XURIDEN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for XURIDEN (XURIDEN).
Xuriden (uridine triacetate) is a prodrug of uridine that restores intracellular uridine nucleotide pools, which are essential for RNA and DNA synthesis, thereby reversing the toxicity of fluorouracil (5-FU) and capecitabine overdose.
| Metabolism | Xuriden is deacetylated by esterases in the plasma and tissues to release uridine, which is then further metabolized via the pyrimidine salvage pathway. |
| Excretion | Renal: predominantly as intact uridine (47-62%) and uracil (16-25%); fecal/biliary: minimal (<5%). |
| Half-life | Terminal elimination half-life: 3.5 hours (range 2.5-4.5 h). Clinically relevant for dosing interval (every 6 hours). |
| Protein binding | <5% bound to plasma proteins (albumin and alpha-1-acid glycoprotein). |
| Volume of Distribution | Vd: 0.5-0.8 L/kg, indicating distribution into total body water. |
| Bioavailability | Oral: approximately 60% (range 40-80%) due to first-pass metabolism. |
| Onset of Action | Oral: clinical effect on nutritional status observed within 2-4 days of initiation. |
| Duration of Action | Duration: approximately 6 hours with every-6-hour dosing. Prolonged nutritional therapy required. |
60 mg/kg orally once daily, rounded to the nearest 60 mg increment. Maximum dose: 6000 mg/day.
| Dosage form | GRANULE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (eGFR <30 mL/min/1.73 m²) or dialysis. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Weight-based dosing: 60 mg/kg orally once daily. Maximum dose 6000 mg/day. Administer with food. |
| Geriatric use | No specific dose adjustment recommended. Use with caution due to age-related decline in renal function; monitor renal function periodically. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for XURIDEN (XURIDEN).
| Breastfeeding | No data on presence in human milk, effects on breastfed infant, or milk production. Given the molecular weight of uridine triacetate (approximately 488 Da) and its metabolic conversion, excretion into breast milk is plausible. M/P ratio not determined. Use during breastfeeding only if clearly needed and consider alternatives or pump and discard. |
| Teratogenic Risk | No adequate and well-controlled studies in pregnant women. In animal reproduction studies, oral administration of uridine triacetate during organogenesis produced teratogenic effects (neural tube defects, skeletal malformations) at doses 0.4 times the human dose based on body surface area. Risk cannot be ruled out. First trimester: potential for major malformations; second and third trimesters: potential for fetal growth impairment and neurodevelopmental effects. |
■ FDA Black Box Warning
None.
| Serious Effects |
["None known."]
| Precautions | ["Not indicated for non-emergency use or as prophylaxis for chemotherapy.","Should be initiated as soon as possible after overdose, ideally within 96 hours.","May cause diarrhea, nausea, vomiting, and abdominal pain."] |
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| Fetal Monitoring | Monitor liver function tests (ALT, AST, bilirubin) and renal function (serum creatinine, BUN) at baseline and periodically during therapy. Perform complete blood counts to monitor for leukopenia. Monitor for signs of hypersensitivity reactions. In pregnancy, consider prenatal ultrasound for fetal growth assessment and anatomy survey. |
| Fertility Effects | No human data on fertility. In animal studies, high doses resulted in decreased spermatogenesis and testicular atrophy in males, and disrupted estrous cycles in females. Potential for reversible impairment of fertility in both sexes. |