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	350.04	27.44	205	5870	124114	50474935
Low density lipoprotein increased	331.80	27.44	86	5989	5560	50593489
Wrong technique in device usage process	280.19	27.44	64	6011	2422	50596627
Device operational issue	239.85	27.44	39	6036	217	50598832
Injury associated with device	225.10	27.44	56	6019	3061	50595988
Drug dose omission by device	207.54	27.44	51	6024	2648	50596401
Device issue	199.99	27.44	79	5996	19893	50579156
Device use issue	187.26	27.44	44	6031	1885	50597164
Influenza like illness	172.33	27.44	99	5976	57360	50541689
Product dose omission issue	170.67	27.44	155	5920	183683	50415366
Injection site bruising	168.41	27.44	84	5991	36684	50562365
Product administered at inappropriate site	157.04	27.44	40	6035	2403	50596646
Injection site pain	136.27	27.44	110	5965	110914	50488135
Injection site erythema	122.20	27.44	88	5987	74848	50524201
Muscle spasms	118.49	27.44	107	5968	125446	50473603
Injection site rash	117.81	27.44	51	6024	16126	50582923
Injection site pruritus	91.00	27.44	58	6017	40353	50558696
Injection site swelling	77.17	27.44	53	6022	41720	50557329
Injection site haemorrhage	61.79	27.44	36	6039	21310	50577739
Rhinorrhoea	60.79	27.44	50	6025	51533	50547516
Device defective	58.32	27.44	16	6059	1279	50597770
Pruritus	55.93	27.44	112	5963	283456	50315593
Incorrect dose administered by device	50.21	27.44	18	6057	3457	50595592
Injection site reaction	49.75	27.44	44	6031	49988	50549061
Low density lipoprotein decreased	49.27	27.44	10	6065	213	50598836
Rash	45.54	27.44	135	5940	437336	50161713
Blood triglycerides increased	40.66	27.44	22	6053	11290	50587759
Therapeutic response decreased	40.05	27.44	38	6037	47193	50551856
Underdose	38.06	27.44	26	6049	20252	50578797
Pain in extremity	35.02	27.44	91	5984	272774	50326275
Arthralgia	32.71	27.44	121	5954	438581	50160468
Device difficult to use	29.46	27.44	17	6058	9869	50589180
Device malfunction	27.46	27.44	19	6056	15102	50583947

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	355.38	31.14	186	4188	73833	29496320
Low density lipoprotein increased	191.97	31.14	54	4320	3850	29566303
Influenza like illness	156.55	31.14	75	4299	24395	29545758
Drug dose omission by device	140.24	31.14	33	4341	1149	29569004
Wrong technique in device usage process	106.52	31.14	26	4348	1059	29569094
Muscle spasms	106.06	31.14	83	4291	64999	29505154
Device issue	96.20	31.14	38	4336	7742	29562411
Low density lipoprotein decreased	87.82	31.14	22	4352	998	29569155
Injury associated with device	86.64	31.14	21	4353	830	29569323
Device operational issue	76.78	31.14	14	4360	131	29570022
Fractional exhaled nitric oxide increased	74.68	31.14	16	4358	360	29569793
Product dose omission issue	74.49	31.14	81	4293	96302	29473851
Injection site bruising	69.82	31.14	30	4344	7550	29562603
Secretion discharge	57.10	31.14	22	4352	4188	29565965
Plantar fasciitis	55.20	31.14	16	4358	1265	29568888
Injection site erythema	55.15	31.14	31	4343	13925	29556228
Rhinorrhoea	52.22	31.14	35	4339	21484	29548669
Sensation of foreign body	49.92	31.14	16	4358	1774	29568379
Injection site pain	49.76	31.14	40	4334	32406	29537747
Myoglobin blood increased	48.21	31.14	16	4358	1979	29568174
Injection site pruritus	46.89	31.14	21	4353	5828	29564325
Injection site swelling	45.77	31.14	24	4350	9393	29560760
Pruritus	44.12	31.14	69	4305	116780	29453373
Arthralgia	44.04	31.14	76	4298	139541	29430612
Blood triglycerides increased	44.01	31.14	26	4348	12808	29557345
Brain natriuretic peptide increased	39.79	31.14	17	4357	4213	29565940
Product administered at inappropriate site	38.41	31.14	13	4361	1707	29568446
Nasopharyngitis	37.29	31.14	45	4329	59620	29510533
Injection site reaction	36.63	31.14	22	4352	11166	29558987
Device use issue	35.12	31.14	8	4366	240	29569913
Device defective	34.61	31.14	9	4365	474	29569679
Muscular weakness	31.18	31.14	42	4332	62010	29508143

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	512.00	25.45	292	7943	158325	64332172
Wrong technique in device usage process	345.91	25.45	79	8156	2803	64487694
Low density lipoprotein increased	331.14	25.45	93	8142	7647	64482850
Drug dose omission by device	280.31	25.45	69	8166	3388	64487109
Device operational issue	273	25.45	46	8189	306	64490191
Injury associated with device	262.24	25.45	63	8172	2790	64487707
Device issue	254.25	25.45	99	8136	22549	64467948
Influenza like illness	220.95	25.45	122	8113	61580	64428917
Product dose omission issue	212.71	25.45	185	8050	194562	64295935
Injection site bruising	199.92	25.45	96	8139	36277	64454220
Device use issue	192.01	25.45	45	8190	1788	64488709
Product administered at inappropriate site	163.66	25.45	44	8191	3066	64487431
Injection site pain	152.96	25.45	121	8114	111287	64379210
Muscle spasms	128.17	25.45	121	8114	140902	64349595
Injection site erythema	117.14	25.45	86	8149	70714	64419783
Injection site rash	106.45	25.45	48	8187	15694	64474803
Injection site pruritus	96.19	25.45	60	8175	37766	64452731
Rhinorrhoea	90.59	25.45	69	8166	59900	64430597
Low density lipoprotein decreased	79.52	25.45	20	8215	1070	64489427
Injection site swelling	79.32	25.45	55	8180	41298	64449199
Injection site haemorrhage	70.66	25.45	42	8193	24236	64466261
Arthralgia	68.04	25.45	164	8071	442096	64048401
Pruritus	63.98	25.45	130	8105	312270	64178227
Device defective	57.49	25.45	16	8219	1267	64489230
Incorrect dose administered by device	57.09	25.45	21	8214	4076	64486421
Pain in extremity	51.52	25.45	117	8118	302968	64187529
Rash	46.43	25.45	146	8089	458403	64032094
Blood triglycerides increased	45.61	25.45	29	8206	18837	64471660
Back pain	42.95	25.45	97	8138	250074	64240423
Injection site reaction	42.20	25.45	40	8195	46624	64443873
Therapeutic response decreased	40.23	25.45	41	8194	52147	64438350
Myocardial infarction	39.95	25.45	74	8161	165747	64324750
Underdose	37.39	25.45	29	8206	25800	64464697
Low density lipoprotein abnormal	34.41	25.45	8	8227	306	64490191
Device difficult to use	33.96	25.45	19	8216	9779	64480718
Injection site mass	30.84	25.45	22	8213	17248	64473249
Device malfunction	30.43	25.45	22	8213	17611	64472886
Anaemia	29.94	25.45	6	8229	378674	64111823
Injection site warmth	28.39	25.45	19	8216	13443	64477054
Muscular weakness	28.38	25.45	55	8180	127283	64363214
Blood creatine phosphokinase increased	28.11	25.45	36	8199	58522	64431975
Off label use	27.86	25.45	24	8211	632782	63857715
Blood cholesterol increased	27.60	25.45	33	8202	50033	64440464
Incorrect dose administered	25.53	25.45	35	8200	60730	64429767

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
9620	INN_ID
DB09302	DRUGBANK_ID
PP0SHH6V16	UNII
1659152	RXNORM
31129	MMSL
d08374	MMSL
715186005	SNOMEDCT_US
781355008	SNOMEDCT_US
C3491162	UMLSCUI
016342	NDDF

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