What is the comparison of Pitavastatin (Pitavastatin calcium), a statin (HMG-CoA reductase inhibitor)?

From the Guidelines

Pitavastatin is a potent statin medication that offers several advantages compared to other statins, including effective LDL cholesterol reduction and minimal impact on glucose metabolism, making it a good choice for patients with diabetes or prediabetes, as supported by the most recent evidence from 2024 1.

Key Characteristics of Pitavastatin

• Provides effective LDL cholesterol reduction (up to 45% at maximum doses)
• Has minimal drug interactions due to its unique metabolism pathway that doesn't heavily rely on the CYP3A4 enzyme system
• Less likely to cause muscle-related side effects than some other statins like simvastatin or atorvastatin
• Has minimal impact on glucose metabolism, making it a good choice for patients with diabetes or prediabetes

Dosage and Administration

• Typical starting dose is 1-2 mg daily, with a maximum dose of 4 mg daily
• Has a long half-life allowing for once-daily dosing, typically at bedtime

Considerations

• Generally well-tolerated, but tends to be more expensive than generic statins like atorvastatin or rosuvastatin
• Regular monitoring of liver function tests is recommended when starting therapy, though serious liver toxicity is rare

Comparison to Other Statins

• Pitavastatin has a unique profile that positions it between high-intense and moderate-intense statins, with a mean LDL-C reduction of 43-47% 1
• The 2024 recommendations on the optimal use of lipid-lowering therapy suggest pitavastatin as a rational treatment choice in patients with metabolic disturbances, diabetes/risk of diabetes, and pre-diabetes 1

From the FDA Drug Label

Pitavastatin tablets were compared with atorvastatin calcium tablets (referred to as atorvastatin) in a randomized, multicenter, double-blind, double-dummy, active-controlled, non-inferiority study of 817 adult patients with primary hyperlipidemia or mixed dyslipidemia Pitavastatin tablets were compared with simvastatin tablets (referred to as simvastatin) in a randomized, multicenter, double-blind, double-dummy, active-controlled, non-inferiority study of 843 adult patients with primary hyperlipidemia or mixed dyslipidemia Pitavastatin tablets were compared with pravastatin sodium tablets (referred to as pravastatin) in a randomized, multicenter, double-blind, double-dummy, parallel group, active-controlled non-inferiority study of 942 geriatric patients (≥65 years) with primary hyperlipidemia or mixed dyslipidemia

The comparison of Pitavastatin to other statins is as follows:

• Pitavastatin was non-inferior to Atorvastatin for the two pairwise comparisons: Pitavastatin 2 mg vs. atorvastatin 10 mg and pitavastatin 4 mg vs. atorvastatin 20 mg.
• Pitavastatin was non-inferior to Simvastatin for the two pairwise comparisons: Pitavastatin 2 mg vs. simvastatin 20 mg and pitavastatin 4 mg vs. simvastatin 40 mg.
• Pitavastatin significantly reduced LDL-C compared to Pravastatin as demonstrated by the following pairwise dose comparisons: Pitavastatin 1 mg vs. pravastatin 10 mg, pitavastatin 2 mg vs. pravastatin 20 mg and pitavastatin 4 mg vs. pravastatin 40 mg. 2

From the Research

Comparison of Pitavastatin with Other Statins

• Pitavastatin has been shown to have a potent LDL-C-reducing activity, equivalent to that of atorvastatin 10 to 20 mg, with doses of 2 to 4 mg 3
• Clinical trials have revealed that pitavastatin has a superior HDL-C-elevating activity compared to atorvastatin, with sustained and incremental effects in long-term trials 3, 4
• Pitavastatin has been found to have a similar LDL-C-lowering effect to other strong statins, such as rosuvastatin, with equal reductions in LDL-C and LDL particles 5
• The safety and efficacy of pitavastatin have been compared to other statins, including atorvastatin and rosuvastatin, with no significant differences in adverse event rates or efficacy 5, 6

Pharmacokinetic Properties

• Pitavastatin is minimally metabolized by CYP enzymes, resulting in minimal drug-drug interactions (DDIs) 3, 4
• Pitavastatin can interact with some drugs that inhibit drug transporters, but the risk of DDIs is lower compared to other statins 4

Clinical Implications

• Pitavastatin may be preferred in patients with metabolic syndrome, as it produces adequate control of LDL-C and TG, along with potent and incremental HDL-C elevation 3
• The highest dose of pitavastatin (4 mg) may be preferred in high-risk patients, as it has been shown to be more effective in reducing cardiovascular events 4
• Pitavastatin appears to be well suited for long-term use, with relatively few drug-drug interactions and no adverse effects on blood glucose 6