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
3 mg O

ADMET properties:

PropertyValueReference
S (Water solubility) 0.04 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Bocci G, Oprea TI, Benet LZ

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 201.14 19.45 81 4981 32374 63451586
COVID-19 113.03 19.45 84 4978 113019 63370941
Thrombocytosis 71.23 19.45 24 5038 5794 63478166
Deep vein thrombosis 69.98 19.45 56 5006 83744 63400216
Pulmonary embolism 57.68 19.45 58 5004 116626 63367334
COVID-19 pneumonia 56.66 19.45 26 5036 14183 63469777
Therapy cessation 50.46 19.45 31 5031 30426 63453534
Fibrin D dimer increased 43.39 19.45 16 5046 5018 63478942
Sputum culture positive 43.36 19.45 13 5049 2154 63481806
Tooth dislocation 39.88 19.45 6 5056 30 63483930
Herpes zoster 37.11 19.45 39 5023 82423 63401537
Leukopenia 35.58 19.45 37 5025 77253 63406707
Illness 35.10 19.45 30 5032 49029 63434931
Ovarian adenoma 32.55 19.45 7 5055 303 63483657
Cervicobrachial syndrome 29.14 19.45 8 5054 969 63482991
Transaminases increased 28.38 19.45 22 5040 31345 63452615
Herpes simplex reactivation 28.34 19.45 7 5055 561 63483399
Pneumonia haemophilus 27.14 19.45 7 5055 668 63483292
Ultrasound Doppler abnormal 24.81 19.45 5 5057 157 63483803
Pneumonia bacterial 24.77 19.45 13 5049 9452 63474508
Diverticulitis 23.92 19.45 22 5040 39535 63444425
Tubular breast carcinoma 23.65 19.45 4 5058 46 63483914
Sudden death 23.57 19.45 13 5049 10436 63473524
Normochromic normocytic anaemia 23.36 19.45 10 5052 4626 63479334
Liver function test increased 23.33 19.45 20 5042 32791 63451169
Immunodeficiency common variable 22.81 19.45 5 5057 237 63483723
Lymph node tuberculosis 21.34 19.45 6 5056 793 63483167
Tumour necrosis factor receptor-associated periodic syndrome 21.30 19.45 4 5058 86 63483874
Chondrocalcinosis 20.92 19.45 6 5056 852 63483108
Arthrodesis 20.86 19.45 8 5054 2793 63481167
Foeticide 19.94 19.45 3 5059 15 63483945
Inflammatory marker increased 19.65 19.45 10 5052 6829 63477131

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 223.36 31.75 117 2571 89629 34864614
Deep vein thrombosis 170.39 31.75 88 2600 65160 34889083
Off label use 103.01 31.75 142 2546 419382 34534861
Pneumonia bacterial 55.47 31.75 24 2664 11848 34942395
COVID-19 pneumonia 53.21 31.75 26 2662 16941 34937302
Fibrin D dimer increased 46.65 31.75 16 2672 4228 34950015
Bronchopulmonary aspergillosis 44.58 31.75 22 2666 14637 34939606
Immobilisation syndrome 44.16 31.75 9 2679 311 34953932
Pneumothorax spontaneous 38.30 31.75 9 2679 606 34953637
Acute respiratory failure 36.29 31.75 25 2663 30903 34923340
Liver function test increased 35.97 31.75 19 2669 14546 34939697
COVID-19 34.86 31.75 36 2652 77514 34876729
Alanine aminotransferase increased 33.62 31.75 36 2652 80779 34873464
Solar urticaria 33.09 31.75 5 2683 27 34954216

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
Therapy interrupted 256.54 18.55 97 6574 31244 79706473
Pulmonary embolism 222.43 18.55 152 6519 171502 79566215
Deep vein thrombosis 195.35 18.55 123 6548 120796 79616921
COVID-19 pneumonia 95.11 18.55 47 6624 28802 79708915
COVID-19 94.54 18.55 89 6582 157585 79580132
Fibrin D dimer increased 90.04 18.55 32 6639 8622 79729095
Therapy cessation 78.05 18.55 45 6626 37517 79700200
Pneumonia bacterial 74.32 18.55 35 6636 19296 79718421
Sputum culture positive 63.28 18.55 20 6651 3761 79733956
Leukopenia 58.98 18.55 60 6611 116453 79621264
Off label use 56.64 18.55 185 6486 907030 78830687
Herpes zoster 54.67 18.55 52 6619 93031 79644686
Liver function test increased 50.77 18.55 35 6636 39738 79697979
Illness 45.85 18.55 35 6636 46476 79691241
Bronchopulmonary aspergillosis 41.80 18.55 25 6646 22269 79715448
Tooth dislocation 39.76 18.55 6 6665 29 79737688
Leukocytosis 34.91 18.55 29 6642 43426 79694291
Thrombocytosis 34.50 18.55 16 6655 8510 79729207
Alanine aminotransferase increased 34.19 18.55 54 6617 162516 79575201
Ovarian adenoma 33.86 18.55 7 6664 238 79737479
Diverticulitis intestinal perforated 33.47 18.55 7 6664 252 79737465
Acute respiratory failure 32.56 18.55 32 6639 59509 79678208
Respiratory failure 32.53 18.55 56 6615 180855 79556862
PaO2/FiO2 ratio decreased 31.81 18.55 5 6666 33 79737684
Pneumothorax spontaneous 29.86 18.55 9 6662 1445 79736272
Lung adenocarcinoma 29.48 18.55 14 6657 7850 79729867
Herpes simplex reactivation 29.19 18.55 7 6664 472 79737245
Pneumonia staphylococcal 29.00 18.55 12 6659 4862 79732855
Pneumomediastinum 28.69 18.55 11 6660 3656 79734061
Blood culture positive 28.56 18.55 14 6657 8415 79729302
Aspartate aminotransferase increased 27.69 18.55 45 6626 138596 79599121
Staphylococcal infection 27.62 18.55 29 6642 58266 79679451
Pneumonia pseudomonal 26.77 18.55 12 6659 5899 79731818
Solar urticaria 26.37 18.55 5 6666 108 79737609
Drug ineffective for unapproved indication 25.19 18.55 26 6645 51212 79686505
Ultrasound Doppler abnormal 24.60 18.55 5 6666 156 79737561
Pneumonia haemophilus 22.98 18.55 7 6664 1165 79736552
Pneumocystis jirovecii pneumonia 22.65 18.55 20 6651 32488 79705229
Toxicity to various agents 22.63 18.55 4 6667 421536 79316181
Arthrodesis 21.66 18.55 8 6663 2399 79735318
Lymphocyte count decreased 21.47 18.55 23 6648 47266 79690451
Infection 21.36 18.55 56 6615 241656 79496061
Tumour necrosis factor receptor-associated periodic syndrome 21.11 18.55 4 6667 86 79737631
Acute respiratory distress syndrome 21.01 18.55 22 6649 44045 79693672
Post herpetic neuralgia 21.00 18.55 8 6663 2613 79735104
Legionella infection 20.97 18.55 6 6665 804 79736913
Hypoxia 19.92 18.55 33 6638 103210 79634507
Lymph node tuberculosis 19.64 18.55 6 6665 1008 79736709
Pulseless electrical activity 19.34 18.55 13 6658 14147 79723570

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 9737469 Nov. 2, 2031 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA
2MG OLUMIANT ELI LILLY AND CO N207924 May 31, 2018 RX TABLET ORAL 9737469 Nov. 2, 2031 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA
4MG OLUMIANT ELI LILLY AND CO N207924 May 10, 2022 RX TABLET ORAL 9737469 Nov. 2, 2031 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA
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
4037600 VANDF
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
2047232 RXNORM
C000596027 MESH_SUPPLEMENTAL_RECORD_UI

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 0002-4182 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 0002-4479 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
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