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upadacitinib (Rinvoq, ABT-494)

Indications: - treatment of rheumatoid arthritis [4] (FDA-approved) - 74% improvement in patients with severe atopic dermatitis [2] - superior to dupilumab (Dupixent) for moderate-severe atopic dermatitis [7] Dosage: - 15-30 mg PO QD Adverse effects: - venous thromboembolism - neutropenia [3] - infections - upper respiratory tract infection - pneumonia - enterocolitis - staphylococcal wound infections - Herpes zoster Mechanism of action: - inhibits JAK-1 Clinical trials: - clinical response at week 12 was significantly higher with 15 or 30 mg of upadacitinib than with placebo [6] - 30 mg dose but not the 15 mg dose was superior to adalimumab [6] - adverse events were more frequent with upadacitinib than with placebo [6]

Interactions

drug adverse effects of tyrosine kinase inhibitor(s)

General

Janus kinase inhibitor; JAK inhibitor

Database Correlations

PUBCHEM correlations

References

  1. McNamara D JAK-1 Inhibitor Effective for RA, but Safety Signal Troubles. Medscape - Nov 13, 2017. https://www.medscape.com/viewarticle/888522
  2. Bankhead C Strong Eczema Response to JAK Inhibitor. Half of patients achieved EASI 90 at 16 weeks. MedPage Today. February 19, 2018 https://www.medpagetoday.com/meetingcoverage/aad/71244 - Guttman-Yassky E, et al Primary results from a phase IIb, randomized, placebo controlled trial of upadacitinib for patients with atopic dermatitis. American Academy of Dermatology (AAD) 2018; Abstract 6533.
  3. Walsh N, Promising Results Seen with New JAK-1 Drug. Upadacitinib showed significant efficacy in DMARD inadequate responders. MedPage Today. May 03, 2018 https://www.medpagetoday.com/meetingcoverage/bsr/72680 - Burmester G, et al A phase III randomized placebo-controlled double-blind study of upadacitinib (ABT-494), a selective JAK-1 inhibitor, in patients with active rheumatoid arthritis with inadequate response to conventional synthetic DMARDs. British Society for Rheumatology (BSR) 2018; abstract 242
  4. Walsh N New JAK1 Agent Beats Humira in Rheumatoid Arthritis Thrombotic events balanced between upadacitinib, adalimumab, and placebo. MedPage Today. October 22, 2018 https://www.medpagetoday.com/meetingcoverage/acr/75846 - Fleischmann R, Pangan AL, Mysler E et al A Phase 3, Randomized, Double-Blind Study Comparing Upadacitinib to Placebo and to Adalimumab, in Patients with Active Rheumatoid Arthritis with Inadequate Response to Methotrexate. American College of Rheumatology (ACR) 2018 annual meeting. Abstract 890. https://acrabstracts.org/abstract/a-phase-3-randomized-double-blind-study-comparing-upadacitinib-to-placebo-and-to-adalimumab-in-patients-with-active-rheumatoid-arthritis-with-inadequate-response-to-methotrexate/
  5. Walsh N Rinvoq for RA: Benefits Persist Beyond 1 Year - Manufacturer's extension study shows no loss of clinical response. MedPage Today November 6, 2020 https://www.medpagetoday.com/meetingcoverage/acr/89523 - van Vollenhoven R, et al Upadacitinib monotherapy in methotrexate-naive patients with rheumatoid arthritis: results at 72 weeks. American College of Rheumatology (ACR) 2020; Abstract 0207
  6. McInnes IB, Anderson JK, Magrey M et al Trial of Upadacitinib and Adalimumab for Psoriatic Arthritis. N Engl J Med 2021; 384:1227-1239. April 1. PMID: 33789011 https://www.nejm.org/doi/full/10.1056/NEJMoa2022516
  7. Gever J JAK Inhibitor Tops Mab for Eczema. New disease-modifying treatment option on the horizon. MedPage Today August 4, 2021 https://www.medpagetoday.com/dermatology/atopy/93891 - Blauvelt A, Teixeira HD, Simpson EL et al Efficacy and Safety of Upadacitinib vs Dupilumab in Adults With Moderate-to-Severe Atopic DermatitisA Randomized Clinical Trial. JAMA Dermatol. 2021 Aug 4 PMID: 34347860 https://jamanetwork.com/journals/jamadermatology/fullarticle/2782803