Pitavastatin Calcium

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Cat Number

API147526327

CAS Number

147526-32-7

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CAS Number

147526-32-7

EINECS

807-641-2

Storage

Store at room temperature

Synonyms

Pitavastatin hemicalcium; Pitavastatin calcium salt; MFCD01937979; Itavastatin calcium; Calcium (3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoate

Molecular Formula

C50H46CaF2N2O8

Molecular Weight

881

Smiles

C1C(C1)C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C4=CC=C(C=C4)F.C1C(C1)C2=NC3=CC=CC=C3C(=C2/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C4=CC=C(C=C4)F.[Ca+2]

Appearance

White to off-white powder

Melting Point

>138°C (dec.)

Boiling Point

692.0±55.0°C (Predicted)

Relative Density

1.352±0.06 (Predicted)

General Description

Pitavastatin calcium is the calcium salt of pitavastatin, a synthetic statin with a unique cyclopropyl group and a fluorinated pyrimidine ring, which provides a distinct pharmacokinetic profile. Its structure contains a 7,8-dihydroxyphenyl group and a 2-cyclopropyl-4-(4-fluorophenyl) quinoline moiety. The calcium salt improves stability, and pitavastatin is a white to off-white powder.

Mechanism of Action

Pitavastatin competitively inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, the rate-limiting enzyme in cholesterol synthesis, increasing hepatic LDL receptor expression and clearance of LDL cholesterol. Unlike some statins, pitavastatin has minimal interaction with CYP3A4, leading to fewer drug-drug interactions. It also has beneficial effects on HDL cholesterol and triglycerides.

Application

Pitavastatin is indicated for the treatment of primary hyperlipidemia and mixed dyslipidemia as an adjunct to dietary therapy. It is effective in reducing total cholesterol, LDL-C, apolipoprotein B, and triglycerides while increasing HDL-C. The drug is metabolized primarily by CYP2C9 and glucuronidation, avoiding the CYP3A4 pathway that is responsible for many statin interactions.

In REPRIEVE, 804 people with HIV on antiretroviral therapy and low-to-moderate cardiovascular risk received pitavastatin 4 mg or placebo for 24 months. Pitavastatin reduced noncalcified coronary plaque volume (mean change –1.7 vs +2.6 mm³, adjusted difference –4.3 mm³, P=0.04) and reduced progression risk by 33% (RR 0.67, P=0.003). It also lowered LDL cholesterol, oxidized LDL, and lipoprotein-associated phospholipase A2. These plaque and biomarker changes may explain the 35% MACE reduction previously reported.

Fig. 1 Effect of Biomarkers on Relative Risk of Progression of Noncalcified Plaque. (Lu MT, et al., 2024)

References

Lu MT, et al. Effects of Pitavastatin on Coronary Artery Disease and Inflammatory Biomarkers in HIV: Mechanistic Substudy of the REPRIEVE Randomized Clinical Trial. JAMA Cardiol. 2024;9(4):323-334.

In a Japanese trial (13,054 patients with stable coronary artery disease), high‑dose pitavastatin (4 mg/d) significantly reduced the primary composite endpoint (cardiovascular death, MI, stroke, unstable angina) compared to low‑dose (1 mg/d): 4.3% vs 5.4%, HR 0.81, P=0.01. LDL‑C was 14.7 mg/dL lower with high‑dose. Results were consistent across subgroups including baseline LDL‑C <95 mg/dL. High‑dose pitavastatin is beneficial in Asian patients with stable CAD.

Fig. 2 Changes in lipid parameters and high-sensitivity C-reactive protein (hsCRP) levels over time. (Taguchi I, et al., 2018)

References

Taguchi I, et al. High-Dose Versus Low-Dose Pitavastatin in Japanese Patients With Stable Coronary Artery Disease (REAL-CAD): A Randomized Superiority Trial. Circulation. 2018;137(19):1997-2009.

Does Pitavastatin Calcium require protection from light and moisture during storage?

Yes, it is sensitive to both light and moisture. Light causes photodegradation and moisture promotes hydrolysis of the statin side chain. Store in light-resistant, tightly sealed containers with desiccant.

What is the recommended storage temperature for Pitavastatin Calcium?

Store at controlled room temperature (15-25°C). Avoid temperatures above 30°C, which accelerate oxidative degradation and discoloration.

Is Pitavastatin Calcium stable in tablet formulations with standard excipients?

Yes, when formulated with antioxidants and moisture-protective packaging.

How is the impurity pitavastatin lactone (a degradation product) monitored?

This degradation product is specifically quantified using a stability-indicating HPLC method, ensuring it remains within ICH limits.