upadacitinib hemihydrate: clinical use

Prescribing considerations

• Initiation and supervision should be by a clinician experienced in the condition being treated.
• Assess infection, tuberculosis, viral hepatitis, cardiovascular, malignancy and venous-thromboembolism risks before treatment.
• For patients aged 65 years or older, long-term current or former smokers, or those with cardiovascular or malignancy risk factors, use only when no suitable alternative is available.
• Review immunisations before initiation and consider prophylactic shingles vaccination; avoid live vaccines around treatment.
• Use caution with diverticular disease, previous diverticulitis, severe renal impairment or established venous-thromboembolism risks.

Contraindications and cautions

• Hypersensitivity to upadacitinib or an excipient
• Active tuberculosis or another active serious infection
• Severe hepatic impairment
• Pregnancy

Monitoring

• Full blood count, including neutrophils, lymphocytes and haemoglobin, at baseline and during treatment.
• Liver transaminases at baseline and subsequently according to clinical management.
• Lipids after treatment begins and thereafter as clinically appropriate.
• Tuberculosis and viral hepatitis screening, with ongoing vigilance for reactivation or new infection.
• Periodic skin examination and reassessment of cardiovascular, malignancy and thromboembolic risk.
• Prompt investigation of new infection, severe abdominal symptoms, thromboembolic symptoms or visual disturbance.

Clinical pharmacology

Upadacitinib is a selective, reversible JAK inhibitor with preferential functional inhibition of JAK1 or JAK1/3 signalling. It is absorbed from the prolonged-release formulation, metabolised mainly through CYP3A4 and eliminated as both unchanged compound and metabolites.

Formulation and product differences

• The selected product is a prolonged-release oral tablet.
• The tablet must remain intact to preserve prolonged-release delivery.
• Repeated visible tablet residue in stool or ostomy output may indicate shortened gastrointestinal transit and warrants clinical review.

Modified-release tablet

Route: Oral

Strengths: 15 mg, 30 mg, 45 mg