RYZUMVI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RYZUMVI (RYZUMVI).
RYZUMVI (risankizumab-rzaa) is a humanized IgG1 monoclonal antibody that selectively binds to the p19 subunit of interleukin-23 (IL-23), inhibiting its interaction with the IL-23 receptor. This blocks the release of pro-inflammatory cytokines, including IL-17A, IL-17F, and IL-22, involved in psoriatic inflammation.
| Metabolism | Risankizumab is a monoclonal antibody; metabolism is via catabolic pathways into small peptides and amino acids. No involvement of cytochrome P450 enzymes. |
| Excretion | Primarily hepatic metabolism with renal excretion of metabolites: approximately 60% in urine (mainly as inactive metabolites) and 30% in feces. Less than 1% excreted unchanged in urine. |
| Half-life | Terminal elimination half-life is approximately 15-34 hours (mean ~22 hours) in healthy subjects. Clinical context: The long half-life supports once-daily dosing. Steady-state is achieved within 3-5 days. |
| Protein binding | Highly protein bound (>99%) mainly to albumin. Binding is concentration-independent. |
| Volume of Distribution | Volume of distribution is approximately 1.5-2.5 L/kg, indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 94%, with no significant food effect. |
| Onset of Action | Oral: Onset of action is within 2-4 hours based on pharmacodynamic effects (e.g., improvement in insulin sensitivity). |
| Duration of Action | Duration of action is approximately 24 hours due to once-daily dosing, with sustained effects on glucose metabolism and body weight. |
40 mg orally once daily, with or without food.
| Dosage form | SOLUTION |
| Renal impairment | No dosage adjustment required for GFR ≥30 mL/min. For GFR 15-29 mL/min: 20 mg once daily. Not recommended in ESRD (GFR <15 mL/min) or on dialysis. |
| Liver impairment | Child-Pugh A: no adjustment. Child-Pugh B: 20 mg once daily. Child-Pugh C: not recommended. |
| Pediatric use | Not approved for use in pediatric patients. |
| Geriatric use | No specific dosage adjustment; use caution due to potential increased sensitivity, monitor renal function. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for RYZUMVI (RYZUMVI).
| Breastfeeding | No data on excretion in human milk; M/P ratio unknown. Due to potential for serious adverse reactions in nursing infants, advise against breastfeeding during therapy and for 2 weeks after last dose. |
| Teratogenic Risk | First trimester: No human data; animal studies show embryotoxicity at doses ≥10 mg/kg/day. Second trimester: Potential for fetal pulmonary hypoplasia due to maternal hypotension. Third trimester: Increased risk of fetal/neonatal hypotension and hypoperfusion. Overall: Avoid in pregnancy unless benefit outweighs risks. |
■ FDA Black Box Warning
None.
| Serious Effects |
["Known hypersensitivity to risankizumab or any excipient","Active serious infection (e.g., tuberculosis, sepsis)"]
| Precautions | ["Increased risk of infections; serious infections have occurred. Consider risks vs benefits in patients with chronic or recurrent infections.","Avoid use with live vaccines during treatment.","Hypersensitivity reactions, including angioedema and urticaria, have been reported.","May increase risk of malignancy; monitor for new or worsening lesions."] |
Loading safety data…
| Fetal Monitoring |
| Monitor maternal blood pressure and heart rate every 15 minutes during infusion. Assess fetal heart rate if gestational age >24 weeks. Monitor for signs of fetal distress (e.g., bradycardia) during administration. |
| Fertility Effects | In animal studies, no impairment of male or female fertility at doses up to 30 mg/kg/day. No human data available; theoretical risk of ovarian suppression due to VEGF inhibition, but clinical significance unknown. |