Peringatan Keamanan

The oral lowest published toxic dose (TDLo) is 1820 g/kg in mice and 5096 g/kg in rats.L41765

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.L41760

Baricitinib

DB11817

small molecule approved investigational

Deskripsi

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.L41760

Baricitinib was first approved by the European Commission (EC) in February 2017 for the treatment of rheumatoid arthritis in adults A248395 and was later approved by the FDA in 2018.A248400 The EC later approved baricitinib for the treatment of atopic dermatitis, making it the first JAK inhibitor used for this indication in Europe.A248405 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,L22619 the FDA fully approved the use of baricitinib for the treatment of COVID-19 in May 2022.L41760

Struktur Molekul 2D

Berat 371.42
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (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.[L41760]
Volume Distribusi Following intravenous administration, the volume of distribution was 76 L, indicating distribution into tissues.[L41760]
Klirens (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.[L41760]

Absorpsi

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.L41760

Metabolisme

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.L41760

Rute Eliminasi

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.L41760

Interaksi Makanan

1 Data
  • 1. 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.

Interaksi Obat

1165 Data
Denosumab The risk or severity of adverse effects can be increased when Denosumab is combined with Baricitinib.
Peginterferon alfa-2a The risk or severity of adverse effects can be increased when Peginterferon alfa-2a is combined with Baricitinib.
Interferon alfa-n1 The risk or severity of adverse effects can be increased when Interferon alfa-n1 is combined with Baricitinib.
Interferon alfa-n3 The risk or severity of adverse effects can be increased when Interferon alfa-n3 is combined with Baricitinib.
Peginterferon alfa-2b The risk or severity of adverse effects can be increased when Peginterferon alfa-2b is combined with Baricitinib.
Interferon gamma-1b The risk or severity of adverse effects can be increased when Interferon gamma-1b is combined with Baricitinib.
Interferon alfa-2a The risk or severity of adverse effects can be increased when Interferon alfa-2a is combined with Baricitinib.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Baricitinib.
Pegaspargase The risk or severity of adverse effects can be increased when Pegaspargase is combined with Baricitinib.
Interferon beta-1b The risk or severity of adverse effects can be increased when Interferon beta-1b is combined with Baricitinib.
Interferon alfacon-1 The risk or severity of adverse effects can be increased when Interferon alfacon-1 is combined with Baricitinib.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Baricitinib.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Baricitinib.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Baricitinib.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Baricitinib.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Baricitinib.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Baricitinib.
Alefacept The risk or severity of adverse effects can be increased when Alefacept is combined with Baricitinib.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Baricitinib.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Baricitinib.
Interferon alfa-2b The risk or severity of adverse effects can be increased when Interferon alfa-2b is combined with Baricitinib.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Baricitinib.
Phenylalanine The risk or severity of adverse effects can be increased when Phenylalanine is combined with Baricitinib.
Bortezomib The risk or severity of adverse effects can be increased when Bortezomib is combined with Baricitinib.
Cladribine Baricitinib may increase the immunosuppressive activities of Cladribine.
Carmustine The risk or severity of adverse effects can be increased when Carmustine is combined with Baricitinib.
Amsacrine The risk or severity of adverse effects can be increased when Amsacrine is combined with Baricitinib.
Bleomycin The risk or severity of adverse effects can be increased when Bleomycin is combined with Baricitinib.
Chlorambucil The risk or severity of adverse effects can be increased when Chlorambucil is combined with Baricitinib.
Raltitrexed The risk or severity of adverse effects can be increased when Raltitrexed is combined with Baricitinib.
Mitomycin The risk or severity of adverse effects can be increased when Mitomycin is combined with Baricitinib.
Vindesine The risk or severity of adverse effects can be increased when Vindesine is combined with Baricitinib.
Floxuridine The risk or severity of adverse effects can be increased when Floxuridine is combined with Baricitinib.
Indomethacin The serum concentration of Baricitinib can be increased when it is combined with Indomethacin.
Tioguanine The risk or severity of adverse effects can be increased when Tioguanine is combined with Baricitinib.
Vinorelbine The risk or severity of adverse effects can be increased when Vinorelbine is combined with Baricitinib.
Dexrazoxane The risk or severity of adverse effects can be increased when Dexrazoxane is combined with Baricitinib.
Streptozocin The risk or severity of adverse effects can be increased when Streptozocin is combined with Baricitinib.
Trifluridine The risk or severity of adverse effects can be increased when Trifluridine is combined with Baricitinib.
Gemcitabine The risk or severity of adverse effects can be increased when Gemcitabine is combined with Baricitinib.
Epirubicin The risk or severity of adverse effects can be increased when Epirubicin is combined with Baricitinib.
Lenalidomide The risk or severity of adverse effects can be increased when Lenalidomide is combined with Baricitinib.
Altretamine The risk or severity of adverse effects can be increased when Altretamine is combined with Baricitinib.
Zidovudine The serum concentration of Baricitinib can be increased when it is combined with Zidovudine.
Vincristine The risk or severity of adverse effects can be increased when Vincristine is combined with Baricitinib.
Fluorouracil The risk or severity of adverse effects can be increased when Fluorouracil is combined with Baricitinib.
Propylthiouracil The risk or severity of adverse effects can be increased when Propylthiouracil is combined with Baricitinib.
Pentostatin The risk or severity of adverse effects can be increased when Pentostatin is combined with Baricitinib.
Methotrexate The serum concentration of Baricitinib can be increased when it is combined with Methotrexate.
Linezolid The serum concentration of Baricitinib can be increased when it is combined with Linezolid.
Clofarabine The risk or severity of adverse effects can be increased when Clofarabine is combined with Baricitinib.
Prednisone The risk or severity of adverse effects can be increased when Prednisone is combined with Baricitinib.
Pemetrexed The risk or severity of adverse effects can be increased when Pemetrexed is combined with Baricitinib.
Fludrocortisone The risk or severity of adverse effects can be increased when Fludrocortisone is combined with Baricitinib.
Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Baricitinib.
Irinotecan The risk or severity of adverse effects can be increased when Irinotecan is combined with Baricitinib.
Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Baricitinib.
Dacarbazine The risk or severity of adverse effects can be increased when Dacarbazine is combined with Baricitinib.
Temozolomide The risk or severity of adverse effects can be increased when Temozolomide is combined with Baricitinib.
Penicillamine The risk or severity of adverse effects can be increased when Penicillamine is combined with Baricitinib.
Mechlorethamine The risk or severity of adverse effects can be increased when Mechlorethamine is combined with Baricitinib.
Azacitidine The risk or severity of adverse effects can be increased when Azacitidine is combined with Baricitinib.
Carboplatin The risk or severity of adverse effects can be increased when Carboplatin is combined with Baricitinib.
Dactinomycin The risk or severity of adverse effects can be increased when Dactinomycin is combined with Baricitinib.
Cytarabine The risk or severity of adverse effects can be increased when Cytarabine is combined with Baricitinib.
Azathioprine The risk or severity of adverse effects can be increased when Azathioprine is combined with Baricitinib.
Hydroxyurea The risk or severity of adverse effects can be increased when Hydroxyurea is combined with Baricitinib.
Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Baricitinib.
Mercaptopurine The serum concentration of Baricitinib can be increased when it is combined with Mercaptopurine.
Thalidomide The risk or severity of adverse effects can be increased when Thalidomide is combined with Baricitinib.
Melphalan The risk or severity of adverse effects can be increased when Melphalan is combined with Baricitinib.
Fludarabine The risk or severity of adverse effects can be increased when Fludarabine is combined with Baricitinib.
Flucytosine The risk or severity of adverse effects can be increased when Flucytosine is combined with Baricitinib.
Capecitabine The risk or severity of adverse effects can be increased when Capecitabine is combined with Baricitinib.
Trilostane The risk or severity of adverse effects can be increased when Trilostane is combined with Baricitinib.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Baricitinib.
Arsenic trioxide The risk or severity of adverse effects can be increased when Arsenic trioxide is combined with Baricitinib.
Idarubicin The risk or severity of adverse effects can be increased when Idarubicin is combined with Baricitinib.
Estramustine The risk or severity of adverse effects can be increased when Estramustine is combined with Baricitinib.
Lomustine The risk or severity of adverse effects can be increased when Lomustine is combined with Baricitinib.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Baricitinib.
Decitabine The risk or severity of adverse effects can be increased when Decitabine is combined with Baricitinib.
Nelarabine The risk or severity of adverse effects can be increased when Nelarabine is combined with Baricitinib.
Ciclesonide The risk or severity of adverse effects can be increased when Ciclesonide is combined with Baricitinib.
Stepronin The risk or severity of adverse effects can be increased when Stepronin is combined with Baricitinib.
Hydroxychloroquine The risk or severity of adverse effects can be increased when Hydroxychloroquine is combined with Baricitinib.
Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Baricitinib.
Vorinostat The risk or severity of adverse effects can be increased when Vorinostat is combined with Baricitinib.
2-Methoxyethanol The risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Baricitinib.
Brequinar The risk or severity of adverse effects can be increased when Brequinar is combined with Baricitinib.
Thiotepa The risk or severity of adverse effects can be increased when Thiotepa is combined with Baricitinib.
Aldosterone The risk or severity of adverse effects can be increased when Aldosterone is combined with Baricitinib.
Ixabepilone The risk or severity of adverse effects can be increased when Ixabepilone is combined with Baricitinib.
Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Baricitinib.
Belinostat The risk or severity of adverse effects can be increased when Belinostat is combined with Baricitinib.
Trabectedin The risk or severity of adverse effects can be increased when Trabectedin is combined with Baricitinib.
Interferon alfa The risk or severity of adverse effects can be increased when Interferon alfa is combined with Baricitinib.
Glatiramer The risk or severity of adverse effects can be increased when Glatiramer is combined with Baricitinib.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Baricitinib.
Human interferon omega-1 The risk or severity of adverse effects can be increased when Human interferon omega-1 is combined with Baricitinib.

Target Protein

Tyrosine-protein kinase JAK1 JAK1
Tyrosine-protein kinase JAK2 JAK2
Tyrosine-protein kinase JAK3 JAK3
Non-receptor tyrosine-protein kinase TYK2 TYK2

Referensi & Sumber

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
Artikel (PubMed)
  • PMID: 28255337
    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.
  • PMID: 27028914
    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.
  • PMID: 23532440
    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.
  • PMID: 28290136
    Markham A: Baricitinib: First Global Approval. Drugs. 2017 Apr;77(6):697-704. doi: 10.1007/s40265-017-0723-3.
  • PMID: 30871014
    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.
  • PMID: 34828623
    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.
  • PMID: 34283430
    Ahmad A, Zaheer M, Balis FJ: Baricitinib .

Contoh Produk & Brand

Produk: 25 • International brands: 0
Produk
  • Baricitinib
    Tablet, film coated • 4 mg/1 • Oral • US
  • Olumiant
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  • Olumiant
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  • Olumiant
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  • Olumiant
    Tablet, film coated • 4 mg • Oral • EU • Approved
  • Olumiant
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    Tablet, film coated • 1 mg • Oral • EU • Approved
Menampilkan 8 dari 25 produk.

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