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

Stem definitionDrug idCAS RN
interleukin receptor antagonists 5017 143090-92-0

Description:

MoleculeDescription

Synonyms:

  • anakinra
  • kineret
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA. As IL-1 levels are elevated in patients with COVID-19, anakinra is currently being investigated for its potential to combat cytokine release syndrome (CRS) in patients with severely ill COVID-19.
  • Molecular weight: 17257.66
  • Formula: C759H1186N208O232S10
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 7115.02
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
0.10 g P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
March 8, 2002 EMA
Nov. 14, 2001 FDA BIOVITRUM AB

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
Drug ineffective 724.65 28.19 1144 19061 676694 45989163
Rheumatoid arthritis 526.67 28.19 580 19625 239635 46426222
Synovitis 496.57 28.19 316 19889 60759 46605098
Mobility decreased 343.43 28.19 251 19954 60343 46605514
Joint swelling 342.28 28.19 389 19816 165684 46500173
Red blood cell sedimentation rate abnormal 315.88 28.19 142 20063 13507 46652350
Arthropathy 315.22 28.19 274 19931 84426 46581431
Oral mucosal exfoliation 303.18 28.19 80 20125 1473 46664384
Drug intolerance 302.06 28.19 344 19861 146705 46519152
Body height below normal 299.03 28.19 82 20123 1757 46664100
Bone density decreased 289.62 28.19 121 20084 9631 46656226
Contraindicated product administered 274.21 28.19 247 19958 79700 46586157
Human antichimeric antibody positive 272.93 28.19 72 20133 1324 46664533
Juvenile idiopathic arthritis 268.58 28.19 91 20114 4041 46661816
Ill-defined disorder 266.63 28.19 158 20047 26669 46639188
Haemophagocytic lymphohistiocytosis 262.90 28.19 108 20097 8234 46657623
Rheumatoid factor positive 247.50 28.19 137 20068 20324 46645533
Cutaneous vasculitis 244.18 28.19 84 20121 3907 46661950
Therapeutic product effect decreased 227.40 28.19 226 19979 82375 46583482
Soft tissue disorder 224.99 28.19 80 20125 4106 46661751
Treatment failure 211.86 28.19 230 19975 92857 46573000
Herpes zoster 204.17 28.19 195 20010 67677 46598180
Deformity 195.36 28.19 84 20121 7173 46658684
Off label use 187.28 28.19 467 19738 379374 46286483
Polyarthritis 186.94 28.19 79 20126 6463 46659394
Liver function test abnormal 180.00 28.19 154 20051 46333 46619524
Adrenal insufficiency 178.49 28.19 95 20110 13029 46652828
Fine motor skill dysfunction 177.43 28.19 65 20140 3635 46662222
Therapeutic product effect incomplete 175.82 28.19 192 20013 77961 46587896
Red blood cell sedimentation rate increased 174.68 28.19 114 20091 22775 46643082
Obesity 171.43 28.19 95 20110 14111 46651746
Secretion discharge 164.00 28.19 80 20125 9139 46656718
Arthritis 161.95 28.19 183 20022 77133 46588724
Musculoskeletal disorder 155.54 28.19 92 20113 15453 46650404
Infection 144.75 28.19 229 19976 133363 46532494
Pneumonia viral 140.84 28.19 65 20140 6559 46659298
Loss of consciousness 137.73 28.19 200 20005 108038 46557819
Drug specific antibody 136.71 28.19 41 20164 1219 46664638
Hepatosplenic T-cell lymphoma 135.33 28.19 35 20170 593 46665264
Joint destruction 129.25 28.19 49 20156 3015 46662842
Wheelchair user 123.23 28.19 51 20154 3957 46661900
Ankle operation 121.01 28.19 37 20168 1176 46664681
Adenovirus infection 118.45 28.19 45 20160 2785 46663072
Spinal stenosis 114.51 28.19 70 20135 12473 46653384
Antibody test positive 111.13 28.19 40 20165 2125 46663732
Vasculitic rash 109.90 28.19 35 20170 1275 46664582
Impaired quality of life 109.05 28.19 44 20161 3198 46662659
Arthralgia 105.97 28.19 372 19833 364231 46301626
Growth failure 104.59 28.19 25 20180 301 46665556
Therapy non-responder 101.07 28.19 106 20099 41046 46624811
Arthrodesis 91.16 28.19 35 20170 2229 46663628
Smear cervix abnormal 91.06 28.19 36 20169 2480 46663377
Condition aggravated 89.03 28.19 270 19935 244782 46421075
Ankle arthroplasty 88.84 28.19 25 20180 590 46665267
Fibromyalgia 87.89 28.19 93 20112 36370 46629487
Fall 85.53 28.19 19 20186 329078 46336779
Septic shock 83.98 28.19 114 20091 57779 46608078
C-reactive protein increased 79.91 28.19 112 20093 58478 46607379
C-reactive protein abnormal 79.28 28.19 69 20136 21201 46644656
Infiltration anaesthesia 77.73 28.19 17 20188 133 46665724
Sensitivity to weather change 75.17 28.19 40 20165 5476 46660381
Asthenia 74.93 28.19 21 20184 311054 46354803
Loss of personal independence in daily activities 74.57 28.19 107 20098 57076 46608781
Blood cholesterol increased 74.13 28.19 89 20116 39924 46625933
Complications of bone marrow transplant 67.86 28.19 19 20186 440 46665417
Shoulder arthroplasty 67.63 28.19 31 20174 3077 46662780
Headache 67.23 28.19 65 20140 478287 46187570
Viraemia 64.15 28.19 22 20183 1012 46664845
Clubbing 61.54 28.19 16 20189 277 46665580
Nodule 60.95 28.19 52 20153 15553 46650304
Death 59.31 28.19 36 20169 335512 46330345
Leukopenia 57.75 28.19 105 20100 68238 46597619
Fatigue 57.08 28.19 111 20094 608586 46057271
Body tinea 54.55 28.19 19 20186 916 46664941
Dyspnoea 53.70 28.19 88 20117 515460 46150397
Skin fissures 53.12 28.19 36 20169 7644 46658213
Back disorder 51.95 28.19 38 20167 9103 46656754
Swelling 51.63 28.19 144 20061 124367 46541490
Confusional state 51.16 28.19 5 20200 159887 46505970
Epstein-Barr viraemia 50.92 28.19 17 20188 720 46665137
Hepatitis 50.62 28.19 66 20139 32149 46633708
Constipation 49.52 28.19 8 20197 174089 46491768
Impaired healing 48.24 28.19 69 20136 36674 46629183
Quality of life decreased 47.42 28.19 30 20175 5672 46660185
Joint arthroplasty 46.57 28.19 21 20184 2006 46663851
Psoriasis 46.36 28.19 104 20101 78500 46587357
Injection site reaction 46.23 28.19 78 20127 47771 46618086
Anxiety 46.21 28.19 11 20194 181946 46483911
Immunodeficiency 45.80 28.19 41 20164 13065 46652792
Serum amyloid A protein increased 45.75 28.19 10 20195 78 46665779
Pneumonia 45.26 28.19 58 20147 376262 46289595
Decreased appetite 44.94 28.19 14 20191 193822 46472035
Hair follicle tumour benign 43.91 28.19 13 20192 369 46665488
Dehydration 43.90 28.19 8 20197 159532 46506325
Gastroenteritis viral 43.26 28.19 46 20159 18073 46647784
Pain in extremity 42.61 28.19 30 20175 258650 46407207
Weight decreased 42.57 28.19 19 20186 210830 46455027
Liver function test increased 41.00 28.19 50 20155 22776 46643081
Somnolence 40.66 28.19 9 20196 156512 46509345
Osteomyelitis 40.16 28.19 49 20156 22334 46643523
Toxicity to various agents 39.83 28.19 21 20184 211745 46454112
Adrenal suppression 39.35 28.19 15 20190 936 46664921
Infection susceptibility increased 39.01 28.19 19 20186 2160 46663697
Tremor 38.66 28.19 3 20202 115636 46550221
Foot deformity 38.32 28.19 40 20165 15385 46650472
Knee arthroplasty 37.98 28.19 49 20156 23616 46642241
Varicella zoster virus infection 37.70 28.19 19 20186 2324 46663533
Pulmonary fibrosis 37.70 28.19 45 20160 20047 46645810
Inhibitory drug interaction 37.54 28.19 18 20187 1977 46663880
Endodontic procedure 36.65 28.19 19 20186 2466 46663391
Laryngeal stenosis 36.36 28.19 13 20192 677 46665180
Human anti-human antibody test 36.23 28.19 11 20194 341 46665516
Human herpesvirus 6 infection 34.12 28.19 18 20187 2421 46663436
Cough 33.76 28.19 30 20175 230219 46435638
Overdose 33.11 28.19 3 20202 101976 46563881
Finger deformity 32.87 28.19 23 20182 5139 46660718
Cerebrovascular accident 32.73 28.19 3 20202 101036 46564821
Hypoaesthesia 32.60 28.19 6 20199 118863 46546994
Interstitial lung disease 32.49 28.19 72 20133 53877 46611980
Platelet count decreased 32.32 28.19 3 20202 100021 46565836
Osteoarthritis 32.11 28.19 78 20127 61947 46603910
Mouth ulceration 31.76 28.19 48 20157 26784 46639073
Peripheral swelling 31.73 28.19 144 20061 157927 46507930
Hand deformity 31.60 28.19 55 20150 34519 46631338
Encephalitis viral 31.57 28.19 15 20190 1615 46664242
Abdominal discomfort 31.48 28.19 13 20192 151152 46514705
Diaphragm muscle weakness 31.46 28.19 6 20199 21 46665836
Post transplant lymphoproliferative disorder 31.35 28.19 20 20185 3836 46662021
Foot operation 29.92 28.19 21 20184 4716 46661141
Soft tissue swelling 29.55 28.19 12 20193 886 46664971
Toothache 29.24 28.19 36 20169 16556 46649301
Abdominal pain 29.13 28.19 34 20171 229997 46435860
Drug interaction 29.12 28.19 27 20178 203067 46462790
Myocardial infarction 28.82 28.19 4 20201 97524 46568333
Neuropathy peripheral 28.65 28.19 3 20202 90890 46574967
Drug hypersensitivity 28.63 28.19 192 20013 243633 46422224
Oedema peripheral 28.34 28.19 17 20188 159689 46506168
Embolism 28.30 28.19 24 20181 7114 46658743

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
Apparent death 973.25 40.82 216 7344 3326 29941592
Diverticulitis 679.67 40.82 228 7332 17217 29927701
Joint swelling 482.20 40.82 235 7325 46711 29898207
Off label use 439.18 40.82 415 7145 248875 29696043
Deep vein thrombosis 398.50 40.82 225 7335 60276 29884642
Pulmonary embolism 357.65 40.82 230 7330 77905 29867013
Pulmonary thrombosis 349.20 40.82 108 7452 6235 29938683
Red blood cell sedimentation rate increased 330.25 40.82 107 7453 7188 29937730
Renal failure 260.84 40.82 233 7327 128733 29816185
Drug ineffective 255.67 40.82 366 7194 340021 29604897
Terminal state 243.98 40.82 72 7488 3532 29941386
C-reactive protein abnormal 236.73 40.82 78 7482 5515 29939403
Pain 213.91 40.82 239 7321 172402 29772516
Rheumatoid arthritis 209.72 40.82 130 7430 41067 29903851
Drug specific antibody present 207.12 40.82 56 7504 1991 29942927
Contraindicated product administered 196.70 40.82 93 7467 17138 29927780
Acne cystic 179.95 40.82 38 7522 451 29944467
Haemophagocytic lymphohistiocytosis 166.84 40.82 70 7490 9721 29935197
Thrombosis 165.15 40.82 113 7447 42118 29902800
Intentional product use issue 141.22 40.82 97 7463 36343 29908575
Drug use disorder 140.21 40.82 46 7514 3202 29941716
Photosensitivity reaction 137.86 40.82 61 7499 9633 29935285
Drug intolerance 135.42 40.82 103 7457 45188 29899730
C-reactive protein increased 125.86 40.82 97 7463 43376 29901542
Joint arthroplasty 117.13 40.82 28 7532 599 29944319
Sepsis 112.46 40.82 160 7400 146235 29798683
Intestinal sepsis 110.62 40.82 25 7535 414 29944504
Gait inability 89.51 40.82 57 7503 18784 29926134
Arthropathy 84.55 40.82 57 7503 20670 29924248
Herpes zoster 80.49 40.82 64 7496 29879 29915039
Meningitis viral 78.78 40.82 21 7539 705 29944213
Treatment failure 74.29 40.82 65 7495 34614 29910304
Urticaria 73.00 40.82 79 7481 54527 29890391
Propionibacterium infection 71.78 40.82 16 7544 248 29944670
Stomatitis 62.61 40.82 61 7499 37218 29907700
Interstitial lung disease 60.18 40.82 75 7485 60122 29884796
Stent placement 59.18 40.82 27 7533 4569 29940349
Post transplant lymphoproliferative disorder 58.51 40.82 28 7532 5278 29939640
Central nervous system lymphoma 56.98 40.82 17 7543 863 29944055
Knee arthroplasty 56.93 40.82 28 7532 5602 29939316
Dyspnoea 55.38 40.82 9 7551 333286 29611632
Drug dependence 53.98 40.82 44 7516 21251 29923667
Therapeutic product effect decreased 51.49 40.82 49 7511 29027 29915891
Drug hypersensitivity 46.76 40.82 71 7489 68448 29876470
Feeling abnormal 44.79 40.82 63 7497 56693 29888225
Transplant failure 42.94 40.82 18 7542 2486 29942432

Pharmacologic Action:

SourceCodeDescription
ATC L04AC03 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Interleukin inhibitors
FDA MoA N0000175709 Interleukin 1 Receptor Antagonists
FDA EPC N0000175710 Interleukin-1 Receptor Antagonist
MeSH PA D018501 Antirheumatic Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Rheumatoid arthritis indication 69896004 DOID:7148
Chronic infantile neurological, cutaneous and articular syndrome indication 239826001
Cryopyrin associated periodic syndrome indication 430079001

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
Interleukin-1 receptor, type I Membrane receptor ANTAGONIST Kd 7.82 IUPHAR DRUG LABEL

External reference:

IDSource
9013DUQ28K UNII
D02934 KEGG_DRUG
4021281 VUID
N0000179382 NUI
4021281 VANDF
C0245109 UMLSCUI
CHEMBL1201570 ChEMBL_ID
DB00026 DRUGBANK_ID
D053590 MESH_DESCRIPTOR_UI
139595263 PUBCHEM_CID
7137 INN_ID
6972 IUPHAR_LIGAND_ID
352734 RXNORM
16200 MMSL
42416 MMSL
d04775 MMSL
009431 NDDF
009432 NDDF
385549000 SNOMEDCT_US
395279009 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Kineret HUMAN PRESCRIPTION DRUG LABEL 1 66658-234 INJECTION, SOLUTION 100 mg SUBCUTANEOUS BLA 29 sections