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Atorvastatin

Generic Name
Atorvastatin
Brand Names
Atorvaliq, Caduet, Lipitor, Lypqozet
Drug Type
Small Molecule
Chemical Formula
C33H35FN2O5
CAS Number
134523-00-5
Unique Ingredient Identifier
A0JWA85V8F

Overview

Atorvastatin (Lipitor®), is a lipid-lowering drug included in the statin class of medications. By inhibiting the endogenous production of cholesterol in the liver, statins lower abnormal cholesterol and lipid levels, and ultimately reduce the risk of cardiovascular disease. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase, which catalyzes the conversion of HMG-CoA to mevalonic acid. This conversion is a critical metabolic reaction involved in the production of several compounds involved in lipid metabolism and transport, including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very-low-density lipoprotein (VLDL). Prescribing statins is considered standard practice for patients following any cardiovascular event, and for people who are at moderate to high risk of developing cardiovascular disease. The evidence supporting statin use, coupled with minimal side effects and long term benefits, has resulted in wide use of this medication in North America. Atorvastatin and other statins including lovastatin, pravastatin, rosuvastatin, fluvastatin, and simvastatin are considered first-line treatment options for dyslipidemia. The increasing use of this class of drugs is largely attributed to the rise in cardiovascular diseases (CVD) (such as heart attack, atherosclerosis, angina, peripheral artery disease, and stroke) in many countries. An elevated cholesterol level (elevated low-density lipoprotein (LDL) levels in particular) is a significant risk factor for the development of CVD. Several landmark studies demonstrate that the use of statins is associated with both a reduction in LDL levels and CVD risk. Statins were shown to reduce the incidences of all-cause mortality, including fatal and non-fatal CVD, as well as the need for surgical revascularization or angioplasty following a heart attack. Some evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within five years) statin use leads to a 20%-22% relative reduction in the number of major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks. Atorvastatin was first synthesized in 1985 by Dr. Bruce Roth and approved by the FDA in 1996. It is a pentasubstituted pyrrole formed by two contrasting moieties with an achiral heterocyclic core unit and a 3,5-dihydroxypentanoyl side chain identical to its parent compound. Unlike other members of the statin group, atorvastatin is an active compound and therefore does not require activation.

Background

Atorvastatin (Lipitor®), is a lipid-lowering drug included in the statin class of medications. By inhibiting the endogenous production of cholesterol in the liver, statins lower abnormal cholesterol and lipid levels, and ultimately reduce the risk of cardiovascular disease. More specifically, statin medications competitively inhibit the enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) Reductase, which catalyzes the conversion of HMG-CoA to mevalonic acid. This conversion is a critical metabolic reaction involved in the production of several compounds involved in lipid metabolism and transport, including cholesterol, low-density lipoprotein (LDL) (sometimes referred to as "bad cholesterol"), and very-low-density lipoprotein (VLDL). Prescribing statins is considered standard practice for patients following any cardiovascular event, and for people who are at moderate to high risk of developing cardiovascular disease. The evidence supporting statin use, coupled with minimal side effects and long term benefits, has resulted in wide use of this medication in North America. Atorvastatin and other statins including lovastatin, pravastatin, rosuvastatin, fluvastatin, and simvastatin are considered first-line treatment options for dyslipidemia. The increasing use of this class of drugs is largely attributed to the rise in cardiovascular diseases (CVD) (such as heart attack, atherosclerosis, angina, peripheral artery disease, and stroke) in many countries. An elevated cholesterol level (elevated low-density lipoprotein (LDL) levels in particular) is a significant risk factor for the development of CVD. Several landmark studies demonstrate that the use of statins is associated with both a reduction in LDL levels and CVD risk. Statins were shown to reduce the incidences of all-cause mortality, including fatal and non-fatal CVD, as well as the need for surgical revascularization or angioplasty following a heart attack. Some evidence has shown that even for low-risk individuals (with <10% risk of a major vascular event occurring within five years) statin use leads to a 20%-22% relative reduction in the number of major cardiovascular events (heart attack, stroke, coronary revascularization, and coronary death) for every 1 mmol/L reduction in LDL without any significant side effects or risks. Atorvastatin was first synthesized in 1985 by Dr. Bruce Roth and approved by the FDA in 1996. It is a pentasubstituted pyrrole formed by two contrasting moieties with an achiral heterocyclic core unit and a 3,5-dihydroxypentanoyl side chain identical to its parent compound. Unlike other members of the statin group, atorvastatin is an active compound and therefore does not require activation.

Indication

Atorvastatin is indicated for the treatment of several types of dyslipidemias, including primary hyperlipidemia and mixed dyslipidemia in adults, hypertriglyceridemia, primary dysbetalipoproteinemia, homozygous familial hypercholesterolemia, and heterozygous familial hypercholesterolemia in adolescent patients with failed dietary modifications. Dyslipidemia describes an elevation of plasma cholesterol, triglycerides or both as well as to the presence of low levels of high-density lipoprotein. This condition represents an increased risk for the development of atherosclerosis. Atorvastatin is indicated, in combination with dietary modifications, to prevent cardiovascular events in patients with cardiac risk factors and/or abnormal lipid profiles. Atorvastatin can be used as a preventive agent for myocardial infarction, stroke, revascularization, and angina, in patients without coronary heart disease but with multiple risk factors and in patients with type 2 diabetes without coronary heart disease but multiple risk factors. Atorvastatin may be used as a preventive agent for non-fatal myocardial infarction, fatal and non-fatal stroke, revascularization procedures, hospitalization for congestive heart failure and angina in patients with coronary heart disease. Prescribing of statin medications is considered standard practice following any cardiovascular events and for people with a moderate to high risk of development of CVD. Statin-indicated conditions include diabetes mellitus, clinical atherosclerosis (including myocardial infarction, acute coronary syndromes, stable angina, documented coronary artery disease, stroke, trans ischemic attack (TIA), documented carotid disease, peripheral artery disease, and claudication), abdominal aortic aneurysm, chronic kidney disease, and severely elevated LDL-C levels.

Associated Conditions

  • Anginal Pain
  • Cardiovascular Complications
  • Cardiovascular Disease (CVD)
  • Coronary Artery Disease (CAD)
  • Coronary artery thrombosis
  • Dysbetalipoproteinemia
  • Fredrickson Type III lipidemia
  • Heterozygous Familial Hypercholesterolemia (HeFH)
  • High Cholesterol
  • Homozygous Familial Hypercholesterolaemia (HoFH)
  • Hospitalizations
  • Hypertension, Essential Hypertension
  • Hypertriglyceridemias
  • Mixed Dyslipidemias
  • Mixed Hyperlipidemia
  • Myocardial Infarction
  • Non-familial hypercholesterolemia
  • Nonfatal Myocardial Infarction
  • Postoperative Thromboembolism
  • Primary Hypercholesterolemia
  • Stroke
  • Thrombosis
  • Transient Ischemic Attack
  • Elevation of serum triglyceride levels
  • Heterozygous familial hyperlipidemia
  • Non-familial hyperlipidemia
  • Primary Hyperlipidemia
  • Revascularization procedures

Research Report

Published: May 1, 2025

Comprehensive Report: Atorvastatin

1. Atorvastatin: Overview and Identification

1.1 Introduction to Atorvastatin and Therapeutic Class

Atorvastatin is a widely prescribed synthetic lipid-lowering agent belonging to the statin class of medications.1 As a selective inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, atorvastatin plays a critical role in managing dyslipidemia and preventing cardiovascular disease (CVD).1 Its primary therapeutic action involves reducing elevated levels of total cholesterol (Total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (apo B), and triglycerides (TG) in the blood, while variably increasing high-density lipoprotein cholesterol (HDL-C) levels.1 By modifying these lipid parameters, particularly by lowering LDL-C (often termed "bad cholesterol"), atorvastatin significantly reduces the risk of major cardiovascular events such as myocardial infarction (MI) and stroke.1

The development and widespread adoption of statins, including atorvastatin, represent a major advancement in cardiovascular medicine. Elevated cholesterol levels, especially high LDL-C, are established risk factors for atherosclerosis and subsequent CVD.[1] Atorvastatin, along with other statins like simvastatin, pravastatin, rosuvastatin, and lovastatin, is considered a first-line treatment option for managing dyslipidemia and is integral to standard care protocols following cardiovascular events or for individuals at moderate to high risk of developing CVD.[1] The extensive clinical evidence supporting the efficacy of statins, combined with a generally favorable safety profile for most patients, has led to their extensive use globally.[1]

Continue reading the full research report

Clinical Trials

Title
Posted
Study ID
Phase
Status
Sponsor
2025/06/27
Not Applicable
Not yet recruiting
Asger Lund, MD
2025/06/10
Phase 3
Not yet recruiting
Aarhus University Hospital
2025/06/06
N/A
Completed
2025/05/08
Early Phase 1
Not yet recruiting
2025/04/29
Phase 1
Recruiting
2025/04/11
Phase 2
Recruiting
Centro Cardiologico Monzino
2025/03/25
Phase 4
Recruiting
2025/03/25
Phase 4
Recruiting
2025/03/11
Not Applicable
Completed
2025/03/05
N/A
Recruiting

FDA Drug Approvals

Approved Product
Manufacturer
NDC Code
Route
Strength
Effective Date
H.J Harkins Company Inc.
76519-1063
ORAL
40 mg in 1 1
12/1/2017
NuCare Pharmaceuticals,Inc.
68071-3503
ORAL
10 mg in 1 1
9/20/2023
State of Florida DOH Central Pharmacy
53808-1067
ORAL
20 mg in 1 1
12/7/2014
Rebel Distributors Corp
42254-307
ORAL
10 mg in 1 1
9/25/2012
Dispensing Solutions, Inc.
68258-6041
ORAL
10 mg in 1 1
2/20/2012
Physicians Total Care, Inc.
54868-6319
ORAL
10 mg in 1 1
7/11/2013
PHARMAKON, LLC
49299-1092
ORAL
40 mg in 1 1
12/3/2010
Northwind Pharmaceuticals, LLC
51655-650
ORAL
40 mg in 1 1
10/21/2014
Marlex Pharmaceuticals Inc
10135-650
ORAL
20 mg in 1 1
9/12/2018
Unit Dose Services
50436-9987
ORAL
10 mg in 1 1
7/31/2017

EMA Drug Approvals

Approved Product
Authorization Holder
Status
Issued Date
No EMA approvals found for this drug.

HSA Drug Approvals

Approved Product
Manufacturer
Approval Number
Dosage Form
Strength
Approval Date
INATORVAS FILM-COATED TABLET 10MG
SIN14571P
TABLET, FILM COATED
10mg
7/10/2014
APO-ATORVASTATIN TABLET 20 MG
SIN14403P
TABLET, FILM COATED
20 MG
9/5/2013
ATOCOR 10 FILM COATED TABLET 10MG
SIN15795P
TABLET, FILM COATED
10 mg
9/4/2019
APO-ATORVASTATIN TABLET 80 MG
SIN14405P
TABLET, FILM COATED
80 MG
9/5/2013
CADUET TABLETS 10MG/10MG
SIN13059P
TABLET, FILM COATED
10 MG
3/10/2005
Eturion Tablet 40mg
SIN13300P
TABLET, FILM COATED
40mg
6/22/2007
Torvalipin Tablet 20 mg
SIN14175P
TABLET, FILM COATED
20 mg
6/22/2012
APO-ATORVASTATIN TABLET 40 MG
SIN14404P
TABLET, FILM COATED
40 MG
9/5/2013
INATORVAS FILM-COATED TABLET 80MG
SIN14574P
TABLET, FILM COATED
80mg
7/10/2014
Eturion Tablet 10mg
SIN13298P
TABLET, FILM COATED
10 mg
6/22/2007

NMPA Drug Approvals

Approved Product
Company
Approval Number
Drug Type
Dosage Form
Approval Date
Atorvastatin Calcium Dispersible Tablets
国药准字H20120021
化学药品
片剂
7/30/2021
Atorvastatin Calcium Dispersible Tablets
国药准字H20163163
化学药品
片剂
4/15/2021
Atorvastatin Calcium Capsules
国药准字H20051984
化学药品
胶囊剂
1/9/2020
Atorvastatin Calcium Capsules
国药准字H20070054
化学药品
胶囊剂
2/5/2024
Atorvastatin Calcium Tablets
国药准字HJ20240091
化学药品
片剂
9/10/2024
Atorvastatin Calcium Tablets
国药准字H20051409
化学药品
片剂
5/12/2020
Atorvastatin Calcium Tablets
国药准字H20213513
化学药品
片剂
6/18/2021
Atorvastatin Calcium Tablets
国药准字H20193332
化学药品
片剂
11/18/2019
Atorvastatin Calcium Tablets
国药准字H20233139
化学药品
片剂
2/7/2023
Atorvastatin Calcium Tablets
国药准字H20203100
化学药品
片剂
11/20/2024

PPB Drug Approvals

Approved Product
Registration No.
Company
Licence No.
Strength
Registration Date
No PPB approvals found for this drug.
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