Identification

Summary

Baricitinib is a Janus kinase inhibitor used to treat moderate to severe rheumatoid arthritis that has responded poorly to at least one TNF antagonist.

Brand Names
Olumiant
Generic Name
Baricitinib
DrugBank Accession Number
DB11817
Background

Baricitinib is a Janus kinase (JAK) inhibitor. JAKs are tyrosine protein kinases that play an important role in pro-inflammatory signaling pathways. Overactive JAKs have been implicated in autoimmune disorders, such as rheumatoid arthritis. By inhibiting the actions of JAK1 and JAK2, baricitinib attenuates JAK-mediated inflammation and immune responses.9

Baricitinib was first approved by the European Commission (EC) in February 2017 for the treatment of rheumatoid arthritis in adults 4 and was later approved by the FDA in 2018.5 The EC later approved baricitinib for the treatment of atopic dermatitis, making it the first JAK inhibitor used for this indication in Europe.6 While baricitinib was granted emergency use as a treatment for COVID-19 in combination with remdesivir under the Emergency Use Authorization (EUA) in November 2020,8 the FDA fully approved the use of baricitinib for the treatment of COVID-19 in May 2022.9

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 371.42
Monoisotopic: 371.116443989
Chemical Formula
C16H17N7O2S
Synonyms
  • Baricitinib
External IDs
  • INCB-028050
  • INCB028050
  • LY-3009104
  • LY3009104

Pharmacology

Indication

In the US and Europe, baricitinib is indicated for the treatment of adult patients with moderately to severely active rheumatoid arthritis who have had an inadequate response to one or more TNF blockers. Baricitinib may be used as monotherapy or in combination with methotrexate 9,11 or other DMARDs.9

In Europe, baricitinib is indicated for the treatment of moderate to severe atopic dermatitis in adult patients who are candidates for systemic therapy.11

In the US, baricitinib is also indicated for the treatment of coronavirus disease 2019 (COVID-19) in hospitalized adults requiring supplemental oxygen, non-invasive or invasive mechanical ventilation, or extracorporeal membrane oxygenation.9 Recently, it is also approved as the treatment for severe alopecia areata in adults.12

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Baricitinib is a disease-modifying antirheumatic drug (DMARD) used to ameliorate symptoms and slow down the progression of rheumatoid arthritis. In animal models of inflammatory arthritis, baricitinib was shown to have significant anti-inflammatory effects but also led to the preservation of cartilage and bone, with no detectable suppression of humoral immunity or adverse hematologic effects.1 Baricitinib decreased the levels of immunoglobulins and serum C-reactive protein in patients with rheumatoid arthritis.9

Mechanism of action

As members of the tyrosine kinase family, Janus kinases (JAKs) are intracellular enzymes that modulate signals from cytokines and growth factor receptors involved in hematopoiesis, inflammation, and immune cell function. Upon binding of extracellular cytokines and growth factors, JAKs phosphorylate and activate Signal Transducers and Activators of Transcription (STATs). STATs modulate intracellular activity, including gene transcription of inflammatory mediators that promote an autoimmune response,2,3,7,9 such as IL-2, IL-6, IL-12, IL-15, IL-23, IFN-γ, GM-CSF, and interferons.2,3 The JAK-STAT pathway has been implicated in the pathophysiology of rheumatoid arthritis, as it is associated with an overproduction of inflammatory mediators.3

There are four JAK proteins: JAK 1, JAK 2, JAK 3 and TYK2. JAKs form homodimers or heterodimers and pair differently in different cell receptors to transmit cytokine signaling.7,9 Baricitinib is a selective and reversible inhibitor of JAK1 and JAK2 with less affinity for JAK3 and TYK2; however, the relevance of inhibition of specific JAK enzymes to therapeutic effectiveness is not currently known.9 Baricitinib inhibits the activity of JAK proteins and modulates the signaling pathway of various interleukins, interferons, and growth factors. It was also shown to decrease the proliferation of JAK1/JAK2 expression in mutated cells and induce cell apoptosis.7

TargetActionsOrganism
ATyrosine-protein kinase JAK1
inhibitor
Humans
ATyrosine-protein kinase JAK2
inhibitor
Humans
ATyrosine-protein kinase JAK3
inhibitor
Humans
UNon-receptor tyrosine-protein kinase TYK2
inhibitor
Humans
Absorption

The absolute bioavailability of baricitinib is approximately 80%. The Cmax was reached after one hour of oral drug administration. A high-fat meal decreased the mean AUC and Cmax of baricitinib by approximately 11% and 18%, respectively, and delayed Tmax by 0.5 hours.9

Volume of distribution

Following intravenous administration, the volume of distribution was 76 L, indicating distribution into tissues.9

Protein binding

Baricitinib is approximately 50% bound to plasma proteins and 45% bound to serum proteins.9

Metabolism

Baricitinib is metabolized by CYP3A4. Approximately 6% of the orally administered dose was identified as metabolites in urine and feces; however, no metabolites of baricitinib were quantifiable in plasma.9

Route of elimination

Baricitinib is predominantly excreted via renal elimination. It is cleared via filtration and active secretion. Approximately 75% of the administered dose was eliminated in the urine, with 20% of that dose being the unchanged drug. About 20% of the dose was eliminated in the feces, with 15% of that dose being an unchanged drug.9

Half-life

The elimination half-life in patients with rheumatoid arthritis is approximately 12 hours. The elimination half-life was 10.8 hours in intubated patients with COVID-19 who received baricitinib via nasogastric (NG) or orogastric (OG) tube.9

Clearance

The total body clearance of baricitinib was 8.9 L/h in patients with rheumatoid arthritis. The total body clearance and half-life of baricitinib was 14.2 L/h in intubated patients with COVID-19 who received baricitinib via nasogastric (NG) or orogastric (OG) tube.9

Adverse Effects
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Toxicity

The oral lowest published toxic dose (TDLo) is 1820 g/kg in mice and 5096 g/kg in rats.10

In clinical trials, single doses up to 40 mg and multiple doses of up to 20 mg daily for 10 days did not result in any dose-limiting toxicity. Pharmacokinetic data of a single dose of 40 mg in healthy volunteers indicate that more than 90% of the administered dose is expected to be eliminated within 24 hours. In case of an overdose, it is recommended that patients are monitored for signs and symptoms of drug-related adverse reactions, which should be responded with appropriate treatment.9

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Baricitinib which could result in a higher serum level.
AbametapirThe serum concentration of Baricitinib can be increased when it is combined with Abametapir.
AbataceptThe risk or severity of adverse effects can be increased when Abatacept is combined with Baricitinib.
AbemaciclibThe excretion of Baricitinib can be decreased when combined with Abemaciclib.
AceclofenacAceclofenac may decrease the excretion rate of Baricitinib which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Baricitinib which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Baricitinib which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Baricitinib which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidThe serum concentration of Baricitinib can be increased when it is combined with Acetylsalicylic acid.
AclidiniumAclidinium may decrease the excretion rate of Baricitinib which could result in a higher serum level.
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Food Interactions
  • Take with or without food. A high-fat meal can decrease the mean AUC and Cmax of baricitinib and delay Tmax, but not to a clinically singificant extent.

Products

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Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
BaricitinibTablet, film coated4 mg/1OralEli Lilly and Company2021-12-20Not applicableUS flag
OlumiantTablet, film coated4 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
OlumiantTablet, film coated4 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
OlumiantTablet, film coated2 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
OlumiantTablet, film coated2 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
OlumiantTablet, film coated4 mg/1OralEli Lilly and Company2022-05-10Not applicableUS flag
OlumiantTablet, film coated4 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
OlumiantTablet, film coated1 mg/1OralEli Lilly and Company2019-10-08Not applicableUS flag
OlumiantTablet, film coated4 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
OlumiantTablet, film coated2 mgOralEli Lilly Nederland B.V.2020-12-16Not applicableEU flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
OLUMIANTBaricitinib (2 mg) + Baricitinib (4 mg)Tablet, coatedOralELI LILLY INTERAMERICA INC2019-09-132024-09-30Colombia flag
OLUMIANTBaricitinib (2 mg) + Baricitinib (4 mg)Tablet, coatedOralELI LILLY INTERAMERICA INC2019-09-132024-09-30Colombia flag

Categories

ATC Codes
L04AA37 — Baricitinib
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as pyrrolo[2,3-d]pyrimidines. These are aromatic heteropolycyclic compounds containing a pyrrolo[2,3-d]pyrimidine ring system, which is an pyrrolopyrimidine isomers having the 3 ring nitrogen atoms at the 1-, 5-, and 7-positions.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Pyrrolopyrimidines
Sub Class
Pyrrolo[2,3-d]pyrimidines
Direct Parent
Pyrrolo[2,3-d]pyrimidines
Alternative Parents
Pyrimidines and pyrimidine derivatives / Organosulfonamides / Organic sulfonamides / Sulfonyls / Pyrroles / Pyrazoles / Heteroaromatic compounds / Azetidines / Nitriles / Azacyclic compounds
show 3 more
Substituents
Aromatic heteropolycyclic compound / Azacycle / Azetidine / Azole / Carbonitrile / Heteroaromatic compound / Hydrocarbon derivative / Nitrile / Organic nitrogen compound / Organic oxide
show 13 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
Not Available

Chemical Identifiers

UNII
ISP4442I3Y
CAS number
1187594-09-7
InChI Key
XUZMWHLSFXCVMG-UHFFFAOYSA-N
InChI
InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
IUPAC Name
2-[1-(ethanesulfonyl)-3-(4-{7H-pyrrolo[2,3-d]pyrimidin-4-yl}-1H-pyrazol-1-yl)azetidin-3-yl]acetonitrile
SMILES
CCS(=O)(=O)N1CC(CC#N)(C1)N1C=C(C=N1)C1=C2C=CNC2=NC=N1

References

Synthesis Reference

Mayence, A., & Vanden Eynde, J. J. (2019). Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases. Pharmaceuticals (Basel, Switzerland), 12(1), 37. https://doi.org/10.3390/ph12010037

General References
  1. Kuriya B, Cohen MD, Keystone E: Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential. Ther Adv Musculoskelet Dis. 2017 Feb;9(2):37-44. doi: 10.1177/1759720X16687481. Epub 2017 Jan 23. [Article]
  2. Genovese MC, Kremer J, Zamani O, Ludivico C, Krogulec M, Xie L, Beattie SD, Koch AE, Cardillo TE, Rooney TP, Macias WL, de Bono S, Schlichting DE, Smolen JS: Baricitinib in Patients with Refractory Rheumatoid Arthritis. N Engl J Med. 2016 Mar 31;374(13):1243-52. doi: 10.1056/NEJMoa1507247. [Article]
  3. O'Shea JJ, Kontzias A, Yamaoka K, Tanaka Y, Laurence A: Janus kinase inhibitors in autoimmune diseases. Ann Rheum Dis. 2013 Apr;72 Suppl 2:ii111-5. doi: 10.1136/annrheumdis-2012-202576. [Article]
  4. Markham A: Baricitinib: First Global Approval. Drugs. 2017 Apr;77(6):697-704. doi: 10.1007/s40265-017-0723-3. [Article]
  5. Mayence A, Vanden Eynde JJ: Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases. Pharmaceuticals (Basel). 2019 Mar 12;12(1). pii: ph12010037. doi: 10.3390/ph12010037. [Article]
  6. Radi G, Simonetti O, Rizzetto G, Diotallevi F, Molinelli E, Offidani A: Baricitinib: The First Jak Inhibitor Approved in Europe for the Treatment of Moderate to Severe Atopic Dermatitis in Adult Patients. Healthcare (Basel). 2021 Nov 18;9(11). pii: healthcare9111575. doi: 10.3390/healthcare9111575. [Article]
  7. Ahmad A, Zaheer M, Balis FJ: Baricitinib . [Article]
  8. FDA: Emergency Use Authorization for Baricitinib in Combination with Remdesivir for COVID-19 [Link]
  9. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
  10. Cayman Chemical: Baricitinib MSDS [Link]
  11. EMA Approved Drug Products: Olumiant (baricitinib) Oral Tablets [Link]
  12. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use 2022 [Link]
KEGG Drug
D10308
PubChem Compound
44205240
PubChem Substance
347828164
ChemSpider
26373084
BindingDB
50021656
RxNav
2047232
ChEBI
95341
ChEMBL
CHEMBL2105759
ZINC
ZINC000073069247
PDBe Ligand
3JW
Wikipedia
Baricitinib
PDB Entries
4w9x / 6vn8 / 6wto

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentRheumatoid Arthritis1
4RecruitingPreventionCoronavirus Disease 2019 (COVID‑19) / Psoriatic Arthritis / Rheumatoid Arthritis / Spondylarthritis1
4RecruitingTreatmentCoronavirus Disease 2019 (COVID‑19)1
4RecruitingTreatmentRheumatoid Arthritis2
4RecruitingTreatmentSystemic Sclerosis (SSc)1
3Active Not RecruitingOtherBone Mineral Density / Finger Joints / Rheumatoid Arthritis1
3Active Not RecruitingTreatmentAlopecia Areata (AA)1
3Active Not RecruitingTreatmentAtopic Dermatitis2
3CompletedTreatmentAtopic Dermatitis4
3CompletedTreatmentCoronavirus Disease 2019 (COVID‑19)3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Tablet, film coatedOral4 mg/1
TabletOral2 mg
Tablet, coatedOral
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
Tablet, film coatedOral
Tablet, film coatedOral2.000 mg
Tablet, film coatedOral4.000 mg
Tablet, film coatedOral2 MG
Tablet, film coatedOral4 MG
Tablet, coatedOral2 mg
Tablet, coatedOral4 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8420629No2013-04-162029-03-10US flag
US8158616No2012-04-172030-06-08US flag
US9089574No2015-07-282032-11-30US flag
US11045474No2021-06-292032-11-30US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)707.2MSDS
Predicted Properties
PropertyValueSource
Water Solubility0.357 mg/mLALOGPS
logP1.08ALOGPS
logP-0.19Chemaxon
logS-3ALOGPS
pKa (Strongest Acidic)13.89Chemaxon
pKa (Strongest Basic)3.91Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count6Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area120.56 Å2Chemaxon
Rotatable Bond Count4Chemaxon
Refractivity105.55 m3·mol-1Chemaxon
Polarizability36.72 Å3Chemaxon
Number of Rings4Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
In isolated enzyme assays, baricitinib inhibited the activities of JAK1 with IC50 value of 5.9nM.
General Function
Ubiquitin protein ligase binding
Specific Function
Tyrosine kinase of the non-receptor type, involved in the IFN-alpha/beta/gamma signal pathway. Kinase partner for the interleukin (IL)-2 receptor.
Gene Name
JAK1
Uniprot ID
P23458
Uniprot Name
Tyrosine-protein kinase JAK1
Molecular Weight
133275.995 Da
References
  1. Kuriya B, Cohen MD, Keystone E: Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential. Ther Adv Musculoskelet Dis. 2017 Feb;9(2):37-44. doi: 10.1177/1759720X16687481. Epub 2017 Jan 23. [Article]
  2. Genovese MC, Kremer J, Zamani O, Ludivico C, Krogulec M, Xie L, Beattie SD, Koch AE, Cardillo TE, Rooney TP, Macias WL, de Bono S, Schlichting DE, Smolen JS: Baricitinib in Patients with Refractory Rheumatoid Arthritis. N Engl J Med. 2016 Mar 31;374(13):1243-52. doi: 10.1056/NEJMoa1507247. [Article]
  3. Mayence A, Vanden Eynde JJ: Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases. Pharmaceuticals (Basel). 2019 Mar 12;12(1). pii: ph12010037. doi: 10.3390/ph12010037. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
In isolated enzyme assays, baricitinib inhibited the activities of JAK2 with IC50 value of 5.7nM.
General Function
Sh2 domain binding
Specific Function
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, differentiation or histone modifications. Mediates essential signaling events in both innate and adaptiv...
Gene Name
JAK2
Uniprot ID
O60674
Uniprot Name
Tyrosine-protein kinase JAK2
Molecular Weight
130672.475 Da
References
  1. Genovese MC, Kremer J, Zamani O, Ludivico C, Krogulec M, Xie L, Beattie SD, Koch AE, Cardillo TE, Rooney TP, Macias WL, de Bono S, Schlichting DE, Smolen JS: Baricitinib in Patients with Refractory Rheumatoid Arthritis. N Engl J Med. 2016 Mar 31;374(13):1243-52. doi: 10.1056/NEJMoa1507247. [Article]
  2. Kuriya B, Cohen MD, Keystone E: Baricitinib in rheumatoid arthritis: evidence-to-date and clinical potential. Ther Adv Musculoskelet Dis. 2017 Feb;9(2):37-44. doi: 10.1177/1759720X16687481. Epub 2017 Jan 23. [Article]
  3. Mayence A, Vanden Eynde JJ: Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases. Pharmaceuticals (Basel). 2019 Mar 12;12(1). pii: ph12010037. doi: 10.3390/ph12010037. [Article]
  4. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
Curator comments
In isolated enzyme assays, baricitinib inhibited the activities of JAK3 with IC50 value of >400nM.
General Function
Protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine kinase involved in various processes such as cell growth, development, or differentiation. Mediates essential signaling events in both innate and adaptive immunity and plays a...
Gene Name
JAK3
Uniprot ID
P52333
Uniprot Name
Tyrosine-protein kinase JAK3
Molecular Weight
125097.565 Da
References
  1. Mayence A, Vanden Eynde JJ: Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases. Pharmaceuticals (Basel). 2019 Mar 12;12(1). pii: ph12010037. doi: 10.3390/ph12010037. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
In isolated enzyme assays, baricitinib inhibited the activities of TYK2 with IC50 value of 53nM.
General Function
Protein tyrosine kinase activity
Specific Function
Probably involved in intracellular signal transduction by being involved in the initiation of type I IFN signaling. Phosphorylates the interferon-alpha/beta receptor alpha chain.
Gene Name
TYK2
Uniprot ID
P29597
Uniprot Name
Non-receptor tyrosine-protein kinase TYK2
Molecular Weight
133648.77 Da
References
  1. Mayence A, Vanden Eynde JJ: Baricitinib: A 2018 Novel FDA-Approved Small Molecule Inhibiting Janus Kinases. Pharmaceuticals (Basel). 2019 Mar 12;12(1). pii: ph12010037. doi: 10.3390/ph12010037. [Article]
  2. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
In vitro, less than 10% of baricitinib is oxidatively metabolized by CYP3A4 [FDA Label].
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Coadministration of baricitinib with probenecid, a potent OAT3 inhibitor, resulted in increased AUC with no change in Cmax or Tmax of baricitinib. Concomitant use of OAT3 inhibitors such as diclofenac and ibupprofen may lead to increased exposure of baricitinib, however a clinically relevant interaction is not expected. Methotrexate, a substrate of several transporters including OAT3, is not reported to induce a clinically meaningful effect on baricitinib exposure. The inhibition was observed in vitro.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Inhibition was observed in vitro.
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Inhibition was observed in vitro, however, the FDA label states that this is unlikely to result in clinically significant drug interactions.
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. Posada MM, Cannady EA, Payne CD, Zhang X, Bacon JA, Pak YA, Higgins JW, Shahri N, Hall SD, Hillgren KM: Prediction of Transporter-Mediated Drug-Drug Interactions for Baricitinib. Clin Transl Sci. 2017 Nov;10(6):509-519. doi: 10.1111/cts.12486. Epub 2017 Jul 27. [Article]
  2. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
  3. Baracitinib FDA label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Inhibition was observed in vitro.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
Gene Name
SLC22A6
Uniprot ID
Q4U2R8
Uniprot Name
Solute carrier family 22 member 6
Molecular Weight
61815.78 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Inhibition was observed in vitro.
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Inhibition was observed in vitro.
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: OLUMIANT (baricitinib) tablets, for oral use [Link]

Drug created at October 20, 2016 20:50 / Updated at December 08, 2022 17:54