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

Stem definitionDrug idCAS RN
human origin 5016 1245916-14-6

Description:

MoleculeDescription

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:

DoseUnitRoute
5.40 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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 termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients 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:

SourceCodeDescription
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)

DiseaseRelationSNOMED_IDDOID
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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Proprotein convertase subtilisin/kexin type 9 Enzyme INHIBITOR Kd 9.42 IUPHAR DRUG LABEL

External reference:

IDSource
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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