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

Stem definitionDrug idCAS RN
humanized origin 4969 219685-50-4

Description:

MoleculeDescription

Synonyms:

  • eculizumab
  • soliris
  • h5G1.1
  • h5G1.1VHC+h5G1.1VLC
a recombinant humanized monoclonal IgG2/4k antibody produced by murine myeloma cell culture, specifically binds to the complement protein C5 with high affinity, thereby inhibiting its cleavage to C5a and C5b and preventing the generation of the terminal complement complex C5b-9
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
64 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 16, 2010 PMDA Alexion Pharma
March 16, 2007 FDA ALEXION PHARM
June 20, 2007 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
Haemolysis 459.79 18.38 129 11088 6367 53331482
Haemoglobin decreased 425.04 18.38 296 10921 137011 53200838
Blood lactate dehydrogenase increased 310.25 18.38 130 11087 21651 53316198
Thrombotic microangiopathy 222.55 18.38 81 11136 9256 53328593
Haemoglobinuria 177.28 18.38 33 11184 236 53337613
Platelet count decreased 145.24 18.38 144 11073 107955 53229894
Chromaturia 110.81 18.38 58 11159 15892 53321957
Meningococcal sepsis 97.60 18.38 14 11203 9 53337840
Paroxysmal nocturnal haemoglobinuria 94.58 18.38 18 11199 147 53337702
Incorrect dose administered 93.67 18.38 81 11136 50964 53286885
Inappropriate schedule of product administration 91.78 18.38 95 11122 74783 53263066
Meningococcal bacteraemia 84.75 18.38 12 11205 6 53337843
Reticulocyte count increased 84.03 18.38 22 11195 830 53337019
Aplastic anaemia 80.78 18.38 38 11179 8283 53329566
Haemolytic uraemic syndrome 75.37 18.38 26 11191 2535 53335314
Off label use 72.91 18.38 241 10976 471971 52865878
Haptoglobin decreased 69.49 18.38 18 11199 651 53337198
Exposure during pregnancy 68.48 18.38 106 11111 124754 53213095
Renal impairment 63.83 18.38 83 11134 83235 53254614
Arteriovenous fistula occlusion 63.11 18.38 15 11202 378 53337471
Transfusion 60.42 18.38 37 11180 13650 53324199
Extravascular haemolysis 59.87 18.38 10 11207 34 53337815
Headache 57.75 18.38 244 10973 536577 52801272
Blue toe syndrome 56.92 18.38 14 11203 409 53337440
Gonorrhoea 53.88 18.38 11 11206 133 53337716
Blood lactate dehydrogenase abnormal 52.09 18.38 12 11205 263 53337586
Blood creatinine increased 50.73 18.38 74 11143 82588 53255261
Haemoglobin abnormal 47.66 18.38 22 11195 4592 53333257
Fatigue 46.83 18.38 287 10930 730219 52607630
Platelet count abnormal 46.48 18.38 19 11198 2959 53334890
Dyspnoea exertional 45.58 18.38 57 11160 54943 53282906
Myasthenia gravis 44.66 18.38 20 11197 3893 53333956
Cytomegalovirus infection 44.13 18.38 35 11182 19504 53318345
Atypical haemolytic uraemic syndrome 44.02 18.38 12 11205 529 53337320
Condition aggravated 38.18 18.38 143 11074 296991 53040858
Total complement activity decreased 37.34 18.38 5 11212 0 53337849
Transplant rejection 36.23 18.38 24 11193 10127 53327722
Quality of life decreased 35.52 18.38 20 11197 6318 53331531
Bacteraemia 35.43 18.38 28 11189 15521 53322328
Jaundice 34.49 18.38 37 11180 30276 53307573
Poor venous access 34.20 18.38 23 11194 9952 53327897
Meningitis meningococcal 34.19 18.38 7 11210 86 53337763
Graft loss 33.08 18.38 9 11208 394 53337455
Haematocrit decreased 33.04 18.38 40 11177 37291 53300558
Anaemia 32.93 18.38 130 11087 276588 53061261
Drug hypersensitivity 32.34 18.38 8 11209 265234 53072615
Drug intolerance 32.28 18.38 3 11214 205490 53132359
Proteinuria 31.76 18.38 28 11189 18040 53319809
Iron overload 31.04 18.38 10 11207 789 53337060
Plasmapheresis 30.86 18.38 8 11209 290 53337559
Gonococcal infection 29.87 18.38 4 11213 0 53337849
Pneumonia bacterial 28.89 18.38 19 11198 7921 53329928
Renal pain 28.42 18.38 17 11200 6010 53331839
Toxicity to various agents 28 18.38 6 11211 219592 53118257
Pyrexia 27.96 18.38 162 11055 403031 52934818
Bone marrow transplant 27.86 18.38 9 11208 716 53337133
Cervicitis 27.67 18.38 8 11209 438 53337411
Thrombosis 27.03 18.38 47 11170 60746 53277103
Haptoglobin increased 26.59 18.38 5 11212 38 53337811
Abdominal pain 26.32 18.38 115 11102 255788 53082061
Graft ischaemia 26.04 18.38 5 11212 43 53337806
Cytomegalovirus gastrointestinal infection 25.98 18.38 7 11210 295 53337554
Pre-eclampsia 25.10 18.38 18 11199 8629 53329220
Muscle strain 24.91 18.38 17 11200 7530 53330319
Blood product transfusion dependent 24.88 18.38 6 11211 161 53337688
Device related infection 24.50 18.38 27 11190 22759 53315090
Sepsis 24.47 18.38 77 11140 146352 53191497
Reperfusion injury 24.30 18.38 5 11212 63 53337786
Budd-Chiari syndrome 24.23 18.38 5 11212 64 53337785
Graft thrombosis 24.18 18.38 6 11211 182 53337667
Meningococcal infection 23.81 18.38 5 11212 70 53337779
Complement factor C3 decreased 23.72 18.38 6 11211 197 53337652
Gastroenteritis 23.56 18.38 28 11189 25588 53312261
Pregnancy 23.54 18.38 31 11186 31410 53306439
Small cell lung cancer recurrent 23.44 18.38 4 11213 16 53337833
Hospitalisation 23.03 18.38 48 11169 70964 53266885
Babesiosis 22.62 18.38 6 11211 238 53337611
Waterhouse-Friderichsen syndrome 22.40 18.38 3 11214 0 53337849
Total complement activity increased 22.40 18.38 3 11214 0 53337849
Renal transplant 22.08 18.38 9 11208 1391 53336458
Red blood cell count decreased 21.79 18.38 32 11185 35871 53301978
Rash 21.61 18.38 38 11179 446153 52891696
Viral infection 21.39 18.38 30 11187 32265 53305584
Intravascular haemolysis 21.28 18.38 6 11211 300 53337549
Packed red blood cell transfusion 21.19 18.38 10 11207 2193 53335656
Thrombocytopenia 20.52 18.38 70 11147 138657 53199192
SARS-CoV-2 test negative 20.35 18.38 6 11211 352 53337497
Myelodysplastic syndrome 20.13 18.38 21 11196 16639 53321210
Haemolytic anaemia 20.01 18.38 17 11200 10422 53327427
Neisseria infection 19.86 18.38 4 11213 45 53337804
Meningitis 19.79 18.38 14 11203 6567 53331282
Maternal exposure during breast feeding 19.74 18.38 11 11206 3406 53334443
Dysphagia 19.59 18.38 50 11167 84347 53253502
Product use issue 19.54 18.38 3 11214 139581 53198268
Complement factor abnormal 19.11 18.38 3 11214 6 53337843
Haematocrit abnormal 18.78 18.38 7 11210 852 53336997
Oropharyngeal pain 18.71 18.38 48 11169 81220 53256629
Polyomavirus viraemia 18.70 18.38 6 11211 467 53337382
Multiple organ dysfunction syndrome 18.48 18.38 38 11179 55639 53282210
Arthritis bacterial 18.46 18.38 13 11204 6055 53331794
Ocular icterus 18.44 18.38 11 11206 3868 53333981

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
Haemolysis 388.93 22.03 120 7300 7621 32498485
Haemoglobin decreased 229.57 22.03 201 7219 119470 32386636
Blood lactate dehydrogenase increased 211.69 22.03 102 7318 21703 32484403
Haemoglobinuria 210.40 22.03 44 7376 554 32505552
Thrombotic microangiopathy 182.84 22.03 72 7348 9410 32496696
Paroxysmal nocturnal haemoglobinuria 92.45 22.03 15 7405 36 32506070
Incorrect dose administered 85.81 22.03 68 7352 34960 32471146
Fatigue 82.81 22.03 219 7201 350482 32155624
Chromaturia 81.22 22.03 47 7373 14431 32491675
Meningococcal sepsis 78.05 22.03 12 7408 17 32506089
Transfusion 77.28 22.03 37 7383 7731 32498375
Haptoglobin decreased 74.76 22.03 19 7401 585 32505521
Reticulocyte count increased 72.02 22.03 18 7402 517 32505589
Extravascular haemolysis 70.98 22.03 11 7409 17 32506089
Platelet count decreased 63.37 22.03 102 7318 114489 32391617
Meningococcal bacteraemia 55.85 22.03 8 7412 4 32506102
Off label use 52.57 22.03 171 7249 306149 32199957
Haemoglobin abnormal 52.36 22.03 22 7398 3383 32502723
Inappropriate schedule of product administration 45.23 22.03 54 7366 45771 32460335
Meningococcal infection 44.72 22.03 7 7413 12 32506094
Headache 43.46 22.03 120 7300 196077 32310029
Complement factor increased 41.88 22.03 6 7414 3 32506103
Drug interaction 38.51 22.03 3 7417 218182 32287924
Haematocrit decreased 37.48 22.03 41 7379 31621 32474485
Haemolytic uraemic syndrome 37.40 22.03 15 7405 2049 32504057
End stage renal disease 37.03 22.03 23 7397 8014 32498092
Quality of life decreased 36.07 22.03 17 7403 3425 32502681
Poor venous access 34.79 22.03 16 7404 3050 32503056
Aplastic anaemia 33.72 22.03 21 7399 7352 32498754
Blood product transfusion dependent 33.61 22.03 9 7411 341 32505765
Device related infection 31.92 22.03 29 7391 17904 32488202
Jaundice 31.65 22.03 39 7381 34119 32471987
Encephalitis viral 29.67 22.03 11 7409 1216 32504890
Polyomavirus-associated nephropathy 29.50 22.03 15 7405 3562 32502544
Myasthenia gravis 29.32 22.03 15 7405 3607 32502499
Abdominal pain 28.74 22.03 87 7333 149442 32356664
Bone marrow transplant 28.01 22.03 10 7410 993 32505113
Intravascular haemolysis 26.64 22.03 8 7412 460 32505646
Nasopharyngitis 26.34 22.03 50 7370 63737 32442369
Complement factor C3 decreased 26.18 22.03 5 7415 38 32506068
Malignant atrophic papulosis 25.15 22.03 4 7416 8 32506098
Platelet count abnormal 24.80 22.03 12 7408 2562 32503544
Atypical haemolytic uraemic syndrome 23.85 22.03 6 7414 177 32505929
Brain abscess 23.31 22.03 12 7408 2922 32503184
Mean cell volume increased 23.23 22.03 11 7409 2240 32503866
Blood creatinine abnormal 22.98 22.03 11 7409 2294 32503812
Cholelithiasis 22.88 22.03 26 7394 20886 32485220
Condition aggravated 22.27 22.03 82 7338 155579 32350527
Haptoglobin abnormal 22.16 22.03 3 7417 0 32506106

Pharmacologic Action:

SourceCodeDescription
ATC L04AA25 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA EPC N0000175575 Complement Inhibitor
MeSH PA D051056 Complement Inactivating Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
FDA MoA N0000175974 Complement Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Paroxysmal nocturnal hemoglobinuria indication 1963002 DOID:0060284
Neuromyelitis optica indication 25044007 DOID:8869
Congenital hemolytic uremic syndrome indication 444976001

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
Complement C5 Secreted ANTIBODY BINDING DRUG LABEL DRUG LABEL

External reference:

IDSource
D03940 KEGG_DRUG
4026032 VUID
N0000179786 NUI
4026032 VANDF
CHEMBL1201828 ChEMBL_ID
C481642 MESH_SUPPLEMENTAL_RECORD_UI
6884 IUPHAR_LIGAND_ID
8231 INN_ID
DB01257 DRUGBANK_ID
A3ULP0F556 UNII
591781 RXNORM
108542 MMSL
23533 MMSL
d06673 MMSL
012087 NDDF
426801002 SNOMEDCT_US
427429004 SNOMEDCT_US
C1541483 UMLSCUI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SOLIRIS HUMAN PRESCRIPTION DRUG LABEL 1 25682-001 INJECTION, SOLUTION, CONCENTRATE 300 mg INTRAVENOUS BLA 29 sections