ezetimibe Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antihyperlipidaemics, acyl CoA: cholesterol acyltransferase (ACAT) inhibitors	1125	163222-33-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: SCH58235 SCH-58235 ezetimib ezetimibe ezedoc ezentia ezetrol zetia	An azetidine derivative and ANTICHOLESTEREMIC AGENT that inhibits intestinal STEROL absorption. It is used to reduce total CHOLESTEROL; LDL CHOLESTEROL, and APOLIPOPROTEINS B in the treatment of HYPERLIPIDEMIAS. Molecular weight: 409.43 Formula: C24H21F2NO3 CLOGP: 3.96 LIPINSKI: 0 HAC: 4 HDO: 2 TPSA: 60.77 ALOGS: -4.68 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Drug dosage:

Dose	Unit	Route
10	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	2 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.35 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Oct. 25, 2002	FDA	MSD INTL GMBH

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	752.97	10.17	850	58167	122238	46504807
Rhabdomyolysis	603.84	10.17	467	58550	41442	46585603
Blood creatine phosphokinase increased	284.54	10.17	254	58763	27470	46599575
Low density lipoprotein increased	186.52	10.17	108	58909	5892	46621153
Myopathy	110.70	10.17	91	58926	8790	46618255
Muscle spasms	107.32	10.17	371	58646	122742	46504303
Muscular weakness	89.09	10.17	287	58730	91557	46535488
Toxicity to various agents	86.63	10.17	84	58933	211682	46415363
Drug ineffective	85.93	10.17	505	58512	677333	45949712
Death	83.67	10.17	188	58829	335360	46291685
Blood cholesterol increased	78.43	10.17	163	58854	39850	46587195
Pain in extremity	78.20	10.17	577	58440	258103	46368942
Contraindicated product administered	78.20	10.17	6	59011	79941	46547104
Completed suicide	76.14	10.17	45	58972	145875	46481170
Angina pectoris	74.86	10.17	127	58890	26648	46600397
Maternal exposure during pregnancy	74.25	10.17	19	58998	102530	46524515
Rheumatoid arthritis	71.61	10.17	121	58896	240094	46386951
Pancreatitis acute	70.90	10.17	119	58898	24753	46602292
Coronary artery disease	70.29	10.17	141	58876	33611	46593434
Liver function test abnormal	68.39	10.17	169	58848	46318	46580727
Myocardial infarction	68.30	10.17	274	58743	97254	46529791
Pancreatitis	65.66	10.17	160	58857	43467	46583578
Acute kidney injury	59.10	10.17	504	58513	235351	46391694
Exposure during pregnancy	56.96	10.17	33	58984	108179	46518866
Off label use	56.86	10.17	267	58750	379574	46247471
Synovitis	55.92	10.17	6	59011	61069	46565976
Coronary artery occlusion	54.57	10.17	59	58958	8043	46619002
Acute coronary syndrome	53.04	10.17	65	58952	10139	46616906
Hyperlipidaemia	51.90	10.17	88	58929	18451	46608594
High density lipoprotein decreased	49.75	10.17	30	58987	1764	46625281
Drug abuse	49.38	10.17	10	59007	63398	46563647
Intentional overdose	49.03	10.17	11	59006	64933	46562112
Aspartate aminotransferase increased	47.99	10.17	212	58805	78488	46548557
Arterial stenosis	47.85	10.17	21	58996	630	46626415
Alanine aminotransferase increased	44.26	10.17	225	58792	88226	46538819
Infusion related reaction	43.88	10.17	38	58979	101170	46525875
Blood glucose increased	41.66	10.17	191	58826	71822	46555223
Polymyositis	39.68	10.17	25	58992	1590	46625455
Febrile neutropenia	39.26	10.17	37	58980	94590	46532455
Treatment failure	39.09	10.17	36	58981	93051	46533994
Flatulence	38.32	10.17	101	58916	28777	46598268
Vascular stent stenosis	37.86	10.17	17	59000	539	46626506
Carotid arteriosclerosis	36.87	10.17	20	58997	960	46626085
Blood triglycerides increased	35.76	10.17	58	58959	11725	46615320
Coombs positive haemolytic anaemia	33.34	10.17	14	59003	376	46626669
Product use issue	32.69	10.17	43	58974	94601	46532444
Antinuclear antibody negative	32.44	10.17	12	59005	228	46626817
Arterial occlusive disease	32.38	10.17	35	58982	4769	46622276
Dizziness	32.05	10.17	606	58411	339808	46287237
Lipids increased	30.94	10.17	18	58999	990	46626055
Neutropenia	30.35	10.17	87	58930	143117	46483928
Muscle disorder	30.26	10.17	32	58985	4254	46622791
Myositis	29.76	10.17	43	58974	7861	46619184
Pyrexia	29.19	10.17	291	58726	348511	46278534
Sensorimotor disorder	29.05	10.17	13	59004	409	46626636
Herpes simplex reactivation	27.72	10.17	12	59005	348	46626697
Cardiac failure congestive	27.24	10.17	204	58813	91546	46535499
Disease progression	27.14	10.17	46	58971	91254	46535791
Hyper IgE syndrome	25.97	10.17	10	59007	213	46626832
Immune-mediated myositis	24.58	10.17	15	59002	901	46626144
Device expulsion	24.47	10.17	3	59014	27539	46599506
Body tinea	24.30	10.17	15	59002	920	46626125
Inhibitory drug interaction	23.94	10.17	20	58997	1975	46625070
Hypoglycaemia	23.59	10.17	133	58884	54216	46572829
Coma acidotic	23.01	10.17	8	59009	126	46626919
Palpitations	22.97	10.17	202	58815	95057	46531988
Asthenia	22.80	10.17	534	58483	310541	46316504
Cerebrovascular accident	22.70	10.17	211	58806	100828	46526217
Glucose tolerance impaired	22.29	10.17	29	58988	4802	46622243
Infection	22.29	10.17	90	58927	133502	46493543
Chest pain	22.09	10.17	329	58688	175995	46451050
Sepsis	21.84	10.17	93	58924	135921	46491124
Gangrene	21.38	10.17	28	58989	4667	46622378
Angina unstable	21.35	10.17	36	58981	7512	46619533
Muscle rupture	21.33	10.17	19	58998	2046	46624999
Coronary artery thrombosis	21.29	10.17	15	59002	1150	46625895
Dyslipidaemia	20.65	10.17	30	58987	5510	46621535
Abortion spontaneous	20.65	10.17	15	59002	43631	46583414
Hyperkalaemia	20.64	10.17	122	58895	50587	46576458
Transient ischaemic attack	20.49	10.17	93	58924	34810	46592235
Gait disturbance	20.17	10.17	276	58741	144987	46482058
Back pain	20.09	10.17	375	58642	209664	46417381
Pancytopenia	20.04	10.17	49	58968	85009	46542036
Biliary fibrosis	19.93	10.17	4	59013	4	46627041
Copper metabolism disorder	19.93	10.17	4	59013	4	46627041
Wound	19.88	10.17	15	59002	42787	46584258
Pregnancy	19.68	10.17	5	59012	27132	46599913
Gastritis haemorrhagic	19.55	10.17	15	59002	1311	46625734
Depressed level of consciousness	19.26	10.17	19	58998	47550	46579495
Obstructive pancreatitis	19.08	10.17	8	59009	214	46626831
Cardiac valve disease	18.51	10.17	24	58993	3960	46623085
Toxic epidermal necrolysis	18.45	10.17	3	59014	22275	46604770
Diabetic neuropathy	17.88	10.17	23	58994	3766	46623279
Therapeutic product effect decreased	17.62	10.17	50	58967	82551	46544494
Paresis	17.60	10.17	17	59000	2029	46625016
Blood glucose decreased	17.36	10.17	58	58959	18834	46608211
Fall	17.27	10.17	541	58476	328556	46298489
Therapy cessation	17.18	10.17	73	58944	26556	46600489
Lipids abnormal	17.16	10.17	8	59009	277	46626768
Aortic stenosis	16.73	10.17	24	58993	4358	46622687
Congenital musculoskeletal anomaly	16.48	10.17	9	59008	438	46626607
Low density lipoprotein decreased	16.20	10.17	7	59010	202	46626843
Ischaemic cardiomyopathy	15.84	10.17	18	58999	2592	46624453
Abnormal dreams	15.78	10.17	38	58979	10241	46616804
Platelet count decreased	15.68	10.17	69	58948	99955	46527090
Disease risk factor	15.63	10.17	5	59012	60	46626985
Chromaturia	15.51	10.17	48	58969	14971	46612074
Troponin increased	15.49	10.17	32	58985	7784	46619261
Glossodynia	15.48	10.17	20	58997	44353	46582692
Coronary artery stenosis	15.40	10.17	24	58993	4689	46622356
Foetal exposure during pregnancy	15.30	10.17	10	59007	30737	46596308
Seizure	15.27	10.17	92	58925	122962	46504083
Hepatic cyst	15.20	10.17	24	58993	4742	46622303
Overdose	15.00	10.17	72	58945	101907	46525138
Joint swelling	14.94	10.17	136	58881	165937	46461108
Septic shock	14.73	10.17	32	58985	57861	46569184
Spleen congestion	14.58	10.17	6	59011	153	46626892
Pericarditis	14.55	10.17	6	59011	23921	46603124
Acute myocardial infarction	14.43	10.17	79	58938	31845	46595200
Intentional product use issue	14.42	10.17	28	58989	52752	46574293
Muscle discomfort	14.25	10.17	5	59012	81	46626964
Impaired quality of life	14.24	10.17	19	58998	3223	46623822
Psoriatic arthropathy	14.19	10.17	15	59002	36364	46590681
Anembryonic gestation	14.18	10.17	9	59008	580	46626465
Euglycaemic diabetic ketoacidosis	14.14	10.17	15	59002	2001	46625044
Lactic acidosis	14.07	10.17	82	58935	33827	46593218
Helicobacter gastritis	14.06	10.17	13	59004	1469	46625576
Hospitalisation	13.79	10.17	38	58979	63347	46563698
Pancreatitis relapsing	13.57	10.17	9	59008	625	46626420
Lower respiratory tract infection	13.56	10.17	31	58986	55058	46571987
Chest discomfort	13.55	10.17	174	58843	90095	46536950
Lipoprotein (a) increased	13.53	10.17	4	59013	36	46627009
Blood cholesterol decreased	13.52	10.17	8	59009	454	46626591
C-reactive protein abnormal	13.48	10.17	5	59012	21265	46605780
Gastric disorder	13.39	10.17	68	58949	26637	46600408
Glycosylated haemoglobin increased	13.38	10.17	37	58980	10839	46616206
Blood creatine phosphokinase MM increased	13.34	10.17	4	59013	38	46627007
Malignant neoplasm progression	13.34	10.17	40	58977	64886	46562159
Gingival oedema	13.28	10.17	5	59012	100	46626945
Infection susceptibility increased	13.18	10.17	15	59002	2164	46624881
Peripheral artery haematoma	13.16	10.17	4	59013	40	46627005
Pruritus	13.12	10.17	400	58617	241952	46385093
Hypocholesterolaemia	13.10	10.17	5	59012	104	46626941
Nephropathy	13.02	10.17	23	58994	4982	46622063
White blood cell count decreased	12.85	10.17	86	58931	112145	46514900
Low density lipoprotein abnormal	12.79	10.17	5	59012	111	46626934
Gastrooesophageal reflux disease	12.76	10.17	147	58870	74197	46552848
Suicide attempt	12.73	10.17	32	58985	55004	46572041
Blood cholesterol abnormal	12.64	10.17	15	59002	2262	46624783
Cell death	12.58	10.17	15	59002	2273	46624772
Hypotrichosis	12.55	10.17	5	59012	117	46626928
Pleural effusion	12.53	10.17	58	58959	82894	46544151
Myoglobin blood increased	12.48	10.17	12	59005	1424	46625621
Total cholesterol/HDL ratio decreased	12.21	10.17	3	59014	12	46627033
Mucosal inflammation	12.17	10.17	19	58998	38957	46588088
Non-high-density lipoprotein cholesterol increased	12.17	10.17	5	59012	127	46626918
Hypersensitivity pneumonitis	12.14	10.17	15	59002	2358	46624687
Nasal cyst	12.14	10.17	4	59013	53	46626992
Complex regional pain syndrome	12.12	10.17	14	59003	2052	46624993
Restrictive pulmonary disease	12.11	10.17	11	59006	1215	46625830
Drug dependence	12.08	10.17	5	59012	19896	46607149
Hepatic enzyme increased	12	10.17	157	58860	81630	46545415
Product use in unapproved indication	12.00	10.17	66	58951	90207	46536838
Vitamin D deficiency	11.89	10.17	36	58981	11098	46615947
Language disorder	11.88	10.17	12	59005	1511	46625534
Ear haemorrhage	11.79	10.17	11	59006	1257	46625788
Pulmonary haematoma	11.75	10.17	4	59013	59	46626986
Hypertension	11.69	10.17	328	58689	196028	46431017
Pneumonia	11.59	10.17	375	58642	375945	46251100
Intervertebral disc degeneration	11.57	10.17	40	58977	13212	46613833
Acquired epidermolysis bullosa	11.56	10.17	4	59013	62	46626983
Systemic lupus erythematosus	11.45	10.17	43	58974	65137	46561908
Abdominal pain upper	11.41	10.17	252	58765	145053	46481992
C-reactive protein increased	11.40	10.17	37	58980	58553	46568492
Condition aggravated	11.34	10.17	230	58787	244822	46382223
Cataract	11.30	10.17	97	58920	45318	46581727
Pneumonia aspiration	11.28	10.17	14	59003	31591	46595454
Muscle atrophy	11.28	10.17	24	58993	5960	46621085
Small intestinal haemorrhage	11.21	10.17	13	59004	1913	46625132
Autoimmune hepatitis	11.05	10.17	28	58989	7786	46619259
Bladder irritation	11.01	10.17	5	59012	163	46626882
Intestinal transit time abnormal	10.96	10.17	4	59013	73	46626972
Multiple sclerosis relapse	10.95	10.17	23	58994	42102	46584943
Respiratory disorder	10.94	10.17	11	59006	27289	46599756
Depression	10.93	10.17	287	58730	169817	46457228
Somnolence	10.91	10.17	136	58881	156385	46470660
Encephalopathy	10.85	10.17	16	59001	33573	46593472
Antiphospholipid syndrome	10.72	10.17	12	59005	1700	46625345
Oedema peripheral	10.71	10.17	271	58746	159435	46467610
Sedation	10.67	10.17	8	59009	22902	46604143
Peroneal nerve palsy	10.64	10.17	19	58998	4149	46622896
Cerebellar syndrome	10.44	10.17	17	59000	3448	46623597
Total cholesterol/HDL ratio increased	10.40	10.17	4	59013	85	46626960
Ascites	10.35	10.17	19	58998	36565	46590480
Necrotising myositis	10.31	10.17	6	59011	330	46626715
Premature baby	10.29	10.17	5	59012	18107	46608938
Neutrophil count decreased	10.24	10.17	25	58992	43401	46583644
Type 2 diabetes mellitus	10.24	10.17	51	58966	19824	46607221
Clostridium difficile infection	10.19	10.17	10	59007	25093	46601952

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	937.70	10.65	910	53863	75757	29821948
Blood creatine phosphokinase increased	493.27	10.65	498	54275	43350	29854355
Rhabdomyolysis	465.54	10.65	577	54196	63003	29834702
Myopathy	305.56	10.65	208	54565	10378	29887327
Low density lipoprotein increased	195.17	10.65	110	54663	3906	29893799
Death	120.22	10.65	301	54472	356982	29540723
Blood cholesterol increased	106.62	10.65	143	54630	16827	29880878
Toxicity to various agents	105.73	10.65	101	54672	177082	29720623
Muscular weakness	105.55	10.65	305	54468	63340	29834365
Drug abuse	100.70	10.65	15	54758	82057	29815648
Myocardial infarction	97.43	10.65	471	54302	125154	29772551
Muscle spasms	96.43	10.65	299	54474	64539	29833166
Coronary artery disease	91.02	10.65	247	54526	49465	29848240
Low density lipoprotein decreased	89.10	10.65	41	54732	940	29896765
Angina pectoris	84.95	10.65	175	54598	29343	29868362
Immune-mediated myositis	81.46	10.65	42	54731	1243	29896462
Venous pressure jugular increased	75.03	10.65	33	54740	678	29897027
High density lipoprotein decreased	71.72	10.65	54	54719	3156	29894549
Febrile neutropenia	69.38	10.65	56	54717	106637	29791068
Completed suicide	66.23	10.65	51	54722	99441	29798264
Pancreatitis	60.56	10.65	175	54598	36315	29861390
Off label use	58.52	10.65	246	54527	249044	29648661
Myositis	52.68	10.65	79	54694	10298	29887407
Neutropenia	52.38	10.65	97	54676	128443	29769262
Foetal exposure during pregnancy	52.16	10.65	4	54769	36867	29860838
Hepatic enzyme increased	50.24	10.65	155	54618	33339	29864366
Drug interaction	48.60	10.65	568	54205	199000	29698705
Pancreatitis acute	48.33	10.65	129	54644	25566	29872139
Pneumonia	48.32	10.65	386	54387	333920	29563785
Dizziness	44.05	10.65	547	54226	194362	29703343
Blood triglycerides increased	43.77	10.65	86	54687	13931	29883774
Suicide attempt	42.12	10.65	8	54765	36689	29861016
Blood cholesterol decreased	40.55	10.65	24	54749	935	29896770
Liver function test abnormal	39.89	10.65	136	54637	30814	29866891
Asthenia	39.76	10.65	596	54177	220694	29677011
Type IIa hyperlipidaemia	37.96	10.65	11	54762	60	29897645
Chest pain	37.14	10.65	353	54420	117274	29780431
Treatment failure	36.87	10.65	9	54764	34670	29863035
Acute kidney injury	36.61	10.65	703	54070	273139	29624566
Intentional overdose	36.58	10.65	15	54758	41466	29856239
Chromaturia	36.16	10.65	79	54694	13786	29883919
Pain in extremity	34.41	10.65	330	54443	109891	29787814
Pyrexia	34.24	10.65	359	54414	294130	29603575
Erectile dysfunction	34.16	10.65	91	54682	18011	29879694
Cutaneous lupus erythematosus	33.46	10.65	18	54755	582	29897123
Acute coronary syndrome	32.78	10.65	75	54698	13498	29884207
Malignant neoplasm progression	32.68	10.65	51	54722	72236	29825469
Erythromelalgia	32.05	10.65	9	54764	43	29897662
Dissociation	31.98	10.65	22	54751	1115	29896590
Coronary artery occlusion	31.91	10.65	66	54707	11091	29886614
Amyotrophic lateral sclerosis	31.79	10.65	21	54752	995	29896710
Disease progression	31.00	10.65	62	54711	79812	29817893
Muscle disorder	30.65	10.65	29	54744	2323	29895382
Septic shock	30.58	10.65	43	54730	63564	29834141
Pancytopenia	30.52	10.65	69	54704	84983	29812722
Alanine aminotransferase increased	30.30	10.65	236	54537	74040	29823665
Dyspnoea exertional	29.68	10.65	136	54637	35294	29862411
Muscle rupture	29.27	10.65	27	54746	2094	29895611
Cardiac failure congestive	28.99	10.65	258	54515	84149	29813556
Glycogen storage disease type V	28.88	10.65	8	54765	36	29897669
Sepsis	28.67	10.65	154	54619	146241	29751464
Cardio-respiratory arrest	28.29	10.65	38	54735	57268	29840437
Left ventricular dysfunction	27.95	10.65	54	54719	8637	29889068
Hospitalisation	27.87	10.65	24	54749	44295	29853410
Ischaemic cardiomyopathy	27.86	10.65	45	54728	6252	29891453
Aspartate aminotransferase increased	27.82	10.65	205	54568	63217	29834488
Arthralgia	27.63	10.65	374	54399	135417	29762288
Bone marrow failure	27.54	10.65	10	54763	29775	29867930
Overdose	27.44	10.65	72	54701	84265	29813440
Product use in unapproved indication	27.08	10.65	59	54714	73634	29824071
Angina unstable	26.45	10.65	65	54708	12245	29885460
Exercise lack of	26.43	10.65	9	54764	89	29897616
Muscle atrophy	26.18	10.65	45	54728	6579	29891126
Drug dependence	25.85	10.65	4	54769	21291	29876414
Cytomegalovirus infection	25.45	10.65	6	54767	23668	29874037
Stent placement	24.78	10.65	36	54737	4560	29893145
Pemphigoid	24.49	10.65	47	54726	7481	29890224
Haematocrit increased	24.43	10.65	22	54751	1654	29896051
Rheumatoid arthritis	23.91	10.65	24	54749	41173	29856532
Plasma cell myeloma	23.89	10.65	38	54735	53424	29844281
Muscle injury	23.84	10.65	19	54754	1208	29896497
Intentional product use issue	23.82	10.65	19	54754	36421	29861284
Pancreatic neoplasm	23.37	10.65	17	54756	942	29896763
Delirium	23.20	10.65	24	54749	40607	29857098
Myasthenia gravis	23.19	10.65	28	54745	2964	29894741
Leukopenia	23.18	10.65	42	54731	56117	29841588
Hypercholesterolaemia	23.00	10.65	46	54727	7546	29890159
Oedema peripheral	22.98	10.65	295	54478	105537	29792168
Left atrial dilatation	22.97	10.65	22	54751	1789	29895916
Mucosal inflammation	22.43	10.65	14	54759	30480	29867225
Cardiac disorder	22.33	10.65	137	54636	39756	29857949
Food aversion	22.29	10.65	11	54762	296	29897409
White blood cell count decreased	22.08	10.65	79	54694	83868	29813837
Ascites	21.92	10.65	20	54753	35901	29861804
Cardiac murmur	21.42	10.65	42	54731	6792	29890913
Faeces pale	20.77	10.65	19	54754	1458	29896247
Low density lipoprotein abnormal	20.37	10.65	10	54763	266	29897439
Dyslipidaemia	20.18	10.65	37	54736	5690	29892015
Hypovolaemia	20.17	10.65	47	54726	8558	29889147
Multiple organ dysfunction syndrome	20.04	10.65	55	54718	63432	29834273
Mucosal dryness	19.83	10.65	16	54757	1035	29896670
Hepatitis cholestatic	19.56	10.65	44	54729	7828	29889877
Infection	19.53	10.65	75	54698	77999	29819706
Respiratory arrest	19.44	10.65	15	54758	29243	29868462
Agitation	19.28	10.65	44	54729	54029	29843676
Necrotising myositis	19.22	10.65	11	54762	402	29897303
Laryngeal discomfort	19.16	10.65	8	54765	144	29897561
Self esteem decreased	18.84	10.65	12	54761	534	29897171
Orthostatic hypotension	18.58	10.65	90	54683	23889	29873816
Seizure	18.49	10.65	105	54668	98370	29799335
Toxic epidermal necrolysis	18.41	10.65	5	54768	17935	29879770
Candida infection	18.39	10.65	3	54770	15359	29882346
Tendon rupture	18.14	10.65	40	54733	7024	29890681
Phaeochromocytoma malignant	18.12	10.65	6	54767	54	29897651
Respiratory failure	18.00	10.65	109	54664	100533	29797172
Neck pain	17.99	10.65	81	54692	20863	29876842
Platelet count decreased	17.92	10.65	117	54656	106012	29791693
Coeliac disease	17.71	10.65	12	54761	593	29897112
Blood creatine phosphokinase decreased	17.50	10.65	11	54762	478	29897227
Depressed level of consciousness	17.23	10.65	27	54746	38195	29859510
Myocardial ischaemia	17.21	10.65	70	54703	17247	29880458
Aldolase increased	17.13	10.65	6	54767	65	29897640
Paraesthesia	17.09	10.65	163	54610	54164	29843541
Exercise tolerance decreased	16.54	10.65	27	54746	3785	29893920
Coronary artery stenosis	16.51	10.65	45	54728	9025	29888680
Neutrophil count decreased	16.42	10.65	33	54740	42421	29855284
Suspected suicide attempt	16.04	10.65	7	54766	141	29897564
Haemoglobin increased	16.04	10.65	23	54750	2879	29894826
Pericardial haemorrhage	15.94	10.65	23	54750	2895	29894810
Pneumonia aspiration	15.81	10.65	28	54745	37752	29859953
Syncope	15.70	10.65	230	54543	84673	29813032
Total cholesterol/HDL ratio increased	15.69	10.65	7	54766	149	29897556
Influenza like illness	15.65	10.65	90	54683	25515	29872190
Polymyositis	15.54	10.65	16	54757	1420	29896285
Flatulence	15.48	10.65	70	54703	18059	29879646
Transaminases abnormal	15.48	10.65	8	54765	238	29897467
Spinal stenosis	15.29	10.65	28	54745	4301	29893404
Back pain	15.24	10.65	268	54505	102328	29795377
Arteriosclerosis	15.19	10.65	49	54724	10784	29886921
Lymphocyte count decreased	15.08	10.65	8	54765	19047	29878658
Autoimmune hepatitis	14.81	10.65	25	54748	3602	29894103
Acute myocardial infarction	14.80	10.65	155	54618	52784	29844921
Lipase increased	14.76	10.65	42	54731	8634	29889071
Drug withdrawal syndrome	14.70	10.65	9	54764	19800	29877905
Atrial fibrillation	14.51	10.65	278	54495	107846	29789859
Tumour lysis syndrome	14.38	10.65	3	54770	12882	29884823
Sedation	14.30	10.65	6	54767	16367	29881338
Tachycardia	14.18	10.65	78	54695	73661	29824044
Dyschromatopsia	14.06	10.65	8	54765	289	29897416
Dyspnoea	14.03	10.65	744	54029	332551	29565154
Gait disturbance	13.99	10.65	203	54570	74574	29823131
Bronchopneumopathy	13.94	10.65	9	54764	410	29897295
Thrombocytopenia	13.92	10.65	172	54601	136872	29760833
Hepatitis E virus test positive	13.63	10.65	4	54769	23	29897682
Stomatitis	13.56	10.65	30	54743	37249	29860456
Restrictive pulmonary disease	13.44	10.65	13	54760	1070	29896635
Blood creatine phosphokinase	13.39	10.65	5	54768	66	29897639
Fatigue	13.32	10.65	715	54058	319958	29577747
International normalised ratio abnormal	13.27	10.65	22	54751	3124	29894581
Autoimmune myositis	13.21	10.65	4	54769	26	29897679
Tumour invasion	13.00	10.65	8	54765	335	29897370
Ureteric cancer recurrent	12.72	10.65	4	54769	30	29897675
Abulia	12.66	10.65	9	54764	481	29897224
Aortic embolus	12.63	10.65	3	54770	6	29897699
Pleural neoplasm	12.61	10.65	4	54769	31	29897674
Intentional product misuse	12.53	10.65	28	54745	34639	29863066
Muscle fatigue	12.40	10.65	13	54760	1178	29896527
Prostatic specific antigen increased	12.31	10.65	49	54724	11955	29885750
Blood glucose increased	12.29	10.65	169	54604	61361	29836344
Muscle discomfort	12.28	10.65	4	54769	34	29897671
Neoplasm progression	12.28	10.65	9	54764	18014	29879691
Gastric dilatation	12.20	10.65	9	54764	510	29897195
Infusion related reaction	12.17	10.65	36	54737	40528	29857177
Hypercapnic coma	12.11	10.65	6	54767	163	29897542
C-reactive protein increased	12.04	10.65	40	54733	43433	29854272
Peritonitis bacterial	12.00	10.65	3	54770	11375	29886330
Clostridium difficile infection	11.95	10.65	7	54766	15776	29881929
Obstructive pancreatitis	11.89	10.65	8	54765	391	29897314
Gamma-glutamyltransferase increased	11.81	10.65	93	54680	29257	29868448
Chronic cutaneous lupus erythematosus	11.80	10.65	4	54769	39	29897666
Peritonitis	11.78	10.65	13	54760	21362	29876343
Disseminated intravascular coagulation	11.66	10.65	14	54759	22157	29875548
Glycosylated haemoglobin increased	11.61	10.65	41	54732	9450	29888255
Status epilepticus	11.52	10.65	3	54770	11069	29886636
Pancreatic carcinoma	11.49	10.65	36	54737	7801	29889904
Hypokalaemia	11.43	10.65	50	54723	50142	29847563
Retroperitoneal fibrosis	11.37	10.65	7	54766	293	29897412
Heart valve incompetence	11.37	10.65	12	54761	1096	29896609
Iron binding capacity total increased	11.37	10.65	4	54769	44	29897661
JC polyomavirus test positive	11.23	10.65	9	54764	577	29897128
Erythrasma	11.05	10.65	4	54769	48	29897657
Nasal neoplasm	10.97	10.65	5	54768	112	29897593
Pleural effusion	10.86	10.65	85	54688	73981	29823724
Dyspnoea at rest	10.69	10.65	18	54755	2588	29895117

Pharmacologic Action:

Source	Code	Description
ATC	C10AX09	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Other lipid modifying agents
ATC	C10BA02	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA05	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA06	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
ATC	C10BA10	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, COMBINATIONS Combinations of various lipid modifying agents
FDA PE	N0000008553	Decreased Cholesterol Absorption
MeSH PA	D000924	Anticholesteremic Agents
MeSH PA	D000963	Antimetabolites
MeSH PA	D000960	Hypolipidemic Agents
MeSH PA	D057847	Lipid Regulating Agents
FDA EPC	N0000175911	Dietary Cholesterol Absorption Inhibitor
CHEBI has role	CHEBI:35221	antimetabolite
CHEBI has role	CHEBI:35679	hypolipidemic agent
CHEBI has role	CHEBI:35821	hypocholesteremic agent

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Hypercholesterolemia	indication	13644009
Hyperlipidemia	indication	55822004	DOID:1168
Familial hypercholesterolemia - homozygous	indication	238078005
Familial hypercholesterolemia - heterozygous	indication	238079002
Sitosterolemia	indication	238104009	DOID:0090019
Mixed hyperlipidemia	indication	267434003
Alopecia areata	off-label use	68225006	DOID:986
Alcoholism	contraindication	7200002
Acute nephropathy	contraindication	58574008
Disorder of muscle	contraindication	129565002	DOID:423
Liver function tests abnormal	contraindication	166603001
Acute pancreatitis	contraindication	197456007	DOID:2913
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
SLCO1B1 Gene Variant for OATP1B1 Transporter Affecting Hepatic Clearance	contraindication
Myopathy related to SLCO1B1 Gene Variant	contraindication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.48	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
180MG;10MG	NEXLIZET	ESPERION THERAPS INC	N211617	Feb. 26, 2020	RX	TABLET	ORAL	Feb. 26, 2023	NEW PRODUCT
180MG;10MG	NEXLIZET	ESPERION THERAPS INC	N211617	Feb. 26, 2020	RX	TABLET	ORAL	Feb. 21, 2025	NEW CHEMICAL ENTITY

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Niemann-Pick C1-like protein 1	Membrane other	Q9UHC9	NPCL1_HUMAN	ANTAGONIST	Kd	6.66		IUPHAR	CHEMBL
Niemann-Pick C1-like protein 1	Unclassified		NPCL1_RAT		Ki	6.70		CHEMBL

External reference:

ID	Source
4021366	VUID
N0000148785	NUI
D01966	KEGG_DRUG
4021366	VANDF
C1707992	UMLSCUI
CHEBI:49040	CHEBI
CHEMBL1138	ChEMBL_ID
DB00973	DRUGBANK_ID
D000069438	MESH_DESCRIPTOR_UI
150311	PUBCHEM_CID
6816	IUPHAR_LIGAND_ID
8010	INN_ID
EOR26LQQ24	UNII
341248	RXNORM
17026	MMSL
229065	MMSL
45364	MMSL
d04824	MMSL
009817	NDDF
408041006	SNOMEDCT_US
409149001	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	0591-3713	TABLET	10 mg	ORAL	ANDA	26 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8300	TABLET	10 mg	ORAL	ANDA	27 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	0781-5690	TABLET	10 mg	ORAL	ANDA	27 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6664	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7103	TABLET	10 mg	ORAL	ANDA	26 sections
ezetimibe and simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	16714-778	TABLET	10 mg	ORAL	ANDA	28 sections
ezetimibe and simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	16714-779	TABLET	10 mg	ORAL	ANDA	28 sections
ezetimibe and simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	16714-780	TABLET	10 mg	ORAL	ANDA	28 sections
ezetimibe and simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	16714-781	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe	Human Prescription Drug Label	1	16714-813	TABLET	10 mg	ORAL	ANDA	28 sections
EZETIMIBE	HUMAN PRESCRIPTION DRUG LABEL	1	16729-433	TABLET	10 mg	ORAL	ANDA	29 sections
VYTORIN	HUMAN PRESCRIPTION DRUG LABEL	2	21695-325	TABLET	10 mg	ORAL	NDA	28 sections
VYTORIN	HUMAN PRESCRIPTION DRUG LABEL	2	21695-339	TABLET	10 mg	ORAL	NDA	28 sections
Zetia	HUMAN PRESCRIPTION DRUG LABEL	1	21695-778	TABLET	10 mg	ORAL	NDA	29 sections
VYTORIN	HUMAN PRESCRIPTION DRUG LABEL	2	21695-827	TABLET	10 mg	ORAL	NDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	43598-742	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	43598-743	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	43598-744	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	43598-745	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	45963-565	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	45963-566	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	45963-567	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	45963-568	TABLET	10 mg	ORAL	ANDA	28 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	50090-3087	TABLET	10 mg	ORAL	ANDA	26 sections
Ezetimibe	Human Prescription Drug Label	1	50090-3657	TABLET	10 mg	ORAL	ANDA	27 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	50090-3984	TABLET	10 mg	ORAL	ANDA	27 sections
Ezetimibe and Simvastatin	Human Prescription Drug Label	2	50090-4772	TABLET	10 mg	ORAL	ANDA	27 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	50228-379	TABLET	10 mg	ORAL	ANDA	29 sections
Ezetimibe	HUMAN PRESCRIPTION DRUG LABEL	1	50268-298	TABLET	10 mg	ORAL	ANDA	26 sections
Ezetimibe and Simvastatin	HUMAN PRESCRIPTION DRUG LABEL	2	51407-190	TABLET	10 mg	ORAL	ANDA	28 sections