fluvastatin ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
antihyperlipidaemic substances, HMG CoA reductase inhibitors 1229 93957-54-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lescol
  • fluvastatin
  • leschol
  • fluvastatin sodium
  • XU-62-320
  • fluvastatin sodium salt
  • fluvastatin sodium hydrate
An indole-heptanoic acid derivative that inhibits HMG COA REDUCTASE and is used to treat HYPERCHOLESTEROLEMIA. In contrast to other statins, it does not appear to interact with other drugs that inhibit CYP3A4.
  • Molecular weight: 411.47
  • Formula: C24H26FNO4
  • CLOGP: 4.05
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 3
  • TPSA: 82.69
  • ALOGS: -4.97
  • ROTB: 8

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
60 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 1.50 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 1.62 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 24 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 0.42 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 16 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.01 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 0.70 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Dec. 31, 1993 FDA NOVARTIS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myalgia 138.13 14.61 136 8540 124183 50472265
Blood creatine phosphokinase increased 115.69 14.61 66 8610 26301 50570147
Rhabdomyolysis 115.65 14.61 76 8600 38951 50557497
Limb reduction defect 100.00 14.61 21 8655 366 50596082
Dysmorphism 72.29 14.61 23 8653 2144 50594304
Cleft palate 71.35 14.61 19 8657 944 50595504
Gamma-glutamyltransferase increased 65 14.61 48 8628 29575 50566873
Talipes 64.13 14.61 19 8657 1395 50595053
Atrial septal defect 64.09 14.61 28 8648 6313 50590135
Patent ductus arteriosus 59.54 14.61 23 8653 3797 50592651
Limb hypoplasia congenital 58.58 14.61 12 8664 184 50596264
Antinuclear antibody negative 57.42 14.61 12 8664 204 50596244
Congenital oral malformation 52.80 14.61 11 8665 184 50596264
Coombs positive haemolytic anaemia 52.03 14.61 12 8664 327 50596121
Herpes simplex reactivation 50.14 14.61 12 8664 385 50596063
Retrognathia 49.36 14.61 12 8664 412 50596036
Aspartate aminotransferase increased 48.16 14.61 63 8613 77935 50518513
Drug ineffective 47.12 14.61 43 8633 819290 49777158
Alanine aminotransferase increased 46.43 14.61 66 8610 88293 50508155
Developmental hip dysplasia 44.29 14.61 14 8662 1277 50595171
Myopathy 40.38 14.61 23 8653 9116 50587332
Antiphospholipid syndrome 38.12 14.61 13 8663 1504 50594944
Gastritis haemorrhagic 35.73 14.61 12 8664 1325 50595123
Neck deformity 34.75 14.61 13 8663 1965 50594483
Lactic acidosis 32.38 14.61 34 8642 33321 50563127
Acute kidney injury 32.28 14.61 99 8577 227959 50368489
Jaundice 31.28 14.61 30 8646 26399 50570049
Complex regional pain syndrome 31.06 14.61 12 8664 1981 50594467
Anxiety disorder 30.06 14.61 14 8662 3659 50592789
Pancreatitis acute 30.03 14.61 28 8648 23784 50572664
Premature baby 27.95 14.61 24 8652 18313 50578135
Interstitial lung disease 26.85 14.61 39 8637 53137 50543311
Aplasia 26.53 14.61 13 8663 3800 50592648
Muscle spasms 26.28 14.61 63 8613 125490 50470958
Muscular weakness 25.90 14.61 53 8623 94960 50501488
Blood alkaline phosphatase increased 25.81 14.61 32 8644 37494 50558954
Off label use 23.64 14.61 28 8648 474398 50122050
Hyperlipidaemia 22.89 14.61 21 8655 17469 50578979
Peripheral swelling 22.65 14.61 4 8672 205932 50390516
Neonatal seizure 21.17 14.61 6 8670 376 50596072
Pulmonary artery stenosis 20.84 14.61 5 8671 162 50596286
Alopecia 20.81 14.61 8 8668 245039 50351409
Hypernatraemia 20.39 14.61 13 8663 6308 50590140
Blood creatinine increased 20.18 14.61 42 8634 76118 50520330
Chromaturia 20.04 14.61 18 8658 14572 50581876
Coronary artery disease 19.88 14.61 25 8651 29701 50566747
Erysipelas 19.86 14.61 13 8663 6595 50589853
Joint swelling 19.24 14.61 9 8667 245277 50351171
Otospondylomegaepiphyseal dysplasia 18.92 14.61 4 8672 72 50596376
Angiosclerosis 18.86 14.61 3 8673 9 50596439
Cerebrovascular accident 18.20 14.61 46 8630 94634 50501814
Drug interaction 18.16 14.61 75 8601 199546 50396902
Haematoma 17.82 14.61 24 8652 30486 50565962
Pleuritic pain 17.70 14.61 12 8664 6454 50589994
Blood urea increased 17.66 14.61 21 8655 23564 50572884
Osteonecrosis 16.78 14.61 20 8656 22497 50573951
Bradycardia neonatal 16.48 14.61 6 8670 840 50595608
Sterile pyuria 16.43 14.61 3 8673 24 50596424
Cholestasis 16.41 14.61 21 8655 25380 50571068
Ocular myasthenia 16.40 14.61 4 8672 139 50596309
Cerebral ischaemia 16.26 14.61 11 8665 5897 50590551
Hypothyroidism 15.75 14.61 24 8652 34101 50562347
Fasciitis 15.39 14.61 5 8671 498 50595950
Amyotrophic lateral sclerosis 15.13 14.61 6 8670 1061 50595387

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myalgia 262.85 16.11 195 8173 73824 29492335
Blood creatine phosphokinase increased 161.94 16.11 115 8253 40529 29525630
Myopathy 77.54 16.11 44 8324 10489 29555670
Muscle rupture 74.16 16.11 26 8342 1971 29564188
Gamma-glutamyltransferase increased 48.35 16.11 48 8320 26689 29539470
Rectal prolapse 43.71 16.11 11 8357 260 29565899
Off label use 42.66 16.11 16 8352 300784 29265375
Amyotrophic lateral sclerosis 42.50 16.11 14 8354 877 29565282
Rhabdomyolysis 41.44 16.11 67 8301 60741 29505418
Intraductal papillary mucinous neoplasm 41.24 16.11 11 8357 329 29565830
Vena cava injury 40.95 16.11 10 8358 208 29565951
SARS-CoV-2 antibody test positive 40.29 16.11 10 8358 223 29565936
Renal cyst haemorrhage 39.33 16.11 11 8357 394 29565765
Dysuria 32.87 16.11 36 8332 22404 29543755
Vestibular neuronitis 32.78 16.11 8 8360 166 29565993
Myocardial infarction 31.55 16.11 85 8283 110211 29455948
Face oedema 29.58 16.11 24 8344 10259 29555900
Aspartate aminotransferase increased 29.30 16.11 57 8311 59668 29506491
Angina pectoris 28.15 16.11 37 8331 27813 29538346
General physical health deterioration 28.14 16.11 78 8290 102779 29463380
Tendon rupture 27.78 16.11 19 8349 6276 29559883
Diverticulum intestinal 27.64 16.11 15 8353 3275 29562884
Generalised oedema 25.84 16.11 23 8345 11142 29555017
Carotid arteriosclerosis 25.68 16.11 11 8357 1427 29564732
Delayed graft function 25.65 16.11 12 8356 1915 29564244
Coronary artery disease 25.20 16.11 45 8323 44145 29522014
Febrile bone marrow aplasia 25.13 16.11 19 8349 7332 29558827
Abdominal wall haemorrhage 25.07 16.11 7 8361 249 29565910
Toxicity to various agents 24.96 16.11 9 8359 173652 29392507
Restless legs syndrome 23.76 16.11 18 8350 6966 29559193
Vertigo 23.59 16.11 30 8338 21831 29544328
Death 23.47 16.11 38 8330 342046 29224113
Aortic dilatation 22.43 16.11 9 8359 990 29565169
Renal artery stenosis 22.42 16.11 11 8357 1950 29564209
Glycosylated haemoglobin increased 20.99 16.11 19 8349 9407 29556752
Mean cell volume increased 19.94 16.11 11 8357 2478 29563681
Perioral dermatitis 19.91 16.11 5 8363 117 29566042
Myocardial ischaemia 18.90 16.11 23 8345 16005 29550154
Congenital inguinal hernia 18.48 16.11 5 8363 158 29566001
Vitamin D decreased 18.29 16.11 11 8357 2914 29563245
Actinic keratosis 18.07 16.11 12 8356 3774 29562385
Funguria 17.87 16.11 4 8364 56 29566103
Aortic arteriosclerosis 17.82 16.11 12 8356 3864 29562295
Product dose omission issue 17.69 16.11 3 8365 96380 29469779
Haemorrhoids 17.58 16.11 19 8349 11638 29554521
Hyperparathyroidism secondary 17.16 16.11 8 8360 1267 29564892
Seizure 16.86 16.11 3 8365 93120 29473039
Spinal stenosis 16.53 16.11 12 8356 4351 29561808
Vascular anastomotic haemorrhage 16.34 16.11 4 8364 84 29566075
Perineal cyst 16.12 16.11 4 8364 89 29566070

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Myalgia 307.06 13.33 258 13185 158359 64326930
Blood creatine phosphokinase increased 244.29 13.33 152 13291 58406 64426883
Rhabdomyolysis 112.61 13.33 116 13327 91610 64393679
Myopathy 108.42 13.33 59 13384 17621 64467668
Gamma-glutamyltransferase increased 83.56 13.33 74 13369 48436 64436853
Aspartate aminotransferase increased 65.34 13.33 101 13342 119687 64365602
Off label use 64.09 13.33 26 13417 632780 63852509
Amyotrophic lateral sclerosis 57.58 13.33 19 13424 1631 64483658
Muscle rupture 55.60 13.33 22 13421 3178 64482111
Alanine aminotransferase increased 50.56 13.33 98 13345 138933 64346356
Vena cava injury 43.46 13.33 10 13433 220 64485069
SARS-CoV-2 antibody test positive 42.67 13.33 10 13433 239 64485050
Renal cyst haemorrhage 41.22 13.33 11 13432 451 64484838
Myocardial infarction 40.97 13.33 100 13343 165721 64319568
Coronary artery disease 38.73 13.33 55 13388 60378 64424911
Intraductal papillary mucinous neoplasm 38.43 13.33 11 13432 586 64484703
Toxicity to various agents 32.02 13.33 18 13425 363495 64121794
Completed suicide 30.66 13.33 5 13438 224409 64260880
Muscular weakness 30.59 13.33 76 13367 127262 64358027
Muscle spasms 29.59 13.33 80 13363 140943 64344346
Death 28.81 13.33 35 13408 482670 64002619
Lactic acidosis 28.29 13.33 48 13395 61362 64423927
Myoglobin blood increased 28.17 13.33 13 13430 2734 64482555
Blood alkaline phosphatase increased 27.28 13.33 45 13398 56234 64429055
Rectal prolapse 26.99 13.33 11 13432 1715 64483574
Joint swelling 26.87 13.33 6 13437 215376 64269913
Drug ineffective 26.85 13.33 88 13355 840159 63645130
Peripheral swelling 25.75 13.33 6 13437 209147 64276142
General physical health deterioration 25.52 13.33 97 13346 204328 64280961
Jaundice 25.15 13.33 40 13403 48472 64436817
Carotid arteriosclerosis 25.01 13.33 11 13432 2068 64483221
Cerebrovascular accident 24.91 13.33 74 13369 137509 64347780
Vestibular neuronitis 24.69 13.33 8 13435 648 64484641
Acute kidney injury 24.64 13.33 169 13274 449071 64036218
Blood creatinine increased 24.55 13.33 73 13370 135709 64349580
Delayed graft function 23.95 13.33 12 13431 3024 64482265
Tendon rupture 23.84 13.33 19 13424 10748 64474541
Abdominal wall haemorrhage 23.68 13.33 7 13436 418 64484871
Actinic keratosis 23.00 13.33 14 13429 5151 64480138
Hyperkalaemia 22.86 13.33 59 13384 101070 64384219
Face oedema 22.86 13.33 27 13416 24734 64460555
Myocardial ischaemia 22.54 13.33 26 13417 23225 64462064
Infusion related reaction 21.72 13.33 4 13439 164463 64320826
Renal artery stenosis 21.28 13.33 11 13432 2958 64482331
Blood urea increased 20.98 13.33 35 13408 44118 64441171
Dysuria 20.88 13.33 34 13409 42023 64443266
Benign prostatic hyperplasia 19.92 13.33 16 13427 9149 64476140
Muscle necrosis 19.83 13.33 8 13435 1215 64484074
Chromaturia 19.79 13.33 24 13419 22587 64462702
Product dose omission issue 19.64 13.33 8 13435 194739 64290550
General physical condition 19.13 13.33 3 13440 6 64485283
Aortic dilatation 18.77 13.33 8 13435 1395 64483894
Diverticulum intestinal 18.40 13.33 14 13429 7406 64477883
Aortic arteriosclerosis 18.30 13.33 14 13429 7462 64477827
Angiosclerosis 18.03 13.33 3 13440 10 64485279
Vascular anastomotic haemorrhage 17.56 13.33 4 13439 84 64485205
Perineal cyst 17.47 13.33 4 13439 86 64485203
Perioral dermatitis 17.44 13.33 5 13438 268 64485021
Drug interaction 17.39 13.33 132 13311 361951 64123338
Hepatic function abnormal 17.16 13.33 40 13403 64273 64421016
Blood lactate dehydrogenase increased 16.77 13.33 27 13416 33051 64452238
Acute myocardial infarction 16.09 13.33 41 13402 69677 64415612
Blood creatine phosphokinase MB 15.96 13.33 3 13440 23 64485266
Mean cell volume increased 15.88 13.33 11 13432 5035 64480254
Blood potassium increased 15.69 13.33 23 13420 25957 64459332
Hepatosplenomegaly 15.31 13.33 11 13432 5332 64479957
Interstitial lung disease 15.30 13.33 50 13393 97682 64387607
Pancreatitis acute 15.30 13.33 30 13413 42825 64442464
Palmoplantar keratoderma 15.24 13.33 5 13438 421 64484868
Febrile bone marrow aplasia 15.18 13.33 15 13428 11240 64474049
Product use in unapproved indication 15.16 13.33 9 13434 176609 64308680
Vertigo 14.98 13.33 36 13407 58975 64426314
Hyperparathyroidism secondary 14.90 13.33 8 13435 2322 64482967
Haematoma 14.87 13.33 31 13412 46219 64439070
Rheumatoid arthritis 14.64 13.33 8 13435 164286 64321003
Angina pectoris 14.24 13.33 30 13413 45051 64440238
Product use issue 14.09 13.33 7 13436 151708 64333581
Invasive lobular breast carcinoma 14.04 13.33 5 13438 540 64484749
Glycosylated haemoglobin increased 14.02 13.33 17 13426 16002 64469287
Cholestatic liver injury 13.93 13.33 9 13434 3670 64481619
Ureteric injury 13.88 13.33 3 13440 49 64485240
Activated partial thromboplastin time prolonged 13.55 13.33 15 13428 12816 64472473
Alopecia 13.46 13.33 9 13434 165681 64319608
Blood bilirubin increased 13.44 13.33 34 13409 57519 64427770
Nephrotic syndrome 13.37 13.33 13 13430 9554 64475735

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C10AA04 CARDIOVASCULAR SYSTEM
LIPID MODIFYING AGENTS
LIPID MODIFYING AGENTS, PLAIN
HMG CoA reductase inhibitors
FDA MoA N0000000121 Hydroxymethylglutaryl-CoA Reductase Inhibitors
FDA EPC N0000175589 HMG-CoA Reductase Inhibitor
CHEBI has role CHEBI:35679 antilipemic drugs
CHEBI has role CHEBI:77255 lethal toxin inhibitors
CHEBI has role CHEBI:35821 anticholesteremic drugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hypercholesterolemia indication 13644009
Arteriosclerotic vascular disease indication 72092001
Familial hypercholesterolemia - heterozygous indication 238079002
Mixed hyperlipidemia indication 267434003
Slow Progression of Coronary Artery Disease indication
Cerebrovascular accident off-label use 230690007
Myocardial Infarction Prevention off-label use
Primary Prevention of Coronary Heart Disease off-label use
Prevention of Transient Ischemic Attacks off-label use
Alcoholism contraindication 7200002
Low blood pressure contraindication 45007003
Acute nephropathy contraindication 58574008
Disorder of muscle contraindication 129565002 DOID:423
Liver function tests abnormal contraindication 166603001
Hemorrhagic cerebral infarction contraindication 230706003
Disease of liver contraindication 235856003 DOID:409
Rhabdomyolysis contraindication 240131006
Pregnancy, function contraindication 289908002
Surgical procedure contraindication 387713003
Breastfeeding (mother) contraindication 413712001
Traumatic injury contraindication 417746004
Uncontrolled Epilepsy contraindication




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 4.05 acidic
pKa2 13.34 acidic
pKa3 13.99 acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
3-hydroxy-3-methylglutaryl-coenzyme A reductase Enzyme INHIBITOR IC50 7.55 CHEMBL DRUG LABEL
Cytochrome P450 2C9 Enzyme IC50 6.40 DRUG MATRIX
Retinoic acid receptor RXR-alpha Nuclear hormone receptor Kd 4.96 CHEMBL
Nuclear receptor subfamily 1 group I member 3 Nuclear hormone receptor WOMBAT-PK
Sodium/bile acid cotransporter Transporter IC50 4.40 CHEMBL
NAD-dependent protein deacetylase sirtuin-6 Unclassified EC50 5.15 CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase Enzyme IC50 8.60 CHEMBL

External reference:

IDSource
D00892 KEGG_DRUG
93957-55-2 SECONDARY_CAS_RN
4020854 VANDF
4023909 VANDF
C0082608 UMLSCUI
CHEBI:38561 CHEBI
115 PDB_CHEM_ID
CHEMBL2220442 ChEMBL_ID
CHEMBL1078 ChEMBL_ID
CHEMBL2218894 ChEMBL_ID
D000077340 MESH_DESCRIPTOR_UI
DB01095 DRUGBANK_ID
23663976 PUBCHEM_CID
2951 IUPHAR_LIGAND_ID
6547 INN_ID
4L066368AS UNII
151972 RXNORM
1724 MMSL
189348 MMSL
4757 MMSL
d03183 MMSL
004439 NDDF
004440 NDDF
387585004 SNOMEDCT_US
412392009 SNOMEDCT_US
96307003 SNOMEDCT_US
CHEMBL103585 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
LescolXL HUMAN PRESCRIPTION DRUG LABEL 1 0078-0354 TABLET, EXTENDED RELEASE 80 mg ORAL NDA 30 sections
LescolXL HUMAN PRESCRIPTION DRUG LABEL 1 0078-0354 TABLET, EXTENDED RELEASE 80 mg ORAL NDA 30 sections
Fluvastatin HUMAN PRESCRIPTION DRUG LABEL 1 0093-7442 CAPSULE 20 mg ORAL ANDA 26 sections
Fluvastatin HUMAN PRESCRIPTION DRUG LABEL 1 0093-7443 CAPSULE 40 mg ORAL ANDA 26 sections
Fluvastatin Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0093-7446 TABLET, FILM COATED, EXTENDED RELEASE 80 mg ORAL ANDA 28 sections
Fluvastatin Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-8020 CAPSULE 20 mg ORAL ANDA 26 sections
Fluvastatin Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0378-8021 CAPSULE 40 mg ORAL ANDA 26 sections
Fluvastatin Sodium HUMAN PRESCRIPTION DRUG LABEL 1 0527-2580 TABLET, FILM COATED, EXTENDED RELEASE 80 mg ORAL ANDA 30 sections
FLUVASTATIN SODIUMER HUMAN PRESCRIPTION DRUG LABEL 1 0781-8017 TABLET, EXTENDED RELEASE 80 mg ORAL NDA authorized generic 27 sections
LESCOL HUMAN PRESCRIPTION DRUG LABEL 1 54868-3329 CAPSULE 20 mg ORAL NDA 15 sections
LESCOL HUMAN PRESCRIPTION DRUG LABEL 1 54868-4224 CAPSULE 40 mg ORAL NDA 15 sections
LESCOL XL HUMAN PRESCRIPTION DRUG LABEL 1 54868-4601 TABLET, EXTENDED RELEASE 80 mg ORAL NDA 15 sections
Fluvastatin HUMAN PRESCRIPTION DRUG LABEL 1 63629-8737 CAPSULE 40 mg ORAL ANDA 26 sections
Fluvastatin HUMAN PRESCRIPTION DRUG LABEL 1 63629-8737 CAPSULE 40 mg ORAL ANDA 26 sections
Fluvastatin HUMAN PRESCRIPTION DRUG LABEL 1 63629-8812 CAPSULE 20 mg ORAL ANDA 26 sections
Fluvastatin HUMAN PRESCRIPTION DRUG LABEL 1 63629-8812 CAPSULE 20 mg ORAL ANDA 26 sections
Fluvastatin Sodium HUMAN PRESCRIPTION DRUG LABEL 1 68151-1326 CAPSULE 20 mg ORAL ANDA 25 sections
Fluvastatin Sodium HUMAN PRESCRIPTION DRUG LABEL 1 68151-1334 CAPSULE 40 mg ORAL ANDA 25 sections
Lescol XL HUMAN PRESCRIPTION DRUG LABEL 1 68151-4471 TABLET, EXTENDED RELEASE 80 mg ORAL NDA 26 sections