alirocumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

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 461.65 24.61 253 8140 174872 90445182
Low density lipoprotein increased 366.39 24.61 95 8298 7990 90612064
Wrong technique in device usage process 256.76 24.61 67 8326 5768 90614286
Injury associated with device 244.28 24.61 61 8332 4403 90615651
Influenza like illness 244.08 24.61 128 8265 80483 90539571
Injection site bruising 239.01 24.61 110 8283 52197 90567857
Device issue 199.95 24.61 82 8311 29455 90590599
Product administered at inappropriate site 198.82 24.61 51 8342 4100 90615954
Injection site pain 197.58 24.61 148 8245 173551 90446503
Device operational issue 196.47 24.61 39 8354 971 90619083
Product dose omission issue 174.68 24.61 172 8221 291515 90328539
Injection site erythema 171.11 24.61 109 8284 98393 90521661
Drug dose omission by device 165.43 24.61 54 8339 10177 90609877
Device use issue 165.09 24.61 43 8350 3670 90616384
Injection site rash 146.37 24.61 62 8331 24111 90595943
Product delivery mechanism issue 144.19 24.61 27 8366 489 90619565
Injection site pruritus 136.33 24.61 76 8317 53758 90566296
Injection site swelling 110.79 24.61 69 8324 59770 90560284
Muscle spasms 98.79 24.61 119 8274 251764 90368290
Injection site haemorrhage 88.50 24.61 46 8347 28272 90591782
Product preparation error 74.57 24.61 30 8363 10231 90609823
Rhinorrhoea 60.05 24.61 56 8337 88260 90531794
Blood triglycerides increased 56.76 24.61 27 8366 13734 90606320
Injection site reaction 56.18 24.61 55 8338 92025 90528029
Low density lipoprotein decreased 55.78 24.61 11 8382 264 90619790
Incorrect dose administered by device 49.51 24.61 19 8374 5718 90614336
Pruritus 48.27 24.61 134 8259 541391 90078663
Myocardial infarction 48.01 24.61 54 8339 105918 90514136
Device defective 46.79 24.61 16 8377 3470 90616584
Pain in extremity 45.71 24.61 117 8276 450412 90169642
Injection site mass 44.75 24.61 27 8366 22063 90597991
Device difficult to use 42.30 24.61 24 8369 17501 90602553
Arthralgia 36.15 24.61 155 8238 778367 89841687
Rash 35.82 24.61 157 8236 795943 89824111
Therapeutic response decreased 34.43 24.61 42 8351 89687 90530367
Injection site induration 32.68 24.61 17 8376 10451 90609603
Product storage error 31.64 24.61 21 8372 20220 90599834
Injection site warmth 29.39 24.61 19 8374 17496 90602558
Off label use 28.82 24.61 36 8357 1102216 89517838
Therapy cessation 28.51 24.61 25 8368 36336 90583718
Injection site urticaria 26.50 24.61 18 8375 17993 90602061
Device malfunction 26.29 24.61 19 8374 20958 90599096
Skin pressure mark 24.96 24.61 4 8389 27 90620027

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 383.44 28.35 224 6968 95856 42518287
Fractional exhaled nitric oxide increased 269.82 28.35 61 7131 1548 42612595
Plantar fasciitis 230.66 28.35 61 7131 3009 42611134
Myoglobin blood increased 224.27 28.35 62 7130 3620 42610523
Sensation of foreign body 216.21 28.35 60 7132 3553 42610590
Low density lipoprotein increased 197.10 28.35 61 7131 5294 42608849
Brain natriuretic peptide increased 187.03 28.35 62 7130 6708 42607435
Muscle spasms 186.07 28.35 137 7055 85907 42528236
Exostosis 157.25 28.35 52 7140 5579 42608564
Influenza like illness 147.26 28.35 82 7110 31758 42582385
Secretion discharge 141.76 28.35 52 7140 7583 42606560
Dysphonia 122.68 28.35 70 7122 28380 42585763
Coronary artery disease 112.48 28.35 84 7108 53636 42560507
Obstructive airways disorder 112.36 28.35 63 7129 24696 42589447
Cardiac disorder 110.30 28.35 80 7112 48852 42565291
Nasopharyngitis 94.67 28.35 92 7100 83904 42530239
Eosinophilia 93.39 28.35 62 7130 32837 42581306
Low density lipoprotein decreased 88.87 28.35 24 7168 1280 42612863
Drug dose omission by device 87.20 28.35 34 7158 5852 42608291
Dyspnoea exertional 86.63 28.35 70 7122 50078 42564065
Wheezing 85.31 28.35 72 7120 54709 42559434
Chest discomfort 83.78 28.35 76 7116 63540 42550603
Wrong technique in device usage process 83.16 28.35 27 7165 2730 42611413
Pneumothorax 78.22 28.35 49 7143 23494 42590649
Injection site bruising 74.02 28.35 37 7155 11488 42602655
Injury associated with device 73.55 28.35 21 7171 1376 42612767
Increased upper airway secretion 72.93 28.35 24 7168 2532 42611611
Device issue 71.29 28.35 38 7154 13471 42600672
Device operational issue 66.30 28.35 14 7178 255 42613888
Cough 61.92 28.35 109 7083 177994 42436149
Injection site pain 55.32 28.35 58 7134 57740 42556403
Injection site erythema 54.73 28.35 37 7155 20158 42593985
Product dose omission issue 51.72 28.35 93 7099 154272 42459871
Foreign body in throat 51.21 28.35 13 7179 543 42613600
Blood creatine phosphokinase increased 50.77 28.35 51 7141 48287 42565856
Injection site swelling 50.59 28.35 33 7159 16940 42597203
Low density lipoprotein abnormal 49.92 28.35 12 7180 399 42613744
Rhinorrhoea 45.81 28.35 40 7152 31754 42582389
Injection site pruritus 45.55 28.35 25 7167 9380 42604763
Arthralgia 44.22 28.35 103 7089 205135 42409008
Product delivery mechanism issue 44.11 28.35 10 7182 256 42613887
Myocardial infarction 43.16 28.35 76 7116 123933 42490210
Blood triglycerides increased 42.77 28.35 29 7163 15867 42598276
Product administered at inappropriate site 42.73 28.35 17 7175 3081 42611062
Off label use 41.10 28.35 29 7163 638306 41975837
Pruritus 38.76 28.35 93 7099 188678 42425465
Injection site reaction 38.34 28.35 27 7165 15694 42598449
Atrial fibrillation 37.96 28.35 77 7115 139516 42474627
Acute kidney injury 37.81 28.35 8 7184 367329 42246814
High density lipoprotein decreased 32.58 28.35 15 7177 3882 42610261
Anaemia 31.19 28.35 5 7187 280273 42333870
Bronchospasm 31.12 28.35 22 7170 12863 42601280

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 653.94 22.19 363 11502 222018 110355416
Low density lipoprotein increased 339.65 22.19 98 11767 10568 110566866
Wrong technique in device usage process 290.93 22.19 79 11786 6822 110570612
Injury associated with device 246.10 22.19 63 11802 4326 110573108
Influenza like illness 244.37 22.19 139 11726 88273 110489161
Device issue 230.34 22.19 99 11766 34436 110542998
Device operational issue 227.31 22.19 46 11819 1086 110576348
Drug dose omission by device 209.64 22.19 73 11792 14443 110562991
Injection site bruising 204.69 22.19 103 11762 51160 110526274
Product dose omission issue 173.02 22.19 192 11673 321590 110255844
Device use issue 162.65 22.19 44 11821 3740 110573694
Injection site pain 152.69 22.19 137 11728 177785 110399649
Product administered at inappropriate site 151.58 22.19 45 11820 5348 110572086
Muscle spasms 144.34 22.19 163 11702 277994 110299440
Injection site erythema 135.09 22.19 98 11767 94078 110483356
Fractional exhaled nitric oxide increased 135.02 22.19 28 11837 748 110576686
Injection site rash 108.17 22.19 52 11813 23367 110554067
Injection site pruritus 106.16 22.19 67 11798 51191 110526243
Myocardial infarction 100.26 22.19 113 11752 191970 110385464
Myoglobin blood increased 92.04 22.19 29 11836 4203 110573231
Injection site swelling 90.16 22.19 65 11800 61725 110515709
Plantar fasciitis 86.71 22.19 29 11836 5072 110572362
Low density lipoprotein decreased 82.59 22.19 21 11844 1401 110576033
Rhinorrhoea 80.06 22.19 75 11790 102591 110474843
Sensation of foreign body 70.55 22.19 28 11837 7947 110569487
Increased upper airway secretion 70.49 22.19 25 11840 5207 110572227
Arthralgia 69.51 22.19 212 11653 779420 109798014
Coronary artery disease 69.01 22.19 59 11806 71631 110505803
Blood creatine phosphokinase increased 68.03 22.19 59 11806 73018 110504416
Injection site haemorrhage 67.94 22.19 43 11822 32985 110544449
Brain natriuretic peptide increased 67.74 22.19 30 11835 11179 110566255
Blood triglycerides increased 61.68 22.19 36 11829 23890 110553544
Pruritus 58.30 22.19 165 11700 581395 109996039
Off label use 57.90 22.19 46 11819 1500139 109077295
Pain in extremity 57.66 22.19 147 11718 486971 110090463
Low density lipoprotein abnormal 56.85 22.19 13 11852 552 110576882
Incorrect dose administered by device 53.65 22.19 22 11843 6792 110570642
Foreign body in throat 48.69 22.19 13 11852 1050 110576384
Device difficult to use 47.70 22.19 28 11837 18777 110558657
Back pain 45.99 22.19 114 11751 370882 110206552
Device defective 43.05 22.19 16 11849 3806 110573628
Dysphonia 41.84 22.19 46 11819 75883 110501551
Cardiac disorder 41.66 22.19 46 11819 76234 110501200
Toxicity to various agents 40.13 22.19 3 11862 480552 110096882
Injection site mass 38.44 22.19 27 11838 24586 110552848
Injection site reaction 37.48 22.19 47 11818 89023 110488411
High density lipoprotein decreased 36.76 22.19 16 11849 5717 110571717
Cough 35.93 22.19 120 11745 461521 110115913
Pneumothorax 35.91 22.19 30 11835 35255 110542179
Therapeutic response decreased 33.01 22.19 46 11819 96453 110480981
Cerebrovascular accident 32.96 22.19 65 11800 181219 110396215
Anaemia 32.92 22.19 9 11856 547077 110030357
Rash 32.17 22.19 173 11692 820791 109756643
General physical health deterioration 31.97 22.19 4 11861 425291 110152143
Chest discomfort 31.21 22.19 62 11803 173786 110403648
Secretion discharge 31.13 22.19 22 11843 20222 110557212
Stent placement 30.21 22.19 15 11850 7219 110570215
Therapy cessation 29.74 22.19 30 11835 44827 110532607
Neutropenia 29.47 22.19 3 11862 374617 110202817
Injection site warmth 29.31 22.19 20 11845 17385 110560049
Exostosis 29.13 22.19 30 11835 45926 110531508
Obstructive airways disorder 29.02 22.19 30 11835 46119 110531315
Angina pectoris 28.02 22.19 34 11831 62261 110515173
Death 27.84 22.19 148 11717 698721 109878713
Unevaluable event 27.75 22.19 33 11832 59194 110518240
Device malfunction 26.57 22.19 22 11843 25536 110551898
Injection site induration 26.39 22.19 16 11849 11367 110566067
Dyspnoea exertional 26.19 22.19 43 11822 104017 110473417
Acute kidney injury 23.75 22.19 20 11845 635410 109942024
Eosinophilia 23.46 22.19 30 11835 57906 110519528
Bronchospasm 23.37 22.19 22 11843 30217 110547217
Angina unstable 23.30 22.19 17 11848 16415 110561019
Pulmonary sepsis 22.20 22.19 11 11854 5267 110572167

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 D000091362 PCSK9 Inhibitors
MeSH PA D000924 Anticholesteremic Agents
MeSH PA D000960 Hypolipidemic Agents
MeSH PA D000963 Antimetabolites
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D011480 Protease Inhibitors
MeSH PA D015842 Serine Proteinase Inhibitors
MeSH PA D057847 Lipid Regulating Agents
FDA MoA N0000191730 PCSK9 Inhibitors
FDA EPC N0000191731 PCSK9 Inhibitor
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35821 anticholesteremic drug
CHEBI has role CHEBI:145947 antiatherosclerotic agent

Related Drugs by ATC class:

C10AX Other lipid modifying agents 15 drugs
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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
CHEBI:754310 CHEBI
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:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Praluent HUMAN PRESCRIPTION DRUG LABEL 1 0024-5901 INJECTION, SOLUTION 75 mg SUBCUTANEOUS BLA 33 sections
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 0024-5902 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 0024-5903 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 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 61755-020 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 61755-021 INJECTION, SOLUTION 150 mg SUBCUTANEOUS BLA 33 sections