inclisiran

Acts as a small interfering ribonucleic acid that is taken up by hepatocytes. In hepatocytes, it causes breakdown of mRNA for proprotein convertase subtilisin kexin type 9 (PCSK9), which ultimately increases low-density lipoprotein cholesterol (LDL-C) uptake and lowers LDL-C levels.

Therapeutic effects:

Reduction in LDL-C levels.

Pharmacokinetics ⬆ ⬇

Absorption: Extent of absorption unknown following SUBQ administration.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Primarily metabolized by nucleases to shorter nucleotides. 16% excreted in the urine.

Half-Life: 9 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
SUBQ	unknown	4 hr	unknown

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Hypersensitivity;
OB: Pregnancy.

Use Cautiously in:

End-stage renal disease;
Severe hepatic impairment;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

GI: diarrhea

GU: urinary tract infection

Local: injection site reactions

MS: arthralgia, pain

Resp: bronchitis, dyspnea

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANGIOEDEMA)

Interactions ⬆ ⬇

Drug-drug:

None reported.

Route/Dosage ⬆ ⬇

SC (Adults ): 284 mg as a single dose initially, then in 3 mo, then every 6 mo thereafter.

Availability ⬆ ⬇

Solution for SUBQ injection: 284 mg/1.5 mL

Assessment ⬆ ⬇

Obtain a diet history, especially with regard to fat consumption.
Monitor patient for signs and symptoms of hypersensitivity reactions (shortness of breath, wheezing, urticaria, tachycardia, angioedema).

Lab Test Considerations:

Monitor LDL-C when indicated. LDL-lowering effect may be measured as early as 30 days after starting and anytime thereafter without regard to timing of the dose.

Implementation ⬆ ⬇

Administer in combination with statin therapy.
SC: Inject into abdomen, upper arm, or thigh. Do not inject in areas of active skin disease or injury, sunburns, skin rashes, inflammation, or skin infections. Prepare injection with single dose prefilled syringe. Do not remove the needle cap until ready to inject. Solution is clear and colorless to pale yellow; do not use if cloudy, discolored, or containing particulate matter. Air bubbles may be seen in the liquid, which is normal. Do not try to remove the air.
- If a dose is missed by <3 mo, administer inclisiran and maintain dosing according to original schedule. If a dose is missed by >3 mo, restart with a new dosing schedule; administer inclisiran initially, again at 3 mo, and then every 6 mo.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Explain need for continued medical follow-up to assess effectiveness and possible side effects of medication. Periodic lab tests will be needed.
Advise patient that this medication should be used in conjunction with diet restrictions (fat, cholesterol, carbohydrates, alcohol), exercise, and cessation of smoking.
Educate patient that injection site reaction symptoms are usually mild (redness, swelling, itching, pain, tenderness, warmth, bruising, burning, or a small amount of bleeding) and last for 1–3 days.
Advise patient to notify health care professional of medication regimen before treatment or surgery.
Rep: May cause fetal harm. Advise females or reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding. Discontinue inclisiran when pregnancy is recognized.

Evaluation/Desired Outcomes ⬆ ⬇

Reduction in LDL-C levels.

US Brand Names ⬆ ⬇

Code ⬆

NDC Code

0078- Novartis Pharmaceuticals Corporation
- 0078-1000- LEQVIO
  - 0078-1000-60- 1 SYRINGE, GLASS in 1 CARTON (0078-1000-60) / 1.5 mL in 1 SYRINGE, GLASS

0078- Novartis Pharmaceuticals Corporation
- 0078-1000- LEQVIO
  - 0078-1000-98- 1 SYRINGE, GLASS in 1 CARTON (0078-1000-98) / 1.5 mL in 1 SYRINGE, GLASS

42931- Shanghai Desano Chemical Pharmaceutical Co., Ltd.
- 42931-712-
  - 42931-712-01- 1 kg in 1 DRUM (42931-712-01)

44139- Novartis Pharma Schweizerhalle AG
- 44139-0101-
  - 44139-0101-9- 2 kg in 1 BOTTLE (44139-0101-9)

70596- Agilent Technologies Inc.
- 70596-1002-
  - 70596-1002-1- 50 g in 1 BOTTLE (70596-1002-1)

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇