OLUMIANT

Baricitinib is a

Janus kinase (JAK) inhibitor.

JAKs are tyrosine protein kinases that play an important role in pro-inflammatory signaling pathways.

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.

Baricitinib was first approved by the European Commission (EC) in February for the treatment of rheumatoid arthritis in adults and was later approved by the FDA in 2018.

EC later approved baricitinib for the treatment of atopic dermatitis, making it the first JAK inhibitor used for this indication in Europe.

While baricitinib was granted emergency use as a treatment for COVID-19 in combination with remdesivir under the Emergency Use Authorization (EUA) in November the FDA fully approved the use of baricitinib for the treatment of COVID-19 in May 2022.

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.

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

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.

Recently, it is also approved as the treatment for severe alopecia areata in adults.

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.

Baricitinib decreased the levels of immunoglobulins and serum C-reactive protein in patients with rheumatoid arthritis.

Tyrosine-protein kinase

JAK1 Inhibitor Tyrosine-protein kinase JAK2 Inhibitor Tyrosine-protein kinase JAK3 Inhibitor.

The absolute bioavailability of baricitinib is approximately 80%.

C max was reached after one hour of oral drug administration.

A high-fat meal decreased the mean AUC and C max of baricitinib by approximately 11% and 18%, respectively, and delayed T max by 0.5 hours.

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

Baricitinib is metabolized by

Approximately 6% of the Oral administered dose was identified as metabolites in urine and feces; however, no metabolites of baricitinib were quantifiable in plasma.

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.

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.

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.

Improve decision support & research outcomes With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.

View sample adverse effects data in our new Data Library! See the data Improve decision support & research outcomes with our structured adverse effects data.

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

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.