Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
antihyperlipidaemic substances, HMG CoA reductase inhibitors	1229	93957-54-1

Description:

Molecule	Description
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

Molecule

Description

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:

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

atorvastatin cerivastatin lovastatin pitavastatin pravastatin rosuvastatin simvastatin

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])	Bioact source	MoA source
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme	P04035	HMDH_HUMAN	INHIBITOR	IC50	7.55	CHEMBL	DRUG LABEL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	6.40	DRUG MATRIX
Retinoic acid receptor RXR-alpha	Nuclear hormone receptor	P19793	RXRA_HUMAN		Kd	4.96	CHEMBL
Nuclear receptor subfamily 1 group I member 3	Nuclear hormone receptor	Q14994	NR1I3_HUMAN				WOMBAT-PK
Nuclear receptor subfamily 4 group A member 2	Nuclear other	P43354	NR4A2_HUMAN		EC50	5.72	CHEMBL
NAD-dependent protein deacetylase sirtuin-6	Enzyme	Q8N6T7	SIR6_HUMAN		EC50	5.15	CHEMBL
Sodium/bile acid cotransporter	Transporter	Q14973	NTCP_HUMAN		IC50	4.40	CHEMBL
3-hydroxy-3-methylglutaryl-coenzyme A reductase	Enzyme		HMDH_RAT		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

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fluvastatin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Description:

Drug dosage:

ADMET properties:

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Approvals:

FDA Adverse Event Reporting System (Female)

FDA Adverse Event Reporting System (Male)

FDA Adverse Event Reporting System (Geriatric)

FDA Adverse Event Reporting System (Pediatric)

Pharmacologic Action:

Related Drugs by ATC class:

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

🐶 Veterinary Drug Use

🐶 Veterinary products

Acid dissociation constants calculated using MoKa v3.0.0

Orange Book patent data (new drug applications)

Orange Book exclusivity data (new drug applications)

Bioactivity Summary:

External reference:

Pharmaceutical products: