Dosing & Uses
Dosage Forms & Strengths
injectable solution
- 94.5mg/0.5mL; single-dose vial for SC injection
Hyperoxaluria
Indicated for primary hyperoxaluria type 1 (PH1) to lower urinary oxalate levels
Loading dose: 3 mg/kg SC once monthly x 3 doses
Maintenance dose
- Begin 1 month after last loading dose
- 3 mg/kg SC every 3 months
Dosage Modifications
Renal impairment
- Any severity including patients on hemodialysis: No dosage adjustment necessary
- Administer after hemodialysis on dialysis days
- Peritoneal dialysis: Not studied
Hepatic impairment
- Mild-to-moderate (total bilirubin ≤3x ULN with any AST): No dosage adjustment necessary
- Severe (total bilirubin >3x ULN and any AST): Not studied
Dosage Forms & Strengths
injectable solution
- 94.5mg/0.5mL; single-dose vial for SC injection
Hyperoxaluria
Indicated for primary hyperoxaluria type 1 (PH1) to lower urinary oxalate levels in pediatric and adult patients
Loading dose
Maintenance dose
- Begin 1 month after last loading dose
- <10 kg: 3 mg/kg SC once monthly
- 10 to <20 kg: 6 mg/kg SC once every 3 months
- ≥20 kg: 3 mg/kg SC once every 3 months
Dosage Modifications
Renal impairment
- Any severity including patients on hemodialysis: No dosage adjustment necessary
- Administer after hemodialysis on dialysis days
- Peritoneal dialysis: Not studied
Hepatic impairment
- Mild-to-moderate (total bilirubin ≤3x ULN with any AST): No dosage adjustment necessary
- Severe (total bilirubin >3x ULN and any AST): Not studied
Adverse Effects
>10%
Injection site reaction (38%)
Abdominal pain (15%)
Warnings
Contraindications
None
Pregnancy & Lactation
Pregnancy
No data available on use in pregnant females to evaluate a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes
Lactation
There are no data on drug presence in human milk, effects on breastfed children, or effects on milk production
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Lumasiran, a HAO1-directed double-stranded small interfering ribonucleic acid, reduces levels of glycolate oxidase (GO) enzyme by targeting the hydroxyacid oxidase 1 mRNA in hepatocytes through RNA interference
Decreased GO enzyme levels reduce the amount of available glyoxylate, a substrate for oxalate production
Absorption
Peak plasma concentration at steady-state: 462 ng/mL
AUC at steady-state: 6810 ng⋅hr/mL
Accumulation: None observed
Peak plasma time: 4 hr
Distribution
Vd: 4.9 L
Protein bound: 85%
Metabolism
Metabolized by endonucleases and exonucleases to oligonucleotides of shorter lengths
Elimination
Half-life: 5.2 hr
Estimated clearance: 26.5 L/hr
Excretion: Urine (<26%; unchanged with remaining excreted as inactive metabolite)
Administration
SC Administration
SC administration only
Visually inspect solution; discard if it contains particulate matter or appears cloudy or discolored; solution should appear clear, colorless-to-yellow
Use aseptic technique
Injection volumes >1.5 mL: Divide equally into multiple syringes
Injection volumes <0.3 mL: Use sterile 0.3-mL syringe; if using a 0.3-mL (30-unit) insulin syringe, 1-unit markings indicate 0.01 mL
Administer into abdomen, thigh, or side or back of upper arms
Rotate injection sites; do not inject into scar tissue or areas that are reddened, inflamed, or swollen
If injecting into abdomen, avoid area around the navel
If >1 injection is needed for a single dose, injection sites should be at least 2-cm apart
Discard unused portion of drug
Missed dose
- If dose delayed or missed, administer as soon as possible
- Resume regular scheduled dose (eg, monthly, quarterly)
Storage
Preservative-free
Store at 2-25ºC (36-77ºF)
Store in original container until ready for use
Images
Formulary
Adding plans allows you to compare formulary status to other drugs in the same class.
To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.
Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
