Indication

Rheumatoid Arthritis

Adult Dose

Rheumatoid Arthritis\r\nIndicated for moderately to severely active rheumatoid arthritis in adults who have had an inadequate response or intolerance to methotrexate\r\n\r\n15 mg PO qDay\r\n\r\nMay be used as monotherapy or in combination with methotrexate or other nonbiological DMARDs\r\n\r\nHepatic impairment\r\nMild or moderate (Child-Pugh A or B): No dose adjustment required\r\nSevere (Child-Pugh C): Not recommended

Renal Dose

Renal impairment\r\nMild, moderate, or severe: No dose adjustment required\r\nESRD: Not studied\r\n

Mode of Action

Janus kinase-1 (JAK1)-selective inhibitor; JAK1 is essential for signaling for certain cytokines to elicit signals from various interleukins, cardiotrophin, neurotrophin, and interferons\r\n\r\nThese signals are essential in maintaining the inflammatory condition in rheumatoid arthritis (RA); inhibition of JAK reduces production of and modulates proinflammatory cytokines central to RA

Precaution

Malignancies reported; consider risks and benefits of treatment before initiating in patients with known malignancy, other than previously treated nonmelanoma skin cancer; screen for malignancies during treatment according to guidelines\r\n\r\nThrombosis reported, including DVT, PE, and arterial thrombosis\r\n\r\nGastrointestinal perforation reported; unknown if JAK inhibition is implicated in these events; many patients were also receiving NSAIDs\r\n\r\nMay cause neutropenia, lymphopenia, anemia, elevated lipids, or elevated liver enzymes; monitor for abnormal laboratory values and assess the need to interrupt dosing\r\n\r\nBased on findings in animal studies, may cause fetal harm when administered to pregnant women

Side Effect

>10%\r\nUpper respiratory tract infection (13.5%)\r\n\r\n1-10%\r\nNausea (3.5%)\r\n\r\nNeutropenia (1.1-2.4%)\r\n\r\nLymphopenia (0.3-2.4%)\r\n\r\nCough (2.2%)\r\n\r\nElevated ALT (0.8-2.1%)\r\n\r\nIncreased creatine phosphokinase (0.3-1.6%)\r\n\r\nElevated AST (1-1.5%)\r\n\r\nPyrexia (1.2%)\r\n\r\n<1%\r\nPneumonia\r\n\r\nHerpes zoster\r\n\r\nHerpes simplex (includes oral herpes)\r\n\r\nOral candidiasis\r\n\r\nAnemia (<0.1%)

Pregnancy Category Note