Upadacitinib

Reucent XR is a Janus kinase (JAK) inhibitor indicated for the treatment of-

Adults with moderate to severe active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

Adults and pediatric patients 2 years of age and older with active psoriatic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

... Read more Reucent XR is a Janus kinase (JAK) inhibitor indicated for the treatment of-

Adults with moderate to severe active rheumatoid arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

Adults and pediatric patients 2 years of age and older with active psoriatic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

Adults and pediatric patients 12 years of age and older with refractory, moderate to severe atopic dermatitis whose disease is not adequately controlled with other systemic drug products, including biologics, or when use of those therapies are inadvisable.

Adults with moderately to severely active ulcerative colitis who have had an inadequate response or intolerance to one or more TNF blockers.

Adults with moderately to severely active Crohn’s disease who have had an inadequate response or intolerance to one or more TNF blockers.

Adults with active ankylosing spondylitis who have had an inadequate response or intolerance to one or more TNF blockers.

Adults with active nonradiographic axial spondyloarthritis with objective signs of inflammation who have had an inadequate response or intolerance to TNF blocker therapy.

Patients 2 years of age and older with active polyarticular juvenile idiopathic arthritis who have had an inadequate response or intolerance to one or more TNF blockers.

Upadacitinib is a Janus kinase (JAK) inhibitor. JAKs are intracellular enzymes that transmit signals arising from cytokine or growth factor- receptor interactions on the cellular membrane to influence cellular processes of hematopoiesis and immune cell function. Within the signaling pathway, JAKs phosphorylate and activate signal. Transducers and Activators of Transcription(STATs) which modulate intracellular activity including gene expression. Upadacitinib modulates the signaling pathway at the point of JAKs, preventing the phosphorylation and activation of STATs.

Rheumatoid Arthritis : 15 mg once daily. Psoriatic Arthritis:

Adults 18 Years of Age and Older: 15 mg once daily.

Atopic Dermatitis:

12 kg-65 kg (Weighing at least 40 kg): Initiate with 15 mg once daily. If an adequate response is not achieved, consider increasing the dosage to 30 mg once daily. Discontinue if an adequate response is not achieved with the 30 mg dose.

Adults 65 Years of Age and Older: 15 mg once daily.

Ulcerative Colitis (Adult Patients):

Induction: 45 mg once daily for 8 weeks.

Maintenance: 15 mg once daily. A dosage of 30 mg once daily may be considered for patients with refractory, severe or extensive disease. Discontinue if an adequate therapeutic response is not achieved with the 30 mg dosage.

Crohn's Disease (Adult Patients)

Induction: 45 mg once daily for 12 weeks.

Maintenance: 15 mg once daily. A dosage of 30 mg once daily may be considered for patients with refractory, severe or extensive disease. Discontinue if an adequate therapeutic response is not achieved with the 30 mg dosage.

Ankylosing Spondylitis : 15 mg once daily. Non-radiographic Axial Spondyloarthritis : 15 mg once daily. Polyarticular Juvenile Idiopathic Arthritis : (30 kg and greater): 15 mg once daily.

Strong CYP3A4 Inhibitors : Reucent XR exposure is increased when co-administered with strong CYP3A4 inhibitors (such as ketoconazole). Reucent XR should be used with caution in patients receiving chronic treatment with strong CYP3A4 inhibitors. Strong CYP3A4 Inducers : Reucent XR exposure is decreased when co-administered with strong CYP3A4 inducers (such as rifampin), which may lead to reduced therapeutic effect of Reucent XR. Coadministration of Reucent XR with strong CYP3A4 inducers is not recommended.

Rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and nonradiographic axial spondyloarthritis : Adverse reactions (≥1%) were: upper respiratory tract infections, herpes zoster, herpes simplex, bronchitis, nausea, cough, pyrexia, acne, and headache. Atopic Dermatitis : Adverse reactions (≥1%) are: upper respiratory tract infections, acne, herpes simplex, headache, blood creatine phosphokinase increased, cough, hypersensitivity, folliculitis, nausea, abdominal pain, pyrexia, increased weight, herpes zoster, influenza, fatigue, neutropenia, myalgia, and influenza like illness. Ulcerative Colitis : Adverse reactions (≥5%) reported during induction or maintenance are: upper respiratory tract infections, increased blood creatine phosphokinase, acne, neutropenia, elevated liver enzymes, and rash. Crohn's Disease : Adverse reactions (≥5%) reported during induction or maintenance are: upper respiratory tract infections, anemia, pyrexia, acne, herpes zoster, and headache.

The limited human data on the use of Upadacitinib in pregnant women are not sufficient to evaluate a drug-associated risk for major birth defects or miscarriage. Based on animal studies, upadacitinib has the potential to adversely affect a developing fetus. Advise not to breastfeed.

Serious Infections : Avoid use of Reucent XR in patients with active, serious infection, including localized infections. Malignancy : Consider the risks and benefits of Reucent XR treatment prior to initiating therapy in patients with a known malignancy. Thrombosis : Consider the risks and benefits prior to treating patients who may be at increased risk of thrombosis. Promptly evaluate patients with symptoms of thrombosis and treat appropriately. Gastrointestinal Perforations : Use with caution in patients who may be at increased risk. Laboratory Monitoring: Recommended due to potential changes in lymphocytes, neutrophils, hemoglobin, liver enzymes and lipids. Embryo-Fetal Toxicity : Reucent XR may cause fetal harm based on animal studies. Advise females of reproductive potential of the potential risk to a fetus and to use effective contraception. Vaccinations : Avoid use of Reucent XR with live vaccines.

Reucent XR was administered in clinical trials up to doses equivalent in daily AUC to 60 mg extended-release once daily. Adverse events were comparable to those seen at lower doses and no specific toxicities were identified. Approximately 90% of Reucent XR in the systemic circulation is eliminated within 24 hours of dosing (within the range of doses evaluated in clinical studies). In case of an overdose, it is recommended that the patient be monitored for signs and symptoms of adverse reactions. Patients who develop adverse reactions should receive appropriate treatment.

Do not store above 25°C. Protect from light. Keep out of reach of children.