Use of in combination with other Janus kinase (JAK) inhibitors, biologic disease-modifying antirheumatic drugs (DMARDs), or with potent immunosuppressants such as azathioprine and cyclosporine, is not recommended.
Advise patients not to breastfeed. Upadacitinib is not recommended in patients with severe hepatic impairment.
- TRADE NAME: Rinvoq (AbbVie)
- INDICATIONS: Treatment of adults with moderately to severely active rheumatoid arthritis who have had an inadequate response or intolerance to methotrexate.
- CLASS: Janus kinase (JAK) inhibitor
- HALF-LIFE: 8–14 hours
- FDA APPROVAL DATE: 08/16/2019
- CLINICALLY IMPORTANT, POTENTIALLY HAZARDOUS INTERACTIONS WITH:
Coadministration of upadacitinib with strong CYP3A4 inducers (e.g. rifampin) is not recommended, Rifampin, upadacitinib should be used with caution in patients receiving chronic treatment with strong CYP3A4 inhibitors (e.g. ketoconazole). - PREGNANCY: Based on animal studies, upadacitinib may cause embryo-fetal harm when administered to pregnant women. Advise female patients of reproductive potential to use effective contraception during treatment with upadacitinib and for 4 weeks after the final dose.
- See adverse reactions attributed to class:
WARNING: SERIOUS INFECTIONS, MORTALITY, MALIGNANCY, MAJOR ADVERSE CARDIOVASCULAR EVENTS (MACE), AND THROMBOSIS (amended December 2021).
• INCREASED RISK OF SERIOUS BACTERIAL, FUNGAL, VIRAL, AND OPPORTUNISTIC INFECTIONS LEADING TO HOSPITALIZATION OR DEATH, INCLUDING TUBERCULOSIS (TB). INTERRUPT TREATMENT WITH UPADACITINIB IF SERIOUS INFECTION OCCURS UNTIL THE INFECTION IS CONTROLLED. TEST FOR LATENT TB BEFORE AND DURING THERAPY; TREAT LATENT TB PRIOR TO USE. MONITOR ALL PATIENTS FOR ACTIVE TB DURING TREATMENT, EVEN PATIENTS WITH INITIAL NEGATIVE, LATENT TB TEST.
• HIGHER RATE OF ALL-CAUSE MORTALITY, INCLUDING SUDDEN CARDIOVASCULAR DEATH WITH ANOTHER JANUS KINASE (JAK) INHIBITOR VS. TUMOR NECROSIS FACTOR (TNF) BLOCKERS IN RHEUMATOID ARTHRITIS (RA) PATIENTS.
• MALIGNANCIES HAVE OCCURRED IN PATIENTS TREATED WITH UPADACITINIB. HIGHER RATE OF LYMPHOMAS AND LUNG CANCERS WITH ANOTHER JAK INHIBITOR VS. TNF BLOCKERS IN RA PATIENTS.
• HIGHER RATE OF MACE (DEFINED AS CARDIOVASCULAR DEATH, MYOCARDIAL INFARCTION, AND STROKE) WITH ANOTHER JAK INHIBITOR VS. TNF BLOCKERS IN RA PATIENTS.
• THROMBOSIS HAS OCCURRED IN PATIENTS TREATED WITH UPADACITINIB. INCREASED INCIDENCE OF PULMONARY EMBOLISM, VENOUS AND ARTERIAL THROMBOSIS WITH ANOTHER JAK INHIBITOR VS. TNF BLOCKERS.
See full prescribing information for complete boxed warning
Please login to view the rest of this drug profile.
Click on the DRUG REVIEW ARTICLE tab (above) to see a review of upadacitinib in the Taylor & Francis journal Expert Opinion on Drug Safety.
(Note that non-subscribers to the journal will only be able to see an abstract of the article.)
Page last updated 09/11/2024
