alirocumab 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
Low density lipoprotein increased	354.02	31.82	91	5919	6075	53336981
Myalgia	345.98	31.82	204	5806	133287	53209769
Wrong technique in device usage process	281.71	31.82	64	5946	2523	53340533
Device operational issue	243.10	31.82	39	5971	212	53342844
Injury associated with device	221.87	31.82	55	5955	3160	53339896
Drug dose omission by device	214.06	31.82	51	5959	2478	53340578
Device issue	198.65	31.82	79	5931	21579	53321477
Device use issue	189.89	31.82	44	5966	1892	53341164
Injection site bruising	171.60	31.82	84	5926	37562	53305494
Influenza like illness	170.22	31.82	98	5912	60761	53282295
Product dose omission issue	169.67	31.82	153	5857	191467	53151589
Product administered at inappropriate site	156.76	31.82	40	5970	2582	53340474
Injection site pain	140.40	31.82	110	5900	113281	53229775
Injection site erythema	124.84	31.82	88	5922	77161	53265895
Injection site rash	119.73	31.82	51	5959	16528	53326528
Muscle spasms	115.85	31.82	106	5904	134689	53208367
Injection site pruritus	92.85	31.82	58	5952	41531	53301525
Injection site swelling	76.86	31.82	52	5958	42576	53300480
Injection site haemorrhage	62.83	31.82	36	5974	22015	53321041
Rhinorrhoea	61.91	31.82	50	5960	53528	53289528
Device defective	58.89	31.82	16	5994	1315	53341741
Pruritus	56.92	31.82	111	5899	293721	53049335
Injection site reaction	51.32	31.82	44	5966	51122	53291934
Incorrect dose administered by device	51.00	31.82	18	5992	3521	53339535
Low density lipoprotein decreased	49.72	31.82	10	6000	217	53342839
Rash	48.25	31.82	134	5876	446057	52896999
Therapeutic response decreased	41.88	31.82	38	5972	47531	53295525
Blood triglycerides increased	40.01	31.82	22	5988	12419	53330637
Underdose	38.16	31.82	26	5984	21496	53321560
Pain in extremity	36.19	31.82	91	5919	284959	53058097
Arthralgia	36.12	31.82	120	5890	439663	52903393

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	372.35	29.02	186	3801	81044	32428495
Low density lipoprotein increased	202.19	29.02	55	3932	4191	32505348
Influenza like illness	162.61	29.02	75	3912	27065	32482474
Drug dose omission by device	152.50	29.02	33	3954	949	32508590
Wrong technique in device usage process	107.53	29.02	26	3961	1233	32508306
Device issue	98.12	29.02	38	3949	8874	32500665
Low density lipoprotein decreased	91.23	29.02	22	3965	1031	32508508
Injury associated with device	90.00	29.02	21	3966	853	32508686
Product dose omission issue	81.16	29.02	80	3907	102495	32407044
Device operational issue	79.02	29.02	14	3973	135	32509404
Muscle spasms	75.24	29.02	65	3922	70353	32439186
Injection site bruising	74.36	29.02	30	3957	7790	32501749
Injection site erythema	59.16	29.02	31	3956	14637	32494902
Rhinorrhoea	56.12	29.02	35	3952	22951	32486588
Injection site pain	55.79	29.02	40	3947	33018	32476521
Arthralgia	49.80	29.02	75	3912	148373	32361166
Injection site swelling	46.64	29.02	23	3964	9561	32499978
Injection site pruritus	46.55	29.02	20	3967	6070	32503469
Pruritus	45.98	29.02	67	3920	128635	32380904
Blood triglycerides increased	42.74	29.02	25	3962	14594	32494945
Product administered at inappropriate site	40.23	29.02	13	3974	1786	32507753
Injection site reaction	39.78	29.02	22	3965	11547	32497992
Blood cholesterol increased	38.26	29.02	25	3962	17732	32491807
Device defective	36.56	29.02	9	3978	459	32509080
Pain in extremity	35.52	29.02	57	3930	118844	32390695
Device use issue	35.34	29.02	8	3979	283	32509256
Muscular weakness	34.42	29.02	42	3945	67887	32441652
Product use issue	34.10	29.02	37	3950	52740	32456799
Back pain	32.84	29.02	53	3934	111000	32398539
Rash	31.39	29.02	75	3912	209258	32300281
Injection site rash	31.02	29.02	13	3974	3707	32505832

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 (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

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
016342	NDDF
715186005	SNOMEDCT_US
781355008	SNOMEDCT_US
C3491162	UMLSCUI

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