ONCE-DAILY TIOTROPIUM RESPIMAT ADD-ON TO ICS ± LABA IMPROVES CONTROL ACROSS ASTHMA SEVERITIES

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SPIRIVA Respimat is approved for use in asthma in the EU, Japan, the USA and many other countries. The label varies by country. Please refer to the local product information ONCE-DAILY TIOTROPIUM RESPIMAT ADD-ON TO ICS ± LABA IMPROVES CONTROL ACROSS ASTHMA SEVERITIES Sumit SINGH, 1 William E. BERGER, 2 Kevin MURPHY, 3 Petra MORONI-ZENTGRAF, 4 Michael ENGEL, 4 Hendrik SCHMIDT, 5 Huib KERSTJENS 6 1 Allergy & Asthma Associates of Southern California, Mission Viejo, CA, USA; 2 Southern California Research Center, Mission Viejo, CA, USA; 3 Boys Town National Research Hospital, Boys Town, NE, USA; 4 Boehringer Ingelheim, Ingelheim am Rhein, Germany; 5 Boehringer Ingelheim, Biberach an der Riss, Germany; 6 University of Groningen, University Medical Center Groningen, Groningen, The Netherlands Disclosures: Study funded by Boehringer Ingelheim; medical writing assistance provided by Complete HealthVizion and supported by Boehringer Ingelheim Pharmaceuticals, Inc

Introduction Background Tiotropium Respimat added on to ICS ± LABA has been investigated across asthma severities Tiotropium Respimat add-on therapy improves lung function in patients with symptomatic asthma despite maintenance treatment 1 4 Tiotropium Respimat add-on to ICS ± LABA has a safety profile comparable with that of placebo Respimat (combined treated sets, n=3761) 1 4 Aim To investigate ACQ-7 responses from five Phase III, randomized, double-blind, placebo-controlled, parallel-group trials in patients with symptomatic asthma 1 4 ACQ-7, seven-question Asthma Control Questionnaire; ICS, inhaled corticosteroids; LABA, long-acting β 2 -agonist 1. Kerstjens et al. N Engl J Med 2012; 2. Kerstjens et al. Lancet Respir Med 2015; 3. Paggiaro et al. J Allergy Clin Immunol Pract 2016; 4. Ohta et al. PLoS One 2015

Study designs and endpoints PrimoTinA-asthma a (n=912) MezzoTinA-asthma a (n=2100) GraziaTinA-asthma (n=464) Study NCT00772538 NCT00776984 NCT01172808 NCT01172821 NCT01316380 Duration 48 weeks 24 weeks 12 weeks Background therapy b High-dose ICS + LABA Medium-dose ICS Low-dose ICS Treatment arms Randomization to tiotropium 5 µg (two puffs of 2.5 µg) or placebo (two puffs), both once daily via Respimat Randomization to tiotropium 5 µg c once daily (two puffs of 2.5 µg), 2.5 µg c once daily (two puffs of 1.25 µg), salmeterol HFA-MDI 50 µg d twice daily, or placebo e Randomization to tiotropium 5 µg (two puffs of 2.5 µg), tiotropium 2.5 µg (two puffs of 1.25 µg), or placebo (two puffs), all once daily via Respimat Key inclusion criteria Key exclusion criteria Aged 18 75 years; 5-year (PrimoTinA-asthma ) or 3-month (MezzoTinA-asthma and GraziaTinA-asthma ) documented history of asthma; confirmed diagnosis before the age of 40 years; lifelong non-smoker or ex-smoker (<10 pack-years) with no smoking in the year before enrollment; symptomatic (ACQ-7 mean score of 1.5) No COPD or significant lung disease other than asthma Primary endpoints Time to first severe exacerbation (pooled data) and peak FEV 1(0 3h) and trough FEV 1 responses ACQ-7 responder rate and peak FEV 1(0 3h) and trough FEV 1 responses Peak FEV 1(0 3h) response Secondary endpoint ACQ-7 change from baseline - ACQ-7 responder rate a Pooled data; b Tiotropium Respimat add-on to background therapy; c Plus placebo HFA-MDI twice daily; d Plus placebo Respimat once daily; e Placebo Respimat once daily plus placebo HFA-MDI twice daily COPD, chronic obstructive pulmonary disease; FEV 1, forced expiratory volume in 1 second; HFA-MDI, hydrofluoroalkane metered-dose inhaler; peak FEV 1(0 3h), peak forced expiratory volume in 1 second within 3 hours post-dose

ACQ-7 Developed and validated to measure the adequacy of asthma control Patients are asked to recall experiences of the previous week and respond to six questions: Seven-point Likert scale ranging from 0 to 6 (0 = no impairment; 6 = maximum impairment) Q1: night-time waking Q4: shortness of breath Q2: symptoms on waking Q5: wheeze Q3: activity limitation Q6: rescue use of short-acting β 2 -agonists The clinician scores the seventh question: FEV 1 % predicted pre-bronchodilator ACQ-7 score is the mean of seven items Score below 1.0: asthma is adequately controlled Score above 1.0: asthma is not well controlled All of the studies included in the current analysis had an entrance criterion of an ACQ-7 score of 1.5 = symptomatic asthma The minimal clinically important difference is a change of 0.5 (responder) Juniper et al. Respir Med 2005

Baseline demographics and disease characteristics PrimoTinA-asthma a (n=912) MezzoTinA-asthma a (n=2100) GraziaTinA-asthma (n=464) Female, n (%) 551 (60.4) 1239 (59.0) 281 (60.6) Age, years 53.0 ± 12.4 43.1 ± 12.9 42.9 ± 13.0 Body mass index, kg/m 2 28.2 ± 6.0 26.8 ± 6.2 26.4 ± 5.2 Smoking status, n (%) Never smoked 692 (75.9) 1756 (83.6) 382 (82.3) Ex-smoker 220 (24.1) 344 (16.4) 82 (17.7) Smoking history, pack-years Duration of asthma, years Age at asthma onset, years 5.1 ± 2.7 4.2 ± 2.8 4.7 ± 3.0 30.3 ± 13.9 21.8 ± 14.3 16.2 ± 11.9 22.7 ± 12.9 21.4 ± 12.7 26.7 ± 10.8 FEV 1 % predicted 56.0 ± 13.1 75.1 ± 11.5 77.7 ± 11.9 ACQ-7 score 2.63 ± 0.69 2.18 ± 0.49 2.10 ± 0.42 Treated set. All values are mean ± standard deviation except for sex and smoking status a Pooled data

PrimoTinA-asthma : ACQ-7 responder rate for tiotropium Respimat versus placebo Respimat Response ( 0.5 reduction in ACQ-7) No change Worsening ( 0.5 increase in ACQ-7) Net response rate (response worsening) Patients (%) 60 50 40 30 20 Week 24; tior 5 µg vs pbor: OR=1.32 95% CI: 1.01, 1.73 P=0.043 Responder rate difference between tiotropium and placebo: 7.0% Patients (%) 60 50 40 30 20 Week 48; tior 5 µg vs pbor: OR=1.68 95% CI: 1.28, 2.21 P<0.001 Responder rate difference between tiotropium and placebo: 12.9% 10 10 0 Tiotropium Respimat 5 µg once daily (n=453) Placebo Respimat once daily (n=454) 0 Tiotropium Respimat 5 µg once daily (n=453) Placebo Respimat once daily (n=454) Full analysis set. Pooled data. Add-on to high-dose ICS + LABA CI, confidence interval; OR, odds ratio, active versus placebo Respimat ; pbor, placebo Respimat ; tior, tiotropium Respimat

MezzoTinA-asthma : ACQ-7 responder rate for tiotropium Respimat versus placebo at Week 24 Response ( 0.5 reduction in ACQ-7) No change Worsening ( 0.5 increase in ACQ-7) Net response rate (response worsening) Patients (%) 70 60 50 40 30 TioR 5 µg vs placebo: OR=1.32 95% CI: 1.02, 1.71 P=0.035 TioR 2.5 µg vs placebo: OR=1.33 95% CI: 1.03, 1.72 P=0.031 Salmeterol vs placebo: OR=1.46 95% CI: 1.13, 1.89 P=0.004 Responder rate difference between tiotropium and placebo: 5 µg = 6.6%; 2.5 µg = 6.8% 20 10 0 Tiotropium Respimat 5 µg once daily a (n=513) Tiotropium Respimat 2.5 µg once daily a (n=515) Salmeterol HFA-MDI 50 µg twice daily b (n=535) Placebo c (n=518) Full analysis set. Pooled data. Add-on to medium-dose ICS a Plus placebo HFA-MDI twice daily; b Plus placebo Respimat once daily; c Placebo Respimat once daily plus placebo HFA-MDI twice daily

GraziaTinA-asthma : ACQ-7 responder rate for tiotropium Respimat versus placebo Respimat at Week 12 Response ( 0.5 reduction in ACQ-7) No change Worsening ( 0.5 increase in ACQ-7) Net response rate (response worsening) Patients (%) 70 60 50 40 30 TioR 5 µg vs pbor: OR=0.97 95% CI: 0.60, 1.57 P=1.000 TioR 2.5 µg vs pbor: OR=1.02 95% CI: 0.63, 1.64 P=1.000 Responder rate difference between tiotropium and placebo: 5 µg = 0.6%; 2.5 µg = 0.4% 20 10 0 Tiotropium Respimat 5 µg once daily (n=155) Tiotropium Respimat 2.5 µg once daily (n=154) Placebo Respimat once daily (n=155) Full analysis set. Add-on to low-dose ICS

Discussion and conclusions Discussion A limitation of analyzing mean differences in ACQ-7 score between treatment groups in randomized controlled trials is that a strong placebo effect makes achieving the established minimal clinically important mean difference of 0.5 unlikely 1 Therefore, the most appropriate way of analyzing ACQ data for which a minimal clinically important difference is known, is by responder rates Did assay insensitivity contribute to the findings? Patients with a high unmet need already receive the types of therapies under study in clinical trials Therefore, clinical trials tend to include patients whose need is perhaps not as high as in the real world It is possible that, in the clinic, the likelihood and size of responses might be higher in individuals with poorer control Conclusions Once-daily tiotropium Respimat add-on to at least ICS maintenance therapy is associated with improved asthma control, as measured by ACQ-7, across asthma severities Real-world data 2 complement the clinical trial data, collectively demonstrating that tiotropium is an efficacious add-on controller therapy in the primary care management of asthma These findings build on existing data demonstrating that tiotropium Respimat add-on therapy improves lung function and decreases the risk of severe asthma exacerbations 3,4 1. Bateman et al. J Allergy Clin Immunol 2015; 2. Price et al. J Asthma Allergy 2015; 3. Kerstjens et al. N Engl J Med 2012; 4. Kerstjens et al. Lancet Respir Med 2015