OPUVIZ
Clinical safety rating: caution
Comprehensive clinical and safety monograph for OPUVIZ (OPUVIZ).
Opuviz is a monoclonal antibody that inhibits vascular endothelial growth factor (VEGF) by binding to VEGF-A, preventing its interaction with VEGFR-1 and VEGFR-2 receptors, thereby inhibiting angiogenesis and tumor growth.
| Metabolism | Metabolized via enzymatic proteolysis into small peptides and amino acids; not metabolized by cytochrome P450 enzymes. |
| Excretion | Renal: 70% unchanged; biliary/fecal: 20% as metabolites; 10% other |
| Half-life | Terminal half-life 12-15 hours; supports twice-daily dosing |
| Protein binding | 92% bound to albumin |
| Volume of Distribution | 0.8 L/kg; indicates extensive tissue distribution |
| Bioavailability | Oral: 45% due to first-pass metabolism |
| Onset of Action | Oral: 30-60 minutes; IV: immediate |
| Duration of Action | Oral: 6-8 hours; IV: 8-12 hours |
25 mg subcutaneously once daily. If no response after 4 weeks, increase to 50 mg subcutaneously once daily.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). Not recommended for severe renal impairment (CrCl <30 mL/min) or end-stage renal disease. |
| Liver impairment | Contraindicated in patients with moderate to severe hepatic impairment (Child-Pugh class B or C). Use caution in mild hepatic impairment (Child-Pugh class A) with no dose adjustment. |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dose. |
| Geriatric use | Clinical studies did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently. No specific dose adjustment recommended; use with caution due to potential age-related hepatic, renal, or cardiac dysfunction. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for OPUVIZ (OPUVIZ).
| Breastfeeding | No data on presence in human milk. The M/P ratio is unknown. Because of the potential for serious adverse reactions in nursing infants, breastfeeding is not recommended during treatment and for at least 2 weeks after the last dose. |
| Teratogenic Risk | OPUVIZ (setmelanotide) is a melanocortin 4 receptor agonist. In animal studies, no teratogenic effects were observed at doses up to 10 times the maximum recommended human dose. However, data in pregnant women are insufficient. Use only if benefit outweighs risk. First trimester: unknown risk; second and third trimesters: no specific fetal risks identified in animal studies. |
■ FDA Black Box Warning
WARNING: ENDOPHTHALMITIS AND RETINAL DETACHMENT - Intravitreal injections have been associated with endophthalmitis and retinal detachment. Proper aseptic technique must be used. Patients should be monitored for signs of infection or retinal detachment.
| Serious Effects |
Hypersensitivity to the active substance or any excipients. Active ocular or periocular infections. Active intraocular inflammation.
| Precautions | Increases in intraocular pressure (IOP) have been observed within 60 minutes of injection; IOP should be monitored and managed. Serious adverse events include thromboembolic events, such as myocardial infarction and stroke, though rare. Use caution in patients with a history of recent thromboembolic events. |
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| Fetal Monitoring | Monitor fetal growth via ultrasound if used during pregnancy. Monitor maternal blood pressure and heart rate due to potential cardiovascular effects. Also monitor for hypersensitivity reactions and skin hyperpigmentation. |
| Fertility Effects | In animal studies, no adverse effects on fertility were observed. In humans, no data on fertility effects. OPUVIZ is indicated for obesity due to specific genetic deficiencies; weight reduction may improve fertility in some patients. |