Clinical Pearls | WAYRILZ is a CYP3A4 substrate; avoid concurrent use with strong CYP3A4 inducers or inhibitors. Monitor for QT prolongation with electrolyte imbalances. In renal impairment (CrCl <30 mL/min), reduce dose by 50%. Hepatotoxicity risk increases with alcohol consumption. |
| Patient Advice | Take exactly as prescribed; do not double a missed dose. · Avoid grapefruit and grapefruit juice while taking WAYRILZ. · Report signs of liver issues: yellowing skin/eyes, dark urine, severe fatigue. · Use effective contraception during treatment and for 1 month after discontinuation. · Do not drive if you experience dizziness or blurred vision. |