ZENAVOD
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZENAVOD (ZENAVOD).
ZENAVOD is a monoclonal antibody that targets the EphA2 receptor, inhibiting its tyrosine kinase activity and downstream signaling pathways involved in tumor angiogenesis and proliferation.
| Metabolism | Metabolized via proteolytic degradation into small peptides and amino acids; not metabolized by cytochrome P450 enzymes. |
| Excretion | Renal: 60% as unchanged drug, Biliary/Fecal: 30% as metabolites, 10% unchanged |
| Half-life | Terminal elimination half-life: 12 hours (range 10-14 hr); supports once-daily dosing in most patients. |
| Protein binding | 94% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | Vd: 1.2 L/kg (extensive tissue distribution, high intracellular penetration) |
| Bioavailability | Oral: 75% (fasting); reduced by 20% with high-fat meal. |
| Onset of Action | Oral: 1-2 hours; Intravenous: 5-10 minutes. |
| Duration of Action | 24 hours for bacteriostatic effect; clinical response sustained with daily dosing. |
10 mg orally once daily
| Dosage form | CAPSULE |
| Renal impairment | No adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR < 30 mL/min/1.73 m2). |
| Liver impairment | No adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not recommended in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | No specific dose adjustment required. Clinical studies included patients >65 years; no overall differences in safety or efficacy observed. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZENAVOD (ZENAVOD).
| Breastfeeding | No human lactation data; M/P ratio unknown. Excretion into breast milk likely. Consider risk of infant exposure versus benefit of therapy. |
| Teratogenic Risk | No human data; animal studies show developmental toxicity at maternal toxic doses. First trimester: potential for teratogenicity based on animal findings. Second and third trimesters: risk of fetal toxicity (e.g., low birth weight, skeletal variations) at high doses. |
| Fetal Monitoring |
■ FDA Black Box Warning
No FDA-issued black box warning as of the current data.
| Serious Effects |
["Known hypersensitivity to ZENAVOD or any of its excipients"]
| Precautions | ["Infusion-related reactions","Cardiotoxicity including left ventricular dysfunction","Thromboembolic events","Ocular toxicity including keratitis and uveitis"] |
Loading safety data…
| Monitor maternal liver function tests, blood counts, and renal function. Fetal monitoring includes growth scans and amniotic fluid index assessment during second and third trimesters. |
| Fertility Effects | Animal studies indicate impaired fertility at high doses; human data lacking. May cause reversible menstrual irregularities. |