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fluvastatin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antihyperlipidaemic substances, HMG CoA reductase inhibitors | 1229 | 93957-54-1 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 60 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 µM/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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.777 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 11.668 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 43.853 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 7.568 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 0.500 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 2.140 | % | High | 1 |
| herg | hERG pIC50 | 4.676 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 21.979 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 8.128 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 0.790 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CDK5,CDK9,DYRK1B,EIF2AK3,ERBB2,GRK2,ITK,MAP2K6,MAPK7,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIK3CG,PRKDC,TGFBR1 | 21 | |||
| kinase-selectivity-class | ACVR2B,AXL,GRK2 | 3 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 17.865 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 12.912 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 30.832 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 1.410 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 37.068 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 1 | |
| pppb | Pig plasma protein binding (% unbound) | 1.540 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.011 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 10.715 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 25.570 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 0.900 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 879.023 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 31, 1993 | FDA | NOVARTIS |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Myalgia | 209.12 | 15.45 | 162 | 9410 | 174963 | 90443912 |
| Rhabdomyolysis | 143.86 | 15.45 | 81 | 9491 | 51175 | 90567700 |
| Blood creatine phosphokinase increased | 135.76 | 15.45 | 68 | 9504 | 33955 | 90584920 |
| Limb reduction defect | 100 | 15.45 | 21 | 9551 | 607 | 90618268 |
| Antinuclear antibody negative | 84.40 | 15.45 | 16 | 9556 | 270 | 90618605 |
| Dysmorphism | 79.43 | 15.45 | 23 | 9549 | 2545 | 90616330 |
| Coombs positive haemolytic anaemia | 75.81 | 15.45 | 16 | 9556 | 474 | 90618401 |
| Gamma-glutamyltransferase increased | 75.28 | 15.45 | 48 | 9524 | 37904 | 90580971 |
| Cleft palate | 74.60 | 15.45 | 19 | 9553 | 1297 | 90617578 |
| Alanine aminotransferase increased | 72.09 | 15.45 | 75 | 9497 | 118263 | 90500612 |
| Atrial septal defect | 70.12 | 15.45 | 28 | 9544 | 8206 | 90610669 |
| Talipes | 69.99 | 15.45 | 19 | 9553 | 1661 | 90617214 |
| Patent ductus arteriosus | 66.38 | 15.45 | 23 | 9549 | 4546 | 90614329 |
| Acute kidney injury | 63.60 | 15.45 | 118 | 9454 | 320269 | 90298606 |
| Limb hypoplasia congenital | 62.83 | 15.45 | 12 | 9560 | 211 | 90618664 |
| Herpes simplex reactivation | 59.18 | 15.45 | 15 | 9557 | 1004 | 90617871 |
| Aspartate aminotransferase increased | 58.70 | 15.45 | 63 | 9509 | 102874 | 90516001 |
| Congenital oral malformation | 56.69 | 15.45 | 11 | 9561 | 211 | 90618664 |
| Antiphospholipid syndrome | 55.67 | 15.45 | 17 | 9555 | 2257 | 90616618 |
| Gastritis haemorrhagic | 55.13 | 15.45 | 16 | 9556 | 1784 | 90617091 |
| Retrognathia | 51.73 | 15.45 | 12 | 9560 | 552 | 90618323 |
| Interstitial lung disease | 51.20 | 15.45 | 51 | 9521 | 76354 | 90542521 |
| Myopathy | 50.91 | 15.45 | 26 | 9546 | 13492 | 90605383 |
| Complex regional pain syndrome | 48.98 | 15.45 | 16 | 9556 | 2643 | 90616232 |
| Developmental hip dysplasia | 48.15 | 15.45 | 14 | 9558 | 1571 | 90617304 |
| Pancreatitis acute | 47.81 | 15.45 | 34 | 9538 | 32081 | 90586794 |
| Drug ineffective | 46.39 | 15.45 | 47 | 9525 | 1384251 | 89234624 |
| Anxiety disorder | 46.34 | 15.45 | 18 | 9554 | 4904 | 90613971 |
| Neck deformity | 39.62 | 15.45 | 13 | 9559 | 2176 | 90616699 |
| Jaundice | 38.49 | 15.45 | 30 | 9542 | 32487 | 90586388 |
| Drug interaction | 36.27 | 15.45 | 86 | 9486 | 276367 | 90342508 |
| Lactic acidosis | 36.25 | 15.45 | 35 | 9537 | 50428 | 90568447 |
| Hyperlipidaemia | 35.82 | 15.45 | 25 | 9547 | 22891 | 90595984 |
| Off label use | 35.08 | 15.45 | 39 | 9533 | 1102213 | 89516662 |
| Hepatic function abnormal | 34.95 | 15.45 | 33 | 9539 | 46255 | 90572620 |
| Pneumocystis jirovecii pneumonia | 34.77 | 15.45 | 24 | 9548 | 21592 | 90597283 |
| Erysipelas | 32.90 | 15.45 | 17 | 9555 | 9035 | 90609840 |
| Blood alkaline phosphatase increased | 32.02 | 15.45 | 32 | 9540 | 48047 | 90570828 |
| Premature baby | 31.57 | 15.45 | 24 | 9548 | 25053 | 90593822 |
| Coronary artery disease | 31.35 | 15.45 | 27 | 9545 | 33596 | 90585279 |
| Osteonecrosis | 30.60 | 15.45 | 24 | 9548 | 26217 | 90592658 |
| Aplasia | 28.61 | 15.45 | 12 | 9560 | 3979 | 90614896 |
| Joint swelling | 28.28 | 15.45 | 9 | 9563 | 503291 | 90115584 |
| Pleuritic pain | 27.88 | 15.45 | 16 | 9556 | 10445 | 90608430 |
| Peripheral swelling | 27.88 | 15.45 | 5 | 9567 | 413101 | 90205774 |
| Immunosuppressant drug level increased | 26.78 | 15.45 | 12 | 9560 | 4668 | 90614207 |
| Blood creatinine increased | 26.16 | 15.45 | 42 | 9530 | 101344 | 90517531 |
| Haematoma | 26.02 | 15.45 | 26 | 9546 | 39022 | 90579853 |
| Alopecia | 25.84 | 15.45 | 10 | 9562 | 495061 | 90123814 |
| Cerebrovascular accident | 25.07 | 15.45 | 46 | 9526 | 123487 | 90495388 |
| Synovitis | 24.53 | 15.45 | 3 | 9569 | 329749 | 90289126 |
| Muscle spasms | 24.42 | 15.45 | 70 | 9502 | 251813 | 90367062 |
| Hypothyroidism | 24.27 | 15.45 | 29 | 9543 | 53098 | 90565777 |
| Chromaturia | 23.35 | 15.45 | 18 | 9554 | 19169 | 90599706 |
| Peritonitis | 22.93 | 15.45 | 18 | 9554 | 19687 | 90599188 |
| Ocular myasthenia | 22.67 | 15.45 | 5 | 9567 | 183 | 90618692 |
| Lymphopenia | 22.61 | 15.45 | 19 | 9553 | 22862 | 90596013 |
| Product use issue | 22.24 | 15.45 | 4 | 9568 | 329915 | 90288960 |
| International normalised ratio increased | 21.90 | 15.45 | 26 | 9546 | 47290 | 90571585 |
| Blood urea increased | 21.66 | 15.45 | 21 | 9551 | 30392 | 90588483 |
| Hypernatraemia | 21.46 | 15.45 | 13 | 9559 | 9374 | 90609501 |
| Neonatal seizure | 21.20 | 15.45 | 6 | 9566 | 611 | 90618264 |
| Angiosclerosis | 20.31 | 15.45 | 3 | 9569 | 9 | 90618866 |
| Pulmonary artery stenosis | 20.29 | 15.45 | 5 | 9567 | 298 | 90618577 |
| Cholestasis | 20.29 | 15.45 | 22 | 9550 | 36277 | 90582598 |
| Myocardial infarction | 19.68 | 15.45 | 38 | 9534 | 105934 | 90512941 |
| Renal failure | 19.64 | 15.45 | 43 | 9529 | 130964 | 90487911 |
| Syncope | 19.27 | 15.45 | 43 | 9529 | 132620 | 90486255 |
| Discomfort | 19.21 | 15.45 | 3 | 9569 | 274332 | 90344543 |
| Cerebral ischaemia | 19.16 | 15.45 | 11 | 9561 | 7185 | 90611690 |
| Otospondylomegaepiphyseal dysplasia | 18.97 | 15.45 | 4 | 9568 | 118 | 90618757 |
| Myoglobinuria | 18.79 | 15.45 | 5 | 9567 | 405 | 90618470 |
| Muscular weakness | 18.65 | 15.45 | 56 | 9516 | 206610 | 90412265 |
| Nasopharyngitis | 18.47 | 15.45 | 10 | 9562 | 407094 | 90211781 |
| Sterile pyuria | 17.88 | 15.45 | 3 | 9569 | 24 | 90618851 |
| Bradycardia neonatal | 17.82 | 15.45 | 6 | 9566 | 1087 | 90617788 |
| Systemic lupus erythematosus | 17.76 | 15.45 | 8 | 9564 | 361888 | 90256987 |
| Maternal exposure during pregnancy | 17.61 | 15.45 | 8 | 9564 | 360055 | 90258820 |
| Contraindicated product administered | 17.48 | 15.45 | 6 | 9566 | 320133 | 90298742 |
| Renal impairment | 17.41 | 15.45 | 36 | 9536 | 105385 | 90513490 |
| Therapeutic product effect decreased | 17.38 | 15.45 | 4 | 9568 | 277567 | 90341308 |
| Liver function test abnormal | 17.32 | 15.45 | 24 | 9548 | 50821 | 90568054 |
| Shock | 17.07 | 15.45 | 18 | 9554 | 28760 | 90590115 |
| Hypersensitivity | 16.83 | 15.45 | 14 | 9558 | 454663 | 90164212 |
| Cholangiocarcinoma | 16.79 | 15.45 | 6 | 9566 | 1297 | 90617578 |
| Skin disorder | 16.71 | 15.45 | 20 | 9552 | 36686 | 90582189 |
| Amyotrophic lateral sclerosis | 16.59 | 15.45 | 6 | 9566 | 1342 | 90617533 |
| Fasciitis | 16.58 | 15.45 | 5 | 9567 | 636 | 90618239 |
| Nephroangiosclerosis | 16.53 | 15.45 | 4 | 9568 | 221 | 90618654 |
| Rheumatoid arthritis | 16.31 | 15.45 | 9 | 9563 | 362605 | 90256270 |
| Infection | 16.27 | 15.45 | 9 | 9563 | 362085 | 90256790 |
| Myoglobin blood increased | 15.77 | 15.45 | 6 | 9566 | 1546 | 90617329 |
| Cutaneous T-cell lymphoma | 15.52 | 15.45 | 6 | 9566 | 1614 | 90617261 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Myalgia | 343.41 | 16.34 | 235 | 9640 | 95845 | 42515615 |
| Blood creatine phosphokinase increased | 198.17 | 16.34 | 129 | 9746 | 48209 | 42563251 |
| Off label use | 90.76 | 16.34 | 19 | 9856 | 638316 | 41973144 |
| Rectal prolapse | 85.68 | 16.34 | 21 | 9854 | 547 | 42610913 |
| Renal cyst haemorrhage | 81.62 | 16.34 | 21 | 9854 | 669 | 42610791 |
| Myopathy | 77.40 | 16.34 | 45 | 9830 | 13716 | 42597744 |
| Muscle rupture | 74.14 | 16.34 | 26 | 9849 | 2414 | 42609046 |
| Abdominal wall haemorrhage | 67.34 | 16.34 | 17 | 9858 | 501 | 42610959 |
| Vena cava injury | 63.65 | 16.34 | 15 | 9860 | 329 | 42611131 |
| SARS-CoV-2 antibody test positive | 61.26 | 16.34 | 15 | 9860 | 389 | 42611071 |
| Vascular anastomotic haemorrhage | 59.76 | 16.34 | 14 | 9861 | 299 | 42611161 |
| Delayed graft function | 57.49 | 16.34 | 22 | 9853 | 2613 | 42608847 |
| Carotid arteriosclerosis | 56.43 | 16.34 | 21 | 9854 | 2311 | 42609149 |
| Aortic dilatation | 55.40 | 16.34 | 19 | 9856 | 1650 | 42609810 |
| Diverticulum intestinal | 52.45 | 16.34 | 25 | 9850 | 5088 | 42606372 |
| Vascular compression | 51.56 | 16.34 | 13 | 9862 | 381 | 42611079 |
| Gamma-glutamyltransferase increased | 50.40 | 16.34 | 49 | 9826 | 32448 | 42579012 |
| Renal artery stenosis | 49.32 | 16.34 | 19 | 9856 | 2298 | 42609162 |
| Intraductal papillary mucinous neoplasm | 48.72 | 16.34 | 13 | 9862 | 478 | 42610982 |
| Perineal cyst | 46.91 | 16.34 | 11 | 9864 | 236 | 42611224 |
| Pharyngeal necrosis | 46.58 | 16.34 | 9 | 9866 | 72 | 42611388 |
| Amyotrophic lateral sclerosis | 46.23 | 16.34 | 15 | 9860 | 1097 | 42610363 |
| Hyperparathyroidism secondary | 46.08 | 16.34 | 17 | 9858 | 1825 | 42609635 |
| Mean cell volume increased | 45.87 | 16.34 | 21 | 9854 | 3902 | 42607558 |
| Restless legs syndrome | 45.14 | 16.34 | 28 | 9847 | 9586 | 42601874 |
| Myocardial infarction | 44.00 | 16.34 | 92 | 9783 | 123917 | 42487543 |
| Aortic arteriosclerosis | 43.45 | 16.34 | 22 | 9853 | 5098 | 42606362 |
| Blood 25-hydroxycholecalciferol decreased | 43.32 | 16.34 | 11 | 9864 | 332 | 42611128 |
| Actinic keratosis | 43.23 | 16.34 | 22 | 9853 | 5154 | 42606306 |
| Rhabdomyolysis | 42.99 | 16.34 | 70 | 9805 | 77949 | 42533511 |
| Hepatosplenomegaly | 42.43 | 16.34 | 21 | 9854 | 4639 | 42606821 |
| Intervertebral disc space narrowing | 41.80 | 16.34 | 14 | 9861 | 1131 | 42610329 |
| Dysuria | 41.09 | 16.34 | 43 | 9832 | 31053 | 42580407 |
| Glycosylated haemoglobin increased | 39.88 | 16.34 | 29 | 9846 | 12895 | 42598565 |
| Spinal stenosis | 38.82 | 16.34 | 22 | 9853 | 6384 | 42605076 |
| Oral mucosal eruption | 36.74 | 16.34 | 10 | 9865 | 397 | 42611063 |
| Left ventricular hypertrophy | 35.98 | 16.34 | 24 | 9851 | 9295 | 42602165 |
| Radiation necrosis | 35.92 | 16.34 | 9 | 9866 | 257 | 42611203 |
| Vertigo | 35.88 | 16.34 | 42 | 9833 | 34305 | 42577155 |
| Spinal osteoarthritis | 35.07 | 16.34 | 23 | 9852 | 8663 | 42602797 |
| Haemorrhoids | 32.73 | 16.34 | 29 | 9846 | 17068 | 42594392 |
| Fear | 32.46 | 16.34 | 24 | 9851 | 10941 | 42600519 |
| Ureteric injury | 31.16 | 16.34 | 6 | 9869 | 47 | 42611413 |
| Swelling of eyelid | 30.04 | 16.34 | 13 | 9862 | 2115 | 42609345 |
| Vestibular neuronitis | 29.50 | 16.34 | 8 | 9867 | 313 | 42611147 |
| Death | 29.25 | 16.34 | 40 | 9835 | 471145 | 42140315 |
| General physical health deterioration | 29.15 | 16.34 | 89 | 9786 | 151157 | 42460303 |
| Angina pectoris | 29.12 | 16.34 | 37 | 9838 | 32859 | 42578601 |
| Blood potassium increased | 28.82 | 16.34 | 28 | 9847 | 18508 | 42592952 |
| Vitamin D decreased | 28.70 | 16.34 | 16 | 9859 | 4499 | 42606961 |
| Aspartate aminotransferase increased | 28.22 | 16.34 | 58 | 9817 | 77105 | 42534355 |
| Face oedema | 27.80 | 16.34 | 24 | 9851 | 13642 | 42597818 |
| Arteriosclerosis | 27.64 | 16.34 | 27 | 9848 | 17962 | 42593498 |
| Tendon rupture | 26.91 | 16.34 | 19 | 9856 | 8064 | 42603396 |
| Toxicity to various agents | 26.49 | 16.34 | 10 | 9865 | 229126 | 42382334 |
| Generalised oedema | 25.42 | 16.34 | 24 | 9851 | 15312 | 42596148 |
| Hepatic steatosis | 25.41 | 16.34 | 28 | 9847 | 21420 | 42590040 |
| Coronary artery disease | 25.34 | 16.34 | 45 | 9830 | 53675 | 42557785 |
| Squamous cell carcinoma of skin | 25.18 | 16.34 | 22 | 9853 | 12704 | 42598756 |
| Blood creatinine increased | 24.31 | 16.34 | 68 | 9807 | 109935 | 42501525 |
| Chronic kidney disease | 24.14 | 16.34 | 41 | 9834 | 47200 | 42564260 |
| Complications of transplanted kidney | 23.65 | 16.34 | 15 | 9860 | 5335 | 42606125 |
| Aortic valve incompetence | 23.22 | 16.34 | 16 | 9859 | 6532 | 42604928 |
| Product dose omission issue | 23.05 | 16.34 | 4 | 9871 | 154361 | 42457099 |
| Febrile bone marrow aplasia | 23.01 | 16.34 | 19 | 9856 | 10162 | 42601298 |
| Presyncope | 22.75 | 16.34 | 27 | 9848 | 22360 | 42589100 |
| Large intestine polyp | 22.44 | 16.34 | 18 | 9857 | 9247 | 42602213 |
| Benign prostatic hyperplasia | 22.41 | 16.34 | 26 | 9849 | 21026 | 42590434 |
| Tinea capitis | 21.70 | 16.34 | 4 | 9871 | 24 | 42611436 |
| Blood urea increased | 21.64 | 16.34 | 32 | 9843 | 32761 | 42578699 |
| Systemic infection | 21.54 | 16.34 | 14 | 9861 | 5191 | 42606269 |
| Myocardial ischaemia | 20.71 | 16.34 | 23 | 9852 | 17739 | 42593721 |
| Activated partial thromboplastin time prolonged | 19.25 | 16.34 | 21 | 9854 | 15882 | 42595578 |
| Congenital inguinal hernia | 18.92 | 16.34 | 5 | 9870 | 177 | 42611283 |
| Seizure | 18.27 | 16.34 | 3 | 9872 | 120558 | 42490902 |
| Muscle discomfort | 17.92 | 16.34 | 5 | 9870 | 218 | 42611242 |
| Perioral dermatitis | 17.63 | 16.34 | 5 | 9870 | 231 | 42611229 |
| Funguria | 17.62 | 16.34 | 4 | 9871 | 74 | 42611386 |
| Renal cyst | 17.19 | 16.34 | 16 | 9859 | 10023 | 42601437 |
| Biliary anastomosis | 17.09 | 16.34 | 3 | 9872 | 13 | 42611447 |
| Atrioventricular block first degree | 16.55 | 16.34 | 13 | 9862 | 6478 | 42604982 |
| Atrial fibrillation | 16.46 | 16.34 | 70 | 9805 | 139523 | 42471937 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Myalgia | 424.86 | 14.93 | 312 | 16066 | 222069 | 110350852 |
| Blood creatine phosphokinase increased | 298.80 | 14.93 | 166 | 16212 | 72911 | 110500010 |
| Rhabdomyolysis | 134.65 | 14.93 | 124 | 16254 | 120277 | 110452644 |
| Off label use | 111.21 | 14.93 | 42 | 16336 | 1500143 | 109072778 |
| Myopathy | 111.01 | 14.93 | 60 | 16318 | 24900 | 110548021 |
| Gamma-glutamyltransferase increased | 92.57 | 14.93 | 75 | 16303 | 61234 | 110511687 |
| Renal cyst haemorrhage | 88.90 | 14.93 | 21 | 16357 | 740 | 110572181 |
| Aspartate aminotransferase increased | 70.80 | 14.93 | 102 | 16276 | 159834 | 110413087 |
| Vena cava injury | 69.99 | 14.93 | 15 | 16363 | 337 | 110572584 |
| Abdominal wall haemorrhage | 68.58 | 14.93 | 17 | 16361 | 736 | 110572185 |
| Alanine aminotransferase increased | 68.27 | 14.93 | 108 | 16270 | 183665 | 110389256 |
| SARS-CoV-2 antibody test positive | 67.53 | 14.93 | 15 | 16363 | 400 | 110572521 |
| Myocardial infarction | 66.07 | 14.93 | 109 | 16269 | 191974 | 110380947 |
| Vascular anastomotic haemorrhage | 66.00 | 14.93 | 14 | 16364 | 299 | 110572622 |
| Carotid arteriosclerosis | 63.90 | 14.93 | 22 | 16356 | 3035 | 110569886 |
| Amyotrophic lateral sclerosis | 63.68 | 14.93 | 20 | 16358 | 2071 | 110570850 |
| Rectal prolapse | 63.67 | 14.93 | 21 | 16357 | 2542 | 110570379 |
| Delayed graft function | 56.80 | 14.93 | 22 | 16356 | 4235 | 110568686 |
| Muscle rupture | 55.80 | 14.93 | 22 | 16356 | 4438 | 110568483 |
| Aortic dilatation | 54.18 | 14.93 | 18 | 16360 | 2228 | 110570693 |
| Amaurosis fugax | 53.09 | 14.93 | 18 | 16360 | 2372 | 110570549 |
| Actinic keratosis | 52.42 | 14.93 | 24 | 16354 | 6989 | 110565932 |
| Perineal cyst | 51.94 | 14.93 | 11 | 16367 | 233 | 110572688 |
| Coronary artery disease | 49.48 | 14.93 | 57 | 16321 | 71633 | 110501288 |
| Pharyngeal necrosis | 49.17 | 14.93 | 9 | 16369 | 86 | 110572835 |
| Renal artery stenosis | 48.80 | 14.93 | 19 | 16359 | 3707 | 110569214 |
| Vascular compression | 48.51 | 14.93 | 13 | 16365 | 768 | 110572153 |
| Intraductal papillary mucinous neoplasm | 47.28 | 14.93 | 13 | 16365 | 846 | 110572075 |
| Joint swelling | 45.34 | 14.93 | 6 | 16372 | 442839 | 110130082 |
| Aortic arteriosclerosis | 45.05 | 14.93 | 25 | 16353 | 10913 | 110562008 |
| Blood 25-hydroxycholecalciferol decreased | 44.63 | 14.93 | 11 | 16367 | 465 | 110572456 |
| Presyncope | 44.50 | 14.93 | 45 | 16333 | 48842 | 110524079 |
| Hyperparathyroidism secondary | 43.81 | 14.93 | 17 | 16361 | 3287 | 110569634 |
| Hepatosplenomegaly | 43.46 | 14.93 | 21 | 16357 | 6898 | 110566023 |
| Intervertebral disc space narrowing | 41.02 | 14.93 | 14 | 16364 | 1882 | 110571039 |
| Diverticulum intestinal | 40.79 | 14.93 | 24 | 16354 | 11695 | 110561226 |
| Drug interaction | 40.67 | 14.93 | 164 | 16214 | 500019 | 110072902 |
| Blood creatinine increased | 40.55 | 14.93 | 86 | 16292 | 182803 | 110390118 |
| Blood urea increased | 40.13 | 14.93 | 45 | 16333 | 54912 | 110518009 |
| Mean cell volume increased | 39.77 | 14.93 | 21 | 16357 | 8309 | 110564612 |
| Infusion related reaction | 39.41 | 14.93 | 5 | 16373 | 381157 | 110191764 |
| Acute kidney injury | 39.31 | 14.93 | 192 | 16186 | 635238 | 109937683 |
| Peripheral swelling | 37.90 | 14.93 | 7 | 16371 | 404027 | 110168894 |
| Drug ineffective | 36.79 | 14.93 | 110 | 16268 | 1520430 | 109052491 |
| Fear | 36.32 | 14.93 | 29 | 16349 | 23164 | 110549757 |
| Benign prostatic hyperplasia | 35.60 | 14.93 | 26 | 16352 | 18208 | 110554713 |
| Cerebrovascular accident | 35.38 | 14.93 | 81 | 16297 | 181203 | 110391718 |
| Hepatic function abnormal | 35.25 | 14.93 | 54 | 16324 | 89241 | 110483680 |
| Generalised oedema | 35.01 | 14.93 | 32 | 16346 | 30672 | 110542249 |
| Blood potassium increased | 34.73 | 14.93 | 33 | 16345 | 33216 | 110539705 |
| Urinary tract disorder | 34.49 | 14.93 | 17 | 16361 | 5827 | 110567094 |
| Glycosylated haemoglobin increased | 33.76 | 14.93 | 28 | 16350 | 23591 | 110549330 |
| Pancreatitis acute | 33.57 | 14.93 | 43 | 16335 | 60231 | 110512690 |
| Antinuclear antibody negative | 33.16 | 14.93 | 7 | 16371 | 146 | 110572775 |
| Left ventricular hypertrophy | 33.16 | 14.93 | 22 | 16356 | 13222 | 110559699 |
| Blood alkaline phosphatase increased | 32.48 | 14.93 | 46 | 16332 | 70889 | 110502032 |
| Spinal osteoarthritis | 31.10 | 14.93 | 25 | 16353 | 20158 | 110552763 |
| Jaundice | 31.02 | 14.93 | 41 | 16337 | 59195 | 110513726 |
| Oral mucosal eruption | 30.67 | 14.93 | 10 | 16368 | 1167 | 110571754 |
| Complications of transplanted kidney | 30.62 | 14.93 | 17 | 16361 | 7425 | 110565496 |
| Arteriosclerosis | 30.58 | 14.93 | 27 | 16351 | 24740 | 110548181 |
| Dysuria | 30.49 | 14.93 | 41 | 16337 | 60190 | 110512731 |
| Squamous cell carcinoma of skin | 30.17 | 14.93 | 23 | 16355 | 17180 | 110555741 |
| Renal impairment | 30.15 | 14.93 | 78 | 16300 | 188367 | 110384554 |
| Myoglobin blood increased | 30.12 | 14.93 | 14 | 16364 | 4218 | 110568703 |
| Tendon rupture | 29.60 | 14.93 | 21 | 16357 | 14057 | 110558864 |
| Radiation necrosis | 29.51 | 14.93 | 9 | 16369 | 845 | 110572076 |
| Interstitial lung disease | 29.13 | 14.93 | 64 | 16314 | 139270 | 110433651 |
| Activated partial thromboplastin time prolonged | 28.86 | 14.93 | 25 | 16353 | 22343 | 110550578 |
| Chronic kidney disease | 28.52 | 14.93 | 45 | 16333 | 76246 | 110496675 |
| Ocular discomfort | 28.46 | 14.93 | 17 | 16361 | 8516 | 110564405 |
| Lactic acidosis | 28.35 | 14.93 | 50 | 16328 | 92761 | 110480160 |
| Vertigo | 28.10 | 14.93 | 48 | 16330 | 86822 | 110486099 |
| Spinal stenosis | 28.09 | 14.93 | 23 | 16355 | 19033 | 110553888 |
| Hyperkalaemia | 27.97 | 14.93 | 62 | 16316 | 135734 | 110437187 |
| Ureteric injury | 27.90 | 14.93 | 6 | 16372 | 137 | 110572784 |
| Tinea capitis | 27.89 | 14.93 | 5 | 16373 | 42 | 110572879 |
| Haemorrhoids | 27.40 | 14.93 | 30 | 16348 | 35642 | 110537279 |
| Myocardial ischaemia | 26.95 | 14.93 | 26 | 16352 | 26658 | 110546263 |
| Death | 26.56 | 14.93 | 39 | 16339 | 698830 | 109874091 |
| Product use issue | 26.01 | 14.93 | 7 | 16371 | 311688 | 110261233 |
| Syncope | 25.66 | 14.93 | 77 | 16301 | 202459 | 110370462 |
| Lower respiratory tract infection | 25.58 | 14.93 | 3 | 16375 | 243103 | 110329818 |
| Alopecia | 25.57 | 14.93 | 11 | 16367 | 364742 | 110208179 |
| Haemorrhagic stroke | 25.43 | 14.93 | 19 | 16359 | 13770 | 110559151 |
| Restless legs syndrome | 24.88 | 14.93 | 24 | 16354 | 24602 | 110548319 |
| Product use in unapproved indication | 24.87 | 14.93 | 18 | 16360 | 447359 | 110125562 |
| Toxicity to various agents | 24.62 | 14.93 | 21 | 16357 | 480534 | 110092387 |
| Aortic valve incompetence | 24.53 | 14.93 | 17 | 16361 | 10964 | 110561957 |
| Vestibular neuronitis | 24.44 | 14.93 | 8 | 16370 | 945 | 110571976 |
| Swelling of eyelid | 24.15 | 14.93 | 14 | 16364 | 6639 | 110566282 |
| Large intestine polyp | 23.88 | 14.93 | 19 | 16359 | 15098 | 110557823 |
| Face oedema | 23.74 | 14.93 | 27 | 16351 | 33442 | 110539479 |
| Hepatic steatosis | 22.84 | 14.93 | 32 | 16346 | 48799 | 110524122 |
| Rheumatoid arthritis | 22.71 | 14.93 | 8 | 16370 | 299605 | 110273316 |
| Wound | 22.10 | 14.93 | 4 | 16374 | 234433 | 110338488 |
| Product dose omission issue | 22.08 | 14.93 | 10 | 16368 | 321772 | 110251149 |
| Bradycardia | 21.49 | 14.93 | 61 | 16317 | 155456 | 110417465 |
| Chromaturia | 21.36 | 14.93 | 24 | 16354 | 29336 | 110543585 |
| Immunosuppressant drug level increased | 21.28 | 14.93 | 16 | 16362 | 11708 | 110561213 |
| Completed suicide | 21.07 | 14.93 | 5 | 16373 | 242376 | 110330545 |
| Maternal exposure during pregnancy | 20.74 | 14.93 | 6 | 16372 | 254877 | 110318044 |
| Vitamin D decreased | 20.69 | 14.93 | 16 | 16362 | 12199 | 110560722 |
| Dizziness | 20.11 | 14.93 | 174 | 16204 | 698019 | 109874902 |
| Atrial fibrillation | 19.99 | 14.93 | 77 | 16301 | 229565 | 110343356 |
| Metabolic acidosis | 19.93 | 14.93 | 45 | 16333 | 99699 | 110473222 |
| Haematoma | 19.83 | 14.93 | 33 | 16345 | 58443 | 110514478 |
| Muscle necrosis | 19.49 | 14.93 | 8 | 16370 | 1789 | 110571132 |
| Acute myocardial infarction | 19.26 | 14.93 | 40 | 16338 | 83737 | 110489184 |
| Blood lactate dehydrogenase increased | 19.19 | 14.93 | 28 | 16350 | 44306 | 110528615 |
| Stomatitis | 19.17 | 14.93 | 8 | 16370 | 270234 | 110302687 |
| Systemic infection | 19.16 | 14.93 | 14 | 16364 | 9805 | 110563116 |
| Renal cyst | 18.91 | 14.93 | 18 | 16360 | 18154 | 110554767 |
| Muscle spasms | 18.56 | 14.93 | 86 | 16292 | 278071 | 110294850 |
| Atrioventricular block first degree | 18.55 | 14.93 | 16 | 16362 | 14209 | 110558712 |
| Angiosclerosis | 18.43 | 14.93 | 3 | 16375 | 13 | 110572908 |
| Haematuria | 18.34 | 14.93 | 39 | 16339 | 82966 | 110489955 |
| International normalised ratio increased | 18.29 | 14.93 | 40 | 16338 | 86732 | 110486189 |
| Muscular weakness | 18.21 | 14.93 | 79 | 16299 | 248389 | 110324532 |
| Gastritis haemorrhagic | 18.04 | 14.93 | 9 | 16369 | 3164 | 110569757 |
| Autoimmune hepatitis | 18.00 | 14.93 | 16 | 16362 | 14788 | 110558133 |
| Hypersensitivity | 17.96 | 14.93 | 20 | 16358 | 403978 | 110168943 |
| Blood creatine phosphokinase MB | 17.62 | 14.93 | 3 | 16375 | 18 | 110572903 |
| Wheezing | 17.40 | 14.93 | 8 | 16370 | 255222 | 110317699 |
| Renal failure | 17.34 | 14.93 | 73 | 16305 | 226501 | 110346420 |
| Systemic lupus erythematosus | 17.30 | 14.93 | 8 | 16370 | 254330 | 110318591 |
| Complex regional pain syndrome | 17.25 | 14.93 | 8 | 16370 | 2397 | 110570524 |
| Coombs positive haemolytic anaemia | 17.04 | 14.93 | 7 | 16371 | 1570 | 110571351 |
| Antiphospholipid syndrome | 16.89 | 14.93 | 8 | 16370 | 2515 | 110570406 |
| Anxiety disorder | 16.70 | 14.93 | 10 | 16368 | 5030 | 110567891 |
| Angina unstable | 16.57 | 14.93 | 16 | 16362 | 16416 | 110556505 |
| Intentional product use issue | 16.55 | 14.93 | 8 | 16370 | 247898 | 110325023 |
| Head discomfort | 16.40 | 14.93 | 17 | 16361 | 18983 | 110553938 |
| Sinusitis | 16.40 | 14.93 | 12 | 16366 | 296676 | 110276245 |
| Febrile neutropenia | 16.02 | 14.93 | 14 | 16364 | 316753 | 110256168 |
| Nasopharyngitis | 15.97 | 14.93 | 21 | 16357 | 394340 | 110178581 |
| Pain | 15.96 | 14.93 | 80 | 16298 | 954875 | 109618046 |
| Angina pectoris | 15.81 | 14.93 | 31 | 16347 | 62264 | 110510657 |
| Blindness | 15.79 | 14.93 | 23 | 16355 | 36336 | 110536585 |
| Dry mouth | 15.74 | 14.93 | 5 | 16373 | 199943 | 110372978 |
| Necrotising myositis | 15.43 | 14.93 | 7 | 16371 | 1995 | 110570926 |
| General physical condition | 15.34 | 14.93 | 3 | 16375 | 42 | 110572879 |
| Photophobia | 15.32 | 14.93 | 19 | 16359 | 25752 | 110547169 |
| Eye pain | 15.31 | 14.93 | 27 | 16351 | 50072 | 110522849 |
| Myoglobinuria | 15.16 | 14.93 | 6 | 16372 | 1222 | 110571699 |
| Infection | 14.96 | 14.93 | 19 | 16359 | 362181 | 110210740 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | C10AA04 | CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN HMG CoA reductase inhibitors |
| FDA MoA | N0000000121 | Hydroxymethylglutaryl-CoA Reductase Inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35679 | antilipemic drug |
| CHEBI has role | CHEBI:35821 | anticholesteremic drug |
| CHEBI has role | CHEBI:77255 | EC 3.4.24.83 (anthrax lethal factor endopeptidase) inhibitor |
| FDA EPC | N0000175589 | HMG-CoA Reductase Inhibitor |
| CHEBI has role | CHEBI:22587 | antiviral agent |
| CHEBI has role | CHEBI:35554 | cardiovascular drug |
| CHEBI has role | CHEBI:35620 | vasodilator agent |
Related Drugs by ATC class:
C10AA HMG CoA reductase inhibitors 7 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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 | |||||||
| Nuclear receptor subfamily 4 group A member 2 | Nuclear other | EC50 | 5.72 | CHEMBL | |||||
| NAD-dependent protein deacetylase sirtuin-6 | Enzyme | EC50 | 5.15 | CHEMBL | |||||
| Sodium/bile acid cotransporter | Transporter | IC50 | 4.40 | CHEMBL | |||||
| 3-hydroxy-3-methylglutaryl-coenzyme A reductase | Enzyme | IC50 | 8.60 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 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 |
| CHEMBL2218894 | ChEMBL_ID |
| CHEMBL333442 | ChEMBL_ID |
| D000077340 | MESH_DESCRIPTOR_UI |
| DB01095 | DRUGBANK_ID |
| 1548972 | 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 |
| 4L066368AS | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| 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 | 26 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 | 29 sections |
| FLUVASTATIN SODIUMER | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0781-8017 | TABLET, EXTENDED RELEASE | 80 mg | ORAL | NDA authorized generic | 22 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 | 63629-8812 | CAPSULE | 20 mg | ORAL | ANDA | 26 sections |
| LescolXL | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66758-211 | TABLET, EXTENDED RELEASE | 80 mg | ORAL | NDA | 22 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 |
| Fluvastatin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-2661 | CAPSULE | 40 mg | ORAL | ANDA | 26 sections |
| Fluvastatin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 71335-2933 | CAPSULE | 40 mg | ORAL | ANDA | 26 sections |
| Fluvastatin | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-1034 | CAPSULE | 40 mg | ORAL | ANDA | 26 sections |