Pravastatin is the 6-alpha-hydroxy acid form of mevastatin.¹¹ Pravastatin was firstly approved in 1991 becoming the second available statin in the United States. It was the first statin administered as the active form and not as a prodrug.¹⁰ This drug was developed by Sankyo Co. Ltd.; however, the first approved pravastatin product was developed by Bristol Myers Squibb and FDA approved in 1991.¹⁴

Pravastatin is made through a fermentation process in which mevastatin is first obtained. The manufacturing process is followed by the hydrolysis of the lactone group and the biological hydroxylation with Streptomyces carbophilus to introduce the allylic 6-alcohol group.¹²

Structure

Similar Structures

Synonyms

(+)-(3R,5R)-3,5-dihydroxy-7-[(1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-{[(S)-2-methylbutyryl]oxy}-1,2,6,7,8,8a-hexahydro-1-naphthyl]heptanoic acid
Pravastatin
Pravastatin acid
Pravastatina
Pravastatine
Pravastatinum

Product Ingredients

Ingredient	UNII	CAS	InChI Key
Pravastatin sodium	3M8608UQ61	81131-70-6	VWBQYTRBTXKKOG-IYNICTALSA-M

Product Images

Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
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Act Pravastatin	Tablet	40 mg	Oral	Actavis Pharma Company	2003-12-09	Not applicable
Act Pravastatin	Tablet	20 mg	Oral	Actavis Pharma Company	2003-12-09	Not applicable
Act Pravastatin	Tablet	10 mg	Oral	Actavis Pharma Company	2003-12-09	Not applicable
Bio Pravastatin	Tablet	10 mg	Oral	Bioenhance Medicines Inc.	2001-07-12	2003-02-27
Bio Pravastatin	Tablet	40 mg	Oral	Bioenhance Medicines Inc.	2001-07-12	2003-02-27
Bio Pravastatin	Tablet	20 mg	Oral	Bioenhance Medicines Inc.	2001-07-12	2003-02-27
M-pravastatin	Tablet	40 mg	Oral	Mantra Pharma Inc	Not applicable	Not applicable
M-pravastatin	Tablet	40 mg	Oral	Mantra Pharma Inc	Not applicable	Not applicable
M-pravastatin	Tablet	20 mg	Oral	Mantra Pharma Inc	2018-12-11	Not applicable
M-pravastatin	Tablet	20 mg	Oral	Mantra Pharma Inc	Not applicable	Not applicable

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Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

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Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
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Ach-pravastatin	Tablet	20 mg	Oral	Accord Healthcare Limited	Not applicable	Not applicable
Ach-pravastatin	Tablet	10 mg	Oral	Accord Healthcare Limited	Not applicable	Not applicable
Ach-pravastatin	Tablet	40 mg	Oral	Accord Healthcare Limited	Not applicable	Not applicable
Ag-pravastatin	Tablet	40 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-pravastatin	Tablet	20 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Ag-pravastatin	Tablet	10 mg	Oral	Angita Pharma Inc.	Not applicable	Not applicable
Apo-pravastatin	Tablet	40 mg	Oral	Apotex Corporation	2001-02-27	Not applicable
Apo-pravastatin	Tablet	20 mg	Oral	Apotex Corporation	2001-02-27	Not applicable
Apo-pravastatin	Tablet	10 mg	Oral	Apotex Corporation	2001-02-27	Not applicable
Auro-pravastatin	Tablet	20 mg	Oral	Auro Pharma Inc	Not applicable	Not applicable

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Application Number

A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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Product Code

A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Mixture Products

Name	Ingredients	Dosage	Route	Labeller	Marketing Start	Marketing End
Pal-pravastatin-asa	Pravastatin sodium (40 mg) + Acetylsalicylic acid (81 mg)	Kit; Tablet; Tablet, delayed release	Oral	Paladin Labs Inc	2006-01-13	2015-07-31
Pal-pravastatin-asa	Pravastatin sodium (20 mg) + Acetylsalicylic acid (81 mg)	Kit; Tablet; Tablet, delayed release	Oral	Paladin Labs Inc	2006-01-13	2015-07-31
Pal-pravastatin-asa	Pravastatin sodium (10 mg) + Acetylsalicylic acid (81 mg)	Kit; Tablet; Tablet, delayed release	Oral	Paladin Labs Inc	2006-01-13	2015-07-31
Pravigard Pac	Pravastatin sodium + Acetylsalicylic acid	Tablet		Bristol-Myers Squibb Company	2006-10-12	2006-10-12
Pravigard Pac	Pravastatin sodium (40 mg/1) + Acetylsalicylic acid (81 mg/1)	Kit		E.R. Squibb & Sons, L.L.C.	2005-01-01	2006-12-31
Pravigard Pac	Pravastatin sodium + Acetylsalicylic acid	Tablet		Bristol-Myers Squibb Company	2006-10-12	2006-10-12
Pravigard Pac	Pravastatin sodium + Acetylsalicylic acid	Tablet		Bristol-Myers Squibb Company	2006-10-12	2006-10-12
Pravigard Pac	Pravastatin sodium + Acetylsalicylic acid	Kit		Bristol-Myers Squibb Company	2006-10-12	2006-10-12
Pravigard Pac	Pravastatin sodium (40 mg/1) + Acetylsalicylic acid (325 mg/1)	Kit		E.R. Squibb & Sons, L.L.C.	2006-01-01	2007-04-30

International/Other Brands

Elisor (Baowei Technology Group) / Lipostat (Bristol-Myers Squibb) / Mevalotin (Daiichi Sankyo) / Pravaselect / Selipran (Bristol-Myers Squibb)

Categories

UNII

KXO2KT9N0G

CAS number

81093-37-0

Weight

Average: 424.5277
Monoisotopic: 424.246103506

Chemical Formula

C₂₃H₃₆O₇

InChI Key

TUZYXOIXSAXUGO-PZAWKZKUSA-N

InChI

InChI=1S/C23H36O7/c1-4-13(2)23(29)30-20-11-17(25)9-15-6-5-14(3)19(22(15)20)8-7-16(24)10-18(26)12-21(27)28/h5-6,9,13-14,16-20,22,24-26H,4,7-8,10-12H2,1-3H3,(H,27,28)/t13-,14-,16+,17+,18+,19-,20-,22-/m0/s1

IUPAC Name

(3R,5R)-7-[(1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-{[(2S)-2-methylbutanoyl]oxy}-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]-3,5-dihydroxyheptanoic acid

SMILES

[H][C@]12[C@H](C[C@H](O)C=C1C=C[C@H](C)[C@@H]2CC[C@@H](O)C[C@@H](O)CC(O)=O)OC(=O)[C@@H](C)CC

Pharmacology

Indication

Pravastatin is indicated for primary prevention of coronary events hypercholesterolemic patients without clinical evidence of coronary heart disease. Its use includes the reduction of risk on myocardial infarction, undergoing myocardial revascularization procedures and cardiovascular mortality.¹⁰

As well, pravastatin can be used as a secondary prevention agent for cardiovascular events in patients with clinically evident coronary heart disease. This indication includes the reduction of risk of total mortality by reducing coronary death, myocardial infarction, undergoing myocardial revascularization procedures, stroke, and stroke/transient ischemic attack as well as to slow the progression of coronary atherosclerosis.¹⁰

The term cardiovascular events correspond to all the incidents that can produce damage to the heart muscle including the interruption of blood flow.¹⁵

As adjunctive therapy to diet, pravastatin is used in:

Patients with primary hypercholesterolemia and mixed dyslipidemias including hyperlipidemia type IIa and IIb.
Patients with elevated serum triglycerides including type IV hyperlipidemia.
Patients with heterozygous familial hypercholesterolemia in patients over 8 years of age with low-density lipoprotein (LDL) cholesterol higher than 190 mg/dl after diet modifications or LDL levels higher than 160 mg/dl and familial history of premature cardiovascular diseases or at least two cardiovascular risk factors.¹⁰

In patients that do not respond adequately to diet, pravastatin is used to treat patients with primary dysbetalipoproteinemia (type III hyperlipidemia).¹⁰

Dyslipidemia is defined as 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.¹⁶

Associated Conditions

Pharmacodynamics

The action of pravastatin on the 3-hydroxy-3-methyl-glutaryl-coenzyme A (HMG-CoA) reductase produces an increase in the expression of hepatic LDL receptors which in order decreases the plasma levels of LDL cholesterol.¹⁰

The effect of pravastatin has been shown to significantly reduce the circulating total cholesterol, LDL cholesterol, and apolipoprotein B. As well, it modestly reduces very low-density-lipoproteins (VLDL) cholesterol and triglycerides while increasing the level of high-density lipoprotein (HDL) cholesterol and apolipoprotein A.¹⁷

In clinical trials with patients with a history of myocardial infarction or angina with high total cholesterol, pravastatin decreased the level of total cholesterol by 18%, decreased of LDL by 27%, decreased of triglycerides by 6% and increased of high-density lipoprotein (HDL) by 4%. As well, there was reported a decrease in risk of death due to coronary disease of 24%.¹

When coadministered with cholestyramine, pravastatin can reduce by 50% the levels of LDL and slow the progression of atherosclerosis and the risk of myocardial infarction and death.¹⁰

Mechanism of action

Pravastatin is a specific inhibitor of the hepatic HMG-CoA reductase in humans.¹⁰ The inhibition of this enzyme produces a reduction in cholesterol biosynthesis as HMG-CoA reductase activity is an early-limiting step in cholesterol biosynthesis.⁶

The inhibitory mechanism of action produces a reduction in cholesterol synthesis which in order has been observed to increase the number of LDL receptors on cell surfaces and an enhancement in receptor-mediated metabolism of LDL and clearance.⁵

On the other hand, pravastatin-driven inhibition of LDL production inhibits hepatic synthesis of VLDL as the LDL is the precursor for these molecules.⁷

Target	Actions	Organism
A3-hydroxy-3-methylglutaryl-coenzyme A reductase	inhibitor	Humans

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Absorption

Pravastatin is absorbed 60-90 min after oral administration and it presents a low bioavailability of 17%.² This low bioavailability can be presented due to the polar nature of pravastatin which produces a high range of first-pass metabolism and incomplete absorption.¹²

Pravastatin is rapidly absorbed from the upper part of the small intestine via proton-coupled carrier-mediated transport to be later taken up in the livery by the sodium-independent bile acid transporter.⁴ The reported time to reach the peak serum concentration in the range of 30-55 mcg/L is of 1-1.5 hours with an AUC ranging from 60-90 mcg.h/L.⁸

Volume of distribution

The reported steady-state volume of distribution of pravastatin is reported to be of 0.5 L/kg.⁹ This pharmacokinetic parameter in children was found to range from 31-37 ml/kg.⁸

Protein binding

Due its polarity, pravastatin binding to plasma proteins is very limited and the bound form represents only about 43-48% of the administered dose. However, the activity of p-glycoprotein in luminal apical cells and OATP1B1 produce significant changes to pravastatin distribution and elimination.¹

Metabolism

After initial administration, pravastatin undergoes extensive first-pass extraction in the liver.² However, pravastatin's metabolism is not related to the activity of the cytochrome P-450 isoenzymes and its processing is performed in a minor extent in the liver. Therefore, this drug is highly exposed to peripheral tissues.¹

The metabolism of pravastatin is ruled mainly by the presence of glucuronidation reactions with very minimal intervention of CYP3A enzymes. After metabolism, pravastatin does not produce active metabolites.² This metabolism is mainly done in the stomach followed by a minor portion of renal and hepatic processing.⁴

The major metabolite formed as part of pravastatin metabolism is the 3-alpha-hydroxy isomer. The activity of this metabolite is very clinically negligible.¹⁷

Route of elimination

From the administered dose of pravastatin, about 70% is eliminated in the feces while about 20% is obtained in the urine.¹³

When pravastatin is administered intravenously, approximately 47% of the administered dose is eliminated via the urine with 53% of the dose eliminated either via biotransformation of biliary.¹⁷

Half life

The reported elimination half-life of pravastatin is reported to be of 1.8 hours.²

Clearance

The reported clearance rate of pravastatin ranges from 6.3-13.5 ml.min/kg in adults⁹ while in children it has been reported to be of 4-11 L/min.⁸

Toxicity

The reported oral LD50 of pravastatin in mice is of 8939 mg/kg.^MSDS There haven't been significant overdosage reports however, in the case of overdosage, symptomatic treatment is recommended along with laboratory monitoring and supportive measures.^Label

In carcinogenic studies, high dose administration of pravastatin has been reported to increase the incidence of hepatocellular carcinomas in males and lung carcinomas in females. There is no evidence relating the administration of pravastatin with mutagenicity in different assays not to produce effects in fertility or reproductive potential.^Label

Affected organisms

Humans and other mammals

Pathways

Pathway	Category
Pravastatin Action Pathway	Drug action

Pharmacogenomic Effects/ADRs

Interacting Gene/Enzyme	Allele name	Genotype(s)	Defining Change(s)	Type(s)	Description	Details
Kinesin-like protein KIF6	---	(C;C) / (C;T)	C Allele	Effect Directly Studied	Patients with this genotype have a greater reduction in risk of a major cardiovascular event with high dose pravastatin.	Details
3-hydroxy-3-methylglutaryl-coenzyme A reductase	---	(A;T)	T Allele	Effect Directly Studied	Patients with this genotype have a lesser reduction in LDL cholesterol with pravastatin.	Details

Interactions

Drug Interactions

Drug	Interaction
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(R)-warfarin	The risk or severity of bleeding can be increased when Pravastatin is combined with (R)-warfarin.
(S)-Warfarin	The risk or severity of bleeding can be increased when Pravastatin is combined with (S)-Warfarin.
4-hydroxycoumarin	The risk or severity of bleeding can be increased when Pravastatin is combined with 4-hydroxycoumarin.
Abemaciclib	The serum concentration of Pravastatin can be increased when it is combined with Abemaciclib.
Acebutolol	The serum concentration of Acebutolol can be increased when it is combined with Pravastatin.
Acenocoumarol	The risk or severity of bleeding can be increased when Pravastatin is combined with Acenocoumarol.
Acetaminophen	The serum concentration of Pravastatin can be increased when it is combined with Acetaminophen.
Acetylcysteine	The excretion of Pravastatin can be decreased when combined with Acetylcysteine.
Acetylsalicylic acid	The excretion of Pravastatin can be decreased when combined with Acetylsalicylic acid.
Acipimox	Acipimox may increase the myopathic rhabdomyolysis activities of Pravastatin.

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Food Interactions

Avoid alcohol.
Avoid drastic changes in dietary habit.
Take without regard to meals.

References

Synthesis Reference

US6204032

General References

Salna MP, Singer HM, Dana AN: Pravastatin-Induced Eczematous Eruption Mimicking Psoriasis. Case Rep Dermatol Med. 2017;2017:3418204. doi: 10.1155/2017/3418204. Epub 2017 Jul 31. [PubMed:28831316]
Chastain DB, Stover KR, Riche DM: Evidence-based review of statin use in patients with HIV on antiretroviral therapy. J Clin Transl Endocrinol. 2017 Feb 22;8:6-14. doi: 10.1016/j.jcte.2017.01.004. eCollection 2017 Jun. [PubMed:29067253]
Fitzpatrick T, Perrier L, Tricco AC, Straus SE, Juni P, Zwarenstein M, Lix LM, Smith M, Rosella LC, Henry DA: Protocol for a scoping review of post-trial extensions of randomised controlled trials using individually linked administrative and registry data. BMJ Open. 2017 Feb 17;7(2):e013770. doi: 10.1136/bmjopen-2016-013770. [PubMed:28213601]
Hatanaka T: Clinical pharmacokinetics of pravastatin: mechanisms of pharmacokinetic events. Clin Pharmacokinet. 2000 Dec;39(6):397-412. doi: 10.2165/00003088-200039060-00002. [PubMed:11192473]
Ye YC, Zhao XL, Zhang SY: Use of atorvastatin in lipid disorders and cardiovascular disease in Chinese patients. Chin Med J (Engl). 2015 Jan 20;128(2):259-66. doi: 10.4103/0366-6999.149226. [PubMed:25591572]
McIver LA, Siddique MS: Atorvastatin . [PubMed:28613530]
Ray SK, Rege NN: Atorvastatin: in the management of hyperlipidaemia. J Postgrad Med. 2000 Jul-Sep;46(3):242-3. [PubMed:11298482]
Wiersma HE, Wiegman A, Koopmans RP, Bakker HD, Kastelein JJ, van Boxtel CJ: Steady-state pharmacokinetics of pravastatin in children with familial hypercholesterolaemia. Clin Drug Investig. 2004;24(2):113-20. doi: 10.2165/00044011-200424020-00006. [PubMed:17516697]
Singhvi SM, Pan HY, Morrison RA, Willard DA: Disposition of pravastatin sodium, a tissue-selective HMG-CoA reductase inhibitor, in healthy subjects. Br J Clin Pharmacol. 1990 Feb;29(2):239-43. [PubMed:2106337]
Frishman W., Cheng-Lai A. and Nawarskas J. (2005). Current cardiovascular drugs (4th ed.). Current medicine LLC. [ISBN:1-57340-221-4]
William H. Frishman, MD, Domenic A. Sica, MD (2011). Cardiovascular Pharmacotherapeutics. Cardiotext Publishing. [ISBN:9781935395621]
Wolpe P. and Howard J. (2007). Comprehensive Medicinal Chemistry II. Elsevier.
Lemke T., Williams D., Roche V. and Zito W. (2008). Foye's Principles of Medicinal Chemistry (6th) (6th ed.). Lippincott Williams & Wilkins. [ISBN:978-0-7817-6879-5]
FDA approvals [Link]
Chemocare [Link]
Merck Manuals [Link]
PRAVACHOL (pravastatin) monograph [File]

External Links

Human Metabolome Database: HMDB0005022
KEGG Drug: D08410
KEGG Compound: C01844
PubChem Compound: 54687
PubChem Substance: 46504851
ChemSpider: 49398
BindingDB: 20688
ChEBI: 63618
ChEMBL: CHEMBL1144
Therapeutic Targets Database: DAP000550
PharmGKB: PA451089
Wikipedia: Pravastatin

ATC Codes

C10AA03 — Pravastatin

C10BA03 — Pravastatin and fenofibrate

C10BX02 — Pravastatin and acetylsalicylic acid

AHFS Codes

24:06.08 — Hmg-coa Reductase Inhibitors

FDA label

Download (251 KB)

MSDS

Download (23.5 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
0	Completed	Prevention	Ventilator-associated Bacterial Pneumonia	1
1	Active Not Recruiting	Prevention	Preeclampsia	1
1	Active Not Recruiting	Treatment	Leukemias	1
1	Completed	Not Available	Healthy Volunteers	4
1	Completed	Basic Science	Cancer, Breast	1
1	Completed	Basic Science	Drug Biotransformation / Membrane Transport	1
1	Completed	Basic Science	Drug Drug Interaction (DDI)	1
1	Completed	Basic Science	Drug Interaction Potentiation	1
1	Completed	Basic Science	Genotype-related Drug Metabolism	1
1	Completed	Basic Science	Healthy Volunteers	3
1	Completed	Basic Science	Rheumatoid Arthritis	1
1	Completed	Other	Healthy Volunteers / Rheumatoid Arthritis	1
1	Completed	Prevention	Glomerulonephritis minimal lesion / Hyperlipidemias	1
1	Completed	Treatment	Acute Kidney Injury (AKI)	1
1	Completed	Treatment	Drug Distribution	1
1	Completed	Treatment	HIV Seronegativity / Human Immunodeficiency Virus (HIV) Infections / Lipodystrophies	1
1	Completed	Treatment	Healthy Volunteers	4
1	Completed	Treatment	Human Immunodeficiency Virus (HIV) Infections	3
1	Completed	Treatment	Leukemias	1
1	Completed	Treatment	Therapeutic Equivalency	2
1	Recruiting	Other	Healthy Volunteers	1
1	Recruiting	Treatment	Dyslipidemias / Peripheral Artery Disease (PAD)	1
1, 2	Terminated	Treatment	Adult Acute Megakaryoblastic Leukemia (M7) / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Recurrent Adult Acute Myeloid Leukemia	1
1, 2	Terminated	Treatment	Albinism, Oculocutaneous / Hermansky-Pudlak Syndrome (HPS) / Metabolic Diseases / Platelet Storage Pool Deficiency / Pulmonary Fibrosis	1
2	Active Not Recruiting	Treatment	CHILD B / Hepatocellular,Carcinoma	1
2	Active Not Recruiting	Treatment	Leukemias	1
2	Completed	Treatment	Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia	1
2	Completed	Treatment	Diabetes Mellitus (DM) / High Cholesterol / Metabolic Syndromes	1
2	Completed	Treatment	Dyslipidemias	1
2	Completed	Treatment	Fibrosis	1
2	Completed	Treatment	High Cholesterol / Human Immunodeficiency Virus (HIV) Infections	1
2	Completed	Treatment	High Cholesterol / Statin-Associated Myopathy	1
2	Completed	Treatment	Hutchinson-Gilford Syndrome / Progeria	1
2	Completed	Treatment	Lupus / Systemic Lupus Erythematosus (SLE)	1
2	Completed	Treatment	Type II Hyperlipidaemia	1
2	Enrolling by Invitation	Treatment	Progeria	1
2	Not Yet Recruiting	Treatment	Pulmonary Tuberculosis (TB) / Tuberculosis Infection	1
2	Not Yet Recruiting	Treatment	Tuberculosis Infection	1
2	Recruiting	Prevention	Prophylaxis of preeclampsia	1
2	Recruiting	Treatment	Coronary Heart Disease (CHD) / Human Immunodeficiency Virus (HIV) Infections	1
2	Unknown Status	Treatment	Advanced Hepatocarcinoma	1
2	Withdrawn	Treatment	Human Immunodeficiency Virus Type 1 (HIV-1) Infection	1
2	Withdrawn	Treatment	Mucocutaneous Lymph Node Syndrome	1
3	Active Not Recruiting	Treatment	High Cholesterol	1
3	Completed	Basic Science	High Cholesterol / Hyperlipoproteinemias	1
3	Completed	Prevention	Cardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Diabetes Mellitus (DM) / Heart Diseases / Heart Failure / High Blood Pressure (Hypertension) / High Cholesterol / Myocardial Infarction / Myocardial Ischemia	1
3	Completed	Prevention	Cardiovascular Disease (CVD) / Kidney Diseases / Microalbuminuria	1
3	Completed	Prevention	Stroke, Ischemic	1
3	Completed	Treatment	Arterial Occlusive Diseases / Cardiovascular Disease (CVD) / Diabetes Mellitus (DM) / Heart Diseases / Vascular Diseases	1
3	Completed	Treatment	Atherosclerosis / Cardiovascular Disease (CVD)	1
3	Completed	Treatment	Autosomal Dominant Polycystic Kidney Disease （ADPKD)	1
3	Completed	Treatment	Child-Pugh A Hepatocellular Carcinoma	1
3	Completed	Treatment	Chronic Allograft Nephropathy (CAN) / End-Stage Renal Disease (ESRD)	1
3	Completed	Treatment	Combined Hyperlipidemia	1
3	Completed	Treatment	High Cholesterol	2
3	Completed	Treatment	Human Immunodeficiency Virus (HIV) Infections / Lipodystrophies	1
3	Completed	Treatment	Hypercholesterolemia or Combined Dyslipidemia	1
3	Completed	Treatment	Hyperlipidemias	1
3	Completed	Treatment	Hyperlipoproteinemia Type III	1
3	Completed	Treatment	Liver Cancer	1
3	Completed	Treatment	Lung Cancers	1
3	Completed	Treatment	Relapsing Remitting Multiple Sclerosis (RRMS)	1
3	Not Yet Recruiting	Prevention	Hypertension in Pregnancy / Obstetric Labor Complications / Preeclampsia	1
3	Recruiting	Treatment	High Cholesterol	1
3	Terminated	Treatment	High Blood Pressure (Hypertension)	1
3	Terminated	Treatment	High Cholesterol	1
4	Completed	Prevention	Actue Coronary Syndromes	1
4	Completed	Prevention	Aging / Alzheimer's Disease (AD)	1
4	Completed	Prevention	Cardiovascular Disease (CVD)	1
4	Completed	Prevention	Hyperlipidemias	1
4	Completed	Treatment	Acute Coronary Syndromes (ACS)	1
4	Completed	Treatment	Cardiovascular Disease (CVD) / Glucose Metabolism / Human Immunodeficiency Virus (HIV) Infections / Lipodystrophies / Metabolic Abnormality / Metabolism, Lipids	1
4	Completed	Treatment	Chronic Heart Failure (CHF)	1
4	Completed	Treatment	Chronic Kidney Disease (CKD)	1
4	Completed	Treatment	Chronic Stable Angina Pectoris / Non ST Segment Elevation Myocardial Infarction (NSTEMI) / Unstable Angina Pectoris	1
4	Completed	Treatment	Coronary Arteriosclerosis	1
4	Completed	Treatment	Coronary Heart Disease (CHD) / High Cholesterol	1
4	Completed	Treatment	Diabetes Mellitus (DM) / Prediabetic State	1
4	Completed	Treatment	Dyslipidemias	2
4	Completed	Treatment	High Cholesterol	2
4	Completed	Treatment	Human Immunodeficiency Virus (HIV) Infections / Hyperlipidemias	2
4	Completed	Treatment	Hypertriglycemia / Type 2 Diabetes Mellitus	1
4	Completed	Treatment	Multi-vessel Diseases, Angina	1
4	Completed	Treatment	Mixed hypercholesterolemia / Primary Dyslipidemia	1
4	Completed	Treatment	Schizoaffective Disorders / Schizophrenic Disorders	1
4	Completed	Treatment	Schizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorders	1
4	Completed	Treatment	Type IIa and IIb Hypercholesterolaemia	1
4	Recruiting	Health Services Research	Diabetes Mellitus (DM)	1
4	Recruiting	Prevention	High Blood Pressure (Hypertension) / Strokes / Transient Ischaemic Attack (TIA)	1
4	Recruiting	Treatment	Autosomal Dominant Polycystic Kidney Disease （ADPKD)	1
4	Recruiting	Treatment	Coronary Artery Disease	1
4	Terminated	Not Available	Statin Adverse Reaction / Statin-Associated Myopathy	1
4	Terminated	Treatment	Chronic Kidney Disease (CKD)	1
4	Terminated	Treatment	Heart Failure	1
4	Unknown Status	Prevention	Acute Myocardial Infarction (AMI)	1
4	Unknown Status	Treatment	Coronary Heart Disease (CHD) / High Cholesterol	1
4	Unknown Status	Treatment	Drug-eluting Stent (DES)	1
4	Unknown Status	Treatment	Esophageal Cancers / Malignant Neoplasm of Stomach	1
4	Unknown Status	Treatment	Human Immunodeficiency Virus (HIV) / Human Immunodeficiency Virus (HIV) Infections / Hyperlipidemias	1
Not Available	Completed	Not Available	Cardiovascular Disease (CVD) / Type 2 Diabetes Mellitus	1
Not Available	Completed	Not Available	High Cholesterol	3
Not Available	Completed	Not Available	Pediatrics Patients on Dialysis	1
Not Available	Completed	Not Available	Postpartum Depression	1
Not Available	Completed	Prevention	Cardiovascular Disease Risk / Human Immunodeficiency Virus (HIV) Infections	1
Not Available	Completed	Treatment	Adult Acute Megakaryoblastic Leukemia (M7) / Adult Acute Minimally Differentiated Myeloid Leukemia (M0) / Adult Acute Monoblastic Leukemia (M5a) / Adult Acute Monocytic Leukemia (M5b) / Adult Acute Myeloblastic Leukemia With Maturation (M2) / Adult Acute Myeloblastic Leukemia Without Maturation (M1) / Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities / Adult Acute Myeloid Leukemia With Del(5q) / Adult Acute Myeloid Leukemia With Inv(16)(p13;q22) / Adult Acute Myeloid Leukemia With T(16;16)(p13;q22) / Adult Acute Myeloid Leukemia With T(8;21)(q22;q22) / Adult Acute Myelomonocytic Leukemia (M4) / Adult Erythroleukemia (M6a) / Adult Pure Erythroid Leukemia (M6b) / Chronic Myelomonocytic Leukemia / De Novo Myelodysplastic Syndromes / Myelodysplastic/Myeloproliferative Neoplasm, Unclassifiable / Refractory Anemia With Excess Blasts / Untreated Adult Acute Myeloid Leukemia	1
Not Available	Completed	Treatment	Coronary Artery Disease	1
Not Available	Completed	Treatment	Coronary Artery Occlusive Disease	1
Not Available	Not Yet Recruiting	Treatment	Endometriosis	1
Not Available	Terminated	Prevention	High Blood Pressure (Hypertension) / High Cholesterol / Type 2 Diabetes Mellitus	1
Not Available	Terminated	Treatment	Metabolic Syndromes	1
Not Available	Unknown Status	Screening	Dyslipidemias	1
Not Available	Unknown Status	Treatment	Crohn's Disease (CD)	1
Not Available	Unknown Status	Treatment	Heart Diseases	1
Not Available	Withdrawn	Treatment	Endometriosis	1

Pharmacoeconomics

Manufacturers

Bristol myers squibb
Apotex corp
Dr reddys laboratories inc
Glenmark generics ltd
Lek pharmaceuticals dd
Lupin pharmaceuticals inc
Matrix laboratories ltd
Mylan pharmaceuticals inc
Pliva hrvatska doo
Ranbaxy laboratories ltd
Teva pharmaceuticals usa inc
Teva pharmaceuticals usa
Watson laboratories inc
Zydus pharmaceuticals usa inc

Packagers

Advanced Pharmaceutical Services Inc.
Amerisource Health Services Corp.
Apotex Inc.
A-S Medication Solutions LLC
Bristol-Myers Squibb Co.
Bryant Ranch Prepack
Cadila Healthcare Ltd.
Cardinal Health
Cobalt Pharmaceuticals Inc.
Comprehensive Consultant Services Inc.
Dept Health Central Pharmacy
Dispensing Solutions
Diversified Healthcare Services Inc.
Doctor Reddys Laboratories Ltd.
E.R. Squibb and Sons LLC
Glenmark Generics Ltd.
International Laboratories Inc.
Kaiser Foundation Hospital
Lek Pharmaceuticals Inc.
Lupin Pharmaceuticals Inc.
Major Pharmaceuticals
Medvantx Inc.
Murfreesboro Pharmaceutical Nursing Supply
Mylan
Neuman Distributors Inc.
Ohm Laboratories Inc.
Palmetto Pharmaceuticals Inc.
Par Pharmaceuticals
PD-Rx Pharmaceuticals Inc.
Pharmaceutical Utilization Management Program VA Inc.
Physicians Total Care Inc.
Pliva Inc.
Prepackage Specialists
Prepak Systems Inc.
Ranbaxy Laboratories
Rebel Distributors Corp.
Resource Optimization and Innovation LLC
Sandoz
Southwood Pharmaceuticals
Teva Pharmaceutical Industries Ltd.
UDL Laboratories
Vangard Labs Inc.
Zydus Pharmaceuticals

Dosage forms

Form	Route	Strength
Tablet	Oral	10 mg
Kit; tablet; tablet, delayed release	Oral
Tablet	Oral	10 mg/1
Tablet	Oral	80 mg
Tablet	Oral	20 mg
Tablet	Oral	40 mg
Tablet	Oral	20 mg/1
Tablet	Oral	40 mg/1
Tablet	Oral	80 mg/1
Kit
Tablet

Prices

Unit description	Cost	Unit
Pravachol 40 mg tablet	6.53USD	tablet
Pravachol 80 mg tablet	6.53USD	tablet
Pravastatin sodium 40 mg tablet	4.89USD	tablet
Pravastatin sodium 80 mg tablet	4.89USD	tablet
Pravachol 20 mg tablet	4.39USD	tablet
Pravachol 10 mg tablet	4.38USD	tablet
Pravastatin sodium 20 mg tablet	3.33USD	tablet
Pravastatin sodium 10 mg tablet	3.28USD	tablet
Apo-Pravastatin 40 mg Tablet	1.42USD	tablet
Co Pravastatin 40 mg Tablet	1.42USD	tablet
Jamp-Pravastatin 40 mg Tablet	1.42USD	tablet
Mint-Pravastatin 40 mg Tablet	1.42USD	tablet
Mylan-Pravastatin 40 mg Tablet	1.42USD	tablet
Novo-Pravastatin 40 mg Tablet	1.42USD	tablet
Pms-Pravastatin 40 mg Tablet	1.42USD	tablet
Pravachol 40 mg Tablet	1.42USD	tablet
Ran-Pravastatin 40 mg Tablet	1.42USD	tablet
Ratio-Pravastatin 40 mg Tablet	1.42USD	tablet
Sandoz Pravastatin 40 mg Tablet	1.42USD	tablet
Apo-Pravastatin 20 mg Tablet	1.18USD	tablet
Co Pravastatin 20 mg Tablet	1.18USD	tablet
Jamp-Pravastatin 20 mg Tablet	1.18USD	tablet
Mint-Pravastatin 20 mg Tablet	1.18USD	tablet
Mylan-Pravastatin 20 mg Tablet	1.18USD	tablet
Novo-Pravastatin 20 mg Tablet	1.18USD	tablet
Pms-Pravastatin 20 mg Tablet	1.18USD	tablet
Pravachol 20 mg Tablet	1.18USD	tablet
Ran-Pravastatin 20 mg Tablet	1.18USD	tablet
Ratio-Pravastatin 20 mg Tablet	1.18USD	tablet
Sandoz Pravastatin 20 mg Tablet	1.18USD	tablet
Apo-Pravastatin 10 mg Tablet	1.0USD	tablet
Co Pravastatin 10 mg Tablet	1.0USD	tablet
Jamp-Pravastatin 10 mg Tablet	1.0USD	tablet
Mint-Pravastatin 10 mg Tablet	1.0USD	tablet
Mylan-Pravastatin 10 mg Tablet	1.0USD	tablet
Novo-Pravastatin 10 mg Tablet	1.0USD	tablet
Pms-Pravastatin 10 mg Tablet	1.0USD	tablet
Pravachol 10 mg Tablet	1.0USD	tablet
Ran-Pravastatin 10 mg Tablet	1.0USD	tablet
Ratio-Pravastatin 10 mg Tablet	1.0USD	tablet
Sandoz Pravastatin 10 mg Tablet	1.0USD	tablet

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)
Unlock Additional Data
US5622985	No	1997-04-22	2014-10-22
CA1323836	No	1993-11-02	2010-11-02

Additional Data Available

Filed On

The date on which a patent was filed with the relevant government.

Learn more

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	171.2 - 173°C	'MSDS'
boiling point (°C)	>600 ºC at 760 mmHg	'MSDS'
water solubility	10 mg/ml	'MSDS'
logP	0.59	'MSDS'
pKa	4.2	Dinnekere V. et al. 2016. Scientifica.

Predicted Properties

Property	Value	Source
Water Solubility	0.242 mg/mL	ALOGPS
logP	2.23	ALOGPS
logP	1.65	ChemAxon
logS	-3.2	ALOGPS
pKa (Strongest Acidic)	4.21	ChemAxon
pKa (Strongest Basic)	-2.7	ChemAxon
Physiological Charge	-1	ChemAxon
Hydrogen Acceptor Count	6	ChemAxon
Hydrogen Donor Count	4	ChemAxon
Polar Surface Area	124.29 Å²	ChemAxon
Rotatable Bond Count	11	ChemAxon
Refractivity	113.6 m³·mol^-1	ChemAxon
Polarizability	46.56 Å³	ChemAxon
Number of Rings	2	ChemAxon
Bioavailability	1	ChemAxon
Rule of Five	Yes	ChemAxon
Ghose Filter	Yes	ChemAxon
Veber's Rule	No	ChemAxon
MDDR-like Rule	No	ChemAxon

Predicted ADMET features

Not Available

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0uk9-0009000000-967b377abafe64b73071
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-00di-0002900000-bd7fd66d793ae64426ff
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-4809000000-0ed5a8797dfc49ecf5af
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-2900000000-91b125182ce5d90f16ab
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-1900000000-e8fc6384260de93c5aa8
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-1900000000-11e99968bc0ba393b6f9
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-4900000000-0e4265e6dc1468c1471d
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-00di-0002900000-8795ee00dded0ef8be48
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-3709000000-aa45be15af0471c0a46e
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-2900000000-5617409991f5c58e5130
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-2900000000-2bf5c13979a639625d1c
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-2900000000-9a233e521607e82ab7a0
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0udi-0900000000-2083dfbb67bf2b03ccf9
LC-MS/MS Spectrum - LC-ESI-ITFT , negative	LC-MS/MS	splash10-0uk9-0009000000-4b2c09a295ba7f3ce41b
LC-MS/MS Spectrum - LC-ESI-QFT , negative	LC-MS/MS	splash10-00di-0607900000-e57e263ad3f74bfda195

Taxonomy

Description: This compound belongs to the class of organic compounds known as medium-chain hydroxy acids and derivatives. These are hydroxy acids with a 6 to 12 carbon atoms long side chain.
Kingdom: Organic compounds
Super Class: Organic acids and derivatives
Class: Hydroxy acids and derivatives
Sub Class: Medium-chain hydroxy acids and derivatives
Direct Parent: Medium-chain hydroxy acids and derivatives
Alternative Parents: Fatty alcohols / Medium-chain fatty acids / Hydroxy fatty acids / Fatty acid esters / Branched fatty acids / Beta hydroxy acids and derivatives / Dicarboxylic acids and derivatives / Secondary alcohols / Carboxylic acid esters / Carboxylic acids
show 3 more
Substituents: Fatty alcohol / Medium-chain hydroxy acid / Medium-chain fatty acid / Beta-hydroxy acid / Branched fatty acid / Hydroxy fatty acid / Fatty acid ester / Fatty acyl / Dicarboxylic acid or derivatives / Secondary alcohol
show 10 more
Molecular Framework: Aliphatic homopolycyclic compounds
External Descriptors: statin (semi-synthetic), carboxylic ester, secondary alcohol, 3-hydroxy carboxylic acid, hydroxy monocarboxylic acid, carbobicyclic compound (CHEBI:63618)

Targets

Details1. 3-hydroxy-3-methylglutaryl-coenzyme A reductase

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Nadph binding
Specific Function: Transmembrane glycoprotein that is the rate-limiting enzyme in cholesterol biosynthesis as well as in the biosynthesis of nonsterol isoprenoids that are essential for normal cell function including...
Gene Name: HMGCR
Uniprot ID: P04035
Uniprot Name: 3-hydroxy-3-methylglutaryl-coenzyme A reductase
Molecular Weight: 97475.155 Da

References

Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Ye YC, Zhao XL, Zhang SY: Use of atorvastatin in lipid disorders and cardiovascular disease in Chinese patients. Chin Med J (Engl). 2015 Jan 20;128(2):259-66. doi: 10.4103/0366-6999.149226. [PubMed:25591572]
Ray SK, Rege NN: Atorvastatin: in the management of hyperlipidaemia. J Postgrad Med. 2000 Jul-Sep;46(3):242-3. [PubMed:11298482]
Frishman W., Cheng-Lai A. and Nawarskas J. (2005). Current cardiovascular drugs (4th ed.). Current medicine LLC. [ISBN:1-57340-221-4]

Transporters

Details1. Solute carrier organic anion transporter family member 1B1

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name: SLCO1B1
Uniprot ID: Q9Y6L6
Uniprot Name: Solute carrier organic anion transporter family member 1B1
Molecular Weight: 76447.99 Da

References

Chen C, Mireles RJ, Campbell SD, Lin J, Mills JB, Xu JJ, Smolarek TA: Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos. 2005 Apr;33(4):537-46. Epub 2004 Dec 22. [PubMed:15616150]
Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278]
Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Kameyama Y, Yamashita K, Kobayashi K, Hosokawa M, Chiba K: Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15+C1007G, by using transient expression systems of HeLa and HEK293 cells. Pharmacogenet Genomics. 2005 Jul;15(7):513-22. [PubMed:15970799]
Sharma P, Holmes VE, Elsby R, Lambert C, Surry D: Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions. Xenobiotica. 2010 Jan;40(1):24-37. doi: 10.3109/00498250903351013. [PubMed:19919292]

Details2. Solute carrier organic anion transporter family member 2B1

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name: SLCO2B1
Uniprot ID: O94956
Uniprot Name: Solute carrier organic anion transporter family member 2B1
Molecular Weight: 76709.98 Da

References

Mougey EB, Feng H, Castro M, Irvin CG, Lima JJ: Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet Genomics. 2009 Feb;19(2):129-38. doi: 10.1097/FPC.0b013e32831bd98c. [PubMed:19151602]
Kobayashi D, Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther. 2003 Aug;306(2):703-8. Epub 2003 Apr 30. [PubMed:12724351]
Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45. Epub 2003 Nov 10. [PubMed:14610227]

Details3. Multidrug resistance protein 1

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name: ABCB1
Uniprot ID: P08183
Uniprot Name: Multidrug resistance protein 1
Molecular Weight: 141477.255 Da

References

Chen C, Mireles RJ, Campbell SD, Lin J, Mills JB, Xu JJ, Smolarek TA: Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1. Drug Metab Dispos. 2005 Apr;33(4):537-46. Epub 2004 Dec 22. [PubMed:15616150]
Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]
Salna MP, Singer HM, Dana AN: Pravastatin-Induced Eczematous Eruption Mimicking Psoriasis. Case Rep Dermatol Med. 2017;2017:3418204. doi: 10.1155/2017/3418204. Epub 2017 Jul 31. [PubMed:28831316]

Details4. Solute carrier organic anion transporter family member 1A2

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name: SLCO1A2
Uniprot ID: P46721
Uniprot Name: Solute carrier organic anion transporter family member 1A2
Molecular Weight: 74144.105 Da

References

Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278]

Details5. Solute carrier family 22 member 6

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name: SLC22A6
Uniprot ID: Q4U2R8
Uniprot Name: Solute carrier family 22 member 6
Molecular Weight: 61815.78 Da

References

Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. [PubMed:14978359]

Details6. Solute carrier family 22 member 8

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate
Inhibitor

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name: SLC22A8
Uniprot ID: Q8TCC7
Uniprot Name: Solute carrier family 22 member 8
Molecular Weight: 59855.585 Da

References

Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. [PubMed:14978359]
Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. [PubMed:14762099]
Hasegawa M, Kusuhara H, Sugiyama D, Ito K, Ueda S, Endou H, Sugiyama Y: Functional involvement of rat organic anion transporter 3 (rOat3; Slc22a8) in the renal uptake of organic anions. J Pharmacol Exp Ther. 2002 Mar;300(3):746-53. [PubMed:11861777]

Details7. Canalicular multispecific organic anion transporter 1

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Organic anion transmembrane transporter activity
Specific Function: Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
Gene Name: ABCC2
Uniprot ID: Q92887
Uniprot Name: Canalicular multispecific organic anion transporter 1
Molecular Weight: 174205.64 Da

References

Yamazaki M, Akiyama S, Ni'inuma K, Nishigaki R, Sugiyama Y: Biliary excretion of pravastatin in rats: contribution of the excretion pathway mediated by canalicular multispecific organic anion transporter. Drug Metab Dispos. 1997 Oct;25(10):1123-9. [PubMed:9321514]
Sasaki M, Suzuki H, Ito K, Abe T, Sugiyama Y: Transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II cell monolayer expressing both human organic anion-transporting polypeptide (OATP2/SLC21A6) and Multidrug resistance-associated protein 2 (MRP2/ABCC2). J Biol Chem. 2002 Feb 22;277(8):6497-503. Epub 2001 Dec 17. [PubMed:11748225]
Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]

Details8. Solute carrier family 22 member 11

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name: SLC22A11
Uniprot ID: Q9NSA0
Uniprot Name: Solute carrier family 22 member 11
Molecular Weight: 59970.945 Da

References

Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. [PubMed:14978359]

Details9. ATP-binding cassette sub-family G member 2

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Xenobiotic-transporting atpase activity
Specific Function: High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name: ABCG2
Uniprot ID: Q9UNQ0
Uniprot Name: ATP-binding cassette sub-family G member 2
Molecular Weight: 72313.47 Da

References

Suzuki M, Suzuki H, Sugimoto Y, Sugiyama Y: ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem. 2003 Jun 20;278(25):22644-9. Epub 2003 Apr 7. [PubMed:12682043]
Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [PubMed:15901800]

Details10. Solute carrier family 22 member 7

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates sodium-independent multispecific organic anion transport. Transport of prostaglandin E2, prostaglandin F2, tetracycline, bumetanide, estrone sulfate, glutarate, dehydroepiandrosterone sulf...
Gene Name: SLC22A7
Uniprot ID: Q9Y694
Uniprot Name: Solute carrier family 22 member 7
Molecular Weight: 60025.025 Da

References

Khamdang S, Takeda M, Shimoda M, Noshiro R, Narikawa S, Huang XL, Enomoto A, Piyachaturawat P, Endou H: Interactions of human- and rat-organic anion transporters with pravastatin and cimetidine. J Pharmacol Sci. 2004 Feb;94(2):197-202. [PubMed:14978359]

Details11. Monocarboxylate transporter 1

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Symporter activity
Specific Function: Proton-coupled monocarboxylate transporter. Catalyzes the rapid transport across the plasma membrane of many monocarboxylates such as lactate, pyruvate, branched-chain oxo acids derived from leucin...
Gene Name: SLC16A1
Uniprot ID: P53985
Uniprot Name: Monocarboxylate transporter 1
Molecular Weight: 53943.685 Da

References

Tamai I, Takanaga H, Maeda H, Ogihara T, Yoneda M, Tsuji A: Proton-cotransport of pravastatin across intestinal brush-border membrane. Pharm Res. 1995 Nov;12(11):1727-32. [PubMed:8592677]

Details12. Bile salt export pump

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Transporter activity
Specific Function: Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name: ABCB11
Uniprot ID: O95342
Uniprot Name: Bile salt export pump
Molecular Weight: 146405.83 Da

References

Morisawa Y, Takikawa H: Effect of bile acids on the biliary excretion of pravastatin in rats. Hepatol Res. 2009 Jun;39(6):595-600. doi: 10.1111/j.1872-034X.2009.00493.x. Epub 2009 Feb 24. [PubMed:19260999]

Details13. Solute carrier organic anion transporter family member 1B3

Kind: Protein
Organism: Humans
Pharmacological action: No
Actions: Substrate

General Function: Sodium-independent organic anion transmembrane transporter activity
Specific Function: Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name: SLCO1B3
Uniprot ID: Q9NPD5
Uniprot Name: Solute carrier organic anion transporter family member 1B3
Molecular Weight: 77402.175 Da

References

Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, Kirchgessner TG: A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem. 1999 Dec 24;274(52):37161-8. [PubMed:10601278]
Link [Link]

Drug created on June 13, 2005 07:24 / Updated on July 21, 2019 06:21

Pravastatin

Identification

Structure for Pravastatin (DB00175)

Pharmacology

Interactions

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Clinical Trials

Pharmacoeconomics

Properties

Spectra

Taxonomy

Targets

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Transporters

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