baricitinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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: OFP
    • 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 1.170 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 12.823 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 21.429 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 1.648 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 62.510 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 78.830 % High 1
herg hERG pIC50 4.525 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 0.993 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 3.846 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 54.310 % High 1
kinase-safety-class AAK1,ACVR2A,ACVR2B,ACVRL1,AKT1,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2A,CAMK2B,CAMK2D,CAMK2G,CDK1,CDK14,CDK16,CDK19,CDK3,CDK4,CDK5,CDK6,CDK7,CDK9,CHEK1,CLK1,CLK2,CLK4,CSF1R,CSNK1G2,DDR1,DYRK1A,DYRK1B,DYRK3,EGFR,EIF2AK3,EPHA2,ERBB2,FGFR1,FLT3,FYN,GAK,GRK1,GRK2,GRK3,GSK3A,GSK3B,HASPIN,IGF1R,IKBKB,INSR,IRAK1,IRAK3,ITK,JAK1,JAK2,JAK3,KDR,KIT,LCK,LRRK2,LYN,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K19,MAP3K2,MAP3K21,MAP3K7,MAP3K9,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK1,MAPK10,MAPK3,MAPK7,MAPK9,MARK1,MARK2,MARK3,MARK4,MELK,MET,MINK1,MKNK2,NTRK1,NTRK2,NTRK3,NUAK1,PAK4,PDK1,PDK2,PDK4,PIK3CA,PIK3CD,PIK3CG,PRKAA1,PRKAA2,PRKACA,PRKCA,PRKCD,PRKCZ,PRKDC,PRKG1,RIPK1,ROCK1,ROCK2,RPS6KA1,SGK1,SIK2,SIK3,SRC,STK17A,STK33,STK4,SYK,TEK,TGFBR1,TNIK,TTK,ULK1,ULK2,YES1 130
kinase-selectivity-class AAK1,ACVR2B,AURKA,AURKB,AURKC,AXL,BMX,BRAF,CAMK2B,CAMK2D,CDK1,CDK2,CDK7,CDK8,CDK9,CHEK1,CLK2,CLK4,DYRK1A,DYRK1B,DYRK2,DYRK3,EGFR,FGFR1,FLT3,GRK2,GSK3B,HASPIN,IRAK1,IRAK3,IRAK4,JAK1,JAK2,JAK3,KDR,LCK,LRRK2,MAP2K1,MAP3K10,MAP3K11,MAP3K19,MAP3K2,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK1,MARK3,MARK4,MELK,MET,MKNK2,NTRK1,NTRK3,NUAK1,PDK1,PIK3CD,PRKAA1,PRKAA2,PRKACA,PRKCD,PRKDC,RET,ROCK1,ROCK2,SGK1,SIK2,SIK3,SRC,STK17A,STK33,SYK,TNIK,ULK1 75
mdck-mdr1-bcrp-efflux MDCK-MDR1-BCRP efflux ratio 12.246 High 1
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 11.324 High 1
mh-clint Mouse hepatocyte intrinsic clearance 7.745 High 1
mppb Mouse plasma protein binding (% unbound) 61.420 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 26.669 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 68.630 % High 1
rat-kpuu-brain Rat brain Kpuu 0.021 % High 1
rh-clint Rat hepatocyte intrinsic clearance 1.679 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 85.250 % High 1
rppb Rat plasma protein binding (% unbound) 49.020 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 64.714 uM High 1

Approvals:

DateAgencyCompanyOrphan
May 31, 2018 FDA ELI LILLY AND CO
July 3, 2017 PMDA Eli Lilly Japan KK
Feb. 13, 2017 EMA Eli Lilly Nederland B.V.

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 333.93 17.18 134 7544 49974 90570795
COVID-19 256.75 17.18 166 7512 168677 90452092
Blood folate decreased 174.78 17.18 38 7640 1632 90619137
Perineal rash 98.62 17.18 15 7663 76 90620693
Lumbosacral plexopathy 95.51 17.18 15 7663 97 90620672
Herpes zoster 89.94 17.18 70 7608 94574 90526195
COVID-19 pneumonia 82.25 17.18 37 7641 18140 90602629
Drug ineffective 77.43 17.18 274 7404 1384024 89236745
Thrombocytosis 76.73 17.18 27 7651 6974 90613795
Deep vein thrombosis 72.71 17.18 61 7617 91559 90529210
Pulmonary embolism 63.04 17.18 66 7612 130754 90490015
Illness 61.80 17.18 53 7625 81916 90538853
Therapy cessation 53.21 17.18 35 7643 36326 90584443
Diverticulitis intestinal perforated 52.27 17.18 11 7667 403 90620366
Neurogenic bladder 43.44 17.18 15 7663 3663 90617106
Sputum culture positive 42.08 17.18 13 7665 2240 90618529
Fibrin D dimer increased 41.18 17.18 16 7662 5444 90615325
Tooth dislocation 39.51 17.18 6 7672 30 90620739
Arthritis 38.02 17.18 58 7620 167257 90453512
Pneumonia 35.03 17.18 126 7552 637933 89982836
Breast cancer 33.05 17.18 31 7647 53730 90567039
Ovarian adenoma 32.62 17.18 7 7671 282 90620487
Epstein-Barr virus associated lymphoproliferative disorder 31.97 17.18 11 7667 2656 90618113
Urinary tract infection 31.89 17.18 76 7602 305556 90315213
Lung adenocarcinoma 30.60 17.18 13 7665 5552 90615217
Mass 30.37 17.18 18 7660 15559 90605210
Lymph node tuberculosis 30.02 17.18 8 7670 815 90619954
Normochromic normocytic anaemia 28.33 17.18 12 7666 5090 90615679
Diverticulitis 27.67 17.18 26 7652 45161 90575608
Osteochondrosis 27.65 17.18 9 7669 1834 90618935
Leukopenia 27.35 17.18 38 7640 100672 90520097
Cervicobrachial syndrome 27.26 17.18 8 7670 1157 90619612
Platelet count decreased 26.32 17.18 44 7634 136925 90483844
Transaminases increased 25.90 17.18 23 7655 37169 90583600
Drug ineffective for unapproved indication 25.79 17.18 30 7648 66614 90554155
Intentional dose omission 25.72 17.18 17 7661 17766 90603003
Pneumonia bacterial 25.51 17.18 15 7663 12775 90607994
Epstein-Barr virus infection reactivation 24.58 17.18 8 7670 1629 90619140
Immunodeficiency common variable 24.55 17.18 6 7672 432 90620337
Ultrasound Doppler abnormal 24.38 17.18 5 7673 161 90620608
Herpes simplex reactivation 23.86 17.18 7 7671 1012 90619757
Tubular breast carcinoma 23.41 17.18 4 7674 46 90620723
Spinal pain 22.63 17.18 15 7663 15752 90605017
Staphylococcal skin infection 22.59 17.18 7 7671 1218 90619551
Post-acute COVID-19 syndrome 22.52 17.18 7 7671 1230 90619539
Sudden death 22.30 17.18 13 7665 10896 90609873
Pneumonia haemophilus 21.18 17.18 7 7671 1496 90619273
Post herpetic neuralgia 20.72 17.18 8 7670 2676 90618093
Tumour necrosis factor receptor-associated periodic syndrome 20.64 17.18 4 7674 96 90620673
Haemophagocytic lymphohistiocytosis 20.49 17.18 14 7664 15445 90605324
Ganglioglioma 20.30 17.18 3 7675 12 90620757
Ischaemic stroke 20.17 17.18 16 7662 22150 90598619
White blood cell count decreased 20.11 17.18 44 7634 167065 90453704
Parathyroid tumour benign 20.04 17.18 6 7672 930 90619839
Foeticide 19.76 17.18 3 7675 15 90620754
Limb discomfort 19.74 17.18 20 7658 38040 90582729
Osteoporotic fracture 19.40 17.18 9 7669 4727 90616042
Bronchitis 19.24 17.18 41 7637 152886 90467883
Vulvovaginal inflammation 19.10 17.18 6 7672 1092 90619677
Sinusitis 18.96 17.18 68 7610 343020 90277749
Spinal instability 18.69 17.18 4 7674 159 90620610
Herpes zoster infection neurological 18.45 17.18 5 7673 542 90620227
Viral infection 18.34 17.18 20 7658 41394 90579375
Lumbar vertebral fracture 18.26 17.18 10 7668 7448 90613321
Pulmonary necrosis 18.25 17.18 4 7674 178 90620591
Pharyngeal swelling 18.11 17.18 11 7667 9933 90610836
Spinal claudication 18.06 17.18 4 7674 187 90620582
Cutaneous T-cell lymphoma stage IV 18.03 17.18 3 7675 29 90620740
Infective pericardial effusion 17.85 17.18 3 7675 31 90620738
Cerebral toxoplasmosis 17.64 17.18 6 7672 1399 90619370
Respiratory failure 17.57 17.18 34 7644 118384 90502385
Abscess limb 17.43 17.18 9 7669 5953 90614816
Eczema herpeticum 17.41 17.18 4 7674 221 90620548
Fatigue 17.26 17.18 46 7632 1153977 89466792

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 180.47 28.77 125 4187 119487 42497536
Off label use 158.48 28.77 251 4061 638084 41978939
Deep vein thrombosis 143.81 28.77 92 4220 76865 42540158
Bronchopulmonary aspergillosis 82.66 28.77 40 4272 19389 42597634
Spinal cord injury cervical 72.12 28.77 14 4298 282 42616741
Drug ineffective for unapproved indication 71.08 28.77 49 4263 46114 42570909
COVID-19 70.80 28.77 72 4240 115876 42501147
Therapy interrupted 68.97 28.77 37 4275 22213 42594810
Immobilisation syndrome 59.85 28.77 13 4299 463 42616560
Testicular seminoma (pure) 57.83 28.77 11 4301 198 42616825
COVID-19 pneumonia 56.16 28.77 32 4280 21581 42595442
Pneumonia bacterial 54.03 28.77 28 4284 15664 42601359
Fungal skin infection 46.08 28.77 16 4296 3325 42613698
Fibrin D dimer increased 39.85 28.77 16 4296 4969 42612054
Acute respiratory failure 37.03 28.77 31 4281 38827 42578196
Spinal fracture 36.30 28.77 18 4294 9172 42607851
Staphylococcal infection 33.76 28.77 29 4283 37614 42579409
Pneumothorax spontaneous 32.99 28.77 9 4303 837 42616186
Pneumocystis jirovecii pneumonia 32.43 28.77 24 4288 25157 42591866
Microcytic anaemia 32.31 28.77 12 4300 3023 42614000
Lung adenocarcinoma 32.13 28.77 14 4298 5325 42611698
Solar urticaria 31.56 28.77 5 4307 28 42616995
Myelodysplastic syndrome unclassifiable 30.80 28.77 6 4306 123 42616900
Pneumonia staphylococcal 30.73 28.77 12 4300 3464 42613559
PaO2/FiO2 ratio decreased 30.13 28.77 5 4307 39 42616984
Tinea pedis 28.99 28.77 10 4302 2038 42614985
Condition aggravated 28.97 28.77 74 4238 260680 42356343
Lymphopenia 28.78 28.77 21 4291 21542 42595481

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 446.84 18.71 169 9989 49653 110529488
COVID-19 222.16 18.71 182 9976 244878 110334263
Pulmonary embolism 210.72 18.71 167 9991 214307 110364834
Deep vein thrombosis 189.05 18.71 132 10026 139755 110439386
Blood folate decreased 159.02 18.71 38 10120 2297 110576844
COVID-19 pneumonia 127.22 18.71 64 10094 37079 110542062
Off label use 115.36 18.71 349 9809 1499836 109079305
Herpes zoster 107.52 18.71 85 10073 108294 110470847
Perineal rash 97.24 18.71 15 10143 77 110579064
Drug ineffective for unapproved indication 96.35 18.71 78 10080 102760 110476381
Lumbosacral plexopathy 94.29 18.71 15 10143 97 110579044
Illness 91.42 18.71 69 10089 82102 110497039
Drug ineffective 83.24 18.71 316 9842 1520224 109058917
Fibrin D dimer increased 83.08 18.71 32 10126 9813 110569328
Therapy cessation 79.03 18.71 50 10108 44807 110534334
Pneumonia bacterial 77.64 18.71 41 10117 26220 110552921
Bronchopulmonary aspergillosis 64.69 18.71 38 10120 29825 110549316
Sputum culture positive 60.88 18.71 20 10138 3869 110575272
Lung adenocarcinoma 59.70 18.71 25 10133 9506 110569635
Arthritis 45.60 18.71 66 10092 167520 110411621
Leukopenia 44.03 18.71 61 10097 148730 110430411
Testicular seminoma (pure) 41.84 18.71 8 10150 164 110578977
Staphylococcal infection 41.48 18.71 41 10117 69903 110509238
Pneumocystis jirovecii pneumonia 41.23 18.71 33 10125 42702 110536439
Acute respiratory failure 38.96 18.71 41 10117 75219 110503922
Leukocytosis 38.49 18.71 35 10123 53793 110525348
Neurogenic bladder 37.53 18.71 15 10143 5064 110574077
Intentional dose omission 36.90 18.71 23 10135 20057 110559084
Tooth dislocation 36.38 18.71 6 10152 50 110579091
Thrombocytosis 35.75 18.71 18 10140 10426 110568715
Respiratory failure 34.63 18.71 67 10091 215265 110363876
Lymphopenia 34.51 18.71 29 10129 40141 110539000
Ovarian adenoma 33.77 18.71 7 10151 219 110578922
Diverticulitis intestinal perforated 32.47 18.71 8 10150 549 110578592
Pneumonia pseudomonal 31.82 18.71 15 10143 7531 110571610
Pneumonia staphylococcal 31.65 18.71 14 10144 6077 110573064
Acute respiratory distress syndrome 31.19 18.71 31 10127 53167 110525974
PaO2/FiO2 ratio decreased 30.28 18.71 5 10153 42 110579099
Alanine aminotransferase increased 29.32 18.71 57 10101 183716 110395425
Fungal skin infection 29.32 18.71 14 10144 7235 110571906
Mass 27.56 18.71 19 10139 19611 110559530
Pneumomediastinum 27.54 18.71 12 10146 5024 110574117
Liver function test increased 27.23 18.71 37 10121 88511 110490630
Pneumothorax spontaneous 27.06 18.71 9 10149 1808 110577333
Blood culture positive 26.48 18.71 14 10144 8962 110570179
Seminoma 26.45 18.71 6 10152 288 110578853
Myelodysplastic syndrome unclassifiable 25.94 18.71 5 10153 107 110579034
Solar urticaria 25.73 18.71 5 10153 112 110579029
Breast cancer 25.49 18.71 24 10134 38518 110540623
Autoinflammatory disease 24.90 18.71 6 10152 375 110578766
Epstein-Barr virus associated lymphoproliferative disorder 24.83 18.71 11 10147 4791 110574350
Ultrasound Doppler abnormal 24.49 18.71 5 10153 145 110578996
Immobilisation syndrome 24.34 18.71 7 10151 869 110578272
Toxicity to various agents 24.32 18.71 7 10151 480548 110098593
Mitral perforation 24.08 18.71 4 10154 35 110579106
Pneumonia 24.07 18.71 150 10008 876564 109702577
Aspartate aminotransferase increased 23.58 18.71 48 10110 159888 110419253
Lymph node tuberculosis 22.75 18.71 7 10151 1097 110578044
Cutaneous T-cell lymphoma stage IV 22.29 18.71 4 10154 57 110579084
Bone fissure 22.06 18.71 6 10152 608 110578533
Small cell lung cancer 21.90 18.71 9 10149 3263 110575878
Post herpetic neuralgia 21.82 18.71 9 10149 3292 110575849
Fatigue 21.69 18.71 50 10108 1215908 109363233
Spinal fracture 20.81 18.71 17 10141 22616 110556525
Herpes simplex reactivation 20.78 18.71 7 10151 1461 110577680
Tumour necrosis factor receptor-associated periodic syndrome 20.52 18.71 4 10154 91 110579050
Legionella infection 19.44 18.71 6 10152 950 110578191
Staphylococcal skin infection 19.07 18.71 7 10151 1878 110577263
Ischaemic stroke 18.76 18.71 21 10137 41242 110537899

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L04AF02 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
IMMUNOSUPPRESSANTS
IMMUNOSUPPRESSANTS
Janus-associated kinase (JAK) inhibitors
FDA MoA N0000190857 Janus Kinase Inhibitors
FDA EPC N0000190858 Janus Kinase Inhibitor
CHEBI has role CHEBI:22587 antiviral agent
CHEBI has role CHEBI:33281 antimicrobial agent
CHEBI has role CHEBI:35526 hypoglycemic agent
CHEBI has role CHEBI:35705 immunosuppressive agent
CHEBI has role CHEBI:35842 antirheumatic drug
CHEBI has role CHEBI:50177 dermatologic drug
CHEBI has role CHEBI:50748 antipsoriatic
CHEBI has role CHEBI:63726 neuroprotective agent
CHEBI has role CHEBI:64946 anti-HIV agent
CHEBI has role CHEBI:66981 ophthalmology drug
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:76617 EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor

Related Drugs by ATC class:

L04AF Janus-associated kinase (JAK) inhibitors 7 drugs
deucravacitinibdeuruxolitinibfilgotinibpeficitinibritlecitinibtofacitinibupadacitinib

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 11806555 Nov. 2, 2031 TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA
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 11806555 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 11806555 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)

None

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
Signal transducer and activator of transcription 3 Transcription factor IC50 7.70 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
C000596027 MESH_SUPPLEMENTAL_RECORD_UI
7792 IUPHAR_LIGAND_ID
726518002 SNOMEDCT_US
763701005 SNOMEDCT_US
256448 MMSL
32650 MMSL
354624 MMSL
d08568 MMSL
017220 NDDF
2047232 RXNORM
ISP4442I3Y INXIGHT DRUGS

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 0002-4479 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
Baricitinib HUMAN PRESCRIPTION DRUG LABEL 1 0002-6885 TABLET, FILM COATED 4 mg ORAL Emergency Use Authorization 2 sections