TESULOID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TESULOID (TESULOID).
Tesuloid is a monoclonal antibody that binds to and inhibits the activity of interleukin-23 (IL-23), thereby reducing pro-inflammatory cytokine production and immune-mediated inflammation.
| Metabolism | Metabolized via general protein degradation pathways; not primarily dependent on CYP450 enzymes. |
| Excretion | Primarily renal excretion (85% unchanged, 10% as glucuronide conjugate); 5% fecal. |
| Half-life | 16–20 hours in healthy adults; prolonged to 30–40 hours in moderate renal impairment (CrCl <50 mL/min); clinically significant accumulation risk in renal disease. |
| Protein binding | 92–96% bound, primarily to albumin. |
| Volume of Distribution | 0.8–1.2 L/kg; indicates extensive extravascular distribution with moderate tissue binding. |
| Bioavailability | Oral: 75–85%; IM: 95–100% relative to IV. |
| Onset of Action | IV: 5–10 minutes; Oral: 30–60 minutes; IM: 15–30 minutes. |
| Duration of Action | IV: 6–8 hours; Oral: 8–12 hours; IM: 6–8 hours. Duration prolonged in renal impairment due to reduced clearance. |
Intravenous infusion of 500 mg over 60 minutes every 2 weeks.
| Dosage form | SOLUTION |
| Renal impairment | If GFR 30-59 mL/min: 250 mg every 2 weeks. If GFR <30 mL/min or on dialysis: 250 mg every 4 weeks. |
| Liver impairment | Child-Pugh Class A: No adjustment. Child-Pugh Class B or C: Not recommended (no dosing data). |
| Pediatric use | Not approved for use in pediatric patients (safety and efficacy not established). |
| Geriatric use | No specific dose adjustment based on age alone; monitor renal function and adjust per renal guidelines. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TESULOID (TESULOID).
| Breastfeeding | TESULOID is excreted in human milk with an M/P ratio of 0.8. Due to potential for serious adverse reactions in nursing infants, breast-feeding is not recommended during therapy and for 2 weeks after the last dose. |
| Teratogenic Risk | First trimester: Based on animal studies and limited human data, TESULOID shows a dose-dependent increase in major congenital malformations, particularly neural tube defects and cardiac anomalies. Second trimester: Risk of fetal growth restriction and oligohydramnios. Third trimester: Potential for premature closure of the ductus arteriosus and neonatal renal impairment. TESULOID is contraindicated in pregnancy unless no alternative. |
■ FDA Black Box Warning
None
| Serious Effects |
["Hypersensitivity to tesuloid or any excipients","Active serious infection, including active tuberculosis"]
| Precautions | ["Increased risk of infection due to immunomodulation","Possible hypersensitivity reactions including anaphylaxis","Potential reactivation of latent tuberculosis","Avoid use with live vaccines"] |
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| Fetal Monitoring | Monitor maternal blood pressure, renal function, and liver enzymes every 4 weeks. Fetal surveillance includes ultrasound for growth and amniotic fluid index at 28, 32, and 36 weeks; fetal echocardiography at 20-24 weeks; and nonstress test or biophysical profile weekly after 32 weeks. Monitor for preterm labor. |
| Fertility Effects | In preclinical studies, TESULOID caused reversible impairment of spermatogenesis and reduced fertility in males. In females, it prolonged estrous cycles and reduced ovulation. Human data suggest potential for decreased fertility in both sexes; effects typically reverse within 3 months of discontinuation. |