eculizumab indications/contra

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

Approvals:

DateAgencyCompanyOrphan
June 20, 2007 EMA
March 16, 2007 FDA ALEXION PHARM

FDA Adverse Event Reporting System

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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
Haemoglobin decreased 2103.21 36.46 620 5516 29674 3350049
Haemolysis 2004.27 36.46 363 5773 1679 3378044
Fatigue 1514.95 36.46 675 5461 106565 3273158
Off label use 1113.45 36.46 447 5689 53530 3326193
Blood lactate dehydrogenase increased 1042.56 36.46 259 5877 6221 3373502
Headache 917.46 36.46 458 5678 91522 3288201
Haemoglobinuria 809.80 36.46 124 6012 125 3379598
Platelet count decreased 772.40 36.46 286 5850 27182 3352541
Unevaluable event 638.59 36.46 206 5930 12870 3366853
Pyrexia 608.80 36.46 335 5801 80780 3298943
Inappropriate schedule of drug administration 600.15 36.46 199 5937 13554 3366169
Thrombotic microangiopathy 567.52 36.46 129 6007 2063 3377660
Abdominal pain 556.29 36.46 263 5873 45962 3333761
Incorrect dose administered 507.26 36.46 176 5960 13738 3365985
Condition aggravated 492.48 36.46 230 5906 39003 3340720
Chromaturia 472.59 36.46 129 6007 4469 3375254
Transfusion 449.69 36.46 110 6026 2442 3377281
Nasopharyngitis 405.36 36.46 169 5967 21778 3357945
Dyspnoea 402.23 36.46 281 5855 102653 3277070
Death 396.78 36.46 326 5810 151998 3227725
Quality of life decreased 393.19 36.46 84 6052 988 3378735
Renal impairment 393.18 36.46 157 5979 18104 3361619
Back pain 380.42 36.46 191 5945 37814 3341909
Anaemia 337.37 36.46 199 5937 54134 3325589
Infection 333.80 36.46 154 5982 25248 3354475
Asthenia 322.39 36.46 207 5929 65458 3314265
Aplastic anaemia 317.76 36.46 75 6061 1419 3378304
Sepsis 312.84 36.46 159 5977 32214 3347509
Drug ineffective 304.41 36.46 250 5886 115840 3263883
Nausea 288.37 36.46 254 5882 129391 3250332

Pharmacologic Action:

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SourceCodeDescription
ATC L04AA25 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA EPC N0000175575 Complement Inhibitor
FDA MoA N0000175974 Complement Inhibitors

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Paroxysmal nocturnal hemoglobinuria indication 1963002 DOID:0060284
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:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Complement C5 Secreted ANTIBODY BINDING DRUG LABEL DRUG LABEL

External reference:

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IDSource
6884 IUPHAR_LIGAND_ID
D03940 KEGG_DRUG
4026032 VUID
N0000179786 NUI
C1541483 UMLSCUI
591781 RXNORM
23533 MMSL
d06673 MMSL
4026032 VANDF
426801002 SNOMEDCT_US
427429004 SNOMEDCT_US
N0000176091 NDFRT
N0000179786 NDFRT
012087 NDDF
A3ULP0F556 UNII
8231 INN_ID
CHEMBL1201828 ChEMBL_ID
DB01257 DRUGBANK_ID
C481642 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
SOLIRIS HUMAN PRESCRIPTION DRUG LABEL 1 25682-001 INJECTION, SOLUTION, CONCENTRATE 300 mg INTRAVENOUS BLA 18 sections