Indications

Upacit XR is a Janus Kinase (JAK) inhibitor indicated for the treatment of:

Moderate to severe active Rheumatoid Arthritis in adults who have had an inadequate response or intolerance to one or more TNF blockers.
Active Psoriatic Arthritis in adults and pediatric patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers.
Refractory moderate to severe Atopic Dermatitis in adults and pediatric patients 12 years of age and older whose disease is not adequately controlled with other systemic therapies, including biologics, or when those therapies are not advisable.
Moderately to severely active Ulcerative Colitis in adults who have had an inadequate response or intolerance to one or more TNF blockers.
Moderately to severely active Crohn's Disease in adults who have had an inadequate response or intolerance to one or more TNF blockers.
Active Ankylosing Spondylitis in adults who have had an inadequate response or intolerance to one or more TNF blockers.
Active Non-radiographic Axial Spondyloarthritis in adults with objective signs of inflammation who have had an inadequate response or intolerance to TNF blocker therapy.
Active Polyarticular Juvenile Idiopathic Arthritis in patients 2 years of age and older who have had an inadequate response or intolerance to one or more TNF blockers.

Pharmacology

Upadacitinib is a selective Janus Kinase (JAK) inhibitor. It works by inhibiting JAK enzymes involved in cytokine signaling pathways, thereby reducing inflammation and modulating immune responses. This inhibition prevents the phosphorylation and activation of STAT proteins that regulate gene expression and immune cell function.

Dosage & Administration

Rheumatoid Arthritis

15 mg once daily.

Psoriatic Arthritis

Adults: 15 mg once daily.

Atopic Dermatitis

Patients weighing at least 40 kg: Start with 15 mg once daily.
If adequate response is not achieved, increase to 30 mg once daily.
Discontinue treatment if there is no adequate response at 30 mg.
Adults aged 65 years and older: 15 mg once daily.

Ulcerative Colitis

Induction: 45 mg once daily for 8 weeks.
Maintenance: 15 mg once daily.
30 mg once daily may be considered in refractory, severe, or extensive disease.

Crohn's Disease

Induction: 45 mg once daily for 12 weeks.
Maintenance: 15 mg once daily.
30 mg once daily may be considered in refractory, severe, or extensive disease.

Ankylosing Spondylitis

15 mg once daily.

Non-radiographic Axial Spondyloarthritis

15 mg once daily.

Polyarticular Juvenile Idiopathic Arthritis

Patients weighing 30 kg or more: 15 mg once daily.

Drug Interactions

Strong CYP3A4 Inhibitors (e.g., Ketoconazole)

May increase Upadacitinib exposure.
Use with caution.

Strong CYP3A4 Inducers (e.g., Rifampin)

May decrease Upadacitinib exposure and reduce efficacy.
Concomitant use is not recommended.

Side Effects

Rheumatoid Arthritis, Psoriatic Arthritis, Ankylosing Spondylitis, and Non-radiographic Axial Spondyloarthritis

Upper respiratory tract infections
Herpes zoster
Herpes simplex
Bronchitis
Nausea
Cough
Fever
Acne
Headache

Atopic Dermatitis

Upper respiratory tract infections
Acne
Herpes simplex
Headache
Increased creatine phosphokinase
Cough
Hypersensitivity
Folliculitis
Nausea
Abdominal pain
Weight gain
Herpes zoster
Influenza
Fatigue
Neutropenia
Myalgia

Ulcerative Colitis

Upper respiratory tract infections
Increased creatine phosphokinase
Acne
Neutropenia
Elevated liver enzymes
Rash

Crohn's Disease

Upper respiratory tract infections
Anemia
Fever
Acne
Herpes zoster
Headache