General Information of Drug (ID: DM6A0X7)

Drug Name
Pravastatin
Synonyms
Eptastatin; Oliprevin; Pravastatina; Pravastatine; Pravastatinum; Pravator; Vasten; Pravastatin Sodium Salt; Pravastatina [Spanish]; Pravastatine [French]; Pravastatinum [Latin]; KS-5015; Pravachol (TN); Pravastatin (INN); Pravastatin [INN:BAN]; Pravastatin tert-Octylamine Salt; Pravator (TN); RMS-431; Selektine (TN); SQ-31,000; (3R,5R)-3,5-dihydroxy-7-[(1S,2S,6S,8S,8aR)-6-hydroxy-2-methyl-8-{[(2S)-2-methylbutanoyl]oxy}-1,2,6,7,8,8a-hexahydronaphthalen-1-yl]heptanoic acid; (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; 1,2,6,7,8,8a-hexahydro-beta,delta,6-trihydroxy-2-methyl-8-(2-methyl-1-oxobutoxy)-, (1S-(1alpha(betaS*,deltaS*),2alpha,6alpha,8beta(R*),8aalpha))-1-Naphthaleneheptanoic acid
Indication
Disease Entry ICD 11 Status REF
Adult acute monocytic leukemia N.A. Approved [1]
Arteriosclerosis BD40 Approved [1]
Hypercholesterolaemia 5C80.0 Approved [2]
Hyperlipidemia, familial combined, LPL related N.A. Approved [1]
Hypertriglyceridemia 5C80.1 Approved [1]
Stroke 8B20 Investigative [1]
⏷ Show the Full List of Indication(s)
Therapeutic Class
Anticholesteremic Agents
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 424.5
Logarithm of the Partition Coefficient (xlogp) 1.6
Rotatable Bond Count (rotbonds) 11
Hydrogen Bond Donor Count (hbonddonor) 4
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 60-90 mcgh/L [3]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 30-55 mcg/L [3]
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 3: high solubility and low permeability [4]
Bioavailability
The bioavailability of drug is 17% [3]
Clearance
4-11 L/min for children [5]
Elimination
From the administered dose of pravastatin, about 70% is eliminated in the feces while about 20% is obtained in the urine []
Half-life
The concentration or amount of drug in body reduced by one-half in 1.8 hours [3]
Metabolism
The drug is metabolized via the liver [3]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 1.57112 micromolar/kg/day [6]
Unbound Fraction
The unbound fraction of drug in plasma is 0.5% [7]
Vd
The volume of distribution (Vd) of drug is 0.5 L/kg [5]
Water Solubility
The ability of drug to dissolve in water is measured as 300 mg/mL [4]
Adverse Drug Reaction (ADR)
ADR Term Variation Related DOT DOT ID REF
Acute myocardial infarction Not Available MMP3 OTGBI74Z [8]
Arteriosclerosis Not Available CES1 OT9L0LR8 [8]
Cardiovascular disorder rs20455 KIF6 OTDH3MR4 [9]
LDL cholesterol increased rs17244841 HMGCR OTRT3F3U [10]
Myocardial ischaemia Not Available APOE OTFOWL2H [8]
Chemical Identifiers
Formula
C23H36O7
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
Canonical SMILES
CC[C@H](C)C(=O)O[C@H]1C[C@@H](C=C2[C@H]1[C@H]([C@H](C=C2)C)CC[C@H](C[C@H](CC(=O)O)O)O)O
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
InChIKey
TUZYXOIXSAXUGO-PZAWKZKUSA-N
Cross-matching ID
PubChem CID
54687
ChEBI ID
CHEBI:63618
CAS Number
81093-37-0
DrugBank ID
DB00175
TTD ID
D02RQU
VARIDT ID
DR00045
INTEDE ID
DR1327
ACDINA ID
D00548
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
HMG-CoA reductase (HMGCR) TTPADOQ HMDH_HUMAN Inhibitor [11]

Drug Transporter (DTP)
DTP Name DTP ID UniProt ID MOA REF
Probable small intestine urate exporter (SLC17A4) DTHE530 S17A4_HUMAN Substrate [12]
Organic anion transporter 7 (SLC22A9) DTDI5S3 S22A9_HUMAN Substrate [13]
Bile salt export pump (ABCB11) DTJ0EW4 ABCBB_HUMAN Substrate [14]
Multidrug resistance-associated protein 2 (ABCC2) DTFI42L MRP2_HUMAN Substrate [15]
Organic anion transporter 4 (SLC22A11) DT06JWZ S22AB_HUMAN Substrate [16]
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTPFTEQ SO2B1_HUMAN Substrate [17]
Breast cancer resistance protein (ABCG2) DTI7UX6 ABCG2_HUMAN Substrate [18]
Organic anion transporting polypeptide 1B1 (SLCO1B1) DT3D8F0 SO1B1_HUMAN Substrate [19]
Organic anion transporting polypeptide 1B3 (SLCO1B3) DT9C1TS SO1B3_HUMAN Substrate [20]
Organic anion transporter 3 (SLC22A8) DTVP67E S22A8_HUMAN Substrate [21]
P-glycoprotein 1 (ABCB1) DTUGYRD MDR1_HUMAN Substrate [22]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 3A4 (CYP3A4) DE4LYSA CP3A4_HUMAN Substrate [23]
Cytochrome P450 2C9 (CYP2C9) DE5IED8 CP2C9_HUMAN Substrate [24]
Cytochrome P450 3A5 (CYP3A5) DEIBDNY CP3A5_HUMAN Substrate [25]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
3-hydroxy-3-methylglutaryl-coenzyme A reductase (HMGCR) OTRT3F3U HMDH_HUMAN Drug Response [10]
Apolipoprotein E (APOE) OTFOWL2H APOE_HUMAN Drug Response [8]
Kinesin-like protein KIF6 (KIF6) OTDH3MR4 KIF6_HUMAN Drug Response [9]
Liver carboxylesterase 1 (CES1) OT9L0LR8 EST1_HUMAN Drug Response [8]
Stromelysin-1 (MMP3) OTGBI74Z MMP3_HUMAN Drug Response [8]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Adult acute monocytic leukemia
ICD Disease Classification
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
HMG-CoA reductase (HMGCR) DTT HMGCR 1.01E-05 0.65 1.53
Organic anion transporter 3 (SLC22A8) DTP OAT3 1.54E-03 -5.09E-01 -1.49E+00
P-glycoprotein 1 (ABCB1) DTP P-GP 3.29E-14 -7.08E-01 -1.99E+00
Organic anion transporting polypeptide 2B1 (SLCO2B1) DTP OATP2B1 3.80E-01 -1.23E-02 -5.33E-02
Bile salt export pump (ABCB11) DTP BSEP 2.41E-01 -3.08E-02 -2.35E-01
Breast cancer resistance protein (ABCG2) DTP BCRP 2.28E-08 -3.66E-01 -8.07E-01
Probable small intestine urate exporter (SLC17A4) DTP SLC17A4 1.00E-02 -1.74E-01 -8.13E-01
Multidrug resistance-associated protein 2 (ABCC2) DTP MRP2 4.30E-02 -2.29E-01 -9.10E-01
Organic anion transporter 7 (SLC22A9) DTP OAT7 1.92E-04 -4.34E-01 -1.40E+00
Organic anion transporting polypeptide 1B3 (SLCO1B3) DTP OATP1B3 1.65E-01 -6.07E-02 -3.77E-01
Organic anion transporting polypeptide 1B1 (SLCO1B1) DTP OATP1B1 3.27E-01 -5.78E-02 -3.84E-01
Organic anion transporter 4 (SLC22A11) DTP OAT4 3.76E-03 -3.49E-01 -8.70E-01
Cytochrome P450 3A5 (CYP3A5) DME CYP3A5 3.65E-02 -8.90E-02 -5.58E-01
Cytochrome P450 2C9 (CYP2C9) DME CYP2C9 2.63E-03 -1.18E-01 -3.80E-01
Cytochrome P450 3A4 (CYP3A4) DME CYP3A4 3.24E-05 -3.48E-01 -1.34E+00
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Pravastatin
DDI Drug Name DDI Drug ID Severity Mechanism Disease REF
Mipomersen DMGSRN1 Major Increased risk of hepatotoxicity by the combination of Pravastatin and Mipomersen. Hyper-lipoproteinaemia [5C80] [26]
Teriflunomide DMQ2FKJ Major Increased risk of hepatotoxicity by the combination of Pravastatin and Teriflunomide. Hyper-lipoproteinaemia [5C80] [27]
BMS-201038 DMQTAGO Major Increased risk of hepatotoxicity by the combination of Pravastatin and BMS-201038. Hyper-lipoproteinaemia [5C80] [28]
Coadministration of a Drug Treating the Disease Different from Pravastatin (Comorbidity)
DDI Drug Name DDI Drug ID Severity Mechanism Comorbidity REF
Remdesivir DMBFZ6L Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Remdesivir. 1D6YCoronavirus Disease 2019 [1D6YCoronavirus Disease 2019] [29]
Thioguanine DM7NKEV Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Thioguanine. Acute myeloid leukaemia [2A60] [30]
Midostaurin DMI6E0R Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Midostaurin. Acute myeloid leukaemia [2A60] [31]
Arn-509 DMT81LZ Moderate Accelerated clearance of Pravastatin due to the transporter induction by Arn-509. Acute myeloid leukaemia [2A60] [31]
Bedaquiline DM3906J Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Bedaquiline. Antimicrobial drug resistance [MG50-MG52] [32]
Erythromycin DM4K7GQ Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Erythromycin. Bacterial infection [1A00-1C4Z] [33]
Clarithromycin DM4M1SG Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Clarithromycin. Bacterial infection [1A00-1C4Z] [33]
Ag-221 DMS0ZBI Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Ag-221. BCR-ABL1-negative chronic myeloid leukaemia [2A41] [29]
Pexidartinib DMS2J0Z Major Increased risk of hepatotoxicity by the combination of Pravastatin and Pexidartinib. Bone/articular cartilage neoplasm [2F7B] [34]
Anisindione DM2C48U Minor Increased risk of bleeding by the combination of Pravastatin and Anisindione. Coagulation defect [3B10] [35]
MK-8228 DMOB58Q Moderate Decreased clearance of Pravastatin due to the transporter inhibition by MK-8228. Cytomegaloviral disease [1D82] [36]
Cannabidiol DM0659E Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Cannabidiol. Epileptic encephalopathy [8A62] [31]
ABT-450 DMFW860 Major Decreased clearance of Pravastatin due to the transporter inhibition by ABT-450. Hepatitis virus infection [1E50-1E51] [37]
Simeprevir DMLUA9D Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Simeprevir. Hepatitis virus infection [1E50-1E51] [38]
GS-9857 DMYU6P5 Major Decreased clearance of Pravastatin due to the transporter inhibition by GS-9857. Hepatitis virus infection [1E50-1E51] [39]
Brentuximab vedotin DMWLC57 Moderate Increased risk of peripheral neuropathy by the combination of Pravastatin and Brentuximab vedotin. Hodgkin lymphoma [2B30] [40]
Fostemsavir DM50ILT Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Fostemsavir. Human immunodeficiency virus disease [1C60-1C62] [41]
Nevirapine DM6HX9B Moderate Increased metabolism of Pravastatin caused by Nevirapine mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [42]
Cobicistat DM6L4H2 Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Cobicistat. Human immunodeficiency virus disease [1C60-1C62] [29]
Efavirenz DMC0GSJ Moderate Increased metabolism of Pravastatin caused by Efavirenz mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [42]
Zalcitabine DMH7MUV Moderate Increased risk of peripheral neuropathy by the combination of Pravastatin and Zalcitabine. Human immunodeficiency virus disease [1C60-1C62] [43]
Ritonavir DMU764S Moderate Increased metabolism of Pravastatin caused by Ritonavir mediated induction of UGT. Human immunodeficiency virus disease [1C60-1C62] [37]
Methotrexate DM2TEOL Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Methotrexate. Leukaemia [2A60-2B33] [31]
Porfimer Sodium DM7ZWNY Moderate Increased risk of photosensitivity reactions by the combination of Pravastatin and Porfimer Sodium. Lung cancer [2C25] [44]
Calaspargase pegol DMQZBXI Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Calaspargase pegol. Malignant haematopoietic neoplasm [2B33] [45]
Idelalisib DM602WT Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Idelalisib. Mature B-cell leukaemia [2A82] [46]
Clofarabine DMCVJ86 Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Clofarabine. Mature B-cell lymphoma [2A85] [47]
Dabrafenib DMX6OE3 Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Dabrafenib. Melanoma [2C30] [29]
Thalidomide DM70BU5 Moderate Increased risk of peripheral neuropathy by the combination of Pravastatin and Thalidomide. Multiple myeloma [2A83] [43]
Bortezomib DMNO38U Moderate Increased risk of peripheral neuropathy by the combination of Pravastatin and Bortezomib. Multiple myeloma [2A83] [43]
Darolutamide DMV7YFT Moderate Decreased clearance of Pravastatin due to the transporter inhibition by Darolutamide. Prostate cancer [2C82] [31]
Leflunomide DMR8ONJ Major Increased risk of hepatotoxicity by the combination of Pravastatin and Leflunomide. Rheumatoid arthritis [FA20] [27]
Epirubicin DMPDW6T Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Epirubicin. Solid tumour/cancer [2A00-2F9Z] [29]
Naltrexone DMUL45H Moderate Increased risk of hepatotoxicity by the combination of Pravastatin and Naltrexone. Substance abuse [6C40] [48]
Warfarin DMJYCVW Minor Increased risk of bleeding by the combination of Pravastatin and Warfarin. Supraventricular tachyarrhythmia [BC81] [35]
Dicumarol DMFQCB1 Minor Increased risk of bleeding by the combination of Pravastatin and Dicumarol. Thrombosis [DB61-GB90] [35]
⏷ Show the Full List of 36 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG
DIG Name DIG ID PubChem CID Functional Classification
FD&C blue no. 1 E00263 19700 Colorant
Mannitol E00103 6251 Diluent; Flavoring agent; Lyophilization aid; Plasticizing agent; Tonicity agent
Meglumine E00181 8567 Buffering agent
Quinoline yellow WS E00309 24671 Colorant
Sodium lauryl sulfate E00464 3423265 Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Sodium stearyl fumarate E00545 23665634 lubricant
Aluminum trihydroxide E00505 10176082 Alkalizing agent; Vaccine adjuvant
Beta-D-lactose E00099 6134 Diluent; Dry powder inhaler carrier; Lyophilization aid
Calcium hydrogenphosphate E00294 24441 Diluent
Calcium stearate E00244 15324 lubricant
Carbonic acid disodium salt E00199 10340 Alkalizing agent; Buffering agent; Diluent; Dispersing agent
Carmellose sodium E00625 Not Available Disintegrant
Crospovidone E00626 Not Available Disintegrant
Dihydroxyaluminum sodium carbonate E00573 23697815 Diluent
Disodium hydrogenorthophosphate E00283 24203 Buffering agent; Complexing agent
Eisenoxyd E00585 56841934 Colorant
Ferric hydroxide oxide yellow E00539 23320441 Colorant
Hypromellose E00634 Not Available Coating agent
Lactose monohydrate E00393 104938 Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium aluminum silicate E00462 3084116 Adsorbent; Binding agent; Disintegrant; Suspending agent; Viscosity-controlling agent
Magnesium oxide E00232 14792 Anticaking agent; Diluent; Emulsifying agent; Glidant; Tonicity agent
Magnesium stearate E00208 11177 lubricant
Polyethylene glycol 6000 E00655 Not Available Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyoxyl 35 castor oil E00660 Not Available Emulsifying agent; Solubilizing agent; Surfactant
Povidone E00667 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Silicon dioxide E00670 Not Available Anticaking agent; Opacifying agent; Viscosity-controlling agent
Sodium bicarbonate E00424 516892 Alkalizing agent; Diluent
Talc E00520 16211421 Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide E00322 26042 Coating agent; Colorant; Opacifying agent
Vinylpyrrolidone E00668 Not Available Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Hydrophobic colloidal silica E00285 24261 Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
Cellulose microcrystalline E00698 Not Available Adsorbent; Suspending agent; Diluent
Pregelatinized starch E00674 Not Available Binding agent; Diluent; Disintegrant
⏷ Show the Full List of 33 Pharmaceutical Excipients of This Drug
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Pravastatin 40 mg tablet 40 mg Oral Tablet Oral
Pravastatin 10 mg tablet 10 mg Oral Tablet Oral
Pravastatin 20 mg tablet 20 mg Oral Tablet Oral
Pravastatin Sodium 40mg tablet 40mg Tablet Oral
Pravastatin Sodium 10mg tablet 10mg Tablet Oral
Pravastatin 80 mg tablet 80 mg Oral Tablet Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

References

1 Pravastatin FDA Label
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4 BDDCS predictions, self-correcting aspects of BDDCS assignments, BDDCS assignment corrections, and classification for more than 175 additional drugs
5 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.
6 Estimating the safe starting dose in phase I clinical trials and no observed effect level based on QSAR modeling of the human maximum recommended daily dose
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12 A Na+-phosphate cotransporter homologue (SLC17A4 protein) is an intestinal organic anion exporter. Am J Physiol Cell Physiol. 2012 Jun 1;302(11):C1652-60.
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14 Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin. J Pharmacol Exp Ther. 2005 Aug;314(2):876-82.
15 Role of transporters in the tissue-selective distribution and elimination of drugs: transporters in the liver, small intestine, brain and kidney. J Control Release. 2002 Jan 17;78(1-3):43-54.
16 Inhibition of human organic anion transporter 3 mediated pravastatin transport by gemfibrozil and the metabolites in humans. Xenobiotica. 2007 Apr;37(4):416-26.
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40 Product Information. Accolate (zafirlukast). Zeneca Pharmaceuticals, Wilmington, DE.
41 Product Information. Rukobia (fostemsavir). ViiV Healthcare, Research Triangle Park, NC.
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47 Product Information. Clolar (clofarabine). sanofi-aventis, Bridgewater, NJ.
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