Transcript Radium-223
Más es posible: CPRC con Metástasis Óseas Sintomáticas Javier Puente, MD, PhD Hospital Universitario Clinico San Carlos Medical Oncology Department Complutense University Associate Professor of Medicine Prostate Cancer Disease Landscape: N=230,000 in USA (some speculation…) Non – Metastatic Prostate Cancer Patients at Diagnosis Localized Prostate Cancer Local Disease with Rising PSA Post Radical Therapy Non-Metastatic Hormone Sens N=55,000 ADT 95% of 230,000 ~ 220,000 ~75% no relapse Progression 5% relapse post local Rx & mets* ~10,000 Newly diagnosed 5% of 230,000 ~ 10,000 Non-Metastatic castration resistant (M0) Intermittent ADT and develop mets on Rx break with normal testo Metastatic Hormone Sensitive Prostate Cancer ADT *either relapse with mets or Observe rising PSA and mets ~10,000 M0 CRPC prior to mCRPC (25% BCR) Metastatic CRPC N=30,000 in USA ~20,000 M1 HSPC prior to CRPC Bone metastases: very common in prostate cancer Prostate ~90% Myeloma 70-95% Breast 65-75% Thyroid 60% Bladder 40% Lung 30-40% Renal 20-25% Melanoma 14-45% INCIDENCE OF BONE METASTASES de Bono1 (COU-AA-301) 89-90% Scher2 (AFFIRM) 91-92% Tannock3 (TAX 327) 90-92% Petrylak4 (SWOG 99-16) 84-88% AFFIRM, A Study Evaluating the Efficacy and Safety of the Investigational Drug MDV3100; CRPC, castration-resistant prostate cancer; SWOG, Southwest Oncology Group. 1. de Bono J, et al. N Engl J Med. 2011;364:1995–2005. 2. Scher H, et al. N Engl J Med. 2012;367:1187–1197. [supplemental appendix] 3. Tannock I, et al. N Engl J Med. 2004;351:1502–1512. 4. Petrylak D, et al. N Engl J Med. 2004;351:1513–1520. Hormonal signals impact bone structure Boiley WJ, et al. Nature 2003 The “vicious cycle” of bone metastases Gatrell B & Saad F, Nat Rev Clin Oncol 2014 Osteoclast differentiation and activation Boiley WJ, et al. Nature 2003 Discovery of the RANK signalling pathway Boiley WJ, et al. Nature 2003 “Traditional” drug development strategies have failed microenvironment targeting drugs Antonarakis ES, J Clin Oncol 2013 Radiopharmaceuticals Inhibitors of osteoclast/osteoblast function reduce SREs but do not prolong survival Saad F, et al. Nat Rev Clin Oncol 2014 Phase III trial of denosumab in bone metastases from CRPC Fizazi K, et al. Lancet 2011; 377(9768): 813-22 Denosumab: Time to first SRE Fizazi K, et al. Lancet 2011; 377(9768): 813-22 Can the bone tropism of PC be turned into an Achilles Heel? • Prostate Cancer is the MOST BONE TROPIC of the major solid tumors • Bone/Soft tissue ratios are exceptionally high for metastatic prostate cancer compared to other solid tumors • More than 90% of metastatic prostate cancer patients enrolled in recent mCRPC trials have evidence of bony spread. • Can we exploit bone tropism for therapeutic benefit? Proposed Spiral Model for Pca progression Logothetis et al. Cancer Discov 2013 Bone stromal targeted therapy: many attempts and few successes! • Bone stromal-targeted radioharmaceutical • Strontium-89, samarium-153, radium-223 • Bone stromal + tumor targeting with endothelin antagonism • ZD4054 and atrasentan • Bone stromal + tumor targeting with p60src inhibition • Dasatinib • Bone stromal tumor targeting via antiRANK ligand inhibition • AntiRANK ligand monoclonal (denosumab) • Bone stroma targeting with biphosphonates • Clodronate and zoledronic acid Overview: Radium-223 MOA • Radium-223 is a targeted alpha emitter that selectively binds to areas of increased bone turnover in bone metastases and emits high-energy alpha particles of a short range (<100 μm)1 • As a bone-seeking calcium mimetic, it is bound into newly formed bone stroma, especially within the microenvironment of osteoblastic or sclerotic metastases2,3 • The high-energy alpha particle radiation induces α mainly double-stranded β DNA breaks that result γ in a potent and highly localized cytotoxic effect in target areas2,4-6 • The short path of the alpha particles also means that the toxic effects on adjacent healthy tissue and particularly the bone marrow may be minimized3,7-8 1. Bruland OS, et al. Clin Cancer Res. 2006;12:6250s–7s. 2. Henriksen G, et al. Cancer Res. 2002;62:3120–3125. 3. Henriksen G, et al. J Nuc Med. 2003;44:252–59. 4. Lewington VJ. J Nucl Med. 2005;46(suppl):38S–47S. 5. Liepe K. Curr Opin Investig Drugs. 2009;10:1346–58. 6. McDevitt MR, et al. Eur J Nucl Med. 1998;25:1341–51. 7. Kerr C. Lancet Oncol. 2002;3:453. 8. Li Y, et al. Expert Rev Anticancer Ther. 2004;4:459–68. ALSYMPCA (ALpharadin in SYMptomatic Prostate CAncer) phase III study design ALSYMPCA was halted early after the positive efficacy results reported from a planned interim analysis of 809 patients with 314 deaths occurred. An updated analysis of efficacy and safety was performed from all 921 enrolled patients when 528 deaths had occurred. Parker C, et al. N Engl J Med. 2013;369(3):213–223. ALSYMPCA: Inclusion Criteria • Histologically confirmed, progressive CRPCa with ≥2 bone metastases (on skeletal scintigraphy) and no known visceral metastases • Patients were receiving best standard of care • Patients had either received docetaxel, were not fit enough or willing to receive docetaxel, or did not have docetaxel available • Symptomatic disease, defined as regular use of analgesic medication for cancer-related bone pain or treatment with EBRT for bone pain within previous 12 weeks • PSA ≥5 ng/mL with evidence of progressively rising PSA valuesb • ECOG PS score of 0 to 2c • Life expectancy of ≥6 months • Adequate hematologic, renal, and liver function CRPC, castration-resistant prostate cancer; EBRT, external beam radiation therapy; ECOG PS, Eastern Cooperative Oncology Group Performance Status; PSA, prostate-specific antigen. a. Castration-resistant disease was defined as serum testosterone ≤50 ng/dL (≤1.7 nmol/L) after bilateral orchiectomy or during maintenance on androgen-ablation therapy with luteinizing hormone-releasing hormone agonist or polyestradiol phosphate throughout the study. b.Two consecutive increases over previous reference value. c. Score 0 denotes a patient fully active with no functional restriction, and increasing numbers denote greater functional compromise. 18 ALSYMPCA: patient demographics and baseline characteristics (ITT population) CHARACTERISTIC RADIUM-223 (n=614) PLACEBO (n=307) 71 (49-90) 171 (28) 71 (44-94) 90 (29) Caucasian race, n (%) 575 (94) 290 (94) Total ALP, n (%) <220 U/L ≥220 U/L 348 (57) 266 (43) 169 (55) 138 (45) Current use of bisphosphonates, n (%) Yes No 250 (41) 364 (59) 124 (40) 183 (60) Any prior use of docetaxel, n (%) Yes No 352 (57) 262 (43) 174 (57) 133 (43) ECOG PS, n (%) 0 1 ≥2 165 (27) 371 (60) 77 (13) 78 (25) 187 (61) 41 (13) WHO ladder for cancer pain, n (%) 1 2 3 257 (42) 151 (25) 194 (32) 137 (45) 78 (25) 90 (29) Extent of disease, n (%) <6 metastases 6-20 metastases >20 metastases Superscan 100 (16) 262 (43) 195 (32) 54 (9) 38 (12) 147 (48) 91 (30) 30 (10) EBRT within 12 weeks of screening, n (%) Yes No 99 (16) 515 (84) 48 (16) 259 (84) Age, years, Median (range) >75 years, n (%) Parker C, et al. N Engl J Med. 2013;369(3):213–223. ALSYMPCA Updated Analysis: Radium-223 Significantly Improved OS The updated analysis confirmed the 30% reduction in risk of death (HR=0.70) for patients in the radium-223 group compared with placebo. 100 MEDIAN OS (months) ━ Radium-223: 14.9 ━ Placebo: 11.3 Survival, % 80 Increase OS ∆=3.6 mos 60 HR (95% CI): 0.70 (0.58–0.83) P<0.001 40 20 0 0 3 6 9 12 15 18 21 24 27 30 33 36 39 7 4 1 2 0 1 0 0 Months Since Randomization ━ Radium-223 ━ Placebo 614 578 504 369 274 178 105 307 288 228 157 103 67 39 Parker C, et al. N Engl J Med. 2013;369(3):213–223. 60 24 41 14 18 7 ALSYMPCA Updated Analysis: Radium-223 Improved OS Across All Patient Subgroups SUBGROUP All patients Total ALP <220 U/L ≥220 U/L Current use of bisphosphonates Yes No Prior use of docetaxel Yes No Baseline ECOG PS 0 or 1 ≥2 Extent of disease <6 Metastases 6-20 Metastases >20 Metastases Superscan Opioid use Yesa Nob PATIENTS (n) RADIUM-223 PLACEBO MEDIAN OS (months) RADIUM-223 PLACEBO HR 95% CI 614 307 14.9 11.3 0.70 0.58-0.83 348 266 169 138 17.0 11.4 15.8 8.1 0.82 0.62 0.64-1.07 0.49-0.79 250 364 124 183 15.3 14.5 11.5 11.0 0.70 0.74 0.52-0.93 0.59-0.92 352 262 174 133 14.4 16.1 11.3 11.5 0.71 0.74 0.56-0.89 0.56-0.99 536 77 265 41 15.4 10.0 11.9 8.4 0.68 0.82 0.56-0.82 0.50-1.35 100 262 195 54 38 147 91 30 27.0 13.7 12.5 11.3 NE 11.6 9.1 7.1 0.95 0.71 0.64 0.71 0.46-1.95 0.54-0.92 0.47-0.88 0.40-1.27 345 269 168 139 13.9 16.4 10.4 12.8 0.68 0.70 0.54-0.86 0.52-0.93 0.5 Favors 1.0 Favors Radium-223 Placebo 2.0 ALP, alkaline phosphatase; CI, confidence interval; ECOG PS, Eastern Cooperative Oncology Group Performance Status; HR, hazard ratio. a. Includes patients with a score of 2 or 3 on the World Health Organization (WHO) ladder for cancer pain. b.Includes patients without pain or opioid use at baseline and patients with a OURCE: Parker C, et al. N Engl J Med. 2013;369(3):213–223. Parker C, et al. N Engl J Med. 2013;369(3):213–223. ALSYMPCA Updated Analysis: Radium-223 Significantly Improved All Secondary Efficacy Endpoints The significant improvement in all main secondary efficacy endpoints provided support for the benefit of radium-223 (+ BSoC) over placebo (+ BSoC). SECONDARY EFFICACY ENDPOINTS RADIUM-223 (n=614) PLACEBO (n=307) HAZARD RATIO (95% CI) P VALUE Median time to first SSE (months) 15.6 9.8 0.66 (0.52-0.83) <0.001 Median time to total ALP progression (months) 7.4 3.8 0.17 (0.13-0.22) <0.001 Median time to PSA progression (months) 3.6 3.4 0.64 (0.54-0.77) <0.001 Total ALP response (≥30% reduction), n (%)a 233/497 (47) 7/211 (3) — <0.001 Total ALP normalization, n (%)a,b 109/321 (34) 2/140 (1) — <0.001 ALP, alkaline phosphatase; BSoC, best standard of care; CI, confidence interval; ITT, intention-to-treat; PSA prostate-specific antigen; SSE, symptomatic skeletal event. a. Number of patients without missing values. b. .In patients who had elevated total ALP at baseline.. Parker C, et al. N Engl J Med. 2013;369(3):213–223. ALSYMPCA Updated Analysis: Safety Profiles Were Similar Between the Radium-223 and Placebo Arms NUMBER OF PATIENTS WITH AEs OCCURRING IN ≥5% OF PATIENTS IN EITHER TREATMENT GROUP There were few grade 3 AEs and grade 4 AEs were very low, also comparable to placebo. RADIUM-223 (n=600) EVENT Hematologic AEs Anemia Thrombocytopenia Neutropenia Nonhematologic AEs Constipation Diarrhea Nausea Vomiting Asthenia Fatigue General physical health deterioration Peripheral edema Pyrexia Pneumonia PLACEBO (n=301) ALL GRADES, n (%) GRADE 3, n (%) GRADE 4, n (%) GRADE 5,a n (%) ALL GRADES, n (%) GRADE 3, n (%) GRADE 4, n (%) GRADE 5,a n (%) 187 (31) 69 (12) 30 (5) 65 (11) 20 (3) 9 (2) 11(2) 18 (3) 4 (1) 0 1 (<1) 0 92 (31) 17 (6) 3 (1) 37 (12) 5 (2) 2 (1) 2 (1) 1 (<1) 0 1 (<1) 0 0 108 (18) 151 (25) 213 (36) 111 (19) 35 (6) 154 (26) 27 (5) 76 (13) 38 (6) 18 (3) 6 (1) 9 (2) 10 (2) 10 (2) 5 (1) 21 (4) 9 (2) 10 (2) 3 (1) 9 (2) 0 0 0 0 0 3 (1) 2 (<1) 0 0 0 0 0 0 0 0 0 5 (1) 0 0 4 (1) 64 (21) 45 (15) 104 (35) 41 (14) 18 (6) 77 (26) 21 (7) 30 (10) 19 (6) 16 (5) 4 (1) 5 (2) 5 (2) 7 (2) 4 (1) 16 (5) 8 (3) 3 (1) 3 (1) 5 (2) 0 0 0 0 0 2 (1) 2 (1) 1 (<1) 0 2 (1) 0 0 0 0 0 0 2 (1) 0 0 0 AE, adverse event. a. Only 1 grade 5 hematologic AE was considered possibly related to study drug: thrombocytopenia in 1 patient in the radium-223 group. Parker C, et al. N Engl J Med. 2013;369(3):213–223. Overall Survival was Significantly Improved with Radium-223, Regardless of Prior Docetaxel Use The significant survival benefit observed with radium-223, regardless of prior docetaxel use, is consistent with that reported n the ALSYMPCA ITT population (radium-223 14.9 vs 11.3 months with placebo (HR=0.695; 95% CI, 0.581-0.832; P=0.00007). MEDIAN OS, NO PRIOR DTX (months) ━ Radium-223 (n=262): 16.1 ━ Placebo (n=133): 11.5 HR (95% CI): 0.75 (0.56–0.99) P=0.039 100 80 Patients, % Patients, % 80 60 40 60 40 20 20 0 0 0 4 8 12 16 20 24 28 32 36 Months ━ Ra-223 262 236 168 118 ━ PBO 133 113 74 42 70 24 31 14 MEDIAN OS, PRIOR DTX (months) ━ Radium-223 (n=352): 14.4 ━ Placebo (n=174): 11.3 HR (95% CI): 0.71 (0.57–0.89) P=0.003 100 0 4 8 12 16 20 24 28 32 36 40 Months 13 9 7 3 1 1 0 0 Vogelzang NJ, et al. J Clin Oncol. 31, 2013 (suppl; abstr 5068). ━ Ra-223 352 327 238 155 88 ━ PBO 174 152 104 61 35 45 15 27 5 5 4 1 1 0 1 0 0 Safety of cytotoxic chemotherapy following Radium-223 PARAMETER RADIUM-223 (n=93) PLACEBO (n=54) 93 54 Median time to chemotherapy, days (range) 80.0 (1-667) 64.5 (2-448) Median duration of chemotherapy, days (range) 120.0 (1-809) 112.5 (1-863) Patients receiving chemotherapy* after study drug, n Overall Survival in the ITT Population • In the updated ALSYMPCA analysis of all 921 randomized patients prior to placebo crossover, radium-223, compared with placebo, significantly improved OS in patients with CRPC and bone metastases (P=0.00007; HR=0.695; 95% CI, 0.581-0.832) −Median OS was 14.9 months in the radium-223 group vs 11.3 months in the placebo group PARAMETER RADIUM-223 (n=93) PLACEBO (n=54) Deaths on chemotherapy, % 14 15 Causality: PC and skeletal metastases (± other mets) PC with other metastases (or mets not specified) Cerebral hemorrhage due to trauma Cardiopulmonary failure 10 3 1 0 13 0 0 2 Deaths within 30 days after chemotherapy, n (%) 6 4 Causality: PC and skeletal metastases (± other mets) Bronchopneumonia Respiratory failure + pulmonary edema 4 1 0 4 1 0 During Chemotherapy Administration 30 Days After Chemotherapy Administration Sartor O, et al. Ann Oncol 2012 (suppl; abstr 936P). ALSYMPCA Updated Analysis: Radium-223 Significantly Improved Time to SSE Patients Without SSE, % 100 80 Increase TTSSE ∆=5.8 mos 60 MEDIAN TIME TO SSE (months) ━ Radium-223: 15.6 ━ Placebo: 9.8 HR (95% CI): 0.66 (0.52–0.83) P<0.001 40 20 0 0 3 6 9 12 15 18 21 24 27 30 8 4 1 1 0 0 Months Since Randomization ━ Radium-223 ━ Placebo 614 307 496 211 342 117 199 56 129 36 63 20 31 9 BSoC, Best standard of care; CI, confidence interval; HR, hazard ratio; SSE, symptomatic skeletal event. . Parker C, et al. N Engl J Med. 2013;369(3):213–223. 8 7 Radium-223 Reduced the Overall Risk of SSEs Regardless of Baseline Stratification Factors: Bisphosphonate Use at Study Entry (Yes/No) BISPHOSPHONATE USE AT STUDY ENTRY 100 100 NO BISPHOSPHONATE USE AT STUDY ENTRY 80 Patients Without Symptomatic Skeletal Events, % Patients Without Symptomatic Skeletal Events, % MEDIAN TIME TO FIRST SSE (months) ━ Radium-223 (n=364): 11.8 ━ Placebo (n=183): 8.4 60 40 MEDIAN TIME TO FIRST SSE (months) ━ Radium-223 (n=250): 19.6 ━ Placebo (n=124): 10.2 20 80 HR (95% CI): 0.77 (0.58–1.02) P=0.07 60 40 20 HR (95% CI): 0.49 (0.33–0.74) Treatment Period Treatment Period P=0.00048 0 0 0 ━ Radium-223 250 ━ Placebo 124 4 8 12 193 71 115 29 61 17 16 20 Month 25 10 8 3 24 28 32 3 3 1 1 0 0 0 ━ Radium-223 364 ━ Placebo 183 4 8 12 16 20 24 28 32 247 103 120 41 68 19 30 9 12 4 5 1 0 0 0 0 CI, confidence interval. HR, hazard ratio. SSE, symptomatic skeletal event. NOTE: ALSYMPCA was not powered to detect differences between subgroups; P values are for descriptive purpose only and are not adjusted for multiplicity. Very few placebo patients were still evaluable at later time points on the curve; the hazard ratio is the best interpretation of radium-223 effect over the complete observed time frame. . Parker C, et al. N Engl J Med. 2013;369(3):213–223. Exploratory Post Hoc Analysis of Overall Survival by Tertiles of Baseline tALP in the Radium-223 and Placebo Cohorts • There was a trend showing improvement in OS with radium-223 treatment compared with placebo in each tALP tertile* 100 100 RADIUM-223 MEDIAN OS [months (95%CI)] ━ Tertile 1 (N=205): 23.9 (17.5-33.8) tALP min-max: 32-131 ━ Tertile 2 (N=207): 14.1 (12.0-15.9) tALP min-max: 132-333 ━ Tertile 3 (N=202): 10.2 (9.1-11.7) tALP min-max: 334-6431 60 80 Percentage of Patients Percentage of Patients 80 40 60 40 20 20 0 0 0 10 20 Months 30 PLACEBO MEDIAN OS [months (95%CI)] ━ Tertile 1 (N=102): 18.8 (13.9-24.5) tALP min-max: 29-153 ━ Tertile 2 (N=104): 11.5 (9.3-13.5) tALP min-max: 154-353 ━ Tertile 3 (N=101): 7.5 (6.5-9.1) tALP min-max: 360-4805 40 *tALP ranges in the tertiles are slightly different between radium-223 and placebo cohorts. Heinrich D, et al. Presented at the 29th Annual EAU Congress. Stockholm, Sweden. (Abstract 865). 0 10 20 Months 30 40 Radium-223 Patients with a Confirmed tALP Decline at Week 12 Had Significantly Longer Overall Survival Radium-223 patients with a confirmed tALP decline at week 12 had a significantly longer median OS versus radium-223 patients with no confirmed tALP decline (median OS: 17.8 months vs 10.4 months; HR=0.45; 95% CI, 0.34-0.61; P <0.0001). 100 MEDIAN OS (months) ━ Confirmed tALP decline (n=400): 17.8 ━ No confirmed tALP decline (n=97): HR (95% CI): 0.45 (0.34-0.61) P <0.0001 Patients, % 80 10.4 60 40 20 0 0 8 16 24 32 40 Months *Confirmed tALP decline was defined as any decrease from baseline at week 12, confirmed ≥3 weeks later. Sartor O, et al. J Clin Oncol. 31, 2013 (suppl; abstr 5080). 29 Sequencing CRPC therapy-2010 Metastatic, minimally symptomatic CRPC Survival benefit Symptomatic or poorprognosis CRPC Progresssion after docetaxel chemotherapy Secondary hormonal Rx Docetaxel Mitoxantrone BSC Not Known 3 months Not Known Zoledronic acid with CRPC (M1 ddisease) Daniel Petrylak at 2014 ASCO Annual Meeting Sequencing CRPC therapy-2015 Metastatic, minimally symptomatic CRPC 2010 Survival benefit 2015 Survival benefit Symptomatic or poorprognosis CRPC Progresssion after docetaxel chemotherapy Secondary hormonal Rx Docetaxel Mitoxantrone BSC Not Known 3 months Not Known Sipuleucel-T (4 m) Abiraterone (5.2 m) Enzalutamide (NA) Docetaxel Abiraterone (4 m) Cabazitaxel (2.5 m) Enzalutamide (4.8 m) 3 months Radium 223 (3.6 m) Denosumab or Zoledronic acid with CRPC (M1 ddisease) Daniel Petrylak at 2014 ASCO Annual Meeting Disease-modifying agents and skeletal outcomes Gatrell B & Saad F, Nat Rev Clin Oncol 2014 Radium-223 and treatment algorithm Phase 2a Study Evaluating Quantified Bone Scan Response After Treatment With Ra-223 Alone or in Combination With Abiraterone Acetate or Enzalutamide in CRPC Patients with Bone Metastases A randomized, open-label phase 2a study evaluating quantified bone scan response following treatment with radium-223 dichloride alone or in combination with abiraterone acetate or enzalutamide in CRPC patients with bone metastases PATIENTS (N=66) •Histologically or cytologically confirmed adenocarcinoma of the prostate •Known castration-resistant disease •Serum PSA ≥ 2 ng/mL (μg/L) •≥2 bone metastases on bone scan assessed within 12 weeks prior to randomization •ECOG PS 0 to 2 •Visceral and CNS metastases excluded. Radium-223 50 kBq/kg IV every 4 wk × 6 R 1:1:1 Radium-223 50 kBq/kg IV every 4 wk × 6 + abiraterone 1000 mg qd PO and prednisone 5 mg bid × 2 yrs following last radium-223 dose Radium-223 50 kBq/kg IV every 4 wk × 6 + enzalutamide 160 mg qd PO × 2 yrs following last radium-223 dose PRIMARY OBJECTIVE Test bone scan response at week 24 based on quantified BSLA for each regimen SECONDARY OBJECTIVES Safety, rPFS, SSE-FS*, OS, and time to radiologic bone progression. ASSESSMENTS: Imaging assessments will be done at screening and at weeks 8, 16, and 24, then every 12 weeks for 2 years following the last radium-223 dose or until progression. ENROLMENT: This US-based study with 20 planned sites is currently recruiting patients. As of May 16, 4 patients have been recruited, 3 have been enrolled; first patient first visit occurred on March 7, 2014. SSE-FS, symptomatic skeletal event–free survival. SSE-FS will be calculated from time of randomization to date of first SSE or death. *SSEs include time to EBRT use for bone pain or occurrence of new pathologic fracture (vertebral and non-vertebral), spinal cord compression, or tumor-related orthopedic surgery. Petrylak D, et al. J Clin Oncol. 32:5s, 2014 (suppl; abstr TPS5103). ERA 223: A Phase III Trial of Ra-223 Plus Abiraterone Acetate and Prednisone in the Treatment of Asymptomatic or Mildly Symptomatic Chemotherapy-Naïve Patients With Bone-Predominant mCRPC This international, randomized, double-blind, placebo-controlled, phase III study (ERA 223, NCT02043678) is being conducted in North America, Europe, Asia, Australia, Brazil, and Israel at 168 investigative sites. PATIENTS (N=800) •Chemo-naïve bone metastatic CRPC •Asymptomatic or mildly symptomatic •>2 bone metastases •No known brain or visceral metastasis •ECOG PS 0 or 1 STRATIFICATION •Geography (EU, NA, AUS vs Asia vs ROW •Concurrent use of bisphosphonates or denosumab alone •Total ALP <90 U/L or >90 U/L R 1:1 Radium-223 50 kBq/kg IV every 4 wk × 6 + abiraterone (100 mg once daily) and prednisone/prednisolone (5 mg BID) Matching placebo every 4 wk × 6 + abiraterone (100 mg once daily) and prednisone/prednisolone (5 mg BID) PRIMARY OBJECTIVE SSE-free survival (SSE-FS)* SECONDARY OBJECTIVES OS, time to opiate use for cancer pain, pain progression, cytotoxic chemotherapy, rPFS safety EXPLORATORY OBJECTIVES** ENROLMENT: This study is currently recruiting patients. As of September 5, 2014, 74 patients have been screened, 43 have been enrolled. ANALYSIS: 800 patients expected to provide 389 SSE-FS events are needed to detect a 39% increase in SSE-FS; i.e., an overall 0.05 level 2-sided log-rank test has approximately 90% power to detect a difference between the 2 SSE-FS curves if the alternative hypothesis HR is 0.72, assuming the median SSE-FS is 29.2 months for radium-223 versus 21.0 months for control. *SSE-FS defined as the time from randomization to occurrence of on-study SSE (defined as EBRT for skeletal symptoms, new symptomatic pathologic non-vertebral bone fracture, spinal cord compression, tumor-related orthopedic surgical intervention), or death from any cause. **Time to first on-study SSE, ALP progression, PSA progression; percentage change in total ALP from baseline; time to increase in physical symptoms based on the FACT Prostate Symptom Index: Disease-Related Subscale—Physical (FPSI-DRS-P) score. Smith MR, et al.. Ann Oncol. 2014;25 (Suppl 4): iv1 - mdu438.66. abstr 803TiP. Modeling Clinical Prostate Cancer Wan X, et al. Sci Trans Med 2014 FGFR1: Cross-species analysis PC BM Wan X, et al. Sci Trans Med 2014 Conclusions I • mCPRC is associated with complications in bone known as skeletal-related events (SREs) that are associated with decreases QoL and increased mortality. • Osteoclas-targeted agents including the bisphosphonate zoledronic acid and the monoclonal antibody denosumab are used to reduce incidence of SREs and to decrease loss of BMD. • Recently approved agents included pathway inhibitors abiraterone, enzalutamide and radium-223 have been shown to increase survival and to decrease skeletal morbidity in mCPRC. Conclusions II ALSYMPCA conclusions: In CRPC patients with bone metastases: • Only one compound, radium-223 significantly prolongs overall survival • P value=0.00185; HR=0.695; 95% IC: 0.552-0.875 • Radium-223 significantly prolonged time to first clinically relevant SRE • P value=0.00046; HR=0.610; 95%IC: 0.461-0.807 • Radium-223 was very well tolerated THANK YOU Javier Puente, MD, PhD Hospital Universitario Clinico San Carlos Medical Oncology Department Complutense University Associate Professor of Medicine