JAK inhibitor Upadacitinib:FDA approval,Brand name,Indications and Side effects

Upadacitinib is a second-generation selective Janus kinase (JAK) inhibitor targeting the JAK1 enzyme.

Upadacitinib FDA approval

Upadacitinib received FDA approval on August 16, 2019, based on positive and promising results from its multinational phase III trials in subjects with moderate to severe rheumatoid arthritis.

Upadacitinib Brand name

Rinvoq

Rinvoq LQ

Upadacitinib Indications

Upadacitinib is a new FDA-approved second-line agent for treating moderate to severe active rheumatoid arthritis (RA) in patients who have not shown an adequate response or intolerance to the first-line agent, methotrexate.

Using upadacitinib with other JAK inhibitors (JAKinibs) or robust immunosuppressants like azathioprine and cyclosporine is not advised. However, its use in combination with nonbiologic disease-modifying antirheumatic drugs (DMARDs) such as methotrexate is supported, while its use with biological DMARDs is not recommended. When combined with the first-line therapy methotrexate, upadacitinib repressed disease progression on radiographic imaging and maintained clinical efficacy.

Clinical advancements for agents used in other autoimmune diseases, such as psoriatic arthritis (PA), atopic dermatitis (AD), ankylosing spondylitis (AS), giant cell arteritis (GCA), systemic lupus erythematosus (SLE), and inflammatory bowel disease (IBD), Crohn disease (CD) and ulcerative colitis (UC), have shown promising results. Upadacitinib marks a significant milestone as the first oral medication approved by the FDA to treat moderate to severe Crohn disease.

Upadacitinib Side effects

Upadacitinib has various adverse effects, which are listed below.

Upper respiratory tract infections (URTI) (14%)

Nausea (4%)

Elevated liver enzymes (2%)

Fever (1%)

Cough (2%)

Upper respiratory tract infections (URTI) encompass:

Acute sinusitis

Laryngitis

Nasopharyngitis

Oropharyngeal pain

Pharyngitis

Pharyngotonsillitis

Rhinitis

Sinusitis

Tonsillitis

Viral upper respiratory tract infection

Upadacitinib Toxicity

Upadacitinib was found to be teratogenic in animal studies, although no human studies during pregnancy have been reported. Use during pregnancy is not recommended. Contraception is advised during treatment and for 4 weeks after completing treatment with upadacitinib.

Hepatotoxicity

The pattern of liver injury associated with upadacitinib indicates a potential for low-level, direct hepatotoxicity.