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 117.35 18.56 50 3983 25575 56262459
COVID-19 105.33 18.56 66 3967 74992 56213042
Deep vein thrombosis 75.01 18.56 54 3979 76923 56211111
Pulmonary embolism 63.26 18.56 56 3977 107068 56180966
Therapy cessation 56.76 18.56 31 4002 27233 56260801
Thrombocytosis 55.55 18.56 19 4014 5343 56282691
COVID-19 pneumonia 51.89 18.56 22 4011 11080 56276954
Sputum culture positive 47.57 18.56 13 4020 1726 56286308
Fibrin D dimer increased 42.80 18.56 15 4018 4532 56283502
Tooth dislocation 41.23 18.56 6 4027 26 56288008
Herpes zoster 32.04 18.56 33 4000 75856 56212178
Herpes simplex reactivation 29.97 18.56 7 4026 493 56287541
Pneumonia haemophilus 29.34 18.56 7 4026 540 56287494
Ovarian adenoma 28.34 18.56 6 4027 269 56287765
Rheumatoid arthritis 28.19 18.56 75 3958 382529 55905505
Pneumonia bacterial 28.13 18.56 13 4020 8015 56280019
Liver function test increased 27.95 18.56 20 4013 28113 56259921
Ultrasound Doppler abnormal 25.83 18.56 5 4028 142 56287892
Diverticulitis 25.74 18.56 21 4012 35831 56252203
Tubular breast carcinoma 24.08 18.56 4 4029 46 56287988
Illness 22.25 18.56 19 4014 34492 56253542
Arthrodesis 22.08 18.56 8 4025 2658 56285376
Tumour necrosis factor receptor-associated periodic syndrome 21.60 18.56 4 4029 89 56287945
Renal neoplasm 19.73 18.56 6 4027 1161 56286873
Procedural pain 19.53 18.56 13 4020 16258 56271776
Inflammatory marker increased 18.69 18.56 9 4024 6081 56281953

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 243.91 36.92 117 2119 81529 31613579
Deep vein thrombosis 153.85 36.92 78 2158 60658 31634450
Off label use 81.38 36.92 110 2126 347164 31347944
COVID-19 pneumonia 73.01 36.92 29 2207 12626 31682482
Pneumonia bacterial 53.87 36.92 22 2214 10274 31684834
Fibrin D dimer increased 51.29 36.92 16 2220 3430 31691678
Acute respiratory failure 40.50 36.92 25 2211 28030 31667078
Liver function test increased 39.98 36.92 19 2217 12695 31682413
Bronchopulmonary aspergillosis 38.72 36.92 19 2217 13615 31681493
Alanine aminotransferase increased 38.68 36.92 36 2200 74620 31620488
COVID-19 37.56 36.92 31 2205 54790 31640318

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 246.73 19.86 153 5446 155714 70767131
Deep vein thrombosis 203.88 19.86 120 5479 110922 70811923
Therapy interrupted 137.39 19.86 57 5542 24745 70898100
COVID-19 pneumonia 110.00 19.86 47 5552 21922 70900923
COVID-19 109.61 19.86 80 5519 105677 70817168
Fibrin D dimer increased 92.86 19.86 31 5568 7352 70915493
Therapy cessation 82.30 19.86 44 5555 33632 70889213
Pneumonia bacterial 78.03 19.86 34 5565 16607 70906238
Sputum culture positive 66.79 19.86 20 5579 3334 70919511
Liver function test increased 57.81 19.86 35 5564 33812 70889033
Tooth dislocation 40.83 19.86 6 5593 25 70922820
Herpes zoster 39.93 19.86 41 5558 85194 70837651
Off label use 37.57 19.86 136 5463 742924 70179921
Thrombocytosis 36.79 19.86 16 5583 7768 70915077
Alanine aminotransferase increased 36.12 19.86 51 5548 147429 70775416
Acute respiratory failure 35 19.86 31 5568 53634 70869211
Leukocytosis 34.35 19.86 27 5572 39641 70883204
PaO2/FiO2 ratio decreased 32.65 19.86 5 5594 29 70922816
Bronchopulmonary aspergillosis 31.49 19.86 20 5579 20982 70901863
Aspartate aminotransferase increased 31.21 19.86 44 5555 126934 70795911
Herpes simplex reactivation 31.02 19.86 7 5592 383 70922462
Lung adenocarcinoma 30.56 19.86 14 5585 7676 70915169
Pneumonia staphylococcal 30.36 19.86 12 5587 4586 70918259
Pneumomediastinum 30.22 19.86 11 5588 3359 70919486
Blood culture positive 30.15 19.86 14 5585 7912 70914933
Ovarian adenoma 29.28 19.86 6 5593 207 70922638
Respiratory failure 28.26 19.86 49 5550 168686 70754159
Pneumothorax spontaneous 26.64 19.86 8 5591 1345 70921500
Staphylococcal infection 25.56 19.86 26 5573 53378 70869467
Ultrasound Doppler abnormal 25.31 19.86 5 5594 143 70922702
Diverticulitis intestinal perforated 25.02 19.86 5 5594 152 70922693
Pneumonia haemophilus 24.55 19.86 7 5592 983 70921862
Lymphocyte count decreased 24.19 19.86 23 5576 43516 70879329
Illness 24.05 19.86 20 5579 31771 70891074
Arthrodesis 22.56 19.86 8 5591 2265 70920580
Hypoxia 22.42 19.86 32 5567 93312 70829533
Tumour necrosis factor receptor-associated periodic syndrome 21.17 19.86 4 5595 90 70922755
Pulseless electrical activity 20.85 19.86 13 5586 13202 70909643
Septic shock 20.64 19.86 34 5565 112224 70810621
Rheumatoid arthritis 20.60 19.86 60 5539 291745 70631100
Leukopenia 20.57 19.86 33 5566 106527 70816318
Lymphopenia 20.26 19.86 17 5582 27342 70895503

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
Alopecia areata indication 68225006 DOID:986
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
1MG OLUMIANT ELI LILLY AND CO N207924 Oct. 8, 2019 RX TABLET ORAL May 10, 2025 TREATMENT OF COVID-19 IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NONINVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL May 10, 2025 TREATMENT OF COVID-19 IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NONINVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
4MG OLUMIANT ELI LILLY AND CO N207924 May 10, 2022 RX TABLET ORAL May 10, 2025 TREATMENT OF COVID-19 IN HOSPITALIZED ADULTS REQUIRING SUPPLEMENTAL OXYGEN, NONINVASIVE OR INVASIVE MECHANICAL VENTILATION, OR EXTRACORPOREAL MEMBRANE OXYGENATION (ECMO)
1MG OLUMIANT ELI LILLY AND CO N207924 Oct. 8, 2019 RX TABLET ORAL June 13, 2025 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL June 13, 2025 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA
4MG OLUMIANT ELI LILLY AND CO N207924 May 10, 2022 RX TABLET ORAL June 13, 2025 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA

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
9570 INN_ID
7792 IUPHAR_LIGAND_ID
256448 MMSL
32650 MMSL
354624 MMSL
d08568 MMSL
017220 NDDF
726518002 SNOMEDCT_US
763701005 SNOMEDCT_US
4037600 VANDF
C000596027 MESH_SUPPLEMENTAL_RECORD_UI
2047232 RXNORM

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4182 TABLET, FILM COATED 2 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4182 TABLET, FILM COATED 2 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4182 TABLET, FILM COATED 2 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4479 TABLET, FILM COATED 4 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4479 TABLET, FILM COATED 4 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4732 TABLET, FILM COATED 1 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4732 TABLET, FILM COATED 1 mg ORAL NDA 34 sections
Olumiant HUMAN PRESCRIPTION DRUG LABEL 1 0002-4732 TABLET, FILM COATED 1 mg ORAL NDA 34 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