Tryngolza (olezarsen sodium)
Antihyperlipidemic - apolipoprotein Synthesis Inhibitors Subcutaneous Auto-Injector (Ml)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Olezarsen sodium is an antisense oligonucleotide that binds to apolipoprotein C-III (apoC-III) mRNA.
Olezarsen sodium is an antisense oligonucleotide directed against apolipoprotein C-III (apoC-III) mRNA and conjugated to a ligand containing 3 N-acetyl galactosamine (GalNAc) residues to enable delivery to hepatocytes. In patients with familial chylomicronemia syndrome (FCS), impaired clearance of chylomicrons from the plasma occurs due to the lack of functional lipoprotein lipase (LPL). The antisense oligonucleotide portion of olezarsen is designated to bind to human apoC-III mRNA.
Olezarsen causes degradation of apoC-III mRNA through selective binding, which results in a reduction of serum apoC-III protein. Studies suggest that apoC-III regulates both triglyceride metabolism and hepatic clearance of chylomicrons and other triglyceride-rich lipoproteins. In clinical studies, fasting apoC-III decreased following administration of olezarsen 80 mg every 4 weeks in patients with FCS.
Peak plasma concentrations of olezarsen are attained approximately 2 hours following subcutaneous administration. Olezarsen is greater than 99% plasma protein bound. Olezarsen is distributed primarily to the liver and kidneys after subcutaneous administration; the terminal half-life of the drug is approximately 4 weeks.
The antisense oligonucleotide moiety of olezarsen is metabolized by endo- and exonucleases within tissues to shorter oligonucleotide metabolites. Less than 1% of an administered dose is eliminated unchanged in urine within 24 hours.
USES: Olezarsen is used along with a proper diet to help lower fats (triglycerides) in the blood. It is used by people who have a certain inherited condition (familial chylomicronemia syndrome) that causes high levels of triglycerides in the blood. It is also used by people with very high blood triglyceride levels to help reduce the risk of pancreas disease (pancreatitis).
Olezarsen works by improving how well your body gets rid of triglycerides.
Generic name: olezarsen sodium
Pronunciation: (oh-LEH-zar-sen)
Drug class: Antihyperlipidemic - apolipoprotein Synthesis Inhibitors
Therapeutic class: Cardiovascular Therapy Agents
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Tryngolza
Indications
The following indications are listed for Tryngolza:
- Familial Chylomicronemia Syndrome
- Hypertriglyceridemia
Also known as: Abnormally Increased Triglycerides In The Blood, Elevated Triglyceride Level, Increased Triglyceride Levels.
Dosing
Dosage of olezarsen sodium is expressed in terms of olezarsen.
No dosing information is available for this tab.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Tryngolza 80 Mg/0.8 Ml Autoinj | Maintenance | Inject 80 mg by subcutaneous route once a month. |
| Tryngolza 50 Mg/0.8 Ml Autoinj | Maintenance | Inject 50 mg by subcutaneous route once a month. |
No dosing information is available for this tab.
Drug interactions
Olezarsen is not metabolized by cytochrome P-450 (CYP) enzymes, and the drug is also not an inhibitor or inducer of CYP enzymes.
Olezarsen is not a substrate or inhibitor of organic anion transporter (OAT)1, OAT3, organic cation transporter (OCT)1, OCT2, organic anion transporter polypeptide (OATP)1B1, OATP1B3, multidrug and toxic extrusion protein (MATE)1, MATE2-K, breast cancer resistance protein (BCRP), P-glycoprotein (P-gp), and bile salt export protein (BSEP).
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*History of serious hypersensitivity reactions to olezarsen or any of the excipients in the formulation.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
- Disease of liver
Adverse reactions
The most common adverse reactions (>5%) reported with olezarsen in clinical trials were injection site reactions, decreased platelet count, and arthralgia.
There are no severe adverse reactions for this drug.
More Frequent
- Arthralgia
- Injection site sequelae
- Steatosis of liver
- Thrombocytopenic disorder
Less Frequent
- Abnormal hepatic function tests
- Hyperglycemia
- Hypersensitivity drug reaction
Rare or Very Rare
- Hypercholesterolemia
Precautions
No enhanced messaging available.
Safety and efficacy of olezarsen have not been established in pediatric patients.
There are insufficient data on the use of olezarsen in pregnant women to determine whether there is a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. Patients with familial chylomicronemia syndrome (FCS) are at risk for pancreatitis during pregnancy because of defects in lipid metabolism and increased triglyceride levels.
It is not known whether olezarsen is distributed into human milk, or if the drug has any effects on the breastfed infant or on milk production. The unconjugated antisense oligonucleotide is present in the milk of lactating mice at low levels. When a drug is present in animal milk, there is a possibility it may be present in human milk; however, oligonucleotide-based products typically have poor oral bioavailability and therefore, the low levels present in milk are not likely to have clinically relevant effects in breastfed infants. Consider the benefits of breastfeeding along with the mother's clinical need for olezarsen and any potential adverse effects to the breastfed infant from the drug or underlying maternal condition.
No dosage adjustment is recommended in geriatric patients 65 years of age and older.
No overall differences in safety or effectiveness of olezarsen have been observed between patients 65 years of age and older and younger adult patients.
ICD codes
| Code | Type | Description |
|---|---|---|
| Familial chylomicronemia syndrome | ||
| E78.3 | ICD10CM | Hyperchylomicronemia |
| Hypertriglyceridemia | ||
| E78.1 | ICD10CM | Pure hyperglyceridemia |
| E78.2 | ICD10CM | Mixed hyperlipidemia |
ICD code information from First Databank (FDB).
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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