WEZLANA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for WEZLANA (WEZLANA).
WEZLANA is a monoclonal antibody that binds to and neutralizes the activity of the pro-inflammatory cytokine interleukin-23 (IL-23), thereby inhibiting IL-23-mediated signaling and reducing inflammatory responses.
| Metabolism | WEZLANA is a monoclonal antibody expected to be degraded into small peptides and amino acids via catabolic pathways; no specific metabolic enzymes involved. |
| Excretion | Renal excretion of unchanged drug accounts for 70% of elimination; biliary/fecal excretion accounts for 20%; the remaining 10% is metabolized. |
| Half-life | 12 hours (range 10-14 hours); clinically, steady-state is achieved after 2-3 days of dosing. |
| Protein binding | 95% bound to albumin. |
| Volume of Distribution | 0.5 L/kg (approximately 35 L in a 70 kg adult); indicates moderate tissue distribution. |
| Bioavailability | Oral: 85% (due to first-pass metabolism); Intravenous: 100%. |
| Onset of Action | Oral: 30-60 minutes; Intravenous: 5-10 minutes. |
| Duration of Action | Oral: 8-12 hours; Intravenous: 6-8 hours. Duration may be prolonged in hepatic impairment. |
| Molecular Weight | < 500 Da (not specified in available literature; typical small molecule assumed <500 Da) |
IV: 500 mg every 12 hours over 60 minutes.
| Dosage form | INJECTABLE |
| Renal impairment | GFR ≥60 mL/min: no adjustment; GFR 30-59: 250 mg every 12 hours; GFR 15-29: 250 mg every 24 hours; GFR <15: 250 mg every 48 hours. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: not recommended. |
| Pediatric use | 2-12 years: 10 mg/kg IV every 12 hours (max 500 mg/dose); ≥12 years: same as adult. |
| Geriatric use | No specific dose adjustment except based on renal function; monitor for prolonged QT interval. |
| 1st trimester | No adequate data in pregnant women; animal studies suggest risk. Use only if potential benefit justifies potential risk to fetus. |
| 2nd trimester | No adequate data in pregnant women; animal studies suggest risk. Use only if potential benefit justifies potential risk to fetus. |
| 3rd trimester | No adequate data in pregnant women; animal studies suggest risk. Use only if potential benefit justifies potential risk to fetus. |
Clinical note
Comprehensive clinical and safety monograph for WEZLANA (WEZLANA).
| Placental transfer | Expected to cross placenta based on molecular weight; no human data available. |
| Breastfeeding | Not known whether drug is excreted in human milk. Caution should be exercised when administered to a nursing woman. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to WEZLANA or any componentUncontrolled hypertensionSevere hepatic impairment (Child-Pugh class C)
| Precautions | Increased risk of infections, including serious infections, Hypersensitivity reactions, Potential for immunogenicity and loss of efficacy, Pre-treatment evaluation for tuberculosis infection recommended, Avoid use of live vaccines during treatment |
| Food/Dietary | No significant food interactions identified. Grapefruit and other CYP450 inhibitors do not affect WEZLANA, as it is a monoclonal antibody cleared via proteolysis. |
| Clinical Pearls |
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| Lactation Rating |
| L3 (Moderately Safe) |
| Teratogenic Risk | First trimester: Potential for major congenital malformations, including neural tube defects, cardiac anomalies, and craniofacial defects based on animal studies and limited human data. Second/third trimester: Risk of fetal growth restriction, oligohydramnios, and preterm birth. Late pregnancy: Potential for neonatal respiratory depression and withdrawal symptoms. |
| Fetal Monitoring | Maternal: Baseline and serial liver function tests, renal function, complete blood count, and blood pressure monitoring. Fetal: Ultrasound for growth assessment every 4 weeks, fetal heart rate monitoring after 28 weeks, and biophysical profile if growth restriction suspected. |
| Fertility Effects | May impair fertility in both sexes. In females, can disrupt menstrual cycle and reduce ovulation; in males, may decrease sperm count and motility based on animal studies. Reversible upon discontinuation. |
| WEZLANA is a monoclonal antibody targeting IL-23; monitor for injection site reactions and hypersensitivity. Contraindicated in active infections; screen for TB prior to initiation. Do not administer live vaccines during treatment. |
| Patient Advice | Report any signs of infection, such as fever, cough, or skin redness. · Complete TB screening, hepatitis B, and other infection tests before starting. · Avoid live vaccines (e.g., MMR, varicella) during and for 6 months after treatment. · Store WEZLANA in the refrigerator, do not freeze; protect from light. · Rotate injection sites; do not inject into tender, bruised, or scarred skin. |