gemfibrozil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	1285	25812-30-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: gemfibrosil gemfibrozil decrelip lopizid	A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol. Molecular weight: 250.34 Formula: C15H22O3 CLOGP: 3.94 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 46.53 ALOGS: -3.95 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

gemfibrosil
gemfibrozil
decrelip
lopizid

A lipid-regulating agent that lowers elevated serum lipids primarily by decreasing serum triglycerides with a variable reduction in total cholesterol.

Molecular weight: 250.34
Formula: C15H22O3
CLOGP: 3.94
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 46.53
ALOGS: -3.95
ROTB: 6

Status: OFP

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

Drug dosage:

Dose	Unit	Route
1.20	g	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	0.02 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	79.89 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	98 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

Date	Agency	Company	Orphan
Dec. 21, 1981	FDA	PFIZER PHARMS

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
Rhabdomyolysis	224.26	13.05	123	10030	38904	50556067
Drug hypersensitivity	72.44	13.05	157	9996	250853	50344118
Blood triglycerides increased	57.66	13.05	33	10120	11279	50583692
Coronary artery disease	54.02	13.05	46	10107	29680	50565291
Myocardial infarction	46.38	13.05	72	10081	88955	50506016
Blood creatine phosphokinase increased	46.27	13.05	40	10113	26327	50568644
Acute interstitial pneumonitis	42.91	13.05	12	10141	611	50594360
Cardiac failure congestive	35.51	13.05	62	10091	84320	50510651
Myopathy	34.52	13.05	22	10131	9117	50585854
Cerebrovascular accident	32.83	13.05	64	10089	94616	50500355
Myalgia	31.54	13.05	74	10079	124245	50470726
Pancreatitis	30.32	13.05	40	10113	42574	50552397
Pancreatitis acute	28.11	13.05	29	10124	23783	50571188
Drug interaction	27.26	13.05	95	10058	199526	50395445
Lip infection	23.66	13.05	5	10148	76	50594895
Blood glucose increased	23.26	13.05	47	10106	71277	50523694
Diabetes mellitus	21.89	13.05	37	10116	48996	50545975
Off label use	21.54	13.05	39	10114	474387	50120584
Drug intolerance	20.75	13.05	9	10144	219095	50375876
Drug ineffective	20.45	13.05	90	10063	819243	49775728
Tendon rupture	19.35	13.05	14	10139	7130	50587841
Bursitis	17.66	13.05	22	10131	22113	50572858
Microalbuminuria	16.47	13.05	5	10148	340	50594631
Synovitis	15.53	13.05	3	10150	123862	50471109
Hypertriglyceridaemia	15.42	13.05	11	10142	5480	50589491
Chronic kidney disease	15.15	13.05	28	10125	39743	50555228
Blood urea increased	15.04	13.05	21	10132	23564	50571407
Angioedema	14.95	13.05	27	10126	37649	50557322
Hyperlipidaemia	14.95	13.05	18	10135	17472	50577499
Infusion related reaction	14.47	13.05	8	10145	169549	50425422
Transient ischaemic attack	13.97	13.05	24	10129	32186	50562785
Myositis	13.86	13.05	12	10141	7908	50587063
Hypophagia	13.82	13.05	22	10131	27706	50567265
Blood creatine phosphokinase MB increased	13.82	13.05	6	10147	1136	50593835
Diabetes mellitus inadequate control	13.72	13.05	15	10138	13130	50581841
Granulocytopenia	13.60	13.05	10	10143	5221	50589750
Glaucoma	13.17	13.05	16	10137	15670	50579301
Joint swelling	13.16	13.05	18	10135	245268	50349703

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
Rhabdomyolysis	540.34	13.20	349	14268	60459	29499451
Acute kidney injury	112.77	13.20	336	14281	264931	29294979
Blood creatine phosphokinase increased	107.81	13.20	116	14501	40528	29519382
Myalgia	95.86	13.20	148	14469	73871	29486039
Blood triglycerides increased	95.06	13.20	66	14551	12768	29547142
Coronary artery disease	71.16	13.20	98	14519	44092	29515818
Myocardial infarction	58.71	13.20	152	14465	110144	29449766
Drug hypersensitivity	56.17	13.20	112	14505	68294	29491616
Polymyositis	52.45	13.20	21	14596	1307	29558603
Blood cholesterol increased	47.55	13.20	48	14569	15547	29544363
Off label use	45.63	13.20	49	14568	300751	29259159
Cardiac failure congestive	44.32	13.20	109	14508	76472	29483438
Drug interaction	40.06	13.20	198	14419	197187	29362723
Pancreatitis	36.44	13.20	63	14554	34451	29525459
Myopathy	29.54	13.20	31	14586	10502	29549408
International normalised ratio increased	28.71	13.20	66	14551	44306	29515604
Drug ineffective	27.64	13.20	90	14527	363080	29196830
Thunderclap headache	27.10	13.20	6	14611	43	29559867
Hyperglycaemia	25.58	13.20	54	14563	34233	29525677
Drug level below therapeutic	24.87	13.20	19	14598	4252	29555658
Chromaturia	24.61	13.20	31	14586	12771	29547139
Drug abuse	24.19	13.20	5	14612	79878	29480032
Haemodialysis	23.91	13.20	27	14590	9927	29549983
Chronic kidney disease	23.37	13.20	54	14563	36362	29523548
Granulocytopenia	23.10	13.20	21	14596	5973	29553937
Blood glucose increased	22.31	13.20	72	14545	58912	29500998
Death	20.68	13.20	93	14524	341991	29217919
Type 2 diabetes mellitus	20.17	13.20	29	14588	13552	29546358
Myositis	19.92	13.20	25	14592	10258	29549652
Product use in unapproved indication	19.91	13.20	9	14608	86866	29473044
Angioedema	19.04	13.20	46	14571	31869	29528041
Angina unstable	18.84	13.20	25	14592	10840	29549070
General physical health deterioration	18.83	13.20	14	14603	102843	29457067
Blood glucose decreased	18.26	13.20	26	14591	12043	29547867
Erosive duodenitis	18.05	13.20	10	14607	1297	29558613
Tricuspid valve incompetence	17.22	13.20	21	14596	8373	29551537
Reversible cerebral vasoconstriction syndrome	16.99	13.20	6	14611	263	29559647
Pyrexia	16.88	13.20	79	14538	287543	29272367
Treatment noncompliance	16.74	13.20	37	14580	24190	29535720
Lacrimation decreased	16.55	13.20	3	14614	6	29559904
Fanconi syndrome	16.18	13.20	10	14607	1588	29558322
Muscular weakness	16.07	13.20	67	14550	61985	29497925
Hypertriglyceridaemia	15.82	13.20	19	14598	7456	29552454
Pneumonia haemophilus	15.60	13.20	6	14611	335	29559575
Blood creatinine increased	15.54	13.20	83	14534	85019	29474891
Asthenia	15.28	13.20	168	14449	215082	29344828
Otitis externa	14.98	13.20	8	14609	965	29558945
Interstitial lung disease	14.84	13.20	5	14612	57713	29502197
Arteriosclerosis coronary artery	14.81	13.20	22	14595	10583	29549327
Hyperlipidaemia	14.63	13.20	24	14593	12566	29547344
Breast neoplasm	14.31	13.20	3	14614	16	29559894
Metabolic acidosis	14.26	13.20	46	14571	37616	29522294
Coronary artery stenosis	13.76	13.20	19	14598	8554	29551356
Renal tubular necrosis	13.64	13.20	25	14592	14290	29545620
Hyperlactacidaemia	13.62	13.20	11	14606	2667	29557243
Aortic valve sclerosis	13.51	13.20	7	14610	793	29559117
Chest pain	13.41	13.20	98	14519	111875	29448035
Paralysis	13.35	13.20	15	14602	5482	29554428

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
Rhabdomyolysis	707.11	12.63	410	20062	91316	64386944
Blood creatine phosphokinase increased	157.60	12.63	138	20334	58420	64419840
Blood triglycerides increased	157.36	12.63	89	20383	18777	64459483
Coronary artery disease	134.43	12.63	128	20344	60305	64417955
Acute kidney injury	125.71	12.63	369	20103	448871	64029389
Myocardial infarction	117.49	12.63	198	20274	165623	64312637
Myalgia	110.51	12.63	188	20284	158429	64319831
Drug hypersensitivity	88.13	12.63	217	20255	237598	64240662
Cardiac failure congestive	75.80	12.63	143	20329	130437	64347823
Drug interaction	66.89	12.63	259	20213	361824	64116436
Off label use	62.98	12.63	65	20407	632741	63845519
Pancreatitis	58.75	12.63	83	20389	59524	64418736
Myopathy	58.54	12.63	47	20425	17633	64460627
Drug ineffective	50.59	12.63	121	20351	840126	63638134
Polymyositis	46.97	12.63	21	20451	2689	64475571
Granulocytopenia	41.65	12.63	31	20441	10409	64467851
Hyperlipidaemia	37.12	12.63	41	20431	22935	64455325
Myositis	36.97	12.63	35	20437	16342	64461918
Hyperglycaemia	35.62	12.63	67	20405	60901	64417359
Chromaturia	34.22	12.63	39	20433	22572	64455688
Blood glucose increased	32.60	12.63	86	20386	97987	64380273
Acute interstitial pneumonitis	31.37	12.63	12	20460	1035	64477225
International normalised ratio increased	31.11	12.63	74	20398	79093	64399167
Chronic kidney disease	30.59	12.63	61	20411	57858	64420402
Blood cholesterol increased	30.47	12.63	56	20416	50010	64428250
Hypertriglyceridaemia	29.29	12.63	26	20446	11179	64467081
Angioedema	29.00	12.63	62	20410	61759	64416501
Drug intolerance	28.48	12.63	12	20460	187980	64290280
Muscular weakness	28.42	12.63	97	20375	127241	64351019
Blood creatinine increased	28.20	12.63	101	20371	135681	64342579
Treatment failure	26.56	12.63	3	20469	116813	64361447
Pyrexia	26.47	12.63	90	20382	558554	63919706
Drug abuse	26.41	12.63	5	20467	132369	64345891
Pancreatitis acute	26.16	12.63	48	20424	42807	64435453
Haemodialysis	25.07	12.63	29	20443	17048	64461212
Cerebrovascular accident	24.15	12.63	97	20375	137486	64340774
Blood glucose decreased	23.96	12.63	33	20439	23090	64455170
Angina unstable	23.95	12.63	27	20445	15440	64462820
General physical health deterioration	23.86	12.63	18	20454	204407	64273853
Renal failure	23.53	12.63	117	20355	181571	64296689
Type 2 diabetes mellitus	23.20	12.63	40	20432	33980	64444280
Hypoglycaemia	22.30	12.63	71	20401	89821	64388439
Acute myocardial infarction	21.02	12.63	59	20413	69659	64408601
Thunderclap headache	20.63	12.63	6	20466	220	64478040
Joint swelling	20.36	12.63	23	20449	215359	64262901
Erosive duodenitis	19.86	12.63	10	20462	1668	64476592
Infusion related reaction	19.81	12.63	14	20458	164453	64313807
Coronary artery stenosis	19.79	12.63	21	20451	11227	64467033
Treatment noncompliance	19.69	12.63	43	20429	43439	64434821
Cardiac disorder	19.62	12.63	50	20422	55766	64422494
Lip infection	18.99	12.63	5	20467	126	64478134
Chest pain	18.93	12.63	134	20338	235846	64242414
Arteriosclerosis coronary artery	18.93	12.63	24	20448	15505	64462755
High density lipoprotein decreased	18.67	12.63	13	20459	3933	64474327
Rheumatoid arthritis	18.49	12.63	15	20457	164279	64313981
C-reactive protein increased	18.07	12.63	4	20468	94905	64383355
Renal cyst	17.87	12.63	21	20451	12549	64465711
Blood urea increased	17.05	12.63	41	20431	44112	64434148
Bursitis	16.98	12.63	27	20445	21458	64456802
Intervertebral disc displacement	16.78	12.63	6	20466	428	64477832
Metabolic acidosis	16.65	12.63	55	20417	70903	64407357
Hypophagia	16.63	12.63	38	20434	39549	64438711
Fanconi syndrome	16.13	12.63	10	20462	2491	64475769
Tricuspid valve incompetence	15.75	12.63	23	20449	16980	64461280
Blood creatine phosphokinase MB increased	15.70	12.63	10	20462	2611	64475649
Product use issue	15.69	12.63	15	20457	151700	64326560
Hyperkalaemia	15.18	12.63	68	20404	101061	64377199
Condition aggravated	15.01	12.63	64	20408	372362	64105898
Myoglobinuria	14.97	12.63	7	20465	993	64477267
Coronary artery occlusion	14.66	12.63	20	20452	13871	64464389
Hypercholesterolaemia	14.54	12.63	21	20451	15352	64462908
Carotid artery stenosis	14.28	12.63	15	20457	7926	64470334
Ischaemic cardiomyopathy	14.27	12.63	14	20458	6824	64471436
Product complaint	13.82	12.63	18	20454	11936	64466324
Tendon rupture	13.70	12.63	17	20455	10750	64467510
Acute coronary syndrome	13.55	12.63	23	20449	19287	64458973
Product use in unapproved indication	13.51	12.63	22	20450	176596	64301664
Diabetes mellitus	13.41	12.63	49	20423	66425	64411835
Maternal exposure during pregnancy	13.16	12.63	7	20465	95877	64382383
Erectile dysfunction	13.05	12.63	18	20454	12609	64465651
Aspartate aminotransferase increased	12.67	12.63	73	20399	119715	64358545

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C10AB04	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Fibrates
FDA CS	M0199111	PPAR alpha
FDA MoA	N0000175375	Peroxisome Proliferator-activated Receptor alpha Agonists
FDA EPC	N0000175596	Peroxisome Proliferator Receptor alpha Agonist
CHEBI has role	CHEBI:35679	antilipemic drugs
MeSH PA	D000963	Antimetabolites
MeSH PA	D065687	Cytochrome P-450 CYP2C8 Inhibitors
MeSH PA	D065607	Cytochrome P-450 Enzyme Inhibitors
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D000960	Hypolipidemic Agents
MeSH PA	D057847	Lipid Regulating Agents
MeSH PA	D065606	Metabolic Side Effects of Drugs and Substances

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Hypertriglyceridemia	indication	302870006
Primary Prevention of Coronary Heart Disease	indication
Hypoalphalipoproteinemia	off-label use	190785000
Primary biliary cirrhosis	contraindication	31712002	DOID:12236
Disorder of gallbladder	contraindication	39621005	DOID:0060262
Acute nephropathy	contraindication	58574008
Leukopenia	contraindication	84828003	DOID:615
Impaired renal function disorder	contraindication	197663003
Disease of liver	contraindication	235856003	DOID:409
Calculus in biliary tract	contraindication	266474003
Anemia	contraindication	271737000	DOID:2355
Thrombocytopenic disorder	contraindication	302215000	DOID:1588
Breastfeeding (mother)	contraindication	413712001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	5.13	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
Peroxisome proliferator-activated receptor alpha	Nuclear hormone receptor	Q07869	PPARA_HUMAN	AGONIST	EC50	4.23	IUPHAR	CHEMBL
Transthyretin	Secreted	P02766	TTHY_HUMAN		Kd	7	CHEMBL
Cytochrome P450 2C8	Enzyme	P10632	CP2C8_HUMAN		Ki	5.74	WOMBAT-PK
Lipoprotein lipase	Enzyme	P06858	LIPL_HUMAN				WOMBAT-PK
CDGSH iron-sulfur domain-containing protein 1	Unclassified	Q9NZ45	CISD1_HUMAN		Ki	5.14	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		Ki	4.52	WOMBAT-PK
Fatty acid-binding protein, liver	Unclassified		FABPL_RAT		Ki	5.73	CHEMBL

External reference:

ID	Source
4018639	VUID
N0000146952	NUI
D00334	KEGG_DRUG
4018639	VANDF
C0017245	UMLSCUI
CHEBI:5296	CHEBI
4TX	PDB_CHEM_ID
CHEMBL457	ChEMBL_ID
DB01241	DRUGBANK_ID
D015248	MESH_DESCRIPTOR_UI
3463	PUBCHEM_CID
3439	IUPHAR_LIGAND_ID
3899	INN_ID
Q8X02027X3	UNII
4719	RXNORM
4778	MMSL
523	MMSL
d00245	MMSL
002050	NDDF
35282000	SNOMEDCT_US
387189002	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Lopid	HUMAN PRESCRIPTION DRUG LABEL	1	0071-0737	TABLET, FILM COATED	600 mg	ORAL	NDA	18 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9130	TABLET, FILM COATED	600 mg	ORAL	ANDA	17 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	0143-9707	TABLET, FILM COATED	600 mg	ORAL	ANDA	18 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	0615-8354	TABLET, FILM COATED	600 mg	ORAL	ANDA	15 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	10544-569	TABLET, FILM COATED	600 mg	ORAL	ANDA	18 sections
Gemfibrozil	Human Prescription Drug Label	1	16571-784	TABLET, FILM COATED	600 mg	ORAL	ANDA	15 sections
Gemfibrozil	Human Prescription Drug Label	1	16714-101	TABLET	600 mg	ORAL	ANDA	18 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	21695-732	TABLET, FILM COATED	600 mg	ORAL	ANDA	17 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	24658-260	TABLET, FILM COATED	600 mg	ORAL	ANDA	17 sections
GEMFIBROZIL	HUMAN PRESCRIPTION DRUG LABEL	1	31722-128	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	31722-225	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	33261-146	TABLET, FILM COATED	600 mg	ORAL	ANDA	17 sections
GEMFIBROZIL	HUMAN PRESCRIPTION DRUG LABEL	1	42806-260	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	43063-745	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	43063-745	TABLET	600 mg	ORAL	ANDA	11 sections
GEMFIBROZIL	HUMAN PRESCRIPTION DRUG LABEL	1	43063-921	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	43353-090	TABLET, FILM COATED	600 mg	ORAL	ANDA	18 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	43353-772	TABLET, FILM COATED	600 mg	ORAL	ANDA	21 sections
GEMFIBROZIL	HUMAN PRESCRIPTION DRUG LABEL	1	43602-452	TABLET	600 mg	ORAL	ANDA	10 sections
Gemfibrozil	Human Prescription Drug Label	1	50090-2450	TABLET, FILM COATED	600 mg	ORAL	ANDA	15 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	50090-2902	TABLET	600 mg	ORAL	ANDA	11 sections
GEMFIBROZIL	HUMAN PRESCRIPTION DRUG LABEL	1	50090-5808	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	50268-350	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	51138-588	TABLET, FILM COATED	600 mg	ORAL	ANDA	18 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	51655-142	TABLET	600 mg	ORAL	ANDA	9 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	51655-143	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	53002-1068	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	Human Prescription Drug Label	1	53002-2068	TABLET, FILM COATED	600 mg	ORAL	ANDA	15 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	53217-251	TABLET	600 mg	ORAL	ANDA	11 sections
Gemfibrozil	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0251	TABLET, FILM COATED	600 mg	ORAL	ANDA	17 sections