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. |
| Molecular Weight | 350.45 |
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 | Tesuloid is contraindicated in the first trimester due to risk of fetal developmental abnormalities based on animal studies and limited human data. |
| 2nd trimester | Use only if potential benefit justifies potential risk to the fetus; may cause fetal harm based on animal reproduction studies. |
| 3rd trimester | Avoid use in third trimester due to risk of neonatal adverse effects, including potential for neonatal withdrawal or toxicity. |
Clinical note
Comprehensive clinical and safety monograph for TESULOID (TESULOID).
| Placental transfer | Tesuloid crosses the placenta readily in animal models; human data suggest significant placental transfer with fetal drug concentrations approximating maternal levels. |
| Breastfeeding | Tesuloid is excreted into breast milk in small amounts. Caution is advised; monitor infant for potential adverse effects such as sedation or feeding difficulties. Alternative agents are preferred. |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to tesuloid or any excipientSevere hepatic impairmentConcomitant use with MAO inhibitorsPregnancy (first trimester)
| Precautions | Increased risk of infection due to immunomodulation, Possible hypersensitivity reactions including anaphylaxis, Potential reactivation of latent tuberculosis, Avoid use with live vaccines |
| Food/Dietary | Avoid grapefruit and grapefruit juice; may increase drug levels. High-fat meals may delay absorption; take with a low-fat meal. Avoid alcohol as it exacerbates GI side effects. |
| Clinical Pearls |
Loading safety data…
| Lactation Rating | L3 |
| 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. |
| 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. |
| Monitor renal function before and during therapy; adjust dose in CKD. Tessuloid can cause QT prolongation; avoid with other QT-prolonging drugs. Administer with food to reduce GI upset. Do not crush or chew extended-release tablets. |
| Patient Advice | Take exactly as prescribed; do not double doses. · Complete full course even if you feel better. · Report any signs of irregular heartbeat or fainting. · Avoid grapefruit and grapefruit juice. · Store at room temperature away from moisture. |