Lumasiran
Lumasiran Uses, Dosage, Side Effects, Food Interaction and all others data.
Lumasiran is a small interfering RNA used in the treatment of primary hyperoxaluria type 1 (PH1). This condition, caused by a deficiency in the enzyme alanine-glyoxylate aminotransferase, leads to an accumulation of oxalate, causing calcium crystal formation. These patients experience frequent kidney stones, nephrocalcinosis, and renal failure.
Oxlumo, producted by Alnylam Pharmaceuticals, represents the first approved treatment for PH1. Prior to this approval, therapy consisted of symptomatic treatment such as hyperhydration, inhibitors of crystallization, pyridoxine, and renal transplant.
Lumasiran was granted FDA approval on 23 November 2020.
Trade Name | Lumasiran |
Availability | Prescription only |
Generic | Lumasiran |
Lumasiran Other Names | Lumasiran |
Related Drugs | Oxlumo |
Weight | 94.5mg/0.5ml |
Type | Subcutaneous solution |
Protein binding | Lumasiran is 77% to 85% bound to protein in plasma. |
Groups | Approved, Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | United States |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Lumasiran is lumasiran is an interfering RNA that silences hydroxyacid oxidase 1 for the treatment of primary hypoxaluria type 1.
Lumasiran is indicated for the treatment of primary hyperoxaluria type 1.
Lumasiran is also used to associated treatment for these conditions: Primary Hyperoxaluria Type I
How Lumasiran works
Patients with primary hyperoxaluria type 1 produce an excess of oxalate due to a deficiency in the enzyme alanine-glyoxylate aminotransferase.
Lumasiran is a small interfering RNA that silences the gene hydroxyacid oxidase 1 (HOA1). Lumasiran targets HOA1 mRNA, preventing translation to the enzyme glycolate oxidase (GO). Reduced levels of GO, reduce levels of glyoxylate, leaving less reactants available for metabolism to oxalate. In the ILLUMINATE trials, lumasiran reduced oxalate levels in 84% of adults and children over 6 years to at or below 1.5 times the upper limits of normal.
Toxicity
Data regarding overdoses of lumasiran are not readily available. In the event of an overdose, patients should be monitored for signs of adverse reactions and be treated symptomatically.
Food Interaction
No interactions found.Lumasiran Disease Interaction
Volume of Distribution
The apparent central volume of distribution based on population estimate is 4.9 L.
Elimination Route
In patients ≥20 kg; a 3 mg/kg subcutaneous dose of lumasiran reacheas a Cmax of 529 ng/mL, with a Tmax of 4.0 hours, and an AUC of 7400 ng*h/mL. In patients max of 912 ng/mL and an AUC of 7960 ng*h/mL.
Half Life
The mean terminal half life of lumasiran is 5.2 hours.
Clearance
The apparent plasma clearance of lumasiran based on population estimate is 26.5 L/h for an average 70 kg adult. The mean renal clearance is 2.0-3.4 L/h.
Elimination Route
7-26% of a dose of lumasiran is recovered in the urine as the unmetabolized parent compound.
A radiolabelled dose administered to rats was 19.5% recovered in urine and 33.9% recovered in feces.
Innovators Monograph
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