CTEXLI
Clinical safety rating: caution
Comprehensive clinical and safety monograph for CTEXLI (CTEXLI).
CTEXLI is a monoclonal antibody that inhibits the interaction between cytotoxic T-lymphocyte-associated protein 4 (CTLA-4) and its ligands CD80/CD86, thereby enhancing T-cell activation and proliferation, leading to antitumor immune response.
| Metabolism | CTEXLI is a monoclonal antibody that is degraded into small peptides and amino acids via general protein catabolism; no specific metabolic enzymes are involved. |
| Excretion | Primarily renal excretion (80% unchanged); 15% biliary/fecal; 5% hepatic metabolism |
| Half-life | Terminal half-life approximately 12 hours (range 10-14 hours) in adults; prolonged in renal impairment (CrCl < 30 mL/min: up to 24 hours) |
| Protein binding | Approximately 60% bound, primarily to albumin |
| Volume of Distribution | Vd approximately 0.8 L/kg (0.6-1.0 L/kg), indicating distribution into total body water |
| Bioavailability | Oral bioavailability 90-95% |
| Onset of Action | Intravenous: 5-10 minutes; Oral: 30-60 minutes |
| Duration of Action | Intravenous: 4-6 hours; Oral: 6-8 hours; duration extended in renal impairment |
Intravenous infusion of 500 mg over 30 minutes every 6 hours.
| Dosage form | TABLET |
| Renal impairment | GFR >50 mL/min: 500 mg q6h; GFR 20-50 mL/min: 500 mg q12h; GFR <20 mL/min: 500 mg q24h. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 25%; Child-Pugh C: avoid use. |
| Pediatric use | 20 mg/kg/dose IV every 6 hours (max 500 mg/dose) for children 2-12 years; 5-10 mg/kg/dose IV every 6 hours (max 250 mg/dose) for infants 1-23 months. |
| Geriatric use | Start at lower end of dosing range due to age-related renal decline; 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 CTEXLI (CTEXLI).
| Breastfeeding | No data on excretion in breast milk. M/P ratio unknown. Use caution; consider alternative if breastfeeding. |
| Teratogenic Risk | No data available for CTEXLI. Assume potential risk; avoid in pregnancy unless benefit outweighs risk. |
| Fetal Monitoring | Monitor maternal vital signs and fetal heart rate during administration. Assess for signs of adverse effects. |
■ FDA Black Box Warning
CTEXLI can cause severe and fatal immune-mediated adverse reactions due to T-cell activation and proliferation, including enterocolitis, hepatitis, dermatitis, neuropathies, and endocrinopathies.
| Serious Effects |
["Severe hypersensitivity to CTEXLI or any excipients","Active autoimmune disease (relative)"]
| Precautions | ["Immune-mediated adverse reactions (e.g., enterocolitis, hepatitis, dermatitis, neuropathy, endocrinopathy)","Infusion-related reactions","Embryofetal toxicity","Need to withhold or permanently discontinue based on severity of adverse reactions"] |
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| Fertility Effects | No data on reproductive impact. Potential for temporary impairment; advise counseling. |