sarilumab 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
human origin 5237 1189541-98-7

Description:

MoleculeDescription

Synonyms:

  • sarilumab
  • REGN88
  • SAR153191
  • kevzara
Sarilumab is a human recombinant monoclonal antibody of the IgG1 subclass. Sarilumab is produced by recombinant DNA technology in Chinese Hamster Ovary cell suspension culture. Sarilumab binds to both soluble and membrane-bound IL-6 receptors (sIL-6R and mIL-6R), and has been shown to inhibit IL-6-mediated signaling through these receptors. IL-6 is a pleiotropic pro-inflammatory cytokine produced by a variety of cell types including T- and B-cells, lymphocytes, monocytes, and fibroblasts. IL-6 has been shown to be involved in diverse physiological processes such as T-cell activation, induction of immunoglobulin secretion, initiation of hepatic acute phase protein synthesis, and stimulation of hematopoietic precursor cell proliferation and differentiation. IL-6 is also produced by synovial and endothelial cells leading to local production of IL-6 in joints affected by inflammatory processes such as rheumatoid arthritis. Based on encouraging results in China with a similar drug, tocilizumab, a phase 2/3 US study evaluating efficacy and safety of sarilumab in patients hospitalized with severe COVID-19 was performed. At the moment, there are insufficient data to recommend either for or against use of sarilumab for hospitalized patients with COVID-19.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

DoseUnitRoute
14.30 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 23, 2017 EMA sanofi-aventis groupe
May 22, 2017 FDA SANOFI SYNTHELABO
Sept. 27, 2017 PMDA SANOFI KK

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
Rheumatoid factor positive 1414.09 62.46 710 37771 49149 50517494
Anti-cyclic citrullinated peptide antibody positive 1343.92 62.46 771 37710 69816 50496827
Hand deformity 1098.27 62.46 772 37709 99427 50467216
Wound 1092.54 62.46 786 37695 105008 50461635
Synovitis 1053.39 62.46 819 37662 123046 50443597
Glossodynia 1014.94 62.46 779 37702 114790 50451853
Pericarditis 1013.20 62.46 670 37811 78019 50488624
Hepatic enzyme increased 986.98 62.46 823 37658 136557 50430086
Pemphigus 983.67 62.46 777 37704 119389 50447254
Discomfort 959.05 62.46 734 37747 107646 50458997
Systemic lupus erythematosus 925.20 62.46 801 37680 139821 50426822
Joint swelling 903.50 62.46 1017 37464 244269 50322374
Arthropathy 760.36 62.46 756 37725 157150 50409493
Infusion related reaction 756.67 62.46 779 37702 168778 50397865
Drug intolerance 681.68 62.46 834 37647 218270 50348373
Swelling 634.94 62.46 771 37710 200101 50366542
Abdominal discomfort 614.99 62.46 815 37666 230826 50335817
Treatment failure 612.74 62.46 632 37849 137005 50429638
Alopecia 612.29 62.46 837 37644 244210 50322433
Contraindicated product administered 557.46 62.46 624 37857 148334 50418309
Maternal exposure during pregnancy 546.75 62.46 639 37842 159139 50407504
Product use issue 525.06 62.46 606 37875 148869 50417774
Hypersensitivity 514.53 62.46 720 37761 214441 50352202
Duodenal ulcer perforation 460.60 62.46 335 38146 45276 50521367
Helicobacter infection 450.31 62.46 342 38139 49360 50517283
Condition aggravated 420.31 62.46 783 37698 296275 50270368
Hip arthroplasty 385.60 62.46 257 38224 30172 50536471
Rash 330.63 62.46 898 37583 436573 50130070
Knee arthroplasty 318.68 62.46 244 38237 35602 50531041
Rheumatic fever 311.31 62.46 181 38300 16686 50549957
Swollen joint count increased 291.55 62.46 166 38315 14707 50551936
Therapeutic product effect decreased 253.74 62.46 406 38075 135644 50430999
Pain 249.17 62.46 981 37500 577922 49988721
General physical health deterioration 243.94 62.46 409 38072 142025 50424618
Blister 238.67 62.46 309 38172 85109 50481534
Death 223.68 62.46 5 38476 325374 50241269
Drug ineffective 206.04 62.46 1188 37293 818145 49748498
Type 2 diabetes mellitus 199.59 62.46 183 38298 34192 50532451
Blood cholesterol increased 186.78 62.46 220 38261 54995 50511648
Fall 184.52 62.46 20 38461 334912 50231731
Diarrhoea 159.36 62.46 129 38352 588347 49978296
Acute kidney injury 158.63 62.46 3 38478 228055 50338588
Anaemia 155.87 62.46 9 38472 252447 50314196
Musculoskeletal stiffness 154.44 62.46 317 38164 128164 50438479
Hypotension 153.07 62.46 6 38475 235463 50331180
Dyspnoea 145.77 62.46 122 38359 547486 50019157
Adverse drug reaction 142.13 62.46 192 38289 55030 50511613
Toxicity to various agents 139.53 62.46 5 38476 212494 50354149
Intentional product use issue 136.98 62.46 225 38256 76693 50489950
Injury 136.53 62.46 177 38304 48748 50517895
Back pain 124.01 62.46 12 38469 220018 50346625
Live birth 120.71 62.46 100 38381 16308 50550335
Asthenia 118.96 62.46 47 38434 318995 50247648
Adverse event 113.87 62.46 153 38328 43610 50523033
Constipation 113.42 62.46 7 38474 185701 50380942
Cough 108.96 62.46 25 38456 241239 50325404
Oral discomfort 107.01 62.46 70 38411 7947 50558696
Arthralgia 102.10 62.46 625 37856 438077 50128566
Vomiting 89.16 62.46 133 38348 460625 50106018
Weight decreased 86.76 62.46 30 38451 221215 50345428
Pneumonia 85.75 62.46 97 38384 378304 50188339
Product use in unapproved indication 84.98 62.46 236 38245 115583 50451060
Insomnia 81.18 62.46 17 38464 174848 50391795
Haemoglobin decreased 80.11 62.46 4 38477 127212 50439431
Blood pressure increased 78.40 62.46 6 38475 133126 50433517
Mobility decreased 77.46 62.46 181 38300 79767 50486876
Urinary tract infection 77.08 62.46 37 38444 223983 50342660
Seizure 76.54 62.46 3 38478 117871 50448772
Drug tolerance decreased 76.21 62.46 60 38421 9100 50557543
Fatigue 75.70 62.46 845 37636 706756 49859887
Anxiety 73.30 62.46 22 38459 177584 50389059
Thrombocytopenia 71.78 62.46 7 38474 127666 50438977
Tremor 71.13 62.46 4 38477 114899 50451744
Feeling abnormal 70.24 62.46 7 38474 125485 50441158
Dizziness 69.85 62.46 97 38384 346272 50220371
Pyrexia 69.42 62.46 114 38367 380089 50186554
Irritable bowel syndrome 67.78 62.46 132 38349 51309 50515334
Abdominal pain 67.20 62.46 49 38432 236179 50330464
Atrial fibrillation 64.69 62.46 3 38478 101742 50464901
Myalgia 64.46 62.46 9 38472 124310 50442333
Sleep disorder due to general medical condition, insomnia type 64.22 62.46 98 38383 31349 50535294
Nausea 63.99 62.46 298 38183 705100 49861543
Liver injury 63.40 62.46 86 38395 24720 50541923
Tachycardia 63.24 62.46 3 38478 99760 50466883
Retinitis 62.65 62.46 30 38451 1857 50564786

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
Joint swelling 83.21 41.15 37 872 49593 29524025
Arthralgia 63.59 41.15 44 865 139573 29434045
Drug ineffective 60.51 41.15 64 845 363106 29210512
Pain 49.11 41.15 41 868 171391 29402227

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
Rheumatoid factor positive 1089.13 61.87 439 25523 34499 64438271
Anti-cyclic citrullinated peptide antibody positive 1045.21 61.87 472 25490 49090 64423680
Pemphigus 945.00 61.87 469 25493 60232 64412538
Hand deformity 935.97 61.87 471 25491 62300 64410470
Wound 931.68 61.87 501 25461 75976 64396794
Systemic lupus erythematosus 924.74 61.87 501 25461 77111 64395659
Glossodynia 913.78 61.87 468 25494 64228 64408542
Synovitis 831.29 61.87 509 25453 98581 64374189
Pericarditis 818.84 61.87 430 25532 62086 64410684
Discomfort 754.59 61.87 445 25517 80433 64392337
Joint swelling 734.08 61.87 641 25321 214741 64258029
Hepatic enzyme increased 707.81 61.87 510 25452 129433 64343337
Arthropathy 691.51 61.87 489 25473 120478 64352292
Alopecia 608.29 61.87 515 25447 165175 64307595
Swelling 590.15 61.87 499 25463 159719 64313051
Abdominal discomfort 528.62 61.87 496 25466 181826 64290944
Contraindicated product administered 527.55 61.87 397 25565 107432 64365338
Maternal exposure during pregnancy 525.34 61.87 378 25584 95506 64377264
Infusion related reaction 518.61 61.87 469 25493 163998 64308772
Drug intolerance 515.68 61.87 496 25466 187496 64285274
Treatment failure 471.64 61.87 384 25578 116432 64356338
Hypersensitivity 407.23 61.87 446 25516 196006 64276764
Product use issue 403.78 61.87 394 25568 151321 64321449
Helicobacter infection 378.03 61.87 219 25743 38143 64434627
Duodenal ulcer perforation 377.04 61.87 211 25751 34414 64438356
Hip arthroplasty 322.76 61.87 162 25800 21189 64451581
Blister 282.68 61.87 245 25717 80722 64392048
Condition aggravated 266.87 61.87 510 25452 371916 64100854
Knee arthroplasty 262.89 61.87 153 25809 26846 64445924
Pain 249.84 61.87 629 25333 552882 63919888
Rash 247.73 61.87 559 25403 457990 64014780
Rheumatic fever 239.10 61.87 102 25860 9192 64463578
Therapeutic product effect decreased 231.77 61.87 258 25704 115093 64357677
Swollen joint count increased 216.54 61.87 90 25872 7599 64465171
Drug ineffective 185.60 61.87 746 25216 839501 63633269
Death 171.69 61.87 5 25957 482700 63990070
Acute kidney injury 158.49 61.87 5 25957 449235 64023535
Type 2 diabetes mellitus 147.89 61.87 117 25845 33903 64438867
General physical health deterioration 143.47 61.87 278 25684 204147 64268623
Blood cholesterol increased 138.37 61.87 133 25829 49933 64422837
Adverse drug reaction 137.56 61.87 127 25835 45337 64427433
Drug interaction 131.49 61.87 3 25959 362080 64110690
Adverse event 130.65 61.87 116 25846 39373 64433397
Hypotension 128.32 61.87 6 25956 380968 64091802
Injury 127.65 61.87 134 25828 55858 64416912
Irritable bowel syndrome 124.08 61.87 110 25852 37259 64435511
Musculoskeletal stiffness 121.99 61.87 195 25767 123011 64349759
Arthralgia 119.67 61.87 420 25542 441840 64030930
Live birth 113.01 61.87 65 25897 11139 64461631
Anaemia 112.90 61.87 11 25951 378669 64094101
Fall 110.03 61.87 18 25944 416808 64055962
Intentional product use issue 109.95 61.87 162 25800 95202 64377568
Sleep disorder due to general medical condition, insomnia type 109.16 61.87 88 25874 26182 64446588
Exposure during pregnancy 107.44 61.87 144 25818 77531 64395239
Muscle injury 88.10 61.87 78 25884 26359 64446411
Dyspnoea 85.91 61.87 98 25864 718576 63754194
Folliculitis 81.37 61.87 79 25883 29998 64442772
Mobility decreased 78.32 61.87 131 25831 85709 64387061
Constipation 75.91 61.87 4 25958 229333 64243437
Asthenia 75.70 61.87 39 25923 428005 64044765
Retinitis 74.59 61.87 29 25933 2056 64470714
Pneumonia 73.90 61.87 70 25892 559506 63913264
Ill-defined disorder 70.80 61.87 88 25874 43964 64428806
Diarrhoea 70.72 61.87 114 25848 722590 63750180
Somnolence 69.17 61.87 3 25959 203642 64269128
Fibromyalgia 66.65 61.87 77 25885 35654 64437116
Back pain 65.50 61.87 11 25951 250160 64222610
Oral discomfort 64.69 61.87 41 25921 8365 64464405
Fatigue 64.30 61.87 517 25445 748213 63724557
Cough 63.93 61.87 21 25941 302127 64170643
Product use in unapproved indication 62.32 61.87 184 25778 176434 64296336

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AC14 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Interleukin inhibitors
FDA MoA N0000190478 Interleukin 6 Receptor Antagonists
FDA EPC N0000190480 Interleukin-6 Receptor Antagonist

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Rheumatoid arthritis indication 69896004 DOID:7148
Bacterial infectious disease contraindication 87628006




🐶 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
Interleukin-6 receptor Membrane receptor ANTIBODY BINDING Kd 11.10 IUPHAR DRUG LABEL

External reference:

IDSource
NU90V55F8I UNII
C3885145 UMLSCUI
CHEMBL2108730 ChEMBL_ID
DB11767 DRUGBANK_ID
D10161 KEGG_DRUG
7999 IUPHAR_LIGAND_ID
1923319 RXNORM
257686 MMSL
32766 MMSL
d08592 MMSL
735231009 SNOMEDCT_US
763522001 SNOMEDCT_US
4036706 VANDF
017137 NDDF
C000592401 MESH_SUPPLEMENTAL_RECORD_UI
9476 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5908 INJECTION, SOLUTION 150 mg SUBCUTANEOUS BLA 28 sections
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5910 INJECTION, SOLUTION 200 mg SUBCUTANEOUS BLA 28 sections
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5920 INJECTION, SOLUTION 150 mg SUBCUTANEOUS BLA 28 sections
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5922 INJECTION, SOLUTION 200 mg SUBCUTANEOUS BLA 28 sections