Asthma Hetereogeneity, Phenotypes and Endotypes Choosing the Right Biologic for your Patient

Similar documents
Biologic Therapy in the Management of Asthma. Nabeel Farooqui, MD

Biologics in Asthma: Present and Future

Distinguishing Type-2 Asthma

Do We Need Biologics in Pediatric Asthma Management?

Biologics in asthma Are we turning the corner? Roland Buhl Pulmonary Department Mainz University Hospital

Severe Asthma(s): Can THEY be prevented or reversed?

Severe Asthma & Exacerbations: Dawn of a New Era?

Traiter l asthme sévère par le phénotype. Dr. Alain Michils CUB-Hôpital Erasme

Searching for Targets to Control Asthma

Treatment of Severe Asthma: Biologics to Bronchial Thermoplasty. Disclosures

SEVERE ASTHMA - EVIDENCE TABLES APPENDIX 1

Addressing Unmet Medical Needs in Severe Asthma: Where Do We Stand?

Clinical Implications of Asthma Phenotypes. Michael Schatz, MD, MS Department of Allergy

Jamie Lee Memorial Lecture ( ) Targets and Outcomes: Mepolizumab, Benralizumab, Reslizumab

Disclosures. Learning Objective. Biological therapies. Biologics with action against 11/30/2011. Biologic Asthma Therapies and Individualized Medicine

Cigna Drug and Biologic Coverage Policy

Biologic Agents in the treatment of Severe Asthma

Delivering in Respiratory ATS Analyst Briefing

Smooth Muscle & Asthma: Bronchial Thermoplasty - A Smooth Muscle Modifier

New Therapies for Asthma

EFFECTIVE ASTHMA MANAGEMENT IN PRIMARY CARE Severity Assessment, Guidelines, and New Therapeutic Options

ABCs of Immune Modifiers. Relevant Disclosures

Asma e BPCO: le strategie terapeutiche

Different kinds of asthma, different kinds of therapies

10/24/2016. Precision Management of Severe Asthma How, When and Where. The Goals of Today s Presentation

Phenotypes of asthma; implications for treatment. Medical Grand Rounds Feb 2018 Jim Martin MD DSc

Asthma Upate 2018: What s New Since the 2007 Asthma Guidelines of NAEPP?

Pediatric Asthma: Pharmacotherapy. Joseph Spahn, MD Children s Hospital Colorado & University of Colorado Medical School Aurora, Colorado

Biologicals in the management of bronchial asthma. Deepa Shrestha

Endobronchial Thermoplasty

Management of Severe Asthma Including Biologics and Bronchial Thermoplasty. Karen L. Gregory, DNP, APRN, CNS, RRT, AE-C, FAARC

THE PROMISE OF NEW AND NOVEL DRUGS. Pyng Lee Respiratory & Critical Care Medicine National University Hospital

Amanda Hess, MMS, PA-C President-Elect, AAPA-AAI Arizona Asthma and Allergy Institute Scottsdale, AZ

Endobronchial Thermoplasty

Using Patient Characteristics to Individualize and Improve Asthma Care

Bronchial Thermoplasty For Severe Persistent Asthma

Omalizumab (Xolair ) ( Genentech, Inc., Novartis Pharmaceuticals Corp.) September Indication

Robert Kruklitis, MD, PhD Chief, Pulmonary Medicine Lehigh Valley Health Network

The Pharmacist s Role in Managing Severe Asthma. This activity is supported by an educational grant from Genentech. Educational Objectives

Cynthia S. Kelly, M.D. Professor of Pediatrics Eastern Virginia Medical School Division Director Allergy Children s Hospital of The King s Daughters

Pharmacy Management Drug Policy

Learning the Asthma Guidelines by Case Studies

Asthma Therapy 2017 JOSHUA S. JACOBS, M.D.

Biologic Therapies for Treatment of Asthma Associated with Type 2 Inflammation: Effectiveness, Value, and Value-Based Price Benchmarks

Precision Asthma Therapy: Picking the Right Biologic for the Right Patient. The Asthma Umbrella. Asthma. Late onset. Early onset.

Meeting the Challenges of Asthma

Changing Epidemiology: Quick Facts 9/28/2018. During the year New Treatment Options for COPD: Phenotypes, Endotypes or Treatable Traits?

Exhaled Nitric Oxide: An Adjunctive Tool in the Diagnosis and Management of Asthma

Difficult Asthma Assessment: A systematic approach

Complements asthma therapy NOT a CURE for Severe. Non pharmacologic treatment of asthma. limits the ability of the airways to constrict.

What is Severe Persistent Asthma? What is Bronchial Thermoplasty Non pharmacologic treatment of asthma

HCT Medical Policy. Bronchial Thermoplasty. Policy # HCT113 Current Effective Date: 05/24/2016. Policy Statement. Overview

SEVERE ASTHMA NUCALA 100MG SUBCUTANEOUS INJECTION THE FIRST TARGETED ANTI IL-5 ADD-ON TREATMENT FOR ADULTS WITH SEVERE REFRACTORY EOSINOPHILIC ASTHMA

Current Asthma Therapy: Little Need to Phenotype. Phenotypes of Severe Asthma. Cellular Phenotypes 12/7/2012

Asthma Update I have no professional or personal financial conflicts of interest to disclose.

Asthma Update Jennifer W. McCallister, MD, FACP, FCCP

COPD: From Phenotypes to Endotypes. MeiLan K Han, M.D., M.S. Associate Professor of Medicine University of Michigan, Ann Arbor, MI

Bronchial Thermoplasty

5/1/18. Emerging Challenges in Primary Care: The Role of Type 2 Inflammation in Severe Asthma: Integrating Biologic Therapy to Optimize Outcomes

Uncontrolled Moderate-to-Severe-Asthma: Latest Data from the Floor of CHEST 2018

Asthma and Its Many Unmet Needs: Directions for Novel Therapeutic Approaches

Targeting Interleukin-5 in Patients With Severe Eosinophilic Asthma: A Clinical Review

Usefulness of Bronchial Thermoplasty for Patients with a Deteriorating Lung Function

Controversial Issues in the Management of Childhood Asthma: Insights from NIH Asthma Network Studies

Identifying Biologic Targets to Attenuate or Eliminate Asthma Exacerbations

TORCH: Salmeterol and Fluticasone Propionate and Survival in COPD

Update on Biologicals for ABPA and Asthma

The Acute & Maintenance Treatment of Asthma via Aerosolized Medications

Novel Biologics for Asthma: Steps on the Long Road to Therapies for Uncontrolled Asthma

Treatment Options for Complicated/Severe Asthma. Henry J. Kanarek, MD Kanarek Allergy Asthma Immunology

Asthma Phenotypes, Heterogeneity and Severity: The Basis of Asthma Management

Cinqair (reslizumab injection for intravenous use)

Emerging Challenges in Primary Care: The Role of Type 2 Inflammation in Severe Asthma: Integrating Biologic Therapy to Optimize Outcomes

Improving Outcomes in the Management & Treatment of Asthma. April 21, Spring Managed Care Forum

Emerging Challenges in Primary Care: 2018 The Role of Type 2 Inflammation in Severe Asthma: Integrating Biologic Therapy to Optimize Outcomes

Prof Neil Barnes. Respiratory and General Medicine London Chest Hospital and The Royal London Hospital

#1 cause of school absenteeism in children 13 million missed days annually

Global Initiative for Asthma (GINA) What s new in GINA 2016?

LINEE GUIDA DELL ASMA: UP TO DATE

Brooke L. Gildon, Pharm.D., BCPS, BCPPS, AE C

Personalized medicine in childhood asthma. Dr Mariëlle Pijnenburg, Erasmus MC Sophia, Rotterdam, NL

Asthma Treatment Update: 2018

Is reslizumab effective in improving quality of life and asthma control in adolescent and adult patients with poorly controlled eosinophilic asthma?

BRONCHIAL THERMOPLASTY

Bronchial Thermoplasty

PFT s / 2017 Pulmonary Update. Eric S. Papierniak, DO University of Florida NF/SG VHA

Corporate Medical Policy

7/7/2015. Somboon Chansakulporn, MD. History of variable respiratory symptoms. 1. Documented excessive variability in PFT ( 1 test)

Steps to better understand severe asthma in adults

Exhaled Nitric Oxide Today s Asthma Biomarker. Richard F. Lavi, MD FAAAAI FAAP

Asthma in Pregnancy. Michael Schatz, MD, MS Department of Allergy Kaiser Permanente Medical Center San Diego, CA. Introduction

Rising Incidence of Asthma

Policy Effective 4/1/2018

Impact of Asthma in the U.S. per Year. Asthma Epidemiology and Pathophysiology. Risk Factors for Asthma. Childhood Asthma Costs of Asthma

Asthma: Diagnosis and Treatment

Asthma Pathophysiology and Treatment. John R. Holcomb, M.D.

Are emerging PGD2 antagonists a promising therapy class for treating asthma?

New Drug Evaluation: mepolizumab for injection

Phenotyping Asthma: Environmental and Occupational Asthma

Transcription:

Asthma Hetereogeneity, Phenotypes and Endotypes Choosing the Right Biologic for your Patient Mario Castro MD, MPH Asthma & Airway Translational Research Unit Washington University School of Medicine St. Louis, Missouri, USA

DISCLOSURES u Speaker; Honorarium - Boehinger Ingelheim - Genentech - AstraZeneca - Teva - Boston Scientific Principal Investigator; Contracted Research - Boehinger Ingelheim - Vectura - Chiesi - ALA - Sanofi-Aventis - NIH

DISCLOSURES (cont.) u Consultant; Consulting fee - Nuvaira - Sanofi-Aventis - Aviragen - Teva - Genentech - Theravance - Neutronic - Vectura u Author; Royalties - Elsevier u Co-Investigator; Contracted Research - NIH - PCORI

LEARNING OBJECTIVES u Discuss the clinically relevant disease subtypes and molecular targets for new biologic medications in asthma u Identify the impact of biomarkers on understanding future impairment and risk in our asthma patients u Diagnose patients with symptoms of severe asthma to determine the level of disease control and uncover potential phenotypes that can guide ongoing therapy

Asthma is a Complex Heterogeneous Disease Asthma likely encompasses many different disease variants with different etiologies and pathophysiologies Many phenotypes exist and are determined by clinical characteristics, physiology, triggers, and inflammatory parameters Multiple environmental and genetic factors contribute to the disease Old School Kim et al. Nat Immunol. 2010;11:577-584. Lotvall et al. J Allergy Clin Immunol. 2011; 127:355

Categorizing Asthma by Endotype Phenotype: Observable properties of an organism that are produced by the interactions of the genotype and the environment Encompasses the heterogeneity of clinical presentations but do not provide insight into the underlying pathophysiology Endotype: A specific biologic pathway that explains the observable properties of a phenotype A subtype of a condition, which is defined by a distinct functional or pathophysiological mechanism Lotvall et al. J Allergy Clin Immunol. 2011; 127:355-60. Holgate et al. J Allergy Clin Immunol. 2011

Classification by Endotype May Identify Appropriately Targeted Treatment Approaches One of the major unmet needs in asthma lies with delivering mechanism-specific treatments that are highly effective in specific endotypes of asthma Understanding endotypes can identify those patients most likely to benefit from a particular type of therapy This strategy can be advantageous both in clinical study design and for the development of future targeted therapies Lotvall et al. J Allergy Clin Immunol. 2011; 127:355-60.

Phenotypes based on TH2 vs non-th2 TH2 Non-TH2 Severity TH2 Allergy/duration Allergic asthma EIA AERD Late-onset, eosinophilic Non-TH2 Very late-onset, (women) Obesityassociated Smoking-associated, neutrophilic Smooth-muscle mediated, paucigranulocytic Childhood Adult Adult Age at onset Wenzel SE. Nat Med 2012;18:716 25

Potential Biomarkers for Asthma Assessment and Management 1 Biomarker Sputum EOS Blood EOS IgE FeNO Periostin Characteristics Severe allergic and eosinophilic asthma Increased exacerbations and poor lung function Severe allergic and eosinophilic asthma Increased exacerbations and poor lung function Severe allergic asthma Indicator of oxidative and nitrative stress Severe allergic and eosinophilic asthma Potentially allergic and eosinophilic asthma 9 EOS = eosinophil; FeNO = exhaled nitric oxide fraction; Ig = immunoglobulin. 1. Chung KF. Eur Respir J. 2014;43:343-373.

Question 1 40 Year Old African American Male was diagnosed with asthma shortly after birth. He has history of allergic rhinitis. Hospitalized 15 times with one additional burst of steroids in the last year. During one hospitalization for asthma was in the ICU, but never intubated. Medications albuterol PRN and fluticasone/salmeterol 500/50 1 puff BID. ACQ score today was 2.0. FEV1 1.93 L 50% predicted; post bronchodilator FEV1 increased to 2.50L 64% predicted (29% reversibility). 0.408 K/cu mm absolute blood eosinophils and total serum IgE 66 IU/ml. The best predictor of a subsequent exacerbation of asthma in this patient is: A. Bronchodilator reversibility B. Blood eosinophils C. African American race D. ACQ score E. Atopic history

Severe Exacerbations are Associated with High EOS Levels 1 Medical record data to identify primary care patients with asthma aged 12 80 years with 2 years of continuous records, including 1 year before (baseline) and 1 year after 20,929 (16%) of 130 248 had blood eos >400/μL. Adjusted rate ratios (RRs) for severe exacerbations and acute respiratory events, and odds ratios (ORs) for asthma control, for patients with peripheral blood eosinophil count greater than 400 cells per μl (vs 400 cells per μl or less) during 1 outcome year 1 Price DB,et al Lancet Respiratory Medicine, Volume 3, Issue 11, 2015, 849 858

Role of Eosinophils in Severe Asthma Ghosh S et al. Front Pharmacol. 2013;4:8.

Potential phenotype-targeted therapies in severe asthma Characteristic Associations Specifically-targeted treatments Severe allergic asthma High eosinophil High serum IgE High FeNO Anti-IgE (adults and children) Anti-IL-4/IL-13 IL-4/R Eosinophilic asthma Non-eosinophilic, neutrophilic asthma Chronic airflow obstruction Recurrent exacerbations Corticosteroid insensitivity High serum IgE Recurrent exacerbations High FeNO Corticosteroid insensitivity Bacterial infections Airway wall remodelling as increased airway wall thickness Eosinophils in sputum Reduced response to ICS ± OCS High neutrophils in sputum Anti-IL-5 Anti-IL-4/-13 IL-4/R Anti-IL-8 CXCR2 antagonists Anti-LTB4 (adults and children) Macrolides (adults and children) Anti-IL-13 Bronchial thermoplasty Anti-IL-5 Anti-IgE (adults and children) p38 MAPK inhibitors Theophylline (adults and children) Macrolides (adults and children) International ERS/ATS Guidelines Eur Respir J 2014;43:343 73

Question 2 40 Year Old African American Male was diagnosed with asthma shortly after birth. He has history of allergic rhinitis. Hospitalized 15 times with one additional burst of steroids in the last year. During one hospitalization for asthma was in the ICU, but never intubated. Medications albuterol PRN and fluticasone/salmeterol 500/50 1 puff BID. ACQ score today was 2.0. FEV1 1.93 L 50% predicted; post bronchodilator FEV1 increased to 2.50L 64% predicted (29% reversibility). 0.408 K/cu mm absolute blood eosinophils and total serum IgE 66 IU/ml. The best description of this patient s asthma phenotype is: A. Severe eosinophilic asthma B. Severe neutrophilic asthma C. Chronic airflow obstruction asthma D. Severe allergic asthma

Question 3 u 22 Year old female (BMI 33) diagnosed with asthma at age 2 has severe uncontrolled persistent asthma despite high dose fluticasone (1,000 mcg/day), salmeterol, and tiotropium with history of allergic rhinitis and urticaria. She has had 4 courses of corticosteroids in the past year and one hospitalization for asthma resulting in BiPAP therapy. Baseline FEV1 2.70 L 95% of predicted, post-bronchodilator FEV1 increased to 3.02L (107% predicted, 12% reversibility), 0.240 K/cu mm absolute blood eosinophils, FeNO 55 ppb and total serum IgE 660. Which of the following currently available biologic therapy would be most appropriate for this patient? A. Omalizumab B. Mepolizumab C. Dupilumab D. Reslizumab E. Epinephrine pen

Omalizumab: anti-ige therapy for severe eosinophilic asthma? EXTRA study: exacerbations reduced in severe asthma patients treated with high dose ICS+LABA: omalizumab vs. placebo RR 0.75 [0.61-0.92] 1 u Exploratory analysis revealed greatest effect in high biomarker subsets (median FeNO, Blood EOS, Periostin) 2 1. Hanania N, et al. Ann Int Med 2011,154:573 82; 2. Hanania N, et al Am J Respir Crit Care Med 2012; 187:804 11. CI, confidence interval; EOS, eosinophils; FeNO, fraction of exhaled nitric oxide; ICS, inhaled corticosteroid; LABA, long-acting beta-agonist; ppb, parts per billion; RR, rate Rodrigo GJ, et al. Chest. 2011;139:28-35. ratio.

Several (interdependent) determinants of anti-il-5 clinical response in asthma Exposure to drug Individual IL-5 drive Burden of disease in the airway Blood eosinophil level OR Demonstrable airway eosinophilia Treating currently active tissue eosinophilia AND/OR Preventing the influx associated with a future exacerbation Disease severity Based on background medication level Level of baseline control Exacerbation history Other patient factors e.g. Associated comorbidites (e.g. nasal polyps/sinus disease), allergy etc 17

Mepolizumab: DREAM trial Clinically significant exacerbations, n 300 250 200 150 100 50 Primary endpoint Placebo (exac=2.40/year, n=159) Mepolizumab 75 mg (exac=1.24/year, n=154) Mepolizumab 250 mg (exac=1.46/year, n=152) Mepolizumab 750 mg (exac=1.15/year, n=156) 0 0 1 2 3 4 5 6 7 8 9 10 11 12 13 Time from start of treatment (months) exac, exacerbation rate Pavord ID, et al. Lancet 2012;380:651 9

Mepolizumab: DREAM trial Secondary endpoints Placebo Mepolizumab 75 mg Mepolizumab 250 mg Mepolizumab 750 mg 1.0 1.0 Change in blood eosinophil count 0.5 0.25 0.125 Change in sputum eosinophil count 0.5 0.25 0.125 0.063 0.063 0 All mepolizumab doses P<.001 vs placebo at 52 weeks 4 8 12 16 20 24 28 32 36 40 44 48 52 56 60 0.031 0 p=0.0082 for mepolizumab 750 mg vs placebo at 52 weeks 4 8 12 16 20 24 28 32 36 40 44 48 52 56 60 200 Weeks 0 Weeks Change in pre BD FEV1 150 100 50 0 Change in ACQ -0.5-1.0 0 4 8 12 16 20 24 28 32 36 40 44 48 52 56 60 0 4 8 12 16 20 24 28 32 36 40 44 48 52 56 60 Weeks Weeks Pavord ID, et al. Lancet 2012;380:651 9

Mepolizumab : MENSA study Primary endpoint - asthma exacerbations Ortega H, et al. N Engl J Med. 2014;371:1198 207. Mepolizumab 100 mg SC is licensed for the treatment of severe eosinophilic asthma.

Mepolizumab : MENSA study Changes in SGRQ 0 Placebo 75 mg IV 100 mg SC Change from baseline in SGRQ score 2 4 6 8 10 12 14 16 9 15.4 16 18 6.4 points difference * *p<0.001 7.0 points difference* Ortega H, et al. N Engl J Med. 2014;371:1198 207. IV, intravenous; SC, subcutaneous; SGRQ, St. George's Respiratory Questionnaire. Mepolizumab 100 mg SC is licensed for the treatment of severe eosinophilic asthma.

Mepolizumab: Oral Steroid Sparing Bel EH et al. N Engl J Med 2014;371:1189-1197

Mepolizumab summary u Mepolizumab significantly reduces the number of asthma exacerbations in patients with severe eosinophilic asthma compared with placebo u Treatment lowers blood and sputum eosinophil counts (750 mg IV) but SQ 100 mg Q4wks variable effects u There were small effects of mepolizumab on FEV 1 and AQLQ and ACQ scores, which generally did not differ significantly from those reported with placebo u Safety and tolerability profile for mepolizumab comparable to that for placebo Pavord ID, et al. Lancet 2012;380:651 9

Reslizumab* in asthma u 106 patients with inadequately controlled asthma with elevated eosinophils counts were randomly assigned to reslizumab IV 3 mg/kg or placebo at baseline, and at weeks 4, 8, and 12 u 8% of reslizumab vs 19% of placebo group had an asthma exacerbation (p=0.083) *Humanized anti-human IL-5 monoclonal antibody of the IgG4 isotype Castro M, et al. AJRCCM 2011;184:1125 32

The nasal polyp endotype 0.4 Placebo Reslizumab 0.2 Change from baseline in ACQ score 0 0.2 0.4 0.6 0.8 1 1.2 1.4 p=0.0119 p=0.7176 With nasal polyps Without nasal polyps n=22 n=16 n=31 n=37 Castro M, et al. AJRCCM 2011;184:1125 32

Reslizumab 3 mg/kg q 4 weeks over 52 weeks in exacerbation-prone, uncontrolled asthmatics with elevated blood eosinophils Pooled results (Studies 3082/3083) PBO n=476 Reslizumab 3 mg/kg n=477 RR (95% CI) % reduction CAE* 1.81 0.84 0.46 (0.37, 0.58) 54% CAE requiring systemic corticosteroid 1.54 0.66 0.42 (0.33, 0.55) 58% Change from baseline over 52 weeks DResli-PBO (95% CI) FEV 1, L 0.12 0.22 0.11 (0.07, 0.15) AQLQ 0.81 1.08 0.27 (0.16, 0.39) ACQ 0.77 1.02 0.250 ( 0.34, 0.16) ASUI 0.12 0.17 0.05 (0.03, 0.07) *CAE defined as a worsening requiring additional corticosteroid and/or other urgent treatment including ER/hospital Castro M, et al. Lancet Respir Med 2015;3:355 66

Influence of background therapy on asthma exacerbations with reslizumab u Reslizumab was efficacious in reducing CAE regardless of the treatments patients were receiving at baseline Rate-Ratio* (95% CI) n Reslizumab Placebo All OCS at baseline ICS plus LABA ICS no LABA 0.46 (0.37 0.58) 477 476 0.32 (0.18 0.55) 73 73 0.45 (0.35 0.58) 397 383 0.51 (0.29 0.89) 80 93 0.1 0 0.1 0.2 0.3 0.4 0.5 0.6 0.7 0.8 0.9 1.0 1.1 *Reslizumab relative to placebo Rate ratio Castro M, et al. Lancet Respir Med 2015;3:355 66

Reslizumab effect on lung function u Change from baseline to each visit in FEV1 by treatment group: pooled results for studies 3082/3083 ** p<0.01 Castro M, et al. Lancet Respir Med 2015;3:355 66

Predicting response to Reslizumab Percent CAE reduction Annual CAE rate 2.5 2 1.5 1 0.5 0-71% 2.16 1.73 1.72 0.63 0.67 0.7 FEV1 Responder 100 ml -0.5-61% ACQ6 Responder Placebo Reslizumab -60% FEV1 or ACQ6 Responder 2.5 2 1.5 1 0.5 0-25% 1.97 2.12 1.57 1.57 1.17 1.27 FEV1 Non-Responder -36% ACQ Non-Responder -26% FEV1 or ACQ Non-Responder *Castro et al ATS 2016 Late Breaking Abstract (Pooled study 3082/3083)

Reslizumab summary u Patients receiving reslizumab (3 mg/kg IV Q 4wks) showed significantly greater reductions in sputum eosinophils, asthma exacerbations, improvements in airway function, and greater asthma control than those receiving placebo u Reslizumab can be targeted to the patients most likely to benefit by applying fairly simple blood eosinophil, asthma control, lung function, and disease severity criteria u Reslizumab was generally well-tolerated

Question 4 u 42 Year old female (BMI 33), diagnosed asthma age 32, has severe uncontrolled persistent asthma despite high dose fluticasone (1,000 mcg/day), salmeterol, and tiotropium. She has had 4 courses of corticosteroids in the past year and one hospitalization for asthma resulting in BiPAP therapy. Baseline FEV1 of 1.60 L 65% of predicted, post-bronchodilator FEV1 increased to 2.02L. 0.440 K/cu mm absolute blood eosinophils and total serum IgE 660. Which of the following currently available biologic therapy would be most appropriate for this patient? A. Omalizumab B. Mepolizumab C. Dupilumab D. Reslizumab E. Epinephrine pen

Benralizumab (anti-il-5rα) u A targeted, anti-eosinophil therapy under investigation Benralizumab for asthma is a humanized, afucosylated monoclonal antibody (IgG1k) that binds with high affinity to IL-5Rα and efficiently depletes eosinophils through antibody-dependent cell-mediated cytotoxicity (ADCC) 1 Eosinophils are thought to play a critical role in the pathogenesis and severity of asthma 2 ~40 60% of people with severe asthma have eosinophilic inflammation 3 Increased eosinophil count is associated with an increased frequency of exacerbations 2 IL-5R is important in mediating the differentiation, proliferation, and activation of eosinophils by IL-5 4 1. Kolbeck R, et al. J Allergy Clin Immunol 2010;125:1344 53; 2. Green RH, et al. Lancet 2002;360:1715 21 3. Douwes J, et al. Thorax 2002;57:643 8; 4. Long AA. mabs 2009;1:237 46

Benralizumab Eosinophilic phenotype ELEN Index positive and/or Fe NO 50 ppb Non-eosinophilic phenotype ELEN Index negative and Fe NO <50 ppb ELEN Index: mathematical algorithm to predict sputum eosinophils from CBC data 1 Primary endpoint: AER Secondary endpoints: FEV 1, ACQ-6 ACQ-6; Asthma Control Questionnaire-6; AER, annual exacerbation rate (total observed exacerbations to week 52 divided by total duration of person-year follow-up); CBC, complete blood count with differential; Fe NO, fraction of exhaled nitric oxide; FEV 1, forced expiratory volume in 1 second; ICS, inhaled corticosteroids; ppb, parts per billion Castro M, et al. Lancet Resp Med 2014,2:879 90

Benralizumab: primary efficacy endpoint: AER (mitt) Benralizumab 20 mg significantly reduced AER relative to placebo in patients with baseline blood eosinophils 300 cells/µl Benralizumab 100 mg significantly reduced AER relative to placebo in eosinophilic patients and in patients with baseline blood eosinophils 300 and 400 cells/µl *Statistically significant (p<0.169) Data are expressed as mean (80% CI) AERR, annual exacerbation rate reduction; RR, rate reduction Castro M, et al. Lancet Resp Med 2014,2:879 90

Benralizumab: conclusions u u u In patients with uncontrolled eosinophilic asthma, benralizumab 20 mg and 100 mg may have an effect on exacerbations, lung function, and asthma control, compared with placebo Positive correlation between degree of benefit and baseline blood eosinophil counts Benralizumab 30 mg SC is effective in reducing exacerbations and improving lung function Benralizumab had an acceptable safety profile at all doses

Dupilumab, a fully human monoclonal antibody against the IL-4 receptor alpha subunit, inhibits IL-4 and IL-13 signaling Multinational, 24-week, randomized, double-blind, placebo-controlled, dose-ranging study in patients with persistent, uncontrolled asthma despite use of medium-to-high dose ICS/LABA To ensure a balanced distribution of blood eosinophil (Eos) counts in patients across treatment regimens, randomization was stratified by blood Eos count at screening: 300 cells/µl, 200 299 cells/µl, and < 200 cells/µl n = 150 Dupilumab 300 mg q2w with loading dose (600 mg) n = 150 Dupilumab 300 mg q4w with loading dose (600 mg) Screening period (14 21 days) Randomization (1:1:1:1:1) Dupilumab or placebo was added on to therapy with ICS/LABA n = 150 Dupilumab 200 mg q2w with loading dose (400 mg) n = 150 Dupilumab 200 mg q4w with loading dose (400 mg) n = 150 Placebo 24-week treatment period q2w, every 2 weeks; q4w, every 4 weeks. Wenzel S, Castro M, et al ERS 2015

Dupilumab: Severe Exacerbation Rate Eos 300 cells/µl Eos < 300 cells/µl Adjusted annualized severe exacerbation rate, estimate (95% CI) 1.4 1.2 1.0 0.8 0.6 0.4 0.2 0 95% CI 0.57, 1.90 Placebo (n = 68) 66% * 95% CI 0.16, 0.81 200 mg q4w (n = 59) 35% 95% CI 0.36, 1.29 300 mg q4w (n = 66) 71% * 95% CI 0.13, 0.68 200 mg q2w (n = 64) 81% ** 95% CI 0.08, 0.52 300 mg q2w (n = 64) Adjusted annualized severe exacerbation rate, estimate (95% CI) 1.4 1.2 1.0 0.8 0.6 0.4 0.2 0 95% CI 0.49, 1.23 Placebo (n = 90) 43% 95% CI 0.25, 0.79 200 mg q4w (n = 91) 37% 95% CI 0.29, 0.84 300 mg q4w (n = 91) 68% ** 95% CI 0.12, 0.52 200 mg q2w (n = 84) 60% * 95% CI 0.17, 0.58 300 mg q2w (n = 92) Adjusted annualized severe exacerbation rate, estimate (95% CI) 1.4 1.2 1.0 0.8 0.6 0.4 0.2 0 95% CI 0.62, 1.30 Placebo (n = 158) Overall population 54% ** 95% CI 0.26, 0.66 200 mg q4w (n = 150) 33% 95% CI 0.40, 0.91 300 mg q4w (n = 157) 70% *** 95% CI 0.16, 0.46 200 mg q2w (n = 148) 70% *** 95% CI 0.16, 0.45 300 mg q2w (n = 156) At Week 24, the q2w regimens showed a significant decrease in severe asthma exacerbation rates in patients with Eos 300 cells/µl, patients with Eos < 300 cells/µl, and the overall population The annualized exacerbation rate was adjusted for treatment duration in patients who discontinued prematurely. Arrows represent percent change relative to placebo. *P < 0.05, **P < 0.01, ***P < 0.001 vs placebo. CI, confidence interval.

Potential phenotype-targeted therapies in severe asthma Characteristic Associations Specifically-targeted treatments Severe allergic asthma High eosinophil High serum IgE High FeNO Anti-IgE (adults & children) Anti-IL4/IL-13 IL4 Receptor Eosinophilic asthma Non-eosinophilic, neutrophilic asthma Chronic airflow obstruction Recurrent exacerbations Corticosteroid insensitivity High serum IgE Recurrent exacerbations High FeNO Corticosteroid insensitivity Bacterial infections Airway wall remodelling as increased airway wall thickness Eosinophils in sputum Reduced response to ICS ±OCS High neutrophils in sputum 2 Anti-IL5 Anti-IL-4/-13 IL-4R Anti-IL-8 CXCR2 antagonists Anti-LTB4 (adults and children) Macrolides (adults and children) Anti-IL13 Bronchial thermoplasty Anti-IL5 Anti-IgE (adults and children) p38 MAPK inhibitors Theophylline (adults and children) Macrolides (adults and children) International ERS/ATS GUIDELINES Eur Respir J, 2014; 43(2):343-373

Aysola Chest. 2008;134:1183-1191

Bronchial Thermoplasty n The catheter is a flexible tube with an expandable wire array at the tip l The Radiofrequency Controller supplies energy that is converted to heat in the airway wall l Monopolar radiofrequency (RF) energy l Temperature controlled: 65 C l 10 seconds l Multiple safety algorithms to ensure controlled energy delivery

Reduction in Severe Exacerbations Maintained out to 5 years u The reduction in severe exacerbations requiring systemic corticosteroids at 1 year (vs. sham-treated patients) was maintained out to at least 5 years. % of Patients with Severe Exacerbations Severe Exacerbation Event Rates Compared with 1 year prior to BT treatment (baseline): 44% average decrease in percentage of patients having severe exacerbations 48% average decrease in severe exacerbation event rates Wechsler ME, et al. J Allergy Clin Immunol. 2013 Aug 30. doi:pii: S0091-6749(13)01268-2.

Predictors of Bronchial Thermoplasty response u40 severe asthma pts characterized pre BT at Wash Univ: Post-BD FEV 1 70%, range 44-121%, AQLQ score 3.4±1.2, ICS dose 2,185±621 mcg/d, 2.9±3.0 exacerbations requiring pred bursts prior yr. uincrease AQLQ/ACT 1 yr post BT predicted by: 30 (79%) responders, 8 (21%) non-reponders Shorter duration asthma (19±15 vs. 40±12 yrs, p=0.006) *increase in AQLQ 0.5 or ACT 3; Decrease in ICS, 240 mcg/d or OCS, 2.5 mg/d Sarikonda, Sheshadri et al ATS 2014

Predictors of Bronchial Thermoplasty response uics/ocs dose reduction* 1 yr post BT predicted by: Lower AQLQ score (2.9±1.1 vs. 3.9±1.1, p=0.026), Higher OCS dose (13.3±16.4 vs. 1.8±6.1 mg/d, p=0.01) More exacerbations requiring pred burst prior yr 4.8±2.7 vs. 2.3±2.8 (p=0.04) Higher residual volume/tlc on plethysmography (38.7±11.8 vs. 32.4±6.9 L, p=0.09) and resistance (Raw 4.0±1.7 vs. 1.9±1.1, p=0.03) *increase in AQLQ 0.5 or ACT 3; Decrease in ICS, 240 mcg/d or OCS, 2.5 mg/d Sarikonda, Sheshadri et al ATS 2014

3 He Images for our Severe Asthma Patient Pre-Bronchial Thermoplasty

3 He Images for our Severe Asthma Patient Post Bronchial Thermoplasty

Single-session bronchial thermoplasty for severe asthmatics guided by HXe MRI HXe/1H MRI baseline (3 weeks separation) HXe/1H MRI HXe/1H MRI clinical CT and PFT tests screeningenrollment 12 weeks recovery BT treatment session #1 3 wks 12 weeks recovery BT treatments sessions #2 & #3 A double-blind pilot study of 30 severe asthma pts with image-guided BT compared to traditional treatment: u u Specific Aim 1: To determine to what extent the single-session guided treatment is not inferior in benefit to the standard full three session treatment course (revealed by unblinding the analysis). Specific Aim 2: To assess HXe MRI as an imaging biomarker of asthma disease severity in the context of BT and evaluate our proposed image guided airway treatment prioritizing scheme.

Site of action of targeted therapies for severe asthma. Allergen Airway Lumen Dupilumab Lebrikizumab IL-4 IL-13 Omalizumab IgE APC T H 2 Dupilumab Lebrikizumab Mepolizumab Reslizumab Benralizumab IL-5 IL-4 IL-13 *Trivedi A et al Lancet Resp 2016 In press B cell Eosinophil Mast cell Smooth muscle hypertrophy Bronchial thermoplasty

Targeted therapies based on severe asthma phenotypes with associated biomarkers Phenotypes Aspirin-sensitive asthma/aerd Severe T2 Allergic Asthma Severe Eosinophilic asthma Chronic airflow obstruction Biomarkers Elevated FeNO Elevated ulte4 High serum eosinophils High serum IgE High FeNO Recurrent exacerbations High serum IgE High FeNO Airway remodeling Increased airway wall thickness Targeted Therapies Leukotriene modifier Anti-IgE Anti-IL 5/a Anti-IgE Anti-IL-13 IL -4a Anti-IL-5/a Anti IL-4a Bronchial thermoplasty Other biologics *Trivedi A et al Lancet Resp 2016 In press

Phenotype-guided approach in asthma u Many phenotypes exist in asthma though the biologic pathway (endotype) is unclear for most u Ongoing studies of large-scale, molecularly and genetically focused and extensively clinically characterized cohorts of asthma should enhance our ability to molecularly understand these phenotypes u Biologic therapy with anti-il 5 for the eosinophilic uncontrolled asthma is a well established endotype but likely represents less 40% of uncontrolled asthma

Phenotype-guided approach in asthma u Targeted phenotype therapy can lead to personalized medical therapy for asthma u Many questions remain Are there better biomarkers than the blood EOS? Is anti-il-4 and anti-il-13 therapy as effective as anti-il-5? Will other biologic targets work? Anti-IL-17, anti-il-33, TSLP, and more Is chronic airflow obstruction and airway remodeling a phenotype or an end-result from many different pathways?