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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5202 1187594-09-7

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • baricitinib
  • LY3009104
  • INCB028050
  • olumiant
Baricitinib is a selective and reversible inhibitor of Janus kinase (JAK)1 and JAK2. Janus kinases (JAKs) are enzymes that transduce intracellular signals from cell surface receptors for a number of cytokines and growth factors involved in haematopoiesis, inflammation and immune function. Within the intracellular signalling pathway, JAKs phosphorylate and activate signal transducers and activators of transcription (STATs), which activate gene expression within the cell. Baricitinib modulates these signalling pathways by partially inhibiting JAK1 and JAK2 enzymatic activity, thereby reducing the phosphorylation and activation of STATs. FDA issued an Emergency use authorization (EUA) on November 19, 2020 that permits use of baricitinib in combination with remdesivir for treatment of suspected or laboratory-confirmed COVID-19 in hospitalized patients ≥2 years of age requiring supplemental oxygen, invasive mechanical ventilation, or extracorporeal membrane oxygenation (ECMO).
  • Molecular weight: 371.42
  • Formula: C16H17N7O2S
  • CLOGP: 0.48
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 1
  • TPSA: 120.56
  • ALOGS: -3.02
  • ROTB: 4
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Feb. 13, 2017 EMA Eli Lilly Nederland B.V.
May 31, 2018 FDA ELI LILLY AND CO
July 3, 2017 PMDA Eli Lilly Japan 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
Therapy interrupted 111.81 22.78 43 3012 20109 50581960
Deep vein thrombosis 80.92 22.78 52 3003 73252 50528817
COVID-19 80.03 22.78 44 3011 46618 50555451
Therapy cessation 63.18 22.78 31 3024 25980 50576089
Thrombocytosis 60.08 22.78 19 3036 4977 50597092
Pulmonary embolism 55.08 22.78 47 3008 101657 50500412
Sputum culture positive 52.45 22.78 13 3042 1401 50600668
COVID-19 pneumonia 50.42 22.78 19 3036 8376 50593693
Tooth dislocation 42.25 22.78 6 3049 26 50602043
Fibrin D dimer increased 42.21 22.78 14 3041 4258 50597811
Liver function test increased 32.81 22.78 20 3035 25586 50576483
Pneumonia haemophilus 30.81 22.78 7 3048 519 50601550
Ovarian adenoma 29.43 22.78 6 3049 266 50601803
Herpes zoster 29.00 22.78 28 3027 70758 50531311
Diverticulitis 28.08 22.78 20 3035 33162 50568907
Ultrasound Doppler abnormal 26.68 22.78 5 3050 142 50601927
Tubular breast carcinoma 25.10 22.78 4 3051 42 50602027
Pneumonia bacterial 24.84 22.78 11 3044 7298 50594771
Procedural pain 23.55 22.78 13 3042 13819 50588250

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
Pulmonary embolism 251.28 34.56 112 1701 76422 29496292
Deep vein thrombosis 162.51 34.56 76 1737 57323 29515391
COVID-19 pneumonia 58.56 34.56 22 1791 9500 29563214
Off label use 55.41 34.56 79 1734 300721 29271993
Pneumonia bacterial 51.74 34.56 20 1793 9323 29563391
Fibrin D dimer increased 50.84 34.56 15 1798 3073 29569641
Alanine aminotransferase increased 42.60 34.56 35 1778 70909 29501805
Liver function test increased 40.54 34.56 18 1795 11867 29560847
Acute respiratory failure 39.79 34.56 23 1790 26379 29546335
Aspartate aminotransferase increased 34.85 34.56 29 1784 59696 29513018

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
Pulmonary embolism 247.26 21.64 144 4424 146212 64347952
Deep vein thrombosis 211.23 21.64 116 4452 105066 64389098
Therapy interrupted 126.22 21.64 49 4519 19987 64474177
COVID-19 pneumonia 92.14 21.64 37 4531 16467 64477697
Fibrin D dimer increased 90.56 21.64 29 4539 6736 64487428
Therapy cessation 82.46 21.64 42 4526 32447 64461717
COVID-19 78.82 21.64 52 4516 65088 64429076
Pneumonia bacterial 71.31 21.64 30 4538 15005 64479159
Sputum culture positive 70.98 21.64 20 4548 3006 64491158
Liver function test increased 61.50 21.64 34 4534 30936 64463228
Tooth dislocation 41.49 21.64 6 4562 25 64494139
Alanine aminotransferase increased 41.27 21.64 50 4518 138981 64355183
Thrombocytosis 39.77 21.64 16 4552 7140 64487024
Leukocytosis 35.88 21.64 26 4542 37714 64456450
Acute respiratory failure 35.63 21.64 29 4539 49905 64444259
Lung adenocarcinoma 33.61 21.64 14 4554 6819 64487345
PaO2/FiO2 ratio decreased 33.20 21.64 5 4563 29 64494135
Herpes zoster 32.97 21.64 34 4534 79153 64415011
Aspartate aminotransferase increased 32.19 21.64 41 4527 119747 64374417
Pneumonia staphylococcal 32.12 21.64 12 4556 4394 64489770
Blood culture positive 31.71 21.64 14 4554 7854 64486310
Ovarian adenoma 30.02 21.64 6 4562 204 64493960
Lymphocyte count decreased 27.70 21.64 23 4545 40676 64453488
Staphylococcal infection 27.16 21.64 25 4543 50653 64443511
Ultrasound Doppler abnormal 25.85 21.64 5 4563 143 64494021
Pneumonia haemophilus 25.66 21.64 7 4561 933 64493231
Respiratory failure 24.23 21.64 42 4526 161141 64333023
Hypoxia 23.40 21.64 30 4538 88119 64406045
Diverticulitis intestinal perforated 23.26 21.64 4 4564 58 64494106
Leukopenia 23.10 21.64 32 4536 101210 64392954
Pulseless electrical activity 22.60 21.64 13 4555 12726 64481438

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AA37 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Selective immunosuppressants
FDA MoA N0000190857 Janus Kinase Inhibitors
FDA EPC N0000190858 Janus Kinase Inhibitor
CHEBI has role CHEBI:22587 antiviral agents
CHEBI has role CHEBI:35705 immunosuppressive agents
CHEBI has role CHEBI:35842 anti-rheumatic drugs
CHEBI has role CHEBI:67079 anti-inflammatory agents
CHEBI has role CHEBI:76617 BTK inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Atopic dermatitis indication 24079001 DOID:3310
Rheumatoid arthritis indication 69896004 DOID:7148
Pneumonia caused by Severe acute respiratory syndrome coronavirus 2 indication




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 6.49 acidic
pKa2 4.6 Basic
pKa3 1.9 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
1MG OLUMIANT ELI LILLY AND CO N207924 Oct. 8, 2019 RX TABLET ORAL 8420629 March 10, 2029 TREATMENT OF RHEUMATOID ARTHRITIS
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL 8420629 March 10, 2029 TREATMENT OF RHEUMATOID ARTHRITIS
1MG OLUMIANT ELI LILLY AND CO N207924 Oct. 8, 2019 RX TABLET ORAL 11045474 Nov. 30, 2032 TREATMENT OF CORONAVIRUS DISEASE 2019 (COVID-19) IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NON-INVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
1MG OLUMIANT ELI LILLY AND CO N207924 Oct. 8, 2019 RX TABLET ORAL 9089574 Nov. 30, 2032 TREATMENT OF CORONAVIRUS DISEASE 2019 (COVID-19) IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NON-INVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL 11045474 Nov. 30, 2032 TREATMENT OF CORONAVIRUS DISEASE 2019 (COVID-19) IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NON-INVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL 9089574 Nov. 30, 2032 TREATMENT OF CORONAVIRUS DISEASE 2019 (COVID-19) IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NON-INVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
4MG OLUMIANT ELI LILLY AND CO N207924 May 10, 2022 RX TABLET ORAL 11045474 Nov. 30, 2032 TREATMENT OF CORONAVIRUS DISEASE 2019 (COVID-19) IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NON-INVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
4MG OLUMIANT ELI LILLY AND CO N207924 May 10, 2022 RX TABLET ORAL 9089574 Nov. 30, 2032 TREATMENT OF CORONAVIRUS DISEASE 2019 (COVID-19) IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NON-INVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
1MG OLUMIANT ELI LILLY AND CO N207924 Oct. 8, 2019 RX TABLET ORAL May 31, 2023 NEW CHEMICAL ENTITY
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL May 31, 2023 NEW CHEMICAL ENTITY
4MG OLUMIANT ELI LILLY AND CO N207924 May 10, 2022 RX TABLET ORAL May 31, 2023 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Tyrosine-protein kinase JAK1 Kinase INHIBITOR IC50 8.23 SCIENTIFIC LITERATURE DRUG LABEL
Tyrosine-protein kinase JAK2 Kinase INHIBITOR IC50 8.24 SCIENTIFIC LITERATURE DRUG LABEL
Rho-associated protein kinase 1 Kinase Kd 6.32 CHEMBL
Protein kinase C beta type Kinase Kd 4.58 CHEMBL
Protein kinase C delta type Kinase Kd 5.97 CHEMBL
Rho-associated protein kinase 2 Kinase Kd 6.12 CHEMBL
Protein kinase C alpha type Kinase Kd 5.68 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta Kinase Kd 6.51 CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma Kinase Kd 6.61 CHEMBL
AP2-associated protein kinase 1 Kinase INHIBITOR Kd 7.77 IUPHAR
Serine/threonine-protein kinase MARK2 Kinase Kd 6.90 CHEMBL
Serine/threonine-protein kinase N1 Kinase Kd 6.98 CHEMBL
BMP-2-inducible protein kinase Kinase INHIBITOR Kd 7.40 IUPHAR
Dual specificity protein kinase CLK1 Kinase Kd 6.11 CHEMBL
Cyclin-G-associated kinase Kinase INHIBITOR Kd 6.87 IUPHAR
Tyrosine-protein kinase JAK3 Kinase IC50 6.10 CHEMBL
Serine/threonine-protein kinase N2 Kinase Kd 6.57 CHEMBL
Non-receptor tyrosine-protein kinase TNK1 Kinase Kd 6.21 CHEMBL
Casein kinase I isoform gamma-2 Kinase Kd 6.58 CHEMBL
cAMP-dependent protein kinase catalytic subunit alpha Kinase Kd 5.44 CHEMBL
Citron Rho-interacting kinase Kinase Kd 5.36 CHEMBL
Casein kinase I isoform gamma-1 Kinase Kd 5.76 CHEMBL
Serine/threonine-protein kinase ULK1 Kinase Kd 6.09 CHEMBL
Mitogen-activated protein kinase kinase kinase 1 Kinase Kd 5.72 CHEMBL
Eukaryotic translation initiation factor 2-alpha kinase 1 Kinase Kd 6.47 CHEMBL
Uncharacterized protein FLJ45252 Unclassified Kd 7.11 CHEMBL
Septin-9 Enzyme Kd 7.08 CHEMBL
Non-receptor tyrosine-protein kinase TYK2 Kinase INHIBITOR IC50 7.28 SCIENTIFIC LITERATURE
MAP/microtubule affinity-regulating kinase 3 Kinase Kd 6.98 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 6.01 CHEMBL

External reference:

IDSource
ISP4442I3Y UNII
C4044947 UMLSCUI
CHEBI:95341 CHEBI
3JW PDB_CHEM_ID
CHEMBL2105759 ChEMBL_ID
44205240 PUBCHEM_CID
DB11817 DRUGBANK_ID
D10308 KEGG_DRUG
7792 IUPHAR_LIGAND_ID
2047232 RXNORM
256448 MMSL
32650 MMSL
354624 MMSL
d08568 MMSL
726518002 SNOMEDCT_US
763701005 SNOMEDCT_US
4037600 VANDF
017220 NDDF
C000596027 MESH_SUPPLEMENTAL_RECORD_UI
9570 INN_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4182 TABLET, FILM COATED 2 mg ORAL NDA 33 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4182 TABLET, FILM COATED 2 mg ORAL NDA 33 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4479 TABLET, FILM COATED 4 mg ORAL NDA 33 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4732 TABLET, FILM COATED 1 mg ORAL NDA 33 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4732 TABLET, FILM COATED 1 mg ORAL NDA 33 sections
Baricitinib HUMAN PRESCRIPTION DRUG LABEL 1 0002-6885 TABLET, FILM COATED 4 mg ORAL Emergency Use Authorization 2 sections
Baricitinib HUMAN PRESCRIPTION DRUG LABEL 1 0002-6885 TABLET, FILM COATED 4 mg ORAL Emergency Use Authorization 2 sections