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

Stem definitionDrug idCAS RN
human origin 5000 1256937-27-5

Description:

MoleculeDescription

Synonyms:

  • evolocumab
  • repatha
  • AMG-145
  • AMG 145
Evolocumab is a human monoclonal IgG2 directed against human proprotein convertase subtilisin kexin 9 (PCSK9). Evolocumab binds to PCSK9 and inhibits circulating PCSK9 from binding to the low density lipoprotein (LDL) receptor (LDLR), preventing PCSK9-mediated LDLR degradation and permitting LDLR to recycle back to the liver cell surface. By inhibiting the binding of PCSK9 to LDLR, evolocumab increases the number of LDLRs available to clear LDL from the blood, thereby lowering LDL-C levels.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
10 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 22, 2016 PMDA Astellas Pharma
Aug. 28, 2015 FDA REPATHA
May 21, 2015 EMA

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
Wrong technique in product usage process 12245.68 27.91 4183 72568 55849 53216466
Accidental exposure to product 8788.26 27.91 2609 74142 21065 53251250
Injection site pain 7029.15 27.91 3358 73393 110033 53162282
Device difficult to use 4107.94 27.91 1204 75547 9155 53263160
Injection site bruising 4013.62 27.91 1637 75114 36009 53236306
Product dose omission issue 3090.29 27.91 2396 74355 189224 53083091
Injection site haemorrhage 2429.82 27.91 983 75768 21068 53251247
Rhinorrhoea 2301.87 27.91 1244 75507 52334 53219981
Myalgia 1905.74 27.91 1557 75194 131934 53140381
Device issue 1734.35 27.91 770 75981 20888 53251427
Influenza like illness 1513.83 27.91 994 75757 59865 53212450
Device use error 1446.74 27.91 467 76284 5032 53267283
Back pain 1433.18 27.91 1720 75031 232527 53039788
Incorrect dose administered by device 1329.86 27.91 395 76356 3144 53269171
Underdose 1214.54 27.91 601 76150 20921 53251394
Injury associated with device 1075.07 27.91 328 76423 2887 53269428
Muscle spasms 965.07 27.91 1075 75676 133720 53138595
Drug dose omission by device 940.25 27.91 280 76471 2249 53270066
Injection site swelling 843.11 27.91 605 76146 42023 53230292
Low density lipoprotein increased 737.64 27.91 292 76459 5874 53266441
Injection site mass 698.99 27.91 378 76373 15836 53256479
Product storage error 602.16 27.91 319 76432 12811 53259504
Injection site erythema 591.67 27.91 639 76112 76610 53195705
Occupational exposure to product 542.62 27.91 173 76578 1782 53270533
Device defective 536.91 27.91 157 76594 1174 53271141
Wrong technique in device usage process 533.77 27.91 183 76568 2404 53269911
Drug ineffective 515.40 27.91 269 76482 816976 52455339
Pain in extremity 489.69 27.91 1188 75563 283862 52988453
Incorrect disposal of product 481.33 27.91 120 76631 440 53271875
Oropharyngeal pain 386.05 27.91 528 76223 80740 53191575
Low density lipoprotein decreased 360.46 27.91 80 76671 147 53272168
Device malfunction 344.87 27.91 239 76512 15669 53256646
Rheumatoid arthritis 339.56 27.91 31 76720 314500 52957815
Blood glucose increased 324.99 27.91 474 76277 76887 53195428
Injection site discomfort 322.56 27.91 141 76610 3667 53268648
Acute kidney injury 313.06 27.91 12 76739 253856 53018459
Blood cholesterol decreased 301.48 27.91 82 76669 454 53271861
Injection site discolouration 290.60 27.91 161 76590 7069 53265246
Condition aggravated 279.88 27.91 46 76705 297088 52975227
Fear of injection 279.65 27.91 144 76607 5445 53266870
Nasopharyngitis 276.11 27.91 750 76001 191545 53080770
Drug interaction 268.23 27.91 11 76740 219318 53052997
Anaemia 262.47 27.91 42 76709 276676 52995639
Feeling abnormal 242.33 27.91 574 76177 134727 53137588
Injection site pruritus 227.90 27.91 290 76461 41299 53231016
Blood triglycerides increased 215.11 27.91 163 76588 12278 53260037
Pyrexia 210.02 27.91 164 76587 403029 52869286
Vomiting 208.11 27.91 246 76505 496893 52775422
Infusion related reaction 204.58 27.91 4 76747 155953 53116362
Inappropriate schedule of product administration 186.13 27.91 363 76388 74515 53197800
Thrombocytopenia 184.24 27.91 3 76748 138724 53133591
Maternal exposure during pregnancy 183.12 27.91 10 76741 155629 53116686
Injection site urticaria 183.04 27.91 149 76602 12458 53259857
Injection site rash 178.11 27.91 165 76586 16414 53255901
Therapeutic response unexpected 176.17 27.91 167 76584 17103 53255212
Contraindicated product administered 175.81 27.91 4 76747 135625 53136690
Product use issue 164.11 27.91 9 76742 139575 53132740
Treatment failure 161.89 27.91 5 76746 128398 53143917
Hypotension 161.50 27.91 82 76669 253994 53018321
Blood cholesterol increased 150.47 27.91 272 76479 52717 53219598
Influenza 147.75 27.91 383 76368 94996 53177319
Haemoglobin decreased 146.70 27.91 14 76737 137293 53135022
Death 144.77 27.91 181 76570 357051 52915264
Infection 144.54 27.91 35 76716 172170 53100145
White blood cell count decreased 143.35 27.91 9 76742 124466 53147849
General physical health deterioration 142.14 27.91 21 76730 146921 53125394
Arthralgia 140.29 27.91 1096 75655 438687 52833628
Oedema peripheral 137.06 27.91 38 76713 170749 53101566
Memory impairment 136.08 27.91 345 76406 84412 53187903
Drug intolerance 134.05 27.91 64 76687 205429 53066886
Hyponatraemia 130.84 27.91 6 76745 108601 53163714
Systemic lupus erythematosus 130.82 27.91 14 76737 125400 53146915
Pneumonia 130.62 27.91 242 76509 406927 52865388
Product use in unapproved indication 129.66 27.91 8 76743 112281 53160034
Overdose 126.46 27.91 7 76744 107729 53164586
Seizure 126.44 27.91 18 76733 129491 53142824
Sepsis 124.37 27.91 29 76722 146400 53125915
Injection site vesicles 121.01 27.91 65 76686 2681 53269634
Cough 120.63 27.91 705 76046 256188 53016127
Injection site extravasation 119.74 27.91 94 76657 7458 53264857
Pulmonary embolism 118.79 27.91 13 76738 114429 53157886
Hypokalaemia 117.35 27.91 5 76746 96512 53175803
Sleep disorder due to a general medical condition 116.47 27.91 92 76659 7365 53264950
Injection site induration 114.60 27.91 97 76654 8561 53263754
Platelet count decreased 112.91 27.91 12 76739 108087 53164228
Respiratory failure 110.73 27.91 9 76742 100503 53171812
Product administered at inappropriate site 109.80 27.91 60 76691 2562 53269753
Glycosylated haemoglobin increased 106.28 27.91 106 76645 11549 53260766
Sinus disorder 105.19 27.91 132 76619 18522 53253793
Intentional product misuse 102.11 27.91 222 76529 49170 53223145
Drug hypersensitivity 98.61 27.91 143 76608 265099 53007216
Sneezing 97.75 27.91 113 76638 14559 53257756
Tachycardia 94.76 27.91 20 76731 108192 53164123
Pleural effusion 94.67 27.91 9 76742 88570 53183745
Dysphonia 90.71 27.91 192 76559 41746 53230569
Mobility decreased 90.35 27.91 278 76473 75993 53196322
Device failure 90.08 27.91 73 76678 6062 53266253
Musculoskeletal pain 88.99 27.91 274 76477 74926 53197389
Wound 88.71 27.91 13 76738 91544 53180771
Oxygen saturation decreased 86.98 27.91 6 76745 76719 53195596
Cardiac arrest 86.92 27.91 15 76736 93652 53178663
Fall 86.60 27.91 248 76503 358192 52914123
Dehydration 85.57 27.91 70 76681 168340 53103975
Muscle disorder 83.58 27.91 62 76689 4519 53267796
Glossodynia 81.01 27.91 22 76729 100269 53172046
Joint swelling 80.96 27.91 133 76618 234505 53037810
Injection site indentation 80.33 27.91 23 76728 158 53272157
Device dispensing error 78.84 27.91 20 76731 80 53272235
Deep vein thrombosis 77.54 27.91 13 76738 82900 53189415
Intentional product use issue 75.81 27.91 8 76743 72486 53199829
Stomatitis 74.77 27.91 24 76727 98134 53174181
Paranasal sinus hypersecretion 73.93 27.91 51 76700 3315 53269000
Incorrect dose administered 73.92 27.91 200 76551 50845 53221470
Renal failure 72.55 27.91 40 76711 118412 53153903
Interstitial lung disease 71.37 27.91 3 76748 58619 53213696
Low density lipoprotein abnormal 70.34 27.91 21 76730 170 53272145
Stent placement 68.72 27.91 50 76701 3537 53268778
Muscular weakness 68.13 27.91 307 76444 100685 53171630
Lower respiratory tract infection 67.97 27.91 23 76728 90958 53181357
Somnolence 66.74 27.91 86 76665 167648 53104667
Gastrointestinal haemorrhage 66.05 27.91 17 76734 80313 53192002
Nasal congestion 65.69 27.91 197 76554 53090 53219225
Loss of consciousness 65.12 27.91 42 76709 114170 53158145
C-reactive protein increased 64.93 27.91 10 76741 67876 53204439
Bradycardia 64.57 27.91 12 76739 71044 53201271
Cardiac operation 64.49 27.91 44 76707 2809 53269506
Alanine aminotransferase increased 64.47 27.91 28 76723 95067 53177248
Injection site injury 64.26 27.91 26 76725 554 53271761
Suicidal ideation 62.45 27.91 7 76744 60504 53211811
Depressed level of consciousness 62.44 27.91 4 76747 54424 53217891
Hyperkalaemia 62.21 27.91 4 76747 54252 53218063
Injection site reaction 61.98 27.91 188 76563 50978 53221337
Respiratory tract congestion 61.53 27.91 90 76661 14609 53257706
Lack of injection site rotation 61.36 27.91 21 76730 274 53272041
Cardiac failure 60.25 27.91 24 76727 85820 53186495
Confusional state 59.87 27.91 118 76633 194103 53078212
Rash pruritic 59.87 27.91 183 76568 49827 53222488
Aspartate aminotransferase increased 59.79 27.91 23 76728 84006 53188309
Blood cholesterol abnormal 59.64 27.91 40 76711 2482 53269833
Adverse reaction 59.50 27.91 69 76682 8918 53263397
Arthropathy 58.92 27.91 70 76681 141383 53130932
Syncope 58.81 27.91 45 76706 111948 53160367
Needle issue 57.09 27.91 60 76691 6952 53265363
Swelling 56.44 27.91 119 76632 190986 53081329
Pulmonary oedema 55.99 27.91 6 76745 53717 53218598
Osteoarthritis 55.91 27.91 16 76735 70470 53201845
Constipation 53.36 27.91 130 76621 198282 53074033
Abdominal pain 52.68 27.91 190 76561 255713 53016602
Decreased appetite 52.37 27.91 148 76603 214826 53057489
Multiple sclerosis relapse 52.35 27.91 3 76748 44850 53227465
Blood creatinine increased 51.95 27.91 27 76724 82635 53189680
Abortion spontaneous 51.84 27.91 4 76747 46631 53225684
Adverse event 51.74 27.91 153 76598 40908 53231407
Therapy non-responder 51.73 27.91 172 76579 48948 53223367
Circumstance or information capable of leading to medication error 51.62 27.91 43 76708 3711 53268604
Injection site warmth 51.34 27.91 81 76670 14047 53258268
Application site swelling 51.04 27.91 22 76729 552 53271763
Plasma cell myeloma 50.79 27.91 5 76746 47869 53224446
Depression 49.96 27.91 119 76632 182933 53089382
Throat irritation 49.80 27.91 128 76623 31553 53240762
Renal impairment 49.77 27.91 29 76722 83289 53189026
Pruritus 48.89 27.91 641 76110 293191 52979124
Upper-airway cough syndrome 48.40 27.91 63 76688 9164 53263151
Device delivery system issue 47.64 27.91 21 76730 557 53271758
Injection site irritation 47.04 27.91 44 76707 4428 53267887
Incorrect dose administered by product 46.56 27.91 15 76736 160 53272155
Liver function test abnormal 46.15 27.91 7 76744 48064 53224251
Hypoacusis 46.03 27.91 101 76650 22498 53249817
Cellulitis 46.03 27.91 26 76725 75963 53196352
International normalised ratio increased 45.75 27.91 7 76744 47754 53224561
Oedema 45.66 27.91 25 76726 74321 53197994
Mental status changes 45.12 27.91 3 76748 39568 53232747
Impaired healing 44.97 27.91 18 76733 64187 53208128
Dyspnoea 42.64 27.91 591 76160 585641 52686674
Psoriasis 42.01 27.91 38 76713 87051 53185264
Agitation 41.78 27.91 16 76735 58610 53213705
Hepatic function abnormal 41.48 27.91 3 76748 36896 53235419
Encephalopathy 41.36 27.91 3 76748 36805 53235510
Medication error 40.76 27.91 3 76748 36362 53235953
Dizziness 40.50 27.91 756 75995 371503 52900812
Musculoskeletal disorder 40.03 27.91 82 76669 17417 53254898
Injury 39.63 27.91 12 76739 50959 53221356
White blood cell count increased 39.55 27.91 9 76742 46236 53226079
Neck pain 39.37 27.91 181 76570 59835 53212480
Hypoglycaemia 39.01 27.91 18 76733 58995 53213320
Limb discomfort 38.96 27.91 102 76649 25420 53246895
Bone pain 38.64 27.91 160 76591 50562 53221753
Pneumonia aspiration 37.96 27.91 3 76748 34298 53238017
Atrial fibrillation 37.80 27.91 64 76687 111588 53160727
Blood alkaline phosphatase increased 37.54 27.91 7 76744 41355 53230960
Red blood cell count decreased 37.43 27.91 4 76747 35899 53236416
Hepatic failure 37.31 27.91 4 76747 35802 53236513
Unevaluable event 36.81 27.91 155 76596 49343 53222972
Pulmonary hypertension 36.77 27.91 5 76746 37265 53235050
Application site haemorrhage 36.54 27.91 21 76730 989 53271326
Psoriatic arthropathy 36.30 27.91 12 76739 48178 53224137
Hepatic enzyme increased 36.06 27.91 80 76671 126115 53146200
Injection site paraesthesia 35.07 27.91 16 76735 461 53271854
Hepatitis 34.77 27.91 4 76747 33890 53238425
Gamma-glutamyltransferase increased 34.33 27.91 4 76747 33551 53238764
Chronic kidney disease 34.10 27.91 10 76741 43360 53228955
Staphylococcal infection 33.99 27.91 7 76744 38541 53233774
Pneumonitis 33.36 27.91 3 76748 30885 53241430
Haematemesis 33.32 27.91 3 76748 30854 53241461
Femur fracture 33.26 27.91 8 76743 39577 53232738
Nervousness 32.96 27.91 107 76644 30071 53242244
Device leakage 32.65 27.91 42 76709 6038 53266277
Application site pain 32.65 27.91 35 76716 4148 53268167
Jaundice 32.59 27.91 3 76748 30310 53242005
Product quality issue 32.07 27.91 7 76744 37016 53235299
Rash maculo-papular 31.84 27.91 3 76748 29746 53242569
Muscle tightness 31.80 27.91 57 76694 10964 53261351
Headache 31.55 27.91 1002 75749 535819 52736496
Cardiac failure congestive 31.55 27.91 53 76698 92704 53179611
Discomfort 31.15 27.91 56 76695 95416 53176899
High density lipoprotein decreased 31.05 27.91 24 76727 1861 53270454
Melaena 31.01 27.91 3 76748 29126 53243189
Increased tendency to bruise 30.78 27.91 53 76698 9877 53262438
Dysarthria 30.74 27.91 10 76741 40558 53231757
Neuropathy peripheral 30.65 27.91 64 76687 103123 53169192
Injection site hypersensitivity 30.60 27.91 23 76728 1710 53270605
Back disorder 30.23 27.91 52 76699 9683 53262632
Anxiety 30.16 27.91 163 76588 196541 53075774
Respiratory distress 30.12 27.91 6 76745 33821 53238494
Asthma 29.58 27.91 71 76680 108901 53163414
Hepatotoxicity 29.34 27.91 3 76748 27877 53244438
Aphonia 29.18 27.91 49 76702 8949 53263366
Body temperature increased 28.82 27.91 6 76745 32793 53239522
Therapeutic product effect decreased 28.76 27.91 89 76662 125566 53146749
Blister 28.67 27.91 43 76708 78710 53193605
Anaphylactic reaction 28.66 27.91 25 76726 58301 53214014
Drug-induced liver injury 28.66 27.91 4 76747 29229 53243086

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
Wrong technique in product usage process 9566.81 30.13 3103 47774 31956 32430693
Accidental exposure to product 6200.81 30.13 1717 49160 9485 32453164
Injection site pain 3545.44 30.13 1477 49400 31581 32431068
Product dose omission issue 2716.22 30.13 1791 49086 100784 32361865
Device difficult to use 2624.73 30.13 584 50293 965 32461684
Injection site bruising 2366.74 30.13 753 50124 7067 32455582
Myalgia 2005.68 30.13 1360 49517 79870 32382779
Rhinorrhoea 1966.99 30.13 877 50000 22109 32440540
Injection site haemorrhage 1928.31 30.13 659 50218 7869 32454780
Influenza like illness 1599.77 30.13 801 50076 26339 32436310
Back pain 1570.02 30.13 1333 49544 109720 32352929
Incorrect dose administered by device 1482.10 30.13 369 50508 1210 32461439
Device issue 1360.06 30.13 515 50362 8397 32454252
Device use error 1066.58 30.13 305 50572 1898 32460751
Injection site swelling 969.58 30.13 412 50465 9172 32453477
Low density lipoprotein decreased 922.91 30.13 233 50644 820 32461829
Drug dose omission by device 795.20 30.13 204 50673 778 32461871
Underdose 699.86 30.13 362 50515 12707 32449942
Injection site mass 666.18 30.13 269 50608 5232 32457417
Muscle spasms 604.21 30.13 643 50234 69775 32392874
Arthralgia 593.01 30.13 927 49950 147521 32315128
Product storage error 581.36 30.13 264 50613 6914 32455735
Injury associated with device 579.80 30.13 155 50722 719 32461930
Nasopharyngitis 521.63 30.13 568 50309 63219 32399430
Device defective 467.35 30.13 115 50762 353 32462296
Blood cholesterol decreased 466.65 30.13 135 50742 879 32461770
Low density lipoprotein increased 457.46 30.13 191 50686 4055 32458594
Injection site discomfort 431.82 30.13 134 50743 1142 32461507
Acute kidney injury 384.84 30.13 18 50859 293450 32169199
Injection site erythema 370.47 30.13 250 50627 14418 32448231
Pain in extremity 369.08 30.13 664 50213 118237 32344412
Wrong technique in device usage process 334.55 30.13 110 50767 1149 32461500
Device malfunction 315.42 30.13 189 50688 8850 32453799
Oropharyngeal pain 291.09 30.13 299 50578 31053 32431596
Incorrect disposal of product 282.20 30.13 71 50806 245 32462404
Drug interaction 268.56 30.13 19 50858 218166 32244483
Anaemia 257.37 30.13 26 50851 223598 32239051
Pneumonia 216.36 30.13 146 50731 355106 32107543
Injection site discolouration 212.77 30.13 79 50798 1211 32461438
Drug ineffective 211.21 30.13 175 50702 383302 32079347
Hypotension 209.43 30.13 42 50835 216068 32246581
Injection site urticaria 208.22 30.13 83 50794 1556 32461093
Blood glucose increased 197.71 30.13 361 50516 64880 32397769
Injection site pruritus 193.62 30.13 120 50757 5970 32456679
Thrombocytopenia 191.10 30.13 10 50867 148289 32314360
Feeling abnormal 190.28 30.13 340 50537 60083 32402566
Musculoskeletal pain 176.24 30.13 233 50644 31664 32430985
Sepsis 171.30 30.13 23 50854 158811 32303838
Pyrexia 171.10 30.13 150 50727 319818 32142831
Therapeutic response unexpected 169.88 30.13 132 50745 9480 32453169
Nasal congestion 167.32 30.13 182 50695 20169 32442480
Condition aggravated 159.87 30.13 26 50851 155635 32307014
Adverse event 158.07 30.13 160 50717 16312 32446337
Inappropriate schedule of product administration 156.10 30.13 267 50610 45558 32417091
Injection site vesicles 155.44 30.13 50 50827 484 32462165
Respiratory failure 149.04 30.13 4 50873 107178 32355471
Blood cholesterol increased 141.10 30.13 156 50721 17601 32445048
Platelet count decreased 137.89 30.13 11 50866 114580 32348069
Haemoglobin decreased 137.25 30.13 14 50863 119657 32342992
Device failure 136.87 30.13 68 50809 2183 32460466
Renal failure 132.51 30.13 25 50852 134453 32328196
Product administered at inappropriate site 129.48 30.13 61 50816 1738 32460911
Fear of injection 128.72 30.13 48 50829 745 32461904
Pancytopenia 128.37 30.13 3 50874 91232 32371417
General physical health deterioration 128.32 30.13 15 50862 115244 32347405
Blood triglycerides increased 127.65 30.13 135 50742 14484 32448165
Completed suicide 126.61 30.13 4 50873 92513 32370136
Sinus disorder 125.65 30.13 95 50782 6549 32456100
Vomiting 123.83 30.13 112 50765 235445 32227204
Intentional product misuse 118.74 30.13 207 50670 35844 32426805
Influenza 117.62 30.13 237 50640 45777 32416872
Injection site rash 117.48 30.13 73 50804 3647 32459002
Death 117.11 30.13 267 50610 382250 32080399
White blood cell count decreased 114.78 30.13 7 50870 91191 32371458
Product use in unapproved indication 105.93 30.13 8 50869 87196 32375453
Occupational exposure to product 103.00 30.13 33 50844 315 32462334
Overdose 102.96 30.13 9 50868 87068 32375581
Dehydration 102.30 30.13 37 50840 128921 32333728
Seizure 100.81 30.13 20 50857 103834 32358815
Injection site reaction 99.52 30.13 106 50771 11463 32451186
Hyponatraemia 99.23 30.13 4 50873 74509 32388140
Oedema peripheral 98.88 30.13 28 50849 114063 32348586
Application site mass 97.83 30.13 19 50858 7 32462642
Gastrointestinal haemorrhage 94.98 30.13 12 50865 86870 32375779
Disease progression 94.95 30.13 12 50865 86850 32375799
Decreased appetite 93.69 30.13 69 50808 160744 32301905
Low density lipoprotein abnormal 92.62 30.13 29 50848 255 32462394
Blood creatinine increased 92.29 30.13 19 50858 96113 32366536
Hyperkalaemia 92.03 30.13 4 50873 69746 32392903
Pain 90.22 30.13 551 50326 187005 32275644
Adverse reaction 89.17 30.13 57 50820 2993 32459656
Cardiac failure 88.24 30.13 18 50859 91655 32370994
Paranasal sinus hypersecretion 87.52 30.13 37 50840 810 32461839
Mobility decreased 85.68 30.13 157 50720 28252 32434397
Memory impairment 85.54 30.13 193 50684 40286 32422363
Respiratory tract congestion 83.78 30.13 71 50806 5765 32456884
Pleural effusion 83.74 30.13 12 50865 78980 32383669
Injection site induration 83.06 30.13 52 50825 2632 32460017
Glycosylated haemoglobin increased 82.05 30.13 91 50786 10298 32452351
Interstitial lung disease 81.74 30.13 5 50872 64996 32397653
Fall 81.44 30.13 113 50764 196088 32266561
Septic shock 79.23 30.13 8 50869 68981 32393668
Multiple organ dysfunction syndrome 77.93 30.13 9 50868 69845 32392804
Deep vein thrombosis 76.92 30.13 6 50871 63707 32398942
Leukopenia 74.48 30.13 5 50872 60117 32402532
Hypokalaemia 73.20 30.13 3 50874 55091 32407558
Confusional state 72.78 30.13 70 50807 143045 32319604
Pulmonary embolism 71.60 30.13 21 50856 83638 32379011
Plasma cell myeloma 70.77 30.13 5 50872 57609 32405040
Needle issue 70.29 30.13 57 50820 4352 32458297
Cardiac arrest 69.83 30.13 32 50845 96744 32365905
Incorrect dose administered by product 68.02 30.13 15 50862 23 32462626
Muscular weakness 67.75 30.13 247 50630 67682 32394967
Sneezing 66.77 30.13 57 50820 4674 32457975
Atrial fibrillation 66.73 30.13 51 50826 116653 32345996
Sleep disorder due to a general medical condition 65.99 30.13 49 50828 3285 32459364
Hypoxia 65.57 30.13 4 50873 52128 32410521
Device dispensing error 65.17 30.13 15 50862 31 32462618
Fatigue 63.38 30.13 831 50046 349870 32112779
Bradycardia 63.02 30.13 17 50860 71545 32391104
Agitation 62.30 30.13 8 50869 57228 32405421
Tachycardia 62.15 30.13 23 50854 79065 32383584
Upper-airway cough syndrome 61.26 30.13 46 50831 3137 32459512
Syncope 60.21 30.13 33 50844 90091 32372558
Rash pruritic 59.58 30.13 124 50753 24487 32438162
Rhabdomyolysis 59.19 30.13 16 50861 67249 32395400
Injection site hypoaesthesia 58.91 30.13 15 50862 55 32462594
Hypoacusis 58.37 30.13 95 50782 15546 32447103
Musculoskeletal disorder 56.64 30.13 56 50821 5546 32457103
Injection site irritation 56.40 30.13 29 50848 1002 32461647
Incorrect dose administered 55.91 30.13 150 50727 34878 32427771
Hallucination 55.74 30.13 8 50869 52611 32410038
International normalised ratio increased 55.49 30.13 6 50871 49029 32413620
Injection site extravasation 53.49 30.13 38 50839 2378 32460271
Muscle disorder 53.19 30.13 38 50839 2399 32460250
Cardiac operation 52.97 30.13 40 50837 2751 32459898
Muscle tightness 52.37 30.13 50 50827 4744 32457905
C-reactive protein increased 51.69 30.13 7 50870 48095 32414554
Oxygen saturation decreased 51.69 30.13 7 50870 48092 32414557
Hypoglycaemia 51.65 30.13 11 50866 54371 32408278
Headache 51.24 30.13 500 50377 195697 32266952
Intentional product use issue 50.87 30.13 4 50873 42207 32420442
Cardiac failure congestive 49.88 30.13 36 50841 84816 32377833
Infection 48.44 30.13 37 50840 84678 32377971
Off label use 48.41 30.13 709 50168 305611 32157038
Constipation 48.27 30.13 77 50800 126296 32336353
Cardio-respiratory arrest 47.99 30.13 14 50863 55975 32406674
Cough 46.67 30.13 374 50503 138443 32324206
Hypersensitivity 46.21 30.13 196 50681 57562 32405087
Renal impairment 45.54 30.13 46 50831 91926 32370723
Haematuria 45.48 30.13 10 50867 48351 32414298
Device physical property issue 45.34 30.13 23 50854 772 32461877
Ascites 45.26 30.13 5 50872 40186 32422463
Stent placement 44.90 30.13 45 50832 4530 32458119
Oedema 43.14 30.13 9 50868 45138 32417511
Lack of injection site rotation 42.60 30.13 13 50864 104 32462545
Mental status changes 42.60 30.13 5 50872 38332 32424317
Product use issue 42.04 30.13 15 50862 52762 32409887
Dysphonia 40.78 30.13 96 50781 20588 32442061
High density lipoprotein decreased 40.54 30.13 37 50840 3315 32459334
Throat irritation 40.08 30.13 62 50815 9716 32452933
Abdominal pain 39.61 30.13 112 50765 149417 32313232
Injection site injury 39.53 30.13 14 50863 186 32462463
Aggression 39.44 30.13 7 50870 39382 32423267
Application site swelling 38.92 30.13 15 50862 256 32462393
Somnolence 38.91 30.13 64 50813 103733 32358916
Neck pain 38.82 30.13 100 50777 22687 32439962
Blood bilirubin increased 38.60 30.13 7 50870 38777 32423872
Lactic acidosis 38.20 30.13 4 50873 33532 32429117
Pulmonary oedema 37.11 30.13 13 50864 46254 32416395
Rectal haemorrhage 36.72 30.13 7 50870 37416 32425233
Jaundice 36.63 30.13 5 50872 34153 32428496
Injection site paraesthesia 36.43 30.13 12 50865 126 32462523
Musculoskeletal discomfort 36.26 30.13 49 50828 6791 32455858
White blood cell count increased 36.13 30.13 10 50867 41392 32421257
Unevaluable event 35.91 30.13 125 50752 33461 32429188
Dysarthria 35.27 30.13 5 50872 33196 32429453
Cerebral haemorrhage 35.17 30.13 6 50871 34741 32427908
Spinal operation 34.37 30.13 30 50847 2535 32460114
High density lipoprotein increased 34.24 30.13 15 50862 359 32462290
Pruritus 34.03 30.13 329 50548 128373 32334276
Blood alkaline phosphatase increased 33.76 30.13 5 50872 32127 32430522
Respiratory distress 33.73 30.13 7 50870 35239 32427410
Device delivery system issue 33.42 30.13 15 50862 381 32462268
Haemorrhage 33.16 30.13 18 50859 49430 32413219
Sinus congestion 33.13 30.13 40 50837 4955 32457694
Injection site laceration 32.89 30.13 8 50869 23 32462626
Stomatitis 32.79 30.13 11 50866 40218 32422431
Cellulitis 32.66 30.13 19 50858 50211 32412438
Musculoskeletal stiffness 31.98 30.13 134 50743 39130 32423519
Gamma-glutamyltransferase increased 31.86 30.13 5 50872 30777 32431872
Rheumatoid arthritis 31.69 30.13 15 50862 44529 32418120
Circumstance or information capable of leading to medication error 31.50 30.13 25 50852 1850 32460799
Haemoptysis 31.38 30.13 7 50870 33518 32429131
Acute respiratory failure 31.29 30.13 4 50873 28724 32433925
Sluggishness 31.19 30.13 32 50845 3311 32459338
Blood triglycerides decreased 30.92 30.13 9 50868 60 32462589
Alanine aminotransferase increased 30.72 30.13 47 50830 78432 32384217
Type IIa hyperlipidaemia 30.60 30.13 12 50865 215 32462434
Hepatic function abnormal 30.54 30.13 16 50861 44824 32417825
Head discomfort 30.52 30.13 32 50845 3397 32459252
Therapy cessation 30.14 30.13 73 50804 15940 32446709

Pharmacologic Action:

SourceCodeDescription
ATC C10AX13 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
Cardiovascular disease indication 49601007 DOID:1287
Familial hypercholesterolemia - homozygous indication 238078005
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 9.72 IUPHAR SCIENTIFIC LITERATURE

External reference:

IDSource
D10557 KEGG_DRUG
4034786 VANDF
CHEMBL2364655 ChEMBL_ID
C577155 MESH_SUPPLEMENTAL_RECORD_UI
7343 IUPHAR_LIGAND_ID
9643 INN_ID
DB09303 DRUGBANK_ID
LKC0U3A8NJ UNII
1665684 RXNORM
236233 MMSL
31213 MMSL
d08383 MMSL
016368 NDDF
716068004 SNOMEDCT_US
763586000 SNOMEDCT_US
C3529352 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
REPATHA HUMAN PRESCRIPTION DRUG LABEL 1 55513-750 INJECTION, SOLUTION 140 mg SUBCUTANEOUS BLA 33 sections
REPATHA HUMAN PRESCRIPTION DRUG LABEL 1 55513-760 INJECTION, SOLUTION 140 mg SUBCUTANEOUS BLA 33 sections
REPATHA HUMAN PRESCRIPTION DRUG LABEL 1 72511-750 INJECTION, SOLUTION 140 mg SUBCUTANEOUS BLA 33 sections
REPATHA HUMAN PRESCRIPTION DRUG LABEL 1 72511-760 INJECTION, SOLUTION 140 mg SUBCUTANEOUS BLA 33 sections