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Clinical ResearchResearch compound

Pitavastatin (Livalo)

A Japanese-developed statin that largely bypasses the cytochrome P450 system, giving it fewer drug interactions. Its effect on blood glucose is neutral to favourable, which is unusual within the class.

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Pitavastatin (Livalo) vial

WHAT IS PITAVASTATIN (LIVALO)?

Detailed overview

Pitavastatin is an HMG-CoA reductase inhibitor, so it works on the same principle as other statins: it slows hepatic cholesterol synthesis, the cell compensates by upregulating LDL receptors, and more receptors clear more LDL from the circulation. The Cochrane review (Adams 2020) confirmed dose-dependent LDL lowering. Two things separate it from the other statins, and both matter practically. The first is the metabolic route: pitavastatin is cleared predominantly by glucuronidation and largely bypasses the cytochrome P450 enzymes, particularly CYP3A4. That means substantially fewer drug interactions, a real advantage in patients on many medicines. One notable exception is ciclosporin: it inhibits the OATP1B1 transporter by which pitavastatin enters the liver, making co-administration an absolute contraindication. The second is the effect on carbohydrate metabolism. As a class, statins mildly increase the risk of new-onset diabetes. Pitavastatin stands apart here: the Barrios 2016 review reports a neutral to favourable effect on glucose and HbA1c. That matters in patients with diabetes or at risk of it. On clinical outcomes the key study is REAL-CAD (Taguchi 2018): in stable coronary artery disease the higher 4 mg dose produced better outcomes than 1 mg, confirming the general statin principle that more intensive LDL lowering delivers more.

Mechanism

HMG-CoA reductase inhibition: reduced hepatic cholesterol synthesis, upregulated LDL receptors.

What is different

Barely metabolised by cytochrome P450, hence fewer drug interactions.

Blood glucose

Neutral to favourable effect, in contrast to the class's mild diabetes signal.

Outcome data

REAL-CAD: 4 mg produced better outcomes than 1 mg in stable coronary artery disease.

Bioavailability

~51%, relatively high for a statin.

Data console

Lab data

/lab/molecular-data.jsonLIVE
> ATC code-
> PrescriptionN/A
> MechanismPitavastatin competitively inhibits HMG-CoA reductase, the …
> Half-life~12 hours, permitting once-daily dosing, typically in the evening.
> OnsetA fall in lipids is measurable within two weeks, with the full effect at around four weeks.
> Bioavailability~51%, a relatively high figure among statins. This is because pitavastatin undergoes limited extensive first-pass metabolism: clearance occurs largely by glucuronidation, with the cytochrome P450 system, particularly CYP3A4, barely involved.

Safety

Side effects, stop signs, contraindications

Side effects · 3

  • Muscle pain and weakness: the characteristic class effect of statins. Rhabdomyolysis is rare but possible, signalled by dark urine and marked muscle pain, and requires immediate medical attention.
  • Rising liver enzymes: usually mild and transient; worth checking at the start of treatment and on dose increase.
  • Gastrointestinal complaints and headache: common, mild effects that usually do not require stopping treatment.

Contraindications · 4

  • Concurrent ciclosporin: an absolute contraindication, as transporter inhibition raises pitavastatin levels many-fold along with the risk of muscle injury.
  • Active liver disease or persistent unexplained transaminase elevation.
  • Pregnancy and breastfeeding: contraindicated.
  • In severe renal impairment caution and dose adjustment are needed; the risk of rhabdomyolysis is higher.

Related Pharmaceuticals

Same therapeutic category

Studies

Related research and clinical findings

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Educational drug info from official sources (PubMed, FDA, EMA). Does NOT replace medical consultation or the SmPC. Talk to your doctor!

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MolekulaX Editorial Team·Source-verified · PubMed · FDA · EMA

The information here is for educational and scientific purposes only. Medication use requires medical consultation and a prescription. The indications, dose ranges, and side effects listed here do NOT replace the official Summary of Product Characteristics (SmPC) or consultation with a physician. Do not start or stop any medication on your own. In an emergency, call your local emergency number.