bDMARDs Quick Reference Guide

Upadacitinib

Upadacitinib

Active ingredient

Upadacitinib

Mechanism of action

Janus Kinase [JAK] 1 inhibitor

Molecule type

Small molecule

PBS listed indications

Severe active rheumatoid arthritis

Ankylosing spondylitis

Severe psoriatic arthritis

Reference product (brand)

Rinvoq

Administration information

Mode of administration

Oral

Administration devices and strengths

15mg modified release tablet

Swallow whole do not crush or chew.

Frequency of administration

Once daily

Storage

Store below 30oC

Store in the original blister packaging to protect from moisture.

Standard dosing

15mg once daily

 

Treatment with csDMARDs (e.g., methotrexate) may be continued during treatment with upadacitinib

Dose variations

Patients with rheumatoid arthritis who are in remission or have low disease activity may have their dose of upadacitinib down-titrated by their rheumatologist.

 

Special notes

Upadacitinib is metabolised by CYP3A4; giving it with a strong CYP3A4 inhibitor (e.g. ketoconazole) may increase its concentration and the risk of adverse effects. Use combinations with strong CYP3A4 inhibitors cautiously and monitor for adverse effects.
Drugs that induce CYP3A4 (e.g. rifampicin, phenytoin) may decrease upadacitinib concentration and possibly its efficacy; monitor response to upadacitinib carefully if combination is used.

 

Upadacitinib may cause anaemia, neutropenia or lymphopenia; treatment with other drugs that also have these effects may increase the risk of their occurrence; avoid combinations or monitor closely.

 

Monitor lipids 12 weeks after first dose. If needed, patients should then be managed according to local clinical guidelines for management of hyperlipidaemia.

 

Events of DVT, PE and arterial thrombosis have been reported in patients receiving upadacitinib. Use with caution in patients with risk factors for DVT or PE such as older age, obesity, history of DVT / PE or patients undergoing surgery and immobilisation.

 

Avoid use of upadacitinb in patients with an active serious infection, including localised infections. Closely monitor patients for development of signs and symptoms of infection during treatment. Interrupt therapy if patients develop serious or opportunistic infections.

Screen for hepatitis B or C and active or latent TB (begin TB treatment before starting upadacitinib).
Patients with suspected latent or active TB should be treated in consultation with an Infectious Diseases physician.

Patients with a history of herpes zoster infection may be at risk of viral reactivation while being treated with upadacitinib. If a patient develops herpes zoster, consider temporarily interrupting therapy until the episode resolves.

 

Live vaccines should not be given concurrently with upadacitinib.

References

Pharmaceutical benefits Scheme (PBS) listing. Available from  https://www.pbs.gov.au/medicine/item/11979L-11989B [accessed 8/10/21]

Product information. Available from  https://www.ebs.tga.gov.au/ebs/picmi/picmirepository.nsf/pdf?OpenAgent&id=CP-2020-PI-01075-1 [accessed 8/10/21]

Australian Medicines Handbook 2020 (online). Adelaide: Australian Medicines Handbook Pty Ltd; 2020 July. Available from: https://amhonline.amh.net.au/    [accessed 13/5/21]

NPS Medicinewise. Down-titration strategies. Available from https://www.nps.org.au/bdmards/rheumatology-conditions/titration-strategies [accessed 13/5/21]