Inclisiran: Mechanism, Dosage & Side Effects
Inclisiran is an innovative medication used to lower LDL cholesterol levels. It is administered by injection just twice a year and belongs to the class of siRNA therapeutics.
Things worth knowing about "Inclisiran"
Inclisiran is an innovative medication used to lower LDL cholesterol levels. It is administered by injection just twice a year and belongs to the class of siRNA therapeutics.
What is Inclisiran?
Inclisiran is a novel, prescription-only medication used to treat elevated LDL cholesterol levels (hypercholesterolaemia) and mixed dyslipidaemia. It belongs to the class of small interfering RNA (siRNA) therapeutics and works at the molecular level within liver cells. Inclisiran is marketed under the brand name Leqvio® and has been approved by the European Medicines Agency (EMA) as well as other regulatory authorities.
Indications
Inclisiran is indicated for adults with:
- Primary hypercholesterolaemia (heterozygous familial or non-familial) or mixed dyslipidaemia
- Insufficient LDL cholesterol reduction despite maximally tolerated statin therapy
- Statin intolerance or contraindications to statin use
It is used as an adjunct to a low-cholesterol diet and, where appropriate, in combination with other lipid-lowering therapies.
Mechanism of Action
Inclisiran uses RNA interference (RNAi) to inhibit the production of the enzyme PCSK9 (proprotein convertase subtilisin/kexin type 9) in the liver. PCSK9 is an enzyme that degrades LDL receptors, which are responsible for removing LDL cholesterol from the bloodstream.
By silencing PCSK9 production, more LDL receptors remain available on the surface of liver cells, allowing greater uptake and clearance of LDL cholesterol from the blood. This results in a significant reduction in LDL cholesterol levels of up to 50%.
Difference from PCSK9 Antibodies
Unlike monoclonal antibodies such as evolocumab or alirocumab, which block the PCSK9 protein in the bloodstream, inclisiran works upstream by preventing the synthesis of the PCSK9 protein inside liver cells. This mechanism allows for a longer duration of action and a much less frequent dosing schedule.
Dosage and Administration
Inclisiran is administered as a subcutaneous injection (under the skin). The dosing schedule is particularly convenient for patients:
- First injection at the start of treatment
- Second injection after 3 months
- Subsequently, one injection every 6 months
The injection is administered by a healthcare professional, typically in a clinical setting. The dose is 284 mg of inclisiran (as inclisiran sodium).
Side Effects
Inclisiran is generally well tolerated. The most common side effects include:
- Injection site reactions: redness, pain, swelling, or bruising (very common)
- Bronchitis
- Urinary tract infections
- Joint pain (arthralgia)
- Elevated liver enzyme levels (rare)
Serious adverse effects are uncommon. Inclisiran must not be used in patients with a known hypersensitivity to the active substance or any of the excipients.
Clinical Evidence
The clinical efficacy of inclisiran has been extensively evaluated in the ORION clinical trial programme. These large-scale Phase III studies demonstrated a sustained LDL cholesterol reduction of approximately 50% throughout the treatment period. Inclisiran is especially recommended for patients who fail to achieve their LDL target values despite statin therapy or who are unable to tolerate statins.
References
- European Medicines Agency (EMA): Leqvio (inclisiran) - Product information and approval documents. https://www.ema.europa.eu
- Ray KK et al. - Two Phase 3 Trials of Inclisiran in Patients with Elevated LDL Cholesterol. New England Journal of Medicine, 2020; 382:1507-1519.
- Raal FJ et al. - Inclisiran for the Treatment of Heterozygous Familial Hypercholesterolaemia. New England Journal of Medicine, 2020; 382:1520-1530.
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