alirocumab 🐶 Veterinary Use | 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
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 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 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 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 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:

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

DiseaseRelationSNOMED_IDDOID
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:

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
715186005 SNOMEDCT_US
781355008 SNOMEDCT_US
C3491162 UMLSCUI
016342 NDDF

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