KALLIGA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for KALLIGA (KALLIGA).
KALLIGA is a recombinant urate oxidase enzyme that catalyzes the oxidation of uric acid to allantoin, a more soluble and easily excreted metabolite, thereby reducing serum uric acid levels.
| Metabolism | KALLIGA is a protein; it is expected to be degraded into smaller peptides and amino acids via catabolic pathways. No specific CYP450 enzyme involvement. |
| Excretion | Renal excretion: 70% unchanged; biliary/fecal: 20% as metabolites; 10% other |
| Half-life | Terminal elimination half-life: 12-15 hours in adults; prolonged to 24-30 hours in severe renal impairment (CrCl <30 mL/min) |
| Protein binding | 98% bound to albumin and alpha-1-acid glycoprotein |
| Volume of Distribution | 0.8-1.2 L/kg; indicates extensive extravascular distribution with high tissue penetration |
| Bioavailability | Oral: 85-95%; Intramuscular: 90-100% |
| Onset of Action | Oral: 1-2 hours; Intravenous: 5-15 minutes; Intramuscular: 30-60 minutes |
| Duration of Action | Oral: 8-12 hours; Intravenous: 6-8 hours; Intramuscular: 6-10 hours; clinical effect may persist longer in hepatic impairment |
0.5 mg orally once daily, titrated to 1 mg once daily after 2-4 weeks if tolerated.
| Dosage form | TABLET |
| Renal impairment | GFR ≥30 mL/min: no adjustment; GFR 15-29 mL/min: reduce dose by 50%; GFR <15 mL/min: avoid use. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use. |
| Pediatric use | Not approved for pediatric use. |
| Geriatric use | Initiate at 0.25 mg once daily; titrate cautiously due to increased risk of hypotension and electrolyte imbalances. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for KALLIGA (KALLIGA).
| Breastfeeding | Excretion into human milk unknown. Theoretical risk of serious adverse reactions in nursing infants. Due to potential for severe toxicity, breastfeeding is not recommended during therapy and for 3 weeks after last dose. M/P ratio not established. |
| Teratogenic Risk | KALLIGA is contraindicated in pregnancy. First trimester: High risk of major congenital malformations, particularly neural tube defects and cardiovascular anomalies. Second and third trimesters: Risk of fetal renal impairment, oligohydramnios, and neonatal renal failure. Avoid use in pregnant women. |
■ FDA Black Box Warning
Anaphylaxis and infusion reactions have been reported. Therapy should be administered in a healthcare setting prepared to manage anaphylaxis. Hemolysis and methemoglobinemia have occurred in patients with glucose-6-phosphate dehydrogenase (G6PD) deficiency.
| Serious Effects |
["Glucose-6-phosphate dehydrogenase (G6PD) deficiency","History of methemoglobinemia","Known hypersensitivity to KALLIGA or any of its components"]
| Precautions | ["Risk of anaphylaxis and infusion reactions requiring appropriate medical support","Hemolysis and methemoglobinemia in patients with G6PD deficiency; screen all patients at risk","Immunogenicity: neutralizing antibodies may develop, leading to loss of efficacy and risk of hypersensitivity reactions","Do not use in patients with known G6PD deficiency or history of methemoglobinemia"] |
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| Fetal Monitoring |
| Maternal: Renal function, liver function, serum electrolytes, and complete blood count at baseline and monthly. Fetal: Serial ultrasound for growth, amniotic fluid volume (every 2 weeks after 20 weeks), and fetal echocardiography at 18-22 weeks due to cardiac risk. Monitor for oligohydramnios in third trimester. |
| Fertility Effects | KALLIGA may impair fertility in both males and females. In males: Decreased sperm count and motility, potential for permanent azoospermia. In females: Ovarian suppression, amenorrhea, and reduced ovulation. Effects may be reversible after discontinuation but could persist. Contraception recommended during treatment. |