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

Stem definition	Drug id	CAS RN
tyrosine kinase inhibitors	5202	1187594-09-7

Description:

Molecule	Description
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

Molecule

Description

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:

Dose	Unit	Route
3	mg	O

ADMET properties:

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

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Approvals:

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

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	L04AA37	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS IMMUNOSUPPRESSANTS IMMUNOSUPPRESSANTS Selective immunosuppressants
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
FDA EPC	N0000190858	Janus Kinase Inhibitor
FDA MoA	N0000190857	Janus Kinase Inhibitors

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

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Disease	Relation	SNOMED_ID	DOID
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

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.49	acidic
pKa2	4.6	Basic
pKa3	1.9	Basic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
1MG	OLUMIANT	ELI LILLY AND CO	N207924	Oct. 8, 2019	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
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	8420629	March 10, 2029	TREATMENT OF RHEUMATOID ARTHRITIS
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
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	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	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)

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
1MG	OLUMIANT	ELI LILLY AND CO	N207924	Oct. 8, 2019	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)
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	May 31, 2023	NEW CHEMICAL ENTITY
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)
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	May 31, 2023	NEW CHEMICAL ENTITY
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)
4MG	OLUMIANT	ELI LILLY AND CO	N207924	May 10, 2022	RX	TABLET	ORAL	June 13, 2025	TREATMENT OF ADULT PATIENTS WITH SEVERE ALOPECIA AREATA

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Tyrosine-protein kinase JAK1	Kinase	P23458	JAK1_HUMAN	INHIBITOR	IC50	8.23	SCIENTIFIC LITERATURE	DRUG LABEL
Tyrosine-protein kinase JAK2	Kinase	O60674	JAK2_HUMAN	INHIBITOR	IC50	8.24	SCIENTIFIC LITERATURE	DRUG LABEL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN		Kd	6.32	CHEMBL
Protein kinase C beta type	Kinase	P05771	KPCB_HUMAN		Kd	4.58	CHEMBL
Protein kinase C delta type	Kinase	Q05655	KPCD_HUMAN		Kd	5.97	CHEMBL
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN		Kd	6.12	CHEMBL
Protein kinase C alpha type	Kinase	P17252	KPCA_HUMAN		Kd	5.68	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit delta	Kinase	Q13557	KCC2D_HUMAN		Kd	6.51	CHEMBL
Calcium/calmodulin-dependent protein kinase type II subunit gamma	Kinase	Q13555	KCC2G_HUMAN		Kd	6.61	CHEMBL
AP2-associated protein kinase 1	Kinase	Q2M2I8	AAK1_HUMAN	INHIBITOR	Kd	7.77	IUPHAR

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External reference:

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ID	Source
3JW	PDB_CHEM_ID
017220	NDDF
2047232	RXNORM
256448	MMSL
32650	MMSL
354624	MMSL
4037600	VANDF
44205240	PUBCHEM_CID
726518002	SNOMEDCT_US
763701005	SNOMEDCT_US

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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
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

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