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

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 302.47 46.50 114 453 101510 2256008
Joint swelling 229.30 46.50 61 506 16758 2340760
Rheumatoid arthritis 207.53 46.50 58 509 19082 2338436
Contraindicated product administered 177.11 46.50 36 531 2985 2354533
Rash 171.36 46.50 66 501 59492 2298026
Synovitis 145.04 46.50 30 537 2696 2354822
Injection site reaction 141.74 46.50 41 526 15011 2342507
Treatment failure 140.72 46.50 35 532 7204 2350314
Anti-cyclic citrullinated peptide antibody positive 140.30 46.50 20 547 183 2357335
Therapeutic product effect decreased 131.52 46.50 36 531 10753 2346765
Arthralgia 120.14 46.50 50 517 54235 2303283
Pemphigus 116.26 46.50 20 547 656 2356862
Hypersensitivity 115.56 46.50 39 528 23554 2333964
Rheumatoid factor positive 114.73 46.50 19 548 493 2357025
Hand deformity 106.79 46.50 20 547 1066 2356452
Drug intolerance 105.47 46.50 32 535 13685 2343833
Hepatic enzyme increased 97.79 46.50 28 539 9774 2347744
Glossodynia 95.16 46.50 20 547 1925 2355593
Alopecia 94.46 46.50 33 534 21968 2335550
Wound 88.42 46.50 20 547 2708 2354810
Injection site erythema 86.82 46.50 33 534 27854 2329664
Systemic lupus erythematosus 84.76 46.50 21 546 4200 2353318
Hip arthroplasty 78.54 46.50 17 550 1877 2355641
Knee arthroplasty 76.35 46.50 18 549 2917 2354601
Arthropathy 73.31 46.50 21 546 7295 2350223
Swelling 71.86 46.50 25 542 16325 2341193
Nonalcoholic fatty liver disease 67.78 46.50 9 558 45 2357473
Pain 67.33 46.50 35 532 61822 2295696
Pruritus 66.44 46.50 31 536 43309 2314209
Fatigue 62.20 46.50 37 530 84836 2272682
Nausea 59.93 46.50 40 527 112149 2245369
Abdominal discomfort 59.02 46.50 22 545 17434 2340084
Infusion related reaction 58.95 46.50 19 548 9777 2347741
Injection site swelling 58.27 46.50 21 546 15130 2342388
Live birth 55.80 46.50 12 555 1279 2356239
Oral discomfort 55.69 46.50 12 555 1291 2356227
Condition aggravated 49.26 46.50 23 544 31956 2325562
Pericarditis 48.26 46.50 11 556 1529 2355989
Discomfort 48.01 46.50 14 553 5145 2352373
Product use issue 47.24 46.50 17 550 12152 2345366
Herpes zoster 47.01 46.50 16 551 9709 2347809

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

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

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

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5908 INJECTION, SOLUTION 150 mg SUBCUTANEOUS BLA 19 sections
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5910 INJECTION, SOLUTION 200 mg SUBCUTANEOUS BLA 19 sections
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5920 INJECTION, SOLUTION 150 mg SUBCUTANEOUS BLA 19 sections
KEVZARA HUMAN PRESCRIPTION DRUG LABEL 1 0024-5922 INJECTION, SOLUTION 200 mg SUBCUTANEOUS BLA 19 sections