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

Stem definition	Drug id	CAS RN
human origin	5016	1245916-14-6

Description:

Molecule	Description
Synonyms: alirocumab praluent REGN727 SAR236553	antibody to PCSK9 to manage LDL cholesterol Molecular weight: Formula: CLOGP: LIPINSKI: None HAC: None HDO: None TPSA: ALOGS: ROTB: None

Molecule

Description

Synonyms:

alirocumab
praluent
REGN727
SAR236553

antibody to PCSK9 to manage LDL cholesterol

Molecular weight:
Formula:
CLOGP:
LIPINSKI: None
HAC: None
HDO: None
TPSA:
ALOGS:
ROTB: None

Drug dosage:

Dose	Unit	Route
5.40	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company
July 23, 2015	EMA
July 24, 2015	FDA	SANOFI AVENTIS
July 4, 2016	PMDA	Sanofi K.K.

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	390.40	26.82	224	6576	146305	63335917
Low density lipoprotein increased	341.08	26.82	88	6712	6269	63475953
Wrong technique in device usage process	274.16	26.82	66	6734	3532	63478690
Device operational issue	239.96	26.82	39	6761	247	63481975
Injury associated with device	227.37	26.82	57	6743	3609	63478613
Device issue	195.31	26.82	79	6721	23702	63458520
Influenza like illness	193.02	26.82	108	6692	66716	63415506
Drug dose omission by device	184.15	26.82	51	6749	4750	63477472
Product dose omission issue	179.95	26.82	169	6631	234144	63248078
Device use issue	178.67	26.82	44	6756	2586	63479636
Injection site bruising	175.89	26.82	87	6713	41823	63440399
Injection site pain	157.75	26.82	122	6678	129678	63352544
Product administered at inappropriate site	156.28	26.82	41	6759	3108	63479114
Injection site rash	142.51	26.82	59	6741	18750	63463472
Injection site erythema	132.22	26.82	92	6708	83082	63399140
Muscle spasms	124.17	26.82	115	6685	156035	63326187
Injection site pruritus	96.20	26.82	60	6740	45056	63437166
Injection site swelling	81.13	26.82	55	6745	47517	63434705
Injection site haemorrhage	61.24	26.82	36	6764	24278	63457944
Rhinorrhoea	59.28	26.82	52	6748	65525	63416697
Low density lipoprotein decreased	55.50	26.82	11	6789	233	63481989
Pruritus	53.82	26.82	119	6681	361334	63120888
Device defective	53.55	26.82	16	6784	1946	63480276
Product delivery mechanism issue	50.88	26.82	11	6789	361	63481861
Incorrect dose administered by device	48.27	26.82	18	6782	4330	63477892
Injection site reaction	48.12	26.82	44	6756	58480	63423742
Pain in extremity	46.92	26.82	107	6693	331379	63150843
Blood triglycerides increased	46.67	26.82	24	6776	12464	63469758
Rash	39.00	26.82	140	6660	560731	62921491
Therapeutic response decreased	37.01	26.82	39	6761	61486	63420736
Underdose	33.65	26.82	26	6774	27430	63454792
Arthralgia	32.03	26.82	133	6667	569577	62912645
Injection site mass	30.42	26.82	21	6779	18635	63463587
Device difficult to use	27.20	26.82	17	6783	12779	63469443

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	343.86	31.36	194	5285	83916	34867536
Fractional exhaled nitric oxide increased	200.92	31.36	44	5435	1038	34950414
Low density lipoprotein increased	190.75	31.36	56	5423	4380	34947072
Plantar fasciitis	171.57	31.36	44	5435	2072	34949380
Sensation of foreign body	159.62	31.36	44	5435	2739	34948713
Myoglobin blood increased	156.02	31.36	44	5435	2979	34948473
Muscle spasms	155.43	31.36	113	5366	74888	34876564
Influenza like illness	149.42	31.36	77	5402	27557	34923895
Secretion discharge	134.79	31.36	46	5433	5859	34945593
Brain natriuretic peptide increased	132.76	31.36	45	5434	5614	34945838
Drug dose omission by device	117.39	31.36	33	5446	2206	34949246
Exostosis	96.96	31.36	34	5445	4689	34946763
Wrong technique in device usage process	96.44	31.36	26	5453	1486	34949966
Obstructive airways disorder	91.91	31.36	46	5433	15448	34936004
Dysphonia	89.81	31.36	52	5427	23331	34928121
Low density lipoprotein decreased	88.89	31.36	23	5456	1120	34950332
Device issue	85.66	31.36	38	5441	9739	34941713
Injury associated with device	79.63	31.36	21	5458	1102	34950350
Coronary artery disease	78.34	31.36	63	5416	48242	34903210
Cardiac disorder	78.02	31.36	60	5419	43066	34908386
Nasopharyngitis	76.70	31.36	73	5406	69895	34881557
Device operational issue	73.50	31.36	14	5465	159	34951293
Injection site bruising	67.41	31.36	31	5448	8632	34942820
Wheezing	67.11	31.36	54	5425	41348	34910104
Product dose omission issue	65.65	31.36	87	5392	119624	34831828
Eosinophilia	64.57	31.36	44	5435	26178	34925274
Dyspnoea exertional	62.94	31.36	53	5426	43226	34908226
Chest discomfort	61.83	31.36	58	5421	54472	34896980
Injection site erythema	54.83	31.36	33	5446	15866	34935586
Injection site pruritus	54.36	31.36	25	5454	6958	34944494
Cough	51.98	31.36	88	5391	150052	34801400
Rhinorrhoea	49.22	31.36	37	5442	25631	34925821
Low density lipoprotein abnormal	47.28	31.36	11	5468	342	34951110
Injection site pain	47.12	31.36	43	5436	38962	34912490
Injection site swelling	42.54	31.36	25	5454	11502	34939950
Pruritus	42.37	31.36	78	5401	141903	34809549
Blood triglycerides increased	40.26	31.36	26	5453	14133	34937319
Pneumothorax	37.66	31.36	28	5451	19064	34932388
Arthralgia	37.09	31.36	82	5397	169959	34781493
Product administered at inappropriate site	34.34	31.36	13	5466	2223	34949229
Injection site reaction	32.37	31.36	22	5457	13011	34938441
Myocardial infarction	31.75	31.36	63	5416	121022	34830430
Device use issue	31.39	31.36	9	5470	645	34950807

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	561.87	25.10	314	8685	185327	79550062
Low density lipoprotein increased	332.53	25.10	93	8906	8529	79726860
Wrong technique in device usage process	329.27	25.10	79	8920	3949	79731440
Device operational issue	273.72	25.10	46	8953	346	79735043
Injury associated with device	257.05	25.10	63	8936	3443	79731946
Device issue	248.80	25.10	99	8900	27009	79708380
Drug dose omission by device	248.21	25.10	69	8930	6181	79729208
Influenza like illness	228.79	25.10	126	8873	71581	79663808
Product dose omission issue	201.74	25.10	189	8810	247348	79488041
Injection site bruising	200.21	25.10	96	8903	40906	79694483
Device use issue	178.83	25.10	45	8954	2739	79732650
Injection site pain	160.46	25.10	126	8873	129712	79605677
Product administered at inappropriate site	158.44	25.10	44	8955	3921	79731468
Muscle spasms	129.92	25.10	127	8872	174603	79560786
Injection site erythema	128.20	25.10	90	8909	78107	79657282
Injection site rash	112.45	25.10	50	8949	17904	79717485
Injection site pruritus	104.53	25.10	63	8936	42220	79693169
Rhinorrhoea	87.80	25.10	71	8928	76003	79659386
Injection site swelling	86.05	25.10	58	8941	47074	79688315
Low density lipoprotein decreased	79.72	25.10	20	8979	1201	79734188
Injection site haemorrhage	70.09	25.10	42	8957	27828	79707561
Pruritus	66.56	25.10	141	8858	394507	79340882
Arthralgia	65.82	25.10	176	8823	571627	79163762
Pain in extremity	62.32	25.10	131	8868	364407	79370982
Low density lipoprotein abnormal	58.89	25.10	13	8986	446	79734943
Incorrect dose administered by device	55.59	25.10	21	8978	4968	79730421
Myocardial infarction	54.34	25.10	84	8915	184045	79551344
Device defective	53.06	25.10	16	8983	1904	79733485
Blood triglycerides increased	51.07	25.10	31	8968	21009	79714380
Rash	43.05	25.10	153	8846	578205	79157184
Back pain	41.49	25.10	100	8899	304080	79431309
Injection site reaction	40.93	25.10	40	8959	54745	79680644
Off label use	38.39	25.10	28	8971	907187	78828202
Therapeutic response decreased	37.72	25.10	42	8957	66811	79668578
Injection site mass	37.20	25.10	25	8974	20159	79715230
Blood creatine phosphokinase increased	36.40	25.10	41	8958	66049	79669340
Underdose	36.24	25.10	30	8969	33121	79702268
Device difficult to use	35.81	25.10	21	8978	13364	79722025
High density lipoprotein decreased	29.25	25.10	13	8986	4642	79730747
Device malfunction	29.00	25.10	22	8977	21426	79713963
Injection site warmth	28.88	25.10	19	8980	14788	79720601
Anaemia	27.62	25.10	8	8991	445007	79290382
Unevaluable event	26.46	25.10	32	8967	55553	79679836
Muscular weakness	25.35	25.10	56	8943	160673	79574716

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C10AX14	CARDIOVASCULAR SYSTEM LIPID MODIFYING AGENTS LIPID MODIFYING AGENTS, PLAIN Other lipid modifying agents
FDA CS	M0001357	Antibodies, Monoclonal
MeSH PA	D000924	Anticholesteremic Agents
MeSH PA	D000963	Antimetabolites
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D000960	Hypolipidemic Agents
MeSH PA	D057847	Lipid Regulating Agents
MeSH PA	D000091362	PCSK9 Inhibitors
MeSH PA	D011480	Protease Inhibitors
MeSH PA	D015842	Serine Proteinase Inhibitors
FDA MoA	N0000191730	PCSK9 Inhibitors
FDA EPC	N0000191731	PCSK9 Inhibitor

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

Disease	Relation	SNOMED_ID	DOID
Hypercholesterolemia	indication	13644009
Atherosclerosis	indication	38716007	DOID:1936
Familial hypercholesterolemia - heterozygous	indication	238079002
Complex dyslipidemia	indication	109041000119107

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

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
Proprotein convertase subtilisin/kexin type 9	Enzyme	Q8NBP7	PCSK9_HUMAN	INHIBITOR	Kd	9.42		IUPHAR	DRUG LABEL

External reference:

ID	Source
D10335	KEGG_DRUG
4034685	VUID
N0000191810	NUI
4034685	VANDF
CHEMBL2109540	ChEMBL_ID
C571059	MESH_SUPPLEMENTAL_RECORD_UI
6744	IUPHAR_LIGAND_ID
DB09302	DRUGBANK_ID
1659152	RXNORM
31129	MMSL
d08374	MMSL
016342	NDDF
715186005	SNOMEDCT_US
781355008	SNOMEDCT_US
C3491162	UMLSCUI
9620	INN_ID
PP0SHH6V16	UNII

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5901	INJECTION, SOLUTION	75 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5902	INJECTION, SOLUTION	150 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5903	INJECTION, SOLUTION	75 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	0024-5904	INJECTION, SOLUTION	150 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	61755-020	INJECTION, SOLUTION	75 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	61755-021	INJECTION, SOLUTION	150 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	72733-5901	INJECTION, SOLUTION	75 mg	SUBCUTANEOUS	BLA	33 sections
Praluent	HUMAN PRESCRIPTION DRUG LABEL	1	72733-5902	INJECTION, SOLUTION	150 mg	SUBCUTANEOUS	BLA	33 sections