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ruxolitinib (Jakafi, Opzelura)

Indications: - 1st FDA-approved drug for treatment of myelofibrosis - polycythemia vera - atopic dermatitis (topical) [2] - vitiligo (Opzelura, topical FDA-approved)* [3] - glucocorticoid-refractory chronic graft-versus-host disease [4] * after 2 years, 84% with > 50% improvement in facial vitiligo, 52% with 90% improvement [3] Dosage: - 10 mg PO BID [4] - topical (Opzelura) BID Tabs: 5, 10, 15, 20, 25 mg Cream: 1.5% Adverse effects: - thrombocytopenia - anemia - fatigue - diarrhea - dyspnea - headache - dizziness - nausea - confusion Mechanism of action: - inhibits JAK1 & JAK2 - reduces myelofibrosis-related symptoms, including splenomegaly, abdominal pain, night sweats, bone or muscle pain, itching

General

small inhibitory antineoplastic agent (ib drug) enzyme inhibitor

Database Correlations

PUBCHEM correlations

References

  1. Chestecka Z Medscape Oncology, 11/16/2011 FDA Approves Ruxolitinib, First Drug Ever for Myelofibrosis http://www.medscape.com/viewarticle/753682
  2. Kim BS, Howell MD, Sun K et al. Treatment of atopic dermatitis with ruxolitinib cream (JAK1/JAK2 inhibitor) or triamcinolone cream. J Allergy Clin Immunol 2020 Feb; 145:572. PMID: 31629805 Free Article https://www.jacionline.org/article/S0091-6749(19)31326-0/fulltext
  3. Bankhead C Topical JAK Inhibitor Shows Promise in Vitiligo. Half of patients had 90% improvement after 2 years of treatment. MedPage Today April 30, 2021 https://www.medpagetoday.com/meetingcoverage/aad/92371 - Forand RL FDA approves Opzelura cream for vitiligo. Healio. Dermatology. July 19, 2022 https://www.healio.com/news/dermatology/20220719/fda-approves-opzelura-cream-for-vitiligo - Harris JE, et al Safety and efficacy of ruxolitinib cream for the treatment of vitiligo: 104-week data from a phase II study. American Academy of Dermatology (AAD) 2021; Poster 27535. https://www.medpagetoday.com/meetingcoverage/aad/92371 - Pandya AG, et al Addition of narrow-band ultraviolet B phototherapy to ruxolitinib cream in patients with vitiligo. American Academy of Dermatology (AAD) 2021; Poster 27636.
  4. Zeiser R, Polverelli N, Ram R et al Ruxolitinib for Glucocorticoid-Refractory Chronic Graft-versus-Host Disease. N Engl J Med 2021; 385:228-238. July 15. PMID: 34260836 https://www.nejm.org/doi/full/10.1056/NEJMoa2033122