What are the Unmet Needs in the Management of IBD?



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23/6/214 What are the Unmet Needs in the Management of IBD? Shane Devlin, MD, FRCPC Inflammatory Bowel Disease Group The University of Calgary Some Real Cases: #1 32 yo male with pan UC. Grumbling phenotype with 8 BM per day with blood 75% of the time, modestly elevated CRP Poor quality of life No clinical or endoscopic response to dose escalated infliximab, weekly adalimumab and now failing golimumab Some Real Cases: #2 42 yo female with ileal and pan colonic CD Prior ileo-cecal resection in 29 Induction and maintenance infliximab in 21 Developed delayed type hypersensitivity reaction to infliximab in 212 Switched to adalimumab with incomplete response, but recently developed severe psoriaform lesions that are not responding to topical or UV therapy 1

23/6/214 Some Real Cases: #3 78 yo male patient Multiple comorbidities Newly diagnosed steroid dependent pan ulcerative colitis, non responsive to 5-ASA 22 29 Sonic 29 26 24 27 28 21 29 22 29 Sonic 29 26 Episodic Combination Therapy 24 27 28 21 29 2

23/6/214 22 29 Sonic 29 26 Maintenance Combination Therapy 24 27 28 21 29 22 29 Sonic 29 26 Monotherapy? (esp. Humira) 24 27 28 21 29 22 29 Sonic 29 26 HSTCL Monotherapy? 24 27 28 21 29 3

23/6/214 22 29 Sonic 29 26 Earlier Use 24 27 28 21 29 22 29 Sonic 29 26 Combo Therapy Mucosal Healing Anti TNF for UC 24 27 28 21 29 22 29 Sonic 29 26 24 27 Combo Therapy Mucosal Healing Infliximab for UC 28 214 and Beyond TDM Golimumab and 21 Adalimumab for UC 29 4

23/6/214 y Maximize the Use of Anti TNF Therapy Yet.We have unmet needs IBD is a serious, systemic disease Primary non-response Inadequate response Secondary loss of response due to a variety of mechanisms Intolerance due to adverse events Ongoing steroid use The Requirement for Colectomy in IBD remains Higher than we d like Colectomy rates in meta analysis of 3 population based studies Colectomy rate 5 4 3 2 1 U C 4.9% 16.3% 11.6% 33.3% 15.6% 46.6% 1 year 5 year 1 year Frolkis et al. Gastroenterology 213;Online:doi 1.153/j.gastro.213.7.41 5

23/6/214 UC Negatively Impacts Patient Quality of Life Patients & physicians differ in their perception of disease severity 15 Patients Physicians 11 62% say their disease made it difficult to lead a normal life Estimated # disease flares/y 1 5 5 2 8 4 5 Only 42% believed that remission means living without symptoms Mild Moderate Severe Rubin et al. Inflamm Bowel Dis 29; 15:581 8 Colectomy and IPAA Is Not Optimal erative problems are frequent Functional outcomes after colectomy 1 Pouchitis: 46% 1 Female infertility: 48% 2 o (vs. 15% in medically-treated UC) Other complications 1 o Sexual dysfunction, pouch leakage, abscess formation, fistula formation, small bowel ileus, anastomotic stenosis, and fecal incontinence 6 5 4 3 2 1 51% 25% 19% 14% 35% >5 BM/day >2 BM/night Peri anal soreness Dietary restrictions Medication 1. Ferrante et al. Inflamm Bowel Dis 28; 14:2 8; 2. Waljee et al. Gut 26; 55:1575 8 y Disease with Serious Complications Probability of developing penetrating or stricturing complication in CD patients (N=2,2) Cosnes et al. Inflamm Bowel Dis 22;8:244 5 6

23/6/214 Mortality in UC Mortality rates in meta-analysis of 1 population-based studies Greater risk of dying during the first years of follow-up, and in patients with extensive colitis vs. general population o 17% of all deaths were UC-related mortality o Higher rates of mortality from GI diseases, nonalcoholic liver diseases, pulmonary embolisms, and respiratory diseases Jess et al. Am J Gastro 27;12:69 17 CD Associated with Increased Mortality Risk Standardized mortality rates (SMR) in population based cohort studies Overall 1.39 (95%CI 1.18, 1.64) Each year, 114 deaths in Canada are attributed to CD and UC Bewtra et al. Inflamm Bowel Dis 213; 19:599 613 Primary and Inadequate Response 7

23/6/214 We are not successful in inducing remission with a significant proportion of patients Certolizumab Certolizuma 1 pegol 1 pegol 2 Adalimumab 3 Infliximab 4 8 6 4 2 7 27 * 11 * 19 NS * 36 24 12 n 57 6 328 331 74 75 76 25 27 28 4 * NS 48 25 Tx Pbo CzP Pbo CzP Pbo Pbo INF INF 4mg 4 mg 8/4 mg 16/8 mg 5 mg/kg 1 mg/kg Delta 2 8 12 24 44 21 *P<.5 NS=not significant. 1. Schreiber S, et al. Gastroenterology 25;129:87 18. 2. Sandborn WJ, et al. N Engl J Med 27;357:228 38. 3. Hanauer SB, et al. Gastroenterology 26;13:323 33. 4. Targan SR, et al. N Engl J Med ;337:129 35. Overall induction of remission ~3 5% 6 Month Data Certolizumab pegol PRECISE 2 1 1 8 6 4 2 64.1 Open-Label Induction Week 6 Pbo 28.6 CzP 47.9 Week 26 Remission 3.7 18.3 Net Remission Week 26 8 6 4 2 1 Infliximab ACCENT I 2 58.5 Open-Label Induction Week 2 Pbo 21. 39. Week 3 Remission 22.8 12.3 Net Remission Week 3 Certolizumab pegol PRECISE 1 4 1 8 6 4 2 Pbo CzP 29.5 18.3 Net Remission Week 26 Adalimumab CHARM 3 1. Pbo 8. 58. 6. 4. 4. 23.2 17. 2. 9.9. Open-Label Week 26 Net Induction Remission Remission Week 4 Week 26 CD, Crohn s disease. 1. Schreiber S, et al. N Engl J Med 27;357:239 5. 2. Hanauer SB, et al. Lancet 22;359:1541 9. 3. Colombel JF, et al. Gastroenterology 27;132:52 65. 4. Sandborn WJ, et al. N Engl J Med 27;357:228 38. Overall maintenance of remission in CD ~25 3% 1 8 6 4 2 Sustained remission at 12 months in UC Infliximab: ACT1 and 2 1* ACT1 p<.1 p=.2 ACT2 p<.1 p=.1 p=.2 p<.1 26 23 21 2 23 15 8 7 2 Remission at weeks 8 and 3 Remission at weeks 8, 3 and 54 Remission at weeks 8 and 3 1 8 6 4 2 Adalimumab: ULTRA1 2,3 9.2 1 18.5 29.5 Remission at week 8 Remission at week 52 Placebo Infliximab 5 mg Infliximab 1 mg Adalimumab 8/4 Adalimumab 16/8 Overall maintenance of remission in UC ~15 25% All randomised *Clinical remission was defined as a total Mayo score of 2 points or lower, with no individual subscore exceeding 1 point. Non-responder imputation (NRI) analyses, Week 8; mnri analyses, Week 52. a mnri (modified NRI): did not count patients who dose escalated (and were in remission) as failures (post-hoc analyses). Clinical remission: Mayo score 2 with no individual subscore >1. 1. Rutgeerts P, et al. N Engl J Med 25;353:2462 76. 2. Reinisch W, et al. J Crohns Colitis 211;5:S1; 3. Reinisch W, et al. Gut 211;6:78 7. 8

23/6/214 Golimumab Week 54 Primary and major secondary endpoints among randomised responders Percent of subjects 1 8 6 4 2 Secondary: Corticosteroid-free remission rates through Week 3 and 54 18.4 p=.299 27.8 p=.464 22.9 Secondary: Durable clinical remission at both Week 3 and 54 in patients in remission Week 24.1 p=.365 36.5 p=.73 4.4 Placebo N=87 Golimumab 5 mg q4w N=79 Golimumab 1 mg q4w N=83 Placebo N=54 Golimumab 5 mg q4w N=52 Golimumab 1 mg q4w N=57 Sandborn WJ, et al. Gastroenterology 213 Epub ahead of print. DOI: 1.153/j.gastro.213.5.48 Vedolizumab in UC Primary and Secondary Outcomes Through 52 Weeks, ITT Population *** *** *** *** *** *** *** % * ** ** n: 72 7 73 26.1 29.1 32.8 28.5 32. 36.3 11.8 15.3 17.6 31.4 *P<.5. **P<.1. ***P<.1 Feagan, B.G. et al Gastroenterology 212; Volume 142, Issue 5, Suppl 1, Pg S-16-S-161 Vedolizumab in CD Primary and Secondary Outcomes at 52 Weeks Primary Outcome Secondary Outcomes VDZ/PBO VDZ/VDZ Q8W VDZ/VDZ Q4W Patients, % Mean % vs VDZ/PBO 17.4 14.7 13.4 15.3 15.9 12.9 7.2 2. P<.1 vs placebo; P<.5 vs placebo Sandborn WJ. et al. American J Gastro.17: 212: Abstract 155. 9

23/6/214 Secondary Loss of Response Patients Attenuate Over Time ACCENT I 1 CDAI 7 54 weeks CHARM 2 CDAI 7 54 weeks PRECiSE 2&3 3 CDAI 1 8 weeks 52% 38% 54% 43% 61% 54% Anti-TNF Placebo 6 12 18 Months Anti-TNF Placebo 6 12 18 Months Anti-TNF Placebo 6 12 18 Months 1. Hanauer SB, et al. Lancet 22;359:1541 9. 2. Colombel JF, et al. Gastroenterology 27;132:52 65. 3. Lichtenstein GR, et al. Clin Gastroenterol Hepatol 21;8:6 9. Patients with Prior Anti TNF Use CHARM: Remission* rates with adalimumab at week 56, by prior anti TNF use (N=778) Patients in remission* (%) 6 5 4 3 2 1 Adalimumab 4 mg weekly 34% 31% 1 48% 42% 14 Prior anti TNF (N=237) No prior anti TNF (N=262) *Remission defined as CDAI <15 Colombel et al. Gastroenterology 27; 132:52 65 1

23/6/214 Outcomes of maintenance therapy with 3rd anti TNF Retrospective, single-center cohort study (N=664) of CD patients on maintenance anti-tnf therapy examining long-term outcomes by number of prior anti-tnfs (1, n=444; 2, n=178; 3, n=42) 1 SIBDQ 1 HBI Average score 5.9 47.9 4.3 Average score 2.9 3.9 5.2 1 2 3 Number of anti-tnfs received 1 2 3 Number of anti-tnfs received Two thirds of patients on long-term anti-tnf maintenance therapy remained on 1st agent Patients on their 1st or 2nd anti-tnf had similar long-term outcomes. Those on their third anti-tnf agent had significantly worse disease control and higher healthcare utilisation HBI, Harvey-Bradshaw Index; SIBDQ, Short Inflammatory Bowel Disease Questionnaire. Perera et al. Gastroenterology 212; 142(Suppl):S-357. DDW 212; Abstract Sa191. Sometimes we need to stop therapy y Uncommon but Remains a Relevant Concern Adverse events of interest in patients treated with adalimumab in 6 global clinical trials (N=316) Adverse Event Events/1 pt y (N=341.9 p y) Any SAE 34.4 Serious infection 6.6 Malignant neoplasms 1.3 Opportunistic infections 2. Congestive heart failure <.1 Demyelinating disorder.2 Lupus like syndrome.2 Any fatal adverse event.1 (4 patients) Most common infectious SAEs were: abscess 2.5%, GI infection (excluding abscess) 1.%, and pulmonary infection.9% y Colombel et al. Inflamm Bowel Dis 29;15:138 19. 11

23/6/214 Infection and TNF Antagonists TREAT registry n > 6,, f/u > 5yrs Factors independently associated with serious infections (Descending order of risk) : Disease activity mod severe (HR = 2.24, 95% CI = 1.57, 3.19; P <.1), Narcotic analgesic treatment (HR = 1.98, 95% CI = 1.44, 2.73; P <.1) Prednisone therapy (HR = 1.57, 95% CI = 1.17, 2.1; P =.2) Infliximab treatment (HR = 1.43, 95% CI = 1.11, 1.84; P =.6). Lichtenstein GR. Am J Gastroenterol. 212 Sep;17(9):149 22. Our Best Treatment With Earlier Use and Combination Therapy All randomised patients (N=58)* p=.28 p<.1 p=.35 41/17 59/169 78/169 Fewer than half are in remission and off of steroids In most anti TNF trials, the rate of SFR at one year is around 25 *Patients 3% who did not enter the Study Extension were treated as non-responders Colombel JF, et al. N Eng J Med 21; 362:1383-95. In Summary IBD is a serious systemic condition with significant potential complications Anti TNF therapy has, and will continue to markedly enhance our ability to treat patients with a view to affecting a longer term change in disease course However, more than 1 years of wide-spread use has taught us the limitations and heightened our awareness of a need for alternative therapies Loss of response, continued steroid use, systemic effects remain relevant concerns There is considerable room to improve upon as we continue to strive for the safest and most efficacious treatments for our patients with IBD. 12