Immuno-Oncology 2015: A New Landscape in Lung Cancer



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Immuno-Oncology 2015: A New Landscape in Lung Cancer David R. Spigel, M.D. Lung Cancer Program Director Sarah Cannon Research Institute/Tennessee Oncology, PLLC Nashville, TN

Off-Label Use Disclosure(s) I do not intend to discuss an off-label use of a product during this activity. 2

Financial Disclosure(s) I currently have or have had the following relevant financial relations to disclose: Commercial Interest - Genentech, BMS Relationship with Commercial Interest Advisory Board 3

Case: A 70-Year Old Man with Stage IV Squamous NSCLC 8 months ago Diagnosed with metastases to lung, lymph nodes and pleura Treated with carboplatin + paclitaxel 3 months ago Disease progression noted Started treatment with docetaxel 2 weeks ago Disease progression noted PS=1

Poll How would you proceed in managing this patient? Gemcitabine Erlotinib Nivolumab Pemetrexed

Gene Alterations in Lung Cancer 6 Perez-Moreno, CCR 2012

Mutations Across Cancers 7 Kandoth, Nature 2013

The Potential of Immunotherapy Immune system in the Cancer Patient Normal immune systems fight invaders (bacteria, viruses) by recognizing antigens, and destroying anything with those antigens Cancer cells also produce antigens, and should be killed by killer T cells Sometimes the immune system is tricked into not recognizing the antigens on the cancer cells Some cancer cells don t produce antigens 8

PD-1, PDL-1, B7.1 Cancer Immunotherapy 9 Chen, CCR 2012

Cancer Immunotherapy 10

PD-L1 is Broadly Expressed in NSCLC PD-L1 Adenocarcinoma Prevalence of PD-L1 45% Prevalence of PD-L1 50% PD-L1 Squamous cell carcinoma H&E H&E High sensitivity and specificity in FFPE samples 11 Koeppen H. and Kowanetz M., Genentech Proprietary Genentech/Roche PD-L1 IHC

MPDL3280A: PDL1 Expression Nature, 2014 12

Selected Trials with Checkpoint Inhibitors in NSCLC

IMMUNOTHERAPY IN LUNG CANCER: ANTI-PD1 DRUG DEVELOPMENT NIVOLUMAB

CheckMate-003 Nivolumab in Patients with Pre- Treated, Advanced NSCLC: Duration of Response Durable responses observed regardless of histology Gettinger SN, et al. J Clin Oncol. 2015 Apr 20. [Epub ahead of print].

Slide 5 Presented By Scott Gettinger at 2014 ASCO Annual Meeting

CheckMate-003 Phase 1 Study with Nivolumab in Patients with Pre-Treated Advanced NSCLC: Overall Survival At least 1 prior platinum containing regimen, no more than 5 lines. 54% of patients received 3 prior lines of therapy. Responses at all dose levels. Median OS across doses was 9.9 mos 3 mg/kg dose chose for further clinical development Gettinger SN, et al. J Clin Oncol. 2015 Apr 20. [Epub ahead of print].

CheckMate-063 Phase 2 with Nivolumab in Pre- Treated Patients with Squamous NSCLC 65% of patients had failed three lines of therapy Endpoint IRC Assessed (per RECIST v1.1) ORR, % (n) [95% CI] 15 (17) [9, 22] Disease control rate, % (n) 40 (47) Median DOR, months (range) NR (2+, 12+) Ongoing responders, % (n) 76 (13) Median time to response, months (range) 3 (2, 9) PFS rate at 1-year, % (95% CI) 20 (13, 29) Median OS, months (95% CI) 8.2 (6.1, 11) OS rate at 1-year, % (95% CI) 41 (32, 50) Nivolumab demonstrated activity in previously treated patients with advanced squamous NSCLC. Rizvi NA, et al. Lancet Oncol. 2015 Mar;16(3):257-65.

Nivolumab Multi-Dose: <br />Safety in Total Population Presented By Mario Sznol at 2014 ASCO Annual Meeting

CheckMate-017: Nivolumab in Pre-Treated Squamous NSCLC Open label, randomized phase 3 study evaluating nivolumab versus docetaxel in previously treated patients with advanced, squamous cell NSCLC 1 Previously treated patients with advanced or metastatic squamous cell NSCLC (N = 272) R Nivolumab [3 mg/kg IV q 2 wks] (N=135) Primary endpoint: OS Docetaxel [75 mg/m 2 IV q 3 wks] (N=137) Nivolumab demonstrated significantly superior OS vs docetaxel, with 41% reduction in risk of death (hazard ratio: 0.59 [95% CI:0.44, 0.79; p=0.00025] 2 Median OS with nivolumab was 9.2 months [95% CI = 5.1 7.3 months]compared with 6 months [95% CI = 5.1 7.3 months] with docetaxel 2 Based in part on the results from CheckMate-063 and CheckMate- 017, the FDA approved nivolumab for treatment of patients with metastatic squamous NSCLC with progression on or after platinum-based chemotherapy 3 1. ClinicalTrials.gov identifier NCT01642004.; 2. http://www.ascopost.com/issues/april-10,-2015/nivolumabin-metastatic-squamous-non small-cell-lung-cancer-after-platinum-therapy.aspx; 3.http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm436534.htm

CheckMate-057: Nivolumab in Pre-Treated Non- Squamous NSCLC Open label, randomized phase 3 study evaluating nivolumab versus docetaxel in previously treated patients with advanced, non-squamous NSCLC 1 Previously treated patients with advanced or metastatic nonsquamous NSCLC (N = 582) R Nivolumab [3 mg/kg IV q 2 wks] Primary endpoint: OS Docetaxel [75 mg/m 2 IV q 3 wks] Results expected soon! 1. ClinicalTrials.gov identifier NCT01673867.; http://news.bms.com/press-release/checkmate-057-pivotalphase-iii-opdivo-nivolumab-lung-cancer-trial-stopped-early

IMMUNOTHERAPY IN LUNG CANCER: ANTI-PD1 DRUG DEVELOPMENT PEMBROLIZUMAB (MK3475)

KEYNOTE-001 Phase 1 Study with Pembrolizumab in NSCLC: Efficacy (N=33) (N=90) (N=38) (N=280) (N=43) Randomized (N=11) PD-L1+tumors Treatment naive R 1:2 Pembro 2 mg/kg Q3 W Pembro 10 mg/kg Q3W Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

KEYNOTE-001 Phase 1 Study with Pembrolizumab in NSCLC: Efficacy Best overall response rate was stable disease in 21.8% of patients Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

KEYNOTE-001 Phase 1 Study with Pembrolizumab in NSCLC: Efficacy Total ORR- n (%) [95% CI] Previously Treated ORR- n (%) [95% CI] Treatment naïve ORR n (%) [95% CI] PS>50% PS 1-49% PS<1 33 (45.2) [33.5-57.3] 25 (43.9) [30.7-57.6] 8 (50.0) [24.7-75.3] 17 (16.5) [9.9-25.1] 12 (15.6) [8.3-25.6] 5 (19.2) [6.6-39.4] 3 (10.7) [2.3-28.2] 2 (9.1) [1.1-29.2] 1 (16.7) [0.4-64.7] Overall response rate was 19.4% 18.0% in previously treated patients 24.8% in un-treated patients Similar response rate among dose, schedule and histology Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

KEYNOTE-001 Phase 1 Study with Pembrolizumab in NSCLC: PFS mpfs was 3.7 months for all patients mpfs was 3.0 months for previously treated patients mpfs was 6.0 months for treatment naïve patients Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

KEYNOTE-001 Phase 1 Study with Pembrolizumab in NSCLC: OS mos was 12.0 months for all patients mos was 9.3 months for previously treated patients mos was 16.2 months for treatment naïve patients Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

KEYNOTE-001 Phase 1 Study with Pembrolizumab in NSCLC: Efficacy Overall Survival Progression Free Survival PD-L1 expression in at least 50% of tumor cells correlated with improved efficacy of pembrolizumab. Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

Merck Press Release October 27, 2014 Merck Receives FDA Breakthrough Therapy Designation for KEYTRUDA (pembrolizumab) in Advanced Non-Small Cell Lung Cancer WHITEHOUSE STATION, N.J.--(BUSINESS WIRE)--Merck (NYSE:MRK), known as MSD outside the United States and Canada, announced today that the U.S. Food and Drug Administration (FDA) has granted Breakthrough Therapy Designation to KEYTRUDA (pembrolizumab), the company s anti-pd-1 therapy, for the treatment of patients with Epidermal Growth Factor Receptor (EGFR) mutation-negative, and Anaplastic Lymphoma Kinase (ALK) rearrangement-negative non-small cell lung cancer (NSCLC) whose disease has progressed on or following platinum-based chemotherapy. This is the second Breakthrough Therapy Designation granted for KEYTRUDA. 30

Anti-PD-1 Monotherapy in Heavily Pretreated Patients with Advanced NSCLC: Summary of Safety Agent N Safety Data Nivolumab 1 117 74% of patients experienced at least 1 TRAE; most common: fatigue (33%), decreased appetite (19%), asthenia (12%), and nausea (15%); 17% gr3-4 TRAEs: fatigue (4%), pneumonitis (3%), diarrhea (3%), and 2 treatment-associated deaths caused by pneumonia and ischemic stroke Pembrolizumab 2 495 71% of patients experienced at least 1 TRAE; most common: fatigue (19%), pruritus (11%), decreased appetite (10.5%), rash (10%); 9.5% gr 3-5 TRAEs: dyspnea (4%); pneumonitis (1.8%)- including one who died 1. Rizvi NA, et al. Lancet Oncol. 2015;16:257-265. 2. Garon E, et al. N Engl J Med 2015 Apr 19. [Epub ahead of print].

IMMUNOTHERAPY IN LUNG CANCER: ANTI-PDL1 DRUG DEVELOPMENT MPDL3280A

MPDL3280A: ORR 33

MPDL3280A 34

Clinical Activity of MPDL3280A in NSCLC (Squamous) Baseline Post C2 (Week 6) Post C6 (Week 18) Post C16 (Week 48) 73-year-old male, s/p deep neck mass excision, ramucirumab + gemcitabine + carboplatin PD-L1 positive 3 35

36

MPDL3280A Clinical Trial Program [TITLE] 37 Rizvi, ASCO 2014

Genentech Press Release Feb 1, 2015 FDA Grants Breakthrough Therapy Designation for Genentech s Investigational Cancer Immunotherapy MPDL3280A (anti-pdl1) in Non-Small Cell Lung Cancer Genentech, a member of the Roche Group (SIX: RO, ROG; OTCQX: RHHBY), announced today that it has received a second Breakthrough Therapy Designation from the U.S. Food and Drug Administration (FDA) for its investigational cancer immunotherapy MPDL3280A (anti-pdl1). The designation was granted for the treatment of people with PD-L1 (Programmed Death-Ligand 1) positive non-small cell lung cancer (NSCLC) whose disease has progressed during or after platinum-based chemotherapy (and an appropriate targeted therapy for those with an EGFR mutation-positive or ALK-positive tumor). 38

IMMUNOTHERAPY IN LUNG CANCER: ANTI-PDL1 DRUG DEVELOPMENT MEDI-4736

Majority Remain on Treatment<br /> Presented By Neil Segal at 2014 ASCO Annual Meeting

Objective Response Rate<br /> Presented By Neil Segal at 2014 ASCO Annual Meeting

Phase 1 Dose Expansion Study with MEDI4736: Efficacy Segal NH, et al. ASCO 2014. Abstract 3002.

Atlantic 3 rd /4 th -line NSCLC Phase II SAT MEDI4736 in cohorts by EGFR mutation/alk status NSCLC Patients with (Stage IIIB-IV) who have Received at Least Two Prior Systemic Regimens including one Platinum-based Therapy N= Up to 700 Recent ( 3 mo) Biopsy COHORT 1b (EGFR mut /ALK rearrangment +) PDL1+only N=94* MEDI4736 10mg/Kg IV, Q2W up to 12 mos Implement patient selection for PD-L1+ patients only COHORT 2b (EGFR mut /ALK rearrangment -) PDL1+only N=94* Objective Disease Progression Subsequent treatments Follow up for OS *With an assumed 15% non measurable disease rate according to central review, 94 patients are expected to result in 80 patients with measurable disease. Analysis of overall cohort population will also be conducted Primary Endpoint: ORR Blinded Independent Central Review RECIST 1.1* Q 12 weeks during tx; then Q 6 mos. 43

STUDY 1 - (PACIFIC) Phase III RCT: D4191C00001 1 st line Stage 3 Locally Advanced, Unresectable NSCLC n=702 Concomitant Platinumbased Chemo-XRT ( 2 cycles) CR + PR + SD R A N D O M I S E +1 day 2:1 MEDI4736 10mg/Kg IV, Q2W up to 12 mos. Placebo IV, Q2W up to 12 mos. PD FU PD Stratification Age PS 0-1 Gender Primary End point: PFS + OS RECIST 1.1 q 8 weeks during treatment; then q 12 weeks until PD Blinded central review 44

SWOG - LUNG MASTER PROTOCOL Phase II/III - S1400 Advanced stage refractory SCCA patients Screening registration Common Broad Platform CLIA Biomarker Profiling* Specific markers for screening: P13K PI3KCA mutation CDK4/6 CCND1, Cdk6 amplification, CDKN2 deletion and mutation FGFR FGFR amplification, mutation, fusion HGF c-met expression Match (known positive biomarker) Sub-study Assessment** Non-match (unknown negative biomarker) Non-match Sub-study A Anti-PD-L1 CT MEDI4736 Biomarker-driven AZ/MedImmune Sub-study B Target P13K Sub-study C Target CDK4/6 Sub-study D Target FGFR Sub-study E Target HGF GDC-0032 CT Palbociclib CT AZD4547 + CT CT Rilotumumab + E E Genentech Pfizer AZ Amgen Endpoint (interim PFS) OS Endpoint (interim PFS) OS Endpoint (interim PFS) OS Endpoint (interim PFS) OS 45

Selected Trials with Checkpoint Inhibitors in NSCLC

Slide 22 Presented By Scott Gettinger at 2014 ASCO Annual Meeting

Phase 2 Study with Ipilimumab + Chemotherapy in Untreated Patients with Advanced NSCLC: Efficacy Phased ipilimumab in combination with paclitaxel and carboplatin significantly improved irpfs and mwho-pfs Most common nonhematologic AEs ( 15%, any grade) typically associated with paclitaxel and carboplatin, including fatigue, alopecia, nausea, vomiting, and peripheral sensory neuropathy, were generally similar across arms. Common AEs, such as rash, pruritus, and diarrhea, showed a trend for increased incidence in the ipilimumab-containing arms than in paclitaxel and carboplatin arms, and these AEs were also identified as iraes per protocol-defined criteria. Lynch T, et al. J Clin Oncol. 2012; 30:2046-2054.

Ipilimumab + Chemotherapy in Untreated Patients with Advanced NSCLC: Histology Subgroup Analysis Phased ipilimumab appeares to show improved efficacy for squamous histology Lynch T, et al. J Clin Oncol. 2012; 30:2046-2054.

Nivolumab (anti-pd1) plus ipilimumab<br /> in advanced melanoma Presented By Laura Chow at 2014 ASCO Annual Meeting

CheckMate 012 Phase 1 Study with Nivolumab + Ipilimumab: Efficacy Overall RR = 22% Nivolumab + ipilimumab demonstrates antitumor activity in chemotherapy naïve patients Antonia SJ et al. J Clin Oncol 32:5s, 2014 (suppl; abstr 8023).

CheckMate 012 with Nivolumab + Ipilimumab : Select Adverse Events Safety profile of nivolumab combination reflected additive toxicities of each agent Gettinger S et al. J Clin Oncol. 32:5s, 2014; abstract 8024 ; Antonia SJ et al. J Clin Oncol 32:5s, 2014 (suppl; abstr 8023).

Phase 1b Study with MEDI4736 + Tremelimumab: Efficacy Antonia S, et al. ESMO 2014. abstr 15924.

Select Clinical Trials with Immune Checkpoint Inhibitors Combined with Immunotherapy in NSCLC Regimen Evaluated Phase Setting Trial Number Pembrolizumab + ipilimumab MEDI4736 + tremelimumab MEDI4736 + MEDI0680 Nivolumab + ipilimumab Nivolumab + interleukin-21 1/2 Advanced or metastatic NSCLC NCT02039674 1/2 Advanced NSCLC NCT02000947 1 Solid tumors NCT02118337 1 Chemotherapy-naïve, advanced NSCLC NCT01454102 1 Solid tumors NCT01629758 a Insert, if applicable; always end with a period 16 pt. Reference(s) 14 pt.

CheckMate 012 Phase 1 Study with Nivolumab + Erlotinib: Efficacy ORR = 19% Results suggest nivolumab + erlotinib may provide clinical benefit in TKI refractory, EGFR mutated advanced NSCLC Safety findings: Additive toxicities of both agents (grade 3/4 AEs was 24%) Rizvi N et al. J Clin Oncol 32:5s, 2014 (suppl; abstr 8022).

Select Clinical Trials with Immune Checkpoint Inhibitors Combined with Targeted Therapy in NSCLC Regimen Evaluated Phase Setting Trial Number Pembrolizumab + erlotinib or gefitinib Nivolumab + erlotinib MEDI4736 + gefitinib MPDL3280A + cobimetinib 1/2 Advanced/metastatic NSCLC 1 EGFR+, non-squamous NSCLC 1 EGFR TKI naïve and expansion in EGFR+ advanced NSCLC 1 Solid tumors, expanded in NSCLC NCT02039674 NCT01454102 NCT02088112 NCT01988896

CheckMate 012 Phase 1 Study with Nivolumab + Chemotherapy: Efficacy Antonia SJ et al. ASCO 2014; abstr 8113. Grade 3-4 treatment-related AEs reported in 45% of patients. Pneumonitis (7%), fatigue (5%), and acute renal failure (5%)

Select Clinical Trials with Immune Checkpoint Inhibitors in Combination with Chemotherapy in NSCLC Regimen Evaluated Phase Setting Trial Number Ipilimumab + pac/carbo 3 Advanced/recurrent squamous NSCLC NCT01285609 Nivolumab + gem/cis, pem/cis, or pac/carbo 1 Chemotherapy-naïve, advanced/recurrent NSCLC Nivolumab + bevacizumab 1 Given as maintenance therapy in advanced NSCLC NCT01454102 NCT01454102 Pembrolizumab + cis/pem or or pem/carbo or pac/carbo + bev MPDL3280A + pem/carbo or cis MPDL3280A + gem/cis or carbo MPDL3280A + carbo/pac or carbo/nab-pac 1/2 Advanced or metastatic NSCLC NCT02039674 3 PD-L1+, chemotherapy-naïve, nonsquamous metastatic NSCLC 3 PD-L1+, chemotherapy-naïve, squamous metastatic NSCLC 3 Chemotherapy-naïve, squamous metastatic NSCLC NCT02409342 NCT02409355 NCT02367794 MPDL3280A + carbo/nabpac 3 Chemotherapy-naïve, non-squamous metastatic NSCLC NCT02367781

Questions and Challenges What is the optimal agent or combination? Schedule and duration (and sequence)? Can we select the best patients? How can we assess benefit? Is safety fully established? 59

Slide 9 Presented By Mario Sznol at 2014 ASCO Annual Meeting

PD-L1 Expression as a Biomarker: Response (2) Agent(s) N Nivolumab 1 N = 49 Nivolumab 2 N = 38 MPDL3280A 3 N = 184 Ipilimumab + Nivolumab 4 N = 56 Pembrolizumab 5 N = 182 Testing Method Manual staining 5H1 5% cutoff Tumor staining Dako automated 5% cutoff Tumor staining Automated Roche Dx IHC >5% cutoff Tumor staining on tumor cells and tumorinfiltrating immune cells Dako automated 5% cutoff Tumor staining Dako automated 50% cutoff Tumor staining PD-L1 +/Total RR 13/31 42% 7/17 41% 12/53 23% 8/14 57% 33/73 45%

Immunotherapy in Lung Cancer Summary Multiple Agents in Development: Anti-PD1, PDL1, Anti-CTLA4, Vaccine Several Registrational Trials in Progress Nivolumab FDA-Approved Squamous (2 nd+ -Line v. Docetaxel) Adencaracinoma Phase III Positive 2 Agents Fast Tracked Break-Through Status Safety and Early efficacy signals encouraging Many questions and challenges remain: Combinations Schedule Duration Patient selection Sequencing Assessing Benefit 62