9/16/2014. Anti-Immunoglobulin E (IgE) Omalizumab (Xolair ) Dosing Guidance

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Disclosure Statement of Financial Interest New Therapies for Asthma Including Omalizumab and Anti-Cytokine Therapies Marsha Dangler, PharmD, BCACP Clinical Pharmacy Specialist James H. Quillen VA Medical Center I DO NOT have a financial interest/arrangement or affiliation with one or more organizations that could be perceived as a real or apparent conflict of interest in the context of the subject of this presentation. I DO anticipate discussing the unapproved or investigative use of certain drugs during this presentation. The opinions expressed herein are those of the author and DO NOT reflect those of the U.S. Government or any of its agencies. September 19, 2014 Objectives Asthma Disease Burden Identify novel therapeutic targets in the treatment of asthma Demonstrate an understanding of anti-immunoglobulin E (IgE) therapy (omalizumab) and when to refer patients for treatment Understand the mechanism of action and safety profile of emerging anti-cytokine therapies in the treatment of asthma Estimated 300 million people in the world currently have asthma Small percentage of asthmatics with severe subtypes 5-10% inadequately controlled with poor quality of life High risk of serious morbidity and mortality Evaluate the current literature to determine efficacy and benefit of anti-cytokine therapies Allergy, vol. 65,no.5,pp.469-478, 2004 NEJM, vol. 360, no. 10, pp. 1002 1014, 2009 Asthma Phenotypes A Novel Approach Allergic Asthma Associated with a past or family history of allergic disease Non-allergic Asthma Not associated with allergy Late-onset Asthma Non-allergic, onset in adulthood, particularly women Current standards of therapy for asthma Inhaled corticosteroids and beta agonists Role of specific cytokines in asthma pathogenesis Novel therapeutic targets http://www.ginasthma.org/local/uploads/files/gina_report_2014_aug12.pdf Accessed September 1, 2014 Clinical phenotypes of asthma. Curr Opin Pulm Med 2004; 10:44-50 Biomed Res Int. 2013;2013:104315 1

Annals of Allergy, Asthma & Immunology Volume 112, Issue 2, Pages 108 115, February 2014 Nature Reviews Drug Discovery 11, 958-972 (December 2012) Omalizumab (Xolair ) Anti-Immunoglobulin E (IgE) Recombinant humanized monoclonal antibody Prevents binding of IgE to its high affinity receptor on mast cells and basophils Indicated for adults and adolescents ( 12 years of age) Moderate to severe persistent allergic asthma Inadequate control with inhaled corticosteroids and longacting beta agonist Adjunctive therapy in step 5 or 6 per guidelines Xolair [package insert]. South San Francisco, CA. Genentech USA, Inc; Revised March 2014 Dosing Guidance Every 4 Week Dosing Table Every 2 Week Dosing Table http://www.xolair.com/hcp/determining-the-dose.html 2

Administration Warnings/Precautions Store under refrigeration at 2-8 Cº 150mg/1.2mL following reconstitution with 1.4 ml sterile water for injection 150-375 mg SC every 2-4 weeks Subcutaneous injection Maximum 150mg per injection Anaphylaxis (0.2 %) Monitor patients for 2 HOURS following first 3 injection Monitor for 30 minutes following injection thereafter Risk of Anaphylaxis continues throughout treatment Emergency equipment/epinephrine pen available Pain and bruising (5-20%) Malignant neoplasms (0.2%) http://www.xolair.com/hcp/how-to-prepare-and-administer-xolair.html Xolair [package insert]. South San Francisco, CA. Genentech USA, Inc; Revised March 2014 Interlukin-4 (IL-4) Inhibitors Pitrakinra (Aerovant) Pascolizumab Altrakincept AMG-317 Dupilumab Decreases IgE production, excess mucus secretion, airway hyperresponsiveness, and inflammation Not statistically significant for changes in asthma control Pitrakinra may prevent a decrease in FEV1 after allergen challenge Symptomatic patients with atopic disease Am J Respir Crit Care Med. 1999 Dec;160(6):1816-23 Am J Respir Crit Care Med Vol 181. pp 788 796, 2010 Clin Exp Immunol. 2002 Oct;130(1):93-100 N Engl J Med 2013; 368:2455-2466 Interlukin-13 (IL-13) Inhibitors Lebrikizumab Tralokinumab Anrukinzumab Reduction in lung inflammation Decreased airway responsiveness Diminished mucus production /Safety Phase I studies - IV administration well-tolerated, no safety concerns Unknown N Engl J Med. 2011. 365 (12): 1088 1098 3

Interlukin-5 (IL-5) Inhibitors Mepolizumab (Bosatria ) Reslizumab (Cinquil ) Benralizumab Decreases production, activation, and proliferation of eosinophils Reduces exacerbation rates and eosinophil counts Severe eosinophilic asthma Symptomatic patients on conventional therapy and chronic oral/inhaled corticosteroids Expert Rev Clin Immunol. 2011 July ; 7(4): 411 417 Lancet 380 (9842): 651 659 Biologics: Targets and Therapy 2013:7 7 11 J Allergy Clin Immunol. 2012 September; 130(3):563-571 Interlukin-9 (IL-9) Inhibitor MEDI-528 Decreases mast cell infiltration Reduces up regulation of IL-13 and IL-5, eosinophil infiltration Decrease airway responsiveness Reduces mucus production Small phase 2 study showed no effect on fractional exhaled nitric oxide (FeNO) Unknown Complications and Concerns Additional Targets Time to symptoms alleviations delayed with anti-cytokine therapy Inhibiting a cellular and molecular mechanism Anti-cytokine therapy potentially harmful in patients with autoimmune disorders Administer with extreme caution Overall safe and well tolerated Mild injection site reactions, nasopharyngitis, nausea, and headache Hypersensitivity such as edema, rash, urticaria are rare Anti-IL-17 Anti-IL-23 Anti-IL-25 Anti-IL-33 Anti-TSLP Biomed Res Int. 2013;2013:104315 4

Conclusion One FDA approved agent to date for asthma Omalizumab (Xolair) Anti-cytokine therapy is generally well tolerated and safe IL-4 atopic asthma IL-13 unknown place in therapy IL-5 eosinophilic asthma IL-9 unknown place in therapy Jury is out on efficacy and clinical implications of most anticytokine agents Questions? 5