UNITED STATES PATENT AND TRADEMARK OFFICE
`________________
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`________________
`AMERIGEN PHARMACEUTICALS LIMITED
`and
`ARGENTUM PHARMACEUTICALS LLC
`Petitioners
`v.
`JANSSEN ONCOLOGY, INC.,
`Patent Owner
`________________
`Case IPR2016-002861
`________________
`Patent No. 8,822,438 B2
`
`PETITIONERS’ UPDATED EXHIBIT LIST
`
`
`
`
`
`
`
`
`
`
`
`1 Case IPR2016-01317 has been joined with this proceeding.
`
`1
`
`
`________________
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`________________
`AMERIGEN PHARMACEUTICALS LIMITED
`and
`ARGENTUM PHARMACEUTICALS LLC
`Petitioners
`v.
`JANSSEN ONCOLOGY, INC.,
`Patent Owner
`________________
`Case IPR2016-002861
`________________
`Patent No. 8,822,438 B2
`
`PETITIONERS’ UPDATED EXHIBIT LIST
`
`
`
`
`
`
`
`
`
`
`
`1 Case IPR2016-01317 has been joined with this proceeding.
`
`1
`
`
`
`
`
`
`
`
`
`LISTING OF EXHIBITS PURSUANT TO 37 C.F.R. § 42.63(e)
`
`Pursuant to 37 C.F.R. 42.63(e), Petitioner, Amerigen Pharmaceuticals, Ltd. hereby submits a
`current list of its exhibits:
`
`Exhibit
`
`AMG 1001
`
`Description
`
`U.S. Patent No. 8,822,438, Auerbach and Belldegrum, “Methods
`
`and Compositions for Treating Cancer” (“the ‘438 patent”)
`
`AMG 1002 Declaration of Dr. Scott Serels, MD, dated December 4, 2015
`O’Donnell, A. et al., “Hormonal impact of the 17α-hydroxylase/C17-
`20-lyase inhibitor abiraterone acetate (CB7630) in patients with
`
`AMG 1003
`
`prostate cancer,” British Journal of Cancer, (90):2317-2325 (2004)
`
`(“O’Donnell”)
`
`Gerber, G.S. et al., “Prostate specific antigen for assessing response
`
`to ketoconazole and prednisone in patients with hormone refractory
`
`metastatic cancer,” The Journal of Urology, 144(5):1177-9 (1990)
`
`AMG 1004
`
`(“Gerber”)
`
`AMG 1005
`
`U.S. Patent No. 5,604,213, Barrie S.E. et al., “17-Substituted
`
`Steroids Useful In Cancer Treatment” ("the '213 patent")
`
`Tannock et al., “Chemotherapy with mitoxantrone plus prednisone
`
`or prednisone alone for symptomatic hormone-resistant prostate
`
`AMG 1006
`
`cancer: a Canadian randomized trial with palliative end points,” The
`
`Journal of Clinical Oncology, 14:1756-1764 (1996) (“Tannock
`
`1996”)
`February 3, 2012 Office Action (excerpt from prosecution history of
`
`’438 patent)
`July 3, 2012 Response (excerpt from prosecution history of ’438
`
`patent)
`
`AMG 1007
`
`AMG 1008
`
`2
`
`
`
`
`
`Ryan et al., “Abiraterone in metastatic prostate cancer without
`
`AMG 1009
`
`previous chemotherapy,” The New England Journal of Medicine,
`
`368:138-148 (2012).
`
`January 11, 2013 Response (excerpt from prosecution history of
`
`’438 patent)
`March 4, 2013 Office Action (excerpt from prosecution history of
`
`’438 patent)
`June 4, 2013 Response (excerpt from prosecution history of ’438
`
`patent)
`
`July 3, 2013 Notice of Allowance (excerpt from prosecution history
`
`of ’438 patent)
`October 25, 2013 Notice of Allowance (excerpt from prosecution
`
`history of ’438 patent)
`February 11, 2014 Notice of Allowance (excerpt from prosecution
`
`history of ’438 patent)
`June 2, 2014 Notice of Allowance (excerpt from prosecution history
`
`AMG 1010
`
`AMG 1011
`
`AMG 1012
`
`AMG 1013
`
`AMG 1014
`
`AMG 1015
`
`AMG 1016
`
`of ’438 patent)
`AMG 1017 Declaration of Dr. DeForest McDuff, Ph.D., dated December 4, 2015
`
`AMG 1018 2011 Zytiga® Approval Prescribing Information
`AMG 1019 2015 Zytiga® Prescribing Information, Co-administration Brochure
`Harris et al., “Low dose Ketoconazole with replacement doses of
`
`AMG 1020
`
`hydrocortisone in patients with progressive androgen independent
`
`prostate cancer,” The Journal of Urology, volume 168:542-545
`
`(August 2002)
`William Oh, “Secondary hormonal therapies in the treatment of
`
`AMG 1021
`
`prostate cancer,” Urology, volume 60:87-93 (Supplement 3A)
`
`(September 2002)
`
`3
`
`
`
`
`
`Tannock, I. et al., “Docetaxel plus Prednisone or Mitoxantrone plus
`
`AMG 1022
`
`Prednisone for Advanced Prostate Cancer,” N. Eng. J. Med.,
`
`351:1502-12 (2004)
`
`Attard, G. et al., “Selective blockade of androgenic steroid synthesis
`
`AMG 1023
`
`by novel lyase inhibitors as a therapeutic strategy for treating
`
`metastatic prostate cancer,” Br. J. Urol. 96(9): 1241-1246 (2005)
`
`Hellerstedt et al., “The Current State of Hormonal Therapy for
`
`Prostate Cancer,” CA Cancer J. Clin., 52:154-179 (2002).
`
`AMG 1024
`
`AMG 1025
`
`Kasper, D.L. et al. (Eds.), Harrison's Principles of Internal
`Medicine, 16th Edition (2005), p. 549.
`
`Auchus, R.J. “The genetics, pathophysiology, and management of
`
`AMG 1026
`
`human deficiencies of P450c17,” Endocrinol. Metab. Clin. North
`
`Am. (30)1:101-119 (2001)
`
`Costa-Santos, M. et al., “Two Prevalent CYP17 Mutations and
`
`AMG 1027
`
`Genotype-Phenotype Correlations in 24 Brazilian Patients with 17-
`
`Hydroxylase Deficiency,” J. Clin. Endocrin. & Metabol. (89)1:49-
`
`Jubelirer, S.J., et al., “High dose ketoconazole for the treatment of
`
`AMG 1028
`
`hormone refractory metastatic prostate carcinoma,” J. Urol.,
`
`AMG 1029
`
`142(1):89-901 (1989)
`
`U.S. Patent 5,688,977, Sisti, N.J. et al., “Method for Docetaxel
`
`Synthesis”
`
`U.S. Food and Drug Administration ("FDA") FDA News Release
`
`AMG 1030
`
`dated May 19, 2004, “FDA Approves New Indication for Taxotere-
`
`Prostate Cancer”
`
`4
`
`
`
`
`
`AMG 1031
`
`Tannock, I. et al., “Treatment of metastatic prostatic cancer with
`
`low-dose prednisone: evaluation of pain and quality of life as
`
`pragmatic indices of response,” Journal of Clin. Oncology, 7:590-7
`
`(1989)
`
`AMG 1032 Taxotere® Prescribing Information (2004)
`
`Scher, H.I. et al., “Increased survival with Enzalutamide in Prostate
`
`AMG 1033
`
`Cancer after Chemotherapy,” New Eng. J. Med., 367:1187-97
`
`(2012)
`
`de Bono, J.S. et al., “Abiraterone and Increased Survival in
`
`AMG 1034
`
`Metastatic Prostate Cancer,” New Engl. J. Med., 364:1995-2005
`
`(2011)
`
`AMG 1035 Orange Book listing for Zytiga®
`
`AMG 1036 Initial Application (excerpt from prosecution history of ’438 patent)
`
`AMG 1037
`
`AMG 1038
`
`AMG 1039
`
`November 25, 2011 Office Action (excerpt from prosecution history
`
`of ’438 patent)
`
`December 21, 2011 Response (excerpt from prosecution history of
`
`’438 patent)
`
`September 11, 2012 Office Action (excerpt from prosecution history
`
`of ’438 patent)
`Cancer.net (ASCO Patient Website), Treatment of Metastatic
`
`Castration-Resistant Prostate Cancer,
`
`AMG 1040
`
`http://www.cancer.net/research-and-advocacy/asco-careand-
`
`treatment-recommendations-patients/treatment-metastatic-
`
`castrationresistant-prostate-cancer (accessed 7/24/2015).
`
`5
`
`
`
`
`
`Cancer.org (ACS), “What are the key statistics about prostate
`
`AMG 1041
`
`cancer?” http://www.cancer.org/cancer/prostatecancer/detailed
`
`guide/prostatecancerkeystatistics (accessed 8/20/2015).
`
`AMG 1042 Cowen & Company, “Biotechnology Quarterly,” 7/2/2012.
`
`AMG 1043 Cowen & Company, “Quick Take – Johnson & Johnson,”
`12/11/2012.
`Credit Suisse, “Prostate Cancer – Implications of Zytiga’s Pre-
`
`AMG 1044
`
`AMG 1045
`
`Chemo Approval,” 12/11/2012.
`FDA News Release, “FDA expands Zytiga’s use for late-stage
`
`prostate cancer,” 12/10/2012,
`
`http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/u
`
`cm331492.htm.
`FDA Website, Drugs@FDA – Zytiga,
`
`AMG 1046
`
`http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fu
`
`AMG 1047
`
`AMG 1048
`
`seaction=Search.DrugDetails (accessed 7/23/2015).
`FDA Website, Orange Book, Zytiga (NDA 202379),
`
`http://www.accessdata.fda.gov/scripts/cder/ob/docs/patexclnew.cfm
`
`?Appl_No=202379&Product_No=001&table1=OB_Rx (accessed
`
`7/24/2015).
`Galderma Laboratories, L.P. et al. v. Tolmar, Inc., 737 F.3d 731,
`
`740–41 (Fed. Cir. 2013).
`Jevtana Website, Dosing and Administration,
`
`AMG 1049
`
`http://www.jevtana.com/hcp/dosing/default.aspx (accessed
`
`8/20/2015).
`Kirby, M., C. Hirst, and E.D. Crawford (2011), “Characterising the
`
`AMG 1050
`
`Castration-Resistant Prostate Cancer Population: A Systematic
`
`Review,” International Journal of Clinical Practice 65(11): 1180-
`
`1192.
`
`6
`
`
`
`
`
`Mayo Clinic Website, Prostate cancer,
`
`AMG 1051
`
`http://www.mayoclinic.org/diseasesconditions/prostate-
`
`cancer/basics/definition/con-20029597?p=1 (accessed 7/24/2015).
`Medivation Press Release, “U.S. FDA Approves New Indication for
`
`the Use of XTANDI® (Enzalutamide) Capsules for Patients With
`
`AMG 1052
`
`Metastatic Castration-Resistant Prostate Cancer,” 9/10/2014,
`
`http://investors.medivation.com/releasedetail.cfm?ReleaseID=87026
`
`AMG 1053
`
`7.
`Merck & Co., Inc. v. Teva Pharmaceuticals USA, Inc., 395 F.3d
`
`1364, 1376–77 (Fed. Cir. 2005).
`Murphy, William J. John L. Orcutt, and Paul C. Remus (2012),
`
`AMG 1054
`
`Patent Valuation: Improving Decision Making through Analysis,
`
`Hoboken, NJ: Wiley.
`PMLiVE Website, “Top 50 Pharmaceutical Products by Global
`
`AMG 1055
`
`AMG 1056
`
`AMG 1057
`
`AMG 1058
`
`AMG 1059
`
`Sales,”
`
`http://www.pmlive.com/top_pharma_list/Top_50_pharmaceutical_p
`
`roducts_by_global_sales (accessed 9/14/2015).
`RBC Capital Markets (via Barron’s Website), “Xtandi Beats
`
`Casodex, Set to Top Zytiga,” 4/3/2015,
`
`http://online.barrons.com/articles/xtandi-beats-casodexset-to-top-
`
`zytiga-1428075331 (accessed 7/24/2015).
`Syntex (U.S.A.) LLC and Allergan v. Apotex, Inc. et al., 407 F.3d
`
`1371, 1383 (Fed. Cir. 2005).
`
`UBS Investment Research, “Johnson & Johnson – Zytiga Label
`
`Extended,” 12/10/2012.
`UBS Research, “Medivation – A Look at the Growth and Share in
`
`Prostate Cancer,” 2/3/2014.
`
`7
`
`
`
`
`
`AMG 1060
`
`AMG 1062
`
`Wedbush Securities, Inc., “Medivation: Zytiga Market Share
`
`Decline Accelerates From Last Quarter,” 7/14/2015.
`AMG 1061 Wells Fargo Securities, LLC., “Johnson & Johnson,” 6/29/2015.
`William Blair, “Biotechnology – Zytiga Fourth-Quarter Sales Imply
`
`Xtandi Strength,” 1/22/2013.
`William Blair, “Medivation, Inc. – Looking into Recent
`
`AMG 1063
`
`Weaknesses,” 7/15/2015.
`AMG 1064 Zytiga Brochure, Putting Prednisone in Perspective, 3/2015.
`
`AMG 1065 Zytiga Label, 5/20/2015.
`
`Zytiga Website, How Zytiga® (abiraterone acetate) Works,
`
`AMG 1066
`
`https://www.zytiga.com/print/about-zytiga/how-zytiga-works
`
`(accessed 7/23/2015).
`
`AMG 1067 IMS Health Data 2012-2015 for Zytiga®, Xtandi® and Jevtana®
`
`AMG 1068 Expunged
`
`AMG 1069 Expunged
`
`AMG 1070 Expunged
`
`AMG 1071 Expunged
`
`AMG 1072 Expunged
`
`AMG 1073 Petitioners’ Notice of Deposition of Matthew Rettig, M.D.
`
`8
`
`
`
`
`
`Udhane, S.S. et al., “Specificity of anti-prostate cancer CYP7A1
`
`AMG 1074
`
`inhibitors on androgen biosynthesis,” Biochemical and Biophysical
`
`Research Communications, 477:1005-1010 (2016).
`
`Akakura, K. et al., “Possible Mechanism of Dexamethasone
`
`AMG 1075
`
`Therapy for Prostate Cancer: Suppression of Circulating Level of
`
`Interleukin-6,” The Prostate, 56:106-109 (2003).
`
`AMG 1076 Petitioners’ Notice of Deposition of Gerald Walter Chodak, M.D.
`
`Wilkinson, S. and Chodak, G., “An Evaluation of Intermediate-Dose
`
`AMG 1077
`
`Ketoconazole in Hormone Refractory Prostate Cancer,” European
`
`Urology, 45:581-585 (2004).
`
`AMG 1078 Email dated June 29, 2016.
`
`AMG 1079 Email string spanning September 8, 2016 and September 12, 2016.
`
`AMG 1080 Email string spanning September 8, 2016 and September 12, 2016.
`
`AMG 1081 Email dated October 7, 2016.
`
`AMG 1082 Petitioners' Notice of Deposition of Richard Auchus, M.D., Ph.D.
`
`AMG 1083 7-Hydroxylation Deficiency in Man
`
`Novel Steroidal Inhibitors of Human Cytochrome P45017a (17a-
`
`AMG 1084
`
`Hydroxylase-C17,20a-lyase): Potential Agents for the Treatment of
`
`Prostatic Cancer
`
`9
`
`
`
`
`
`Clinical and Biochemical Consequences of CYP7A1 Inhibition with
`
`
`
`AMG 1085 Abiraterone Given with and without Exogenous Glucocorticoids in
`
`Castrate Men with Advanced Prostate Cancer
`
`AMG 1086
`
`Use of Prednisone with Abiraterone Acetate in Metastatic
`
`Castration-Resistant Prostate Cancer
`
`AMG 1087 Petitioner’s Notice of Deposition of Christopher A. Vellturo, Ph.D
`
`AMG 1088 Prednisone vs. Prednisolone for Ulcerative Colitis
`
`Dizdar 2015, Is Dexamethasone a Better Partner for Abiraterone
`
`AMG 1089
`
`Than Prednisolone, The Oncologist May 2015 vol. 20 no. 5 e13,
`
`(http://theoncologist.alphamedpress.org/content/20/5/e13.full)
`
`Abiraterone: a story of scientific innovation and commercial
`
`AMG 1090
`
`partnership (http://www.icr.ac.uk/news-features/latest-
`
`features/abiraterone-a-story-of-scientific-innovation-and-
`
`commercial-partnership)
`
`AMG 1091 Declaration of Dr. Mark J. Ratain, dated January 16, 2017
`
`AMG 1092 CV of Dr. Mark J. Ratain
`
`AMG 1093 Declaration of Dr. Richard Dorin, dated January 16, 2017
`
`AMG 1094 CV of Dr. Richard Dorin
`
`AMG 1095 Declaration of Dr. Scott Serels, dated January 16, 2017
`
`10
`
`
`
`
`
`AMG 1096 Declaration of DeForest McDuff, Ph.D. dated January 16, 2017.
`
`AMG 1097
`
`AMG 1098
`
`AMG 1099
`
`J. Trachtenberg and A. Pont, The Lancet, Ketoconazole Therapy for
`
`Advanced Prostate Cancer, at 433-435 (August 25, 1984)
`K. Kobayashi et al., Cancer, Mineralocorticoid Insufficiency Due to
`
`Suramin Therapy, CANCER, Vol. 78, No. 11 (December 1, 1996).
`
`Motion to Correct Inventorship in Case 2:15cv-05909-KM-JBC,
`
`Docket Entry 176.
`R. De Coster et al., Effects of high-dose ketoconazole and
`
`AMG 1100
`
`dexamethasone on ACTH-stimulated adrenal steroidogenesis in
`
`orchiectomized prostatic cancer patients, Acta Endocrinologica,
`
`115:265-271 (1987).
`
`D. Feldman et al., Ketoconazole and Other Imidazole Derivatives as
`
`AMG 1101
`
`Inhibitors of Steroidogenesis, Endocrine Reviews, Vol. 7, No. 4, pp
`
`409-420 (1986).
`
`M. J. Ratain et al., Statistical and Ethical Issues in the Design and
`
`AMG 1102
`
`Conduct of Phase I and II Clinical Trials of New Anticancer Agents,
`
`Journal of the National Cancer Institute, Vol. 85, No. 20, pp 1637-
`
`(October 20, 1993).
`
`M.B. Sawyer et al., Phase I Study of an Oral Formulation of
`
`AMG 1103
`
`ZD9331 Administered Daily for 28 Days, Journal of Clinical
`
`Oncology, Vol. 21, No. 9, pp 1859-1865 (2003).
`
`AMG 1104
`
`C.J. Ryan et al., Dose-Ranging Study of the Safety and
`
`Pharmacokinetics of Atrasentan in Patients with Refractory
`
`Malignancies, Clinical Cancer Research, Vol. 10, pp 4406-4411
`
`(July 1, 2004).
`
`11
`
`
`
`
`
`I.G. Ron et al., A low-dose adrenocorticotropin test reveals impaired
`
`AMG 1105
`
`adrenal function in cancer patients receiving megestrol acetate
`
`therapy, European Journal of Cancer, 38, 1490-1494 (2002).
`
`S. M. Wilhelm et al., BAY 43-9006 Exhibits Broad Spectrum Oral
`
`Antitumor Activity and Targets the RAF/MEK/ERK Pathway and
`
`AMG 1106
`
`Receptor Tyrosine Kinases Involved in Tumor Progression and
`
`Angiogenesis, Cancer Research, 64, pp 7099-7109 (October 1,
`
`2004).
`
`S. Udhane et al., Specificity of Anti-Prostate Cancer CYP17A1
`
`AMG 1107
`
`Inhibitors on Androgen Biosynthesis, Biochemical and Biophysical
`
`Research Communications, 477, pp 1005-1010 (Elsevier 2016)
`
`Robert Twycross, Corticosteroids in Advanced Cancer, BMJ 305, pp
`
`969-970 (October 24, 1992)
`
`AMG 1108
`
`D.E. Rathkopf et al., Updated Interim Efficacy Analysis and Long-
`
`AMG 1109
`
`Term Safety of Abiraterone Acetate in Metastatic Castration-
`
`Resistant Prostate Cancer Patients Without Prior Chemotherapy
`
`(COU-AA-302), European Urology, No. 66, pp 815-825 (2014).
`
`C.J. Ryan et al., Abiraterone acetate plus prednisone versus placebo
`
`plus prednisone in chemotherapy-naive men with metastatic
`
`AMG 1110
`
`castration-resistant prostate cancer (COU-AA-302): final overall
`
`survival analysis of a randomised, double-blind, placebo-controlled
`
`phase 3 study, The Lancet, Vol. 16, pp 152-160 (February 2015).
`
`12
`
`
`
`
`
`C.J. Ryan et al., Abiraterone in Metastatic Prostate Cancer without
`
`AMG 1111
`
`Previous Chemotherapy, The New England Journal of Medicine,
`
`368; 2, pp 138-148 (January 10, 2013).
`
`W. Berry et al., Phase III Study of Mitoxantrone Plus Low Dose
`
`Prednisone Versus Low Dose Prednisone Alone in Patients with
`
`Asymptomatic Hormone Refractory Prostate Cancer, The Journal of
`
`AMG 1112
`
`Urology, Vol. 168, 2439-2443 (December 2002).
`
`C.N. Sternberg et al., Phase III Trial of Satraplatin, an Oral Platinum
`
`AMG 1113
`
`plus Prednisone vs. Prednisone alone in Patients with Hormone-
`
`Refractory Prostate Cancer, Oncology, 68, pp 2-9 (2005).
`
`Sartor et al., Effect of Prednisone on Prostate-Specific Antigen in
`
`AMG 1114
`
`Patients with Hormone-Refractory Prostate Cancer, Urology, 52 (2)
`
`pp. 252-256 (1998).
`
`S. Oudard et al., Annals of Oncology Vol. 18, Prostate-Specific
`
`AMG 1115
`
`Antigen Doubling Time Before Onset of Chemotherapy as a
`
`Predictor of Survival for Hormone-Refractory Prostate Cancer
`
`Patients, at 1828-
`
`AMG 1116
`
`L. Collette et al., Is Prostate-Specific Antigen a Valid Surrogate End
`
`Point for Survival in Hormonally Treated Patients With Metastatic
`
`Prostate Cancer? Joint Research of the European Organisation for
`
`Research and Treatment of Cancer, the Limburgs Universitair
`
`Centrum, and AstraZeneca Pharmaceuticals, Journal of Clinical
`
`Oncology, Vol. 23, No. 25, pp 6139-6148 (September 1, 2005).
`
`13
`
`
`
`
`
`L. Collette et al., Prostate-specific antigen (PSA) alone is not an
`
`appropriate surrogate marker of long-term therapeutic benefit in
`
`prostate cancer trials, European Journal of Cancer, 42, pp 1344-1350
`
`AMG 1117
`
`(2006).
`
`S. Halabi et al., Prostate-Specific Antigen Changes As Surrogate for
`
`Overall Survival in Men With Metastatic Castration-Resistant
`
`AMG 1118
`
`Prostate Cancer Treated With Second-Line Chemotherapy, Journal
`
`of Clinical Oncology, Vol. 31, No. 31, pp 3944-3950 (November 1,
`
`2013).
`
`H.I. Scher et al., Journal of Clinical Oncology, Vol. 26, No. 7,
`
`Design and End Points of Clinical Trials for Patients with
`
`AMG 1119
`
`Progressive Prostate Cancer and Castrate Levels of Testosterone:
`
`Recommendations of the Prostate Cancer Clinical Trials Working
`
`Group, at 1148-1159 (March 1, 2008).
`
`AMG 1120 FDA Workshop 2004 Prostate Agenda
`
`T. Saika et al., Treatment of androgen-independent prostate cancer
`
`AMG 1121
`
`with dexamethasone: A prospective study in stage D2 patients,
`
`International Journal of Urology, 8, pp 290–294 (2001).
`
`M. Morioka et al., Urologia Internationalis Vol. 68, Prostate-
`
`Specific Antigen Levels and Prognosis in Patients with Hormone-
`
`Refractory Prostate Cancer Treated with Low-Dose Dexamethasone,
`
`AMG 1122
`
`at 10-15 (2002).
`
`14
`
`
`
`
`
`K. Nishimura et al., Cancer Vol. 89, No. 12, Low Doses of Oral
`
`AMG 1123
`
`Dexamethasone for Hormone-Refractory Prostate Carcinoma, at
`
`2570-2576 (December 15, 2000)
`
`D. Trump et al., American Cancer Society Vol. 106, No. 10, Phase
`
`AMG 1124
`
`II Trial of High-Dose, Intermittent Calcitriol (1,25
`
`Dihydroxyvitamin D3) and Dexamethasone in Androgen-
`
`Independent Prostate Cancer.
`
`AMG 1125
`
`Fakih et al., Glucocorticoids and Treatment of Prostate Cancer: A
`
`Preclinical and Clinical Review, Urology, 60(4), pp 553-561 (2002).
`Akakura et al., Possible Mechanism of Dexamethasone Therapy for
`
`AMG 1126
`
`Prostate Cancer: Suppression of Circulating Level of Interleukin-6,
`
`The Prostate, 56:106-109 (2003).
`
`AMG 1127
`
`J.A. Storlie et al., Cancer Vol. 76, No. 1, Prostate Specific Antigen
`
`Levels and Clinical Response to Low Dose Dexamethasone for
`
`Hormone-Refractory Metastatic Prostate Carcinoma, at 96-100 (July
`
`1, 1995).
`
`Attard, Poster: A randomized trial of abiraterone acetate (AA)
`
`AMG 1128
`
`administered with 1 of 4 glucocorticoid (GC) regimens in metastatic
`
`castration-resistant prostate cancer (mCRPC) patients (pts), J. Clin
`
`Oncol 34, 2016 (Suppl 2S: abstr 261).
`
`D. Lorente et al., British Journal of Cancer, Tumour responses
`
`following a steroid switch from prednisone to dexamethasone in
`
`castration-resistant prostate cancer patients progressing on
`
`AMG 1129
`
`abiraterone
`
`15
`
`
`
`
`
`N. Romero-Laorden et al., Journal of Clinical Oncology Vol. 34,
`
`AMG 1130
`
`Prospective Evaluation of the Response to Prednisone-
`
`Dexamethasone Switch in Castration-Resistant Prostate Cancer
`
`Patients Treated (2016).
`
`Dizdar 2015, Is Dexamethasone a Better Partner for Abiraterone
`
`AMG 1131
`
`Than Prednisolone, The Oncologist May 2015 vol. 20 no. 5 e13,
`
`(http://theoncologist.alphamedpress.org/content/20/5/e13.full)
`
`Venkitaraman et al., A Randomised Phase 2 Trial of Dexamethasone
`
`AMG 1132
`
`Versus Prednisolone in Castration-resistant Prostate Cancer,
`
`European Urology, 67, pp 673-679 (2015).
`
`Sonpavde et al., Impact of single-agent daily prednisone on
`
`AMG 1133
`
`outcomes in men with metastatic castration-resistant prostate cancer,
`
`AMG 1134
`
`Prostate Cancer and Prostatic Diseases (2016) 00, pp 1–5.
`Zaferiou et al. in Balaji, Chapter 9, Abiraterone for the Treatment of
`
`mCRPC, pp 125-155.
`Zaferiou et al., Managing Metastatic Castration-Resistant Prostate
`
`AMG 1135
`
`Cancer in the Pre-chemotherapy Setting: A Changing Approach in
`
`the Era of New Targeted Agents, Drugs, 76:421–430 (2016).
`
`Richards et al., Interactions of Abiraterone, Eplerenone, and
`
`AMG 1136
`
`Prednisolone with Wild-type and Mutant Androgen Receptor: A
`
`Rationale for Increasing Abiraterone Exposure or Combining with
`
`MDV31002012, Cancer Res; 72(9) pp 2176-2182, May 1, 2012.
`
`Arora et al., Glucocorticoid Receptor Confers Resistance to Anti-
`
`AMG 1137
`
`Androgens by Bypassing Androgen Receptor Blockade, Cell. 2013
`
`December 5; 155(6): 1309–1322.
`
`16
`
`
`
`
`
`Zhao XY, Malloy PJ, Krishnan AV, Swami S, Navone NM, Peehl
`
`AMG 1138
`
`DM, Feldman D 2000 Glucocorticoids can promote androgen-
`
`independent growth of prostate cancer cells through a mutated
`
`androgen receptor. Nat Med 6: 703–706
`
`AMG 1139 NCT02025010, Clinicaltrials.gov
`
`Zustovich 2016 Therapeutic management of bone metastasis in
`
`AMG 1140
`
`prostate cancer: an update, Expert Review of Anticancer Therapy,
`
`http://dx.doi.org/10.1080/14737140.2016.1241148 (2016).
`
`Crawford et al., Treating Patients with Metastatic Castration
`
`AMG 1141
`
`Resistant Prostate Cancer: A Comprehensive Review of Available
`
`Therapies, The Journal of Urology, Vol. 194, 1537-1547 (2015).
`
`AMG 1142
`
`AMG 1143
`
`AMG 1144
`
`Balaji, Managing Metastatic Prostate Cancer in Your Urological
`
`Oncology Practice (2016).
`DeMario et al., Oral Chemotherapy: Rationale and Future
`
`Directions, Clin Oncol, 16:2557-2567, 1998.
`
`Borner et al., Answering Patients’ Needs: Oral Alternatives to
`
`Intravenous Therapy, The Oncologist 2001;6(suppl 4):12-16.
`
`Fallowfield et al., Patients’ preference for administration of
`
`AMG 1145
`
`endocrine treatments by injection or tablets: results from a study of
`
`women with breast cancer, Annals of Oncology 17: 205–210, 2006.
`
`AMG 1146 US Patent Publication No. 2015/0005268
`
`AMG 1147
`
`Vidal et al., Reversing Resistance to Targeted Therapy, Vol. 16 -
`
`Supplement n. 4 (7-12) 2004.
`
`AMG 1148 Deposition transcript of Gerald W. Chodak
`
`17
`
`
`
`
`
`AMG 1149 Jevtana Label 9/2016
`
`Johnson & Johnson, “Zytiga Approved in the EU for Use in the
`
`AMG 1150
`
`Treatment of Metastatic Castration-Resistant Prostate Cancer Before
`
`Chemotherapy,” 1/11/2013
`
`
`EMA- Zytiga Product Information,
`
`AMG 1151
`
`http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-
`
`_Product_Information/human/002321/WC500112858.pdf
`
`
`AMG 1152 Expunged
`
`Attard G, Reid AH, Auchus RJ et al. Clinical and biochemical
`
`consequences of CYP17A1 inhibition with abiraterone given with
`
`AMG 1153
`
`and without exogenous glucocorticoids in castrate men with
`
`advanced prostate cancer. J Clin Endocrinol Metab 2012; 97(2):507-
`
`516.
`
`Yanase T, Simpson ER, Waterman MR. 17 alpha-
`
`AMG 1154
`
`hydroxylase/17,20-lyase deficiency: from clinical investigation to
`
`molecular definition. Endocr Rev 1991; 12(1):91-108
`
`Van Den Akker EL, Koper JW, Boehmer AL et al. Differential
`
`inhibition of 17alpha-hydroxylase and 17,20-lyase activities by three
`
`AMG 1155
`
`novel missense CYP17 mutations identified in patients with
`
`P450c17 deficiency. J Clin Endocrinol Metab 2002; 87(12):5714-
`
`5721.
`
`18
`
`
`
`
`
`Yanase T, Kagimoto M, Suzuki S, Hashiba K, Simpson ER,
`
`Waterman MR. Deletion of a phenylalanine in the N-terminal region
`
`AMG 1156
`
`of human cytochrome P-450(17 alpha) results in partial combined
`
`17 alpha-hydroxylase/17,20-lyase deficiency. J Biol Chem 1989;
`
`264(30):18076-18082.
`
`AMG 1157 Reserved
`
`AMG 1158 Reserved
`
`AMG 1159 Reserved
`
`AMG 1160
`
`Dorin RI, Qualls CR, Crapo LM. Diagnosis of adrenal insufficiency.
`
`Ann Intern Med 2003; 139(3):194-204.
`
`Grinspoon SK, Biller BM. Clinical review 62: Laboratory
`
`AMG 1161
`
`assessment of adrenal insufficiency. J Clin Endocrinol Metab 1994;
`
`79(4):923-931.
`
`AMG 1162
`
`Oelkers W. Adrenal insufficiency. N Engl J Med 1996;
`
`335(16):1206-1212.
`
`MELBY JC, SPINK WW. Comparative studies on adrenal cortical
`
`AMG 1163
`
`function and cortisol metabolism in healthy adults and in patients
`
`with shock due to infection. J Clin Invest 1958; 37(12):1791-1798.
`
`AMG 1164
`
`MELBY JC, Egdhal RH, SPINK WW. Secretion and metabolism of
`
`cortisol after injection of endotoxin. J Lab Clin Med 1960; 56:50-62.
`
`19
`
`
`
`
`
`Marik PE, Pastores SM, Annane D et al. Recommendations for the
`
`diagnosis and management of corticosteroid insufficiency in
`
`AMG 1165
`
`critically ill adult patients: consensus statements from an
`
`international task force by the American College of Critical Care
`
`Medicine. Crit Care Med 2008; 36(6):1937-1949.
`
`Abad L, Parrilla JJ, Marcos J, Gimeno F, Lopez BA. Male
`
`AMG 1166
`
`pseudohermaphroditism with 17 alpha-hydroxylase deficiency. A
`
`case report. Br J Obstet Gynaecol 1980; 87(12):1162-1165.
`
`Heremans GF, Moolenaar AJ, van Gelderen HH. Female phenotype
`
`AMG 1167
`
`in a male child due to 17-alpha-hydroxylase deficiency. Arch Dis
`
`Child 1976; 51(9):721-723.
`
`Auchus RJ. Steroid 17-hydroxylase and 17,20-lyase deficiencies,
`
`AMG 1168
`
`genetic and pharmacologic. J Steroid Biochem Mol Biol 2017;
`
`165(Pt A):71-78.
`
`AMG 1169
`
`New MI. Male pseudohermaphroditism due to 17 alpha-hydroxylase
`
`deficiency. J Clin Invest 1970; 49(10):1930-1941.
`
`Ryan CJ, Smith MR, Fong L et al. Phase I clinical trial of the
`
`AMG 1170
`
`CYP17 inhibitor abiraterone acetate demonstrating clinical activity
`
`in patients with castration-resistant prostate cancer who received
`
`prior ketoconazole therapy. J Clin Oncol 2010; 28(9):1481-1488.
`
`Therasse P, Arbuck SG, Eisenhauer EA et al. New guidelines to
`
`evaluate the response to treatment in solid tumors. European
`
`AMG 1171
`
`Organization for Research and Treatment of Cancer, National
`
`Cancer Institute of the United States, National Cancer Institute of
`
`Canada. J Natl Cancer Inst 2000; 92(3):205-216.
`
`20
`
`
`
`
`
`Osoba D, Tannock IF, Ernst DS, Neville AJ. Health-related quality
`
`AMG 1172
`
`of life in men with metastatic prostate cancer treated with
`
`prednisone alone or mitoxantrone and prednisone. J Clin Oncol
`
`1999; 17(6):1654-1663.
`
`Auchus RJ, Yu MK, Nguyen S, Mundle SD. Use of prednisone with
`
`AMG 1173
`
`abiraterone acetate in metastatic castration-resistant prostate cancer.
`
`Oncologist 2014; 19(12):1231-1240.
`
`Annane D, Sebille V, Charpentier C et al. Effect of treatment with
`
`AMG 1174
`
`low doses of hydrocortisone and fludrocortisone on mortality in
`
`patients with septic shock. JAMA 2002; 288(7):862-871.
`
`Dickstein G, Spigel D, Arad E, Shechner C. One microgram is the
`
`lowest ACTH dose to cause a maximal cortisol response. There is
`
`no diurnal variation of cortisol response to submaximal ACTH
`
`AMG 1175
`
`stimulation. Eur J Endocrinol 1997; 137(2):172-175.
`
`AMG 1176
`
`Clark PM, Neylon I, Raggatt PR, Sheppard MC, Stewart PM.
`
`Defining the normal cortisol response to the short Synacthen test:
`
`implications for the investigation of hypothalamic-pituitary
`
`disorders. Clin Endocrinol (Oxf) 1998; 49(3):287-292.
`
`Endert E, Ouwehand A, Fliers E, Prummel MF, Wiersinga WM.
`
`AMG 1177
`
`Establishment of reference values for endocrine tests. Part IV:
`
`Adrenal insufficiency. Neth J Med 2005; 63(11):435-443.
`
`21
`
`
`
`
`
`Gonzalbez J, Villabona C, Ramon J et al. Establishment of reference
`
`values for standard dose short synacthen test (250 microgram), low
`
`AMG 1178
`
`dose short synacthen test (1 microgram) and insulin tolerance test
`
`for assessment of the hypothalamo-pituitary-adrenal axis in normal
`
`subjects. Clin Endocrinol (Oxf) 2000; 53(2):199-204.
`
`Brooke AM, Taylor NF, Shepherd JH et al. A novel point mutation
`
`AMG 1179
`
`in P450c17 (CYP17) causing combined 17alpha-hydroxylase/17,20-
`
`lyase deficiency. J Clin Endocrinol Metab 2006; 91(6):2428-2431.
`
`Di Cerbo, Biason-Lauber A, Savino M et al. Combined 17alpha-
`
`AMG 1180
`
`Hydroxylase/17,20-lyase deficiency caused by Phe93Cys mutation
`
`in the CYP17 gene. J Clin Endocrinol Metab 2002; 87(2):898-905.
`
`Ospina NS, Al NA, Bancos I et al. ACTH Stimulation Tests for the
`
`AMG 1181
`
`Diagnosis of Adrenal Insufficiency: Systematic Review and Meta-
`
`Analysis. J Clin Endocrinol Metab 2016; 101(2):427-434.
`
`Dickstein G, Shechner C. Low dose ACTH test--a word of caution
`
`AMG 1182
`
`to the word of caution: when and how to use it. J Clin Endocrinol
`
`Metab 1997; 82(1):322.
`
`Oelkers W, Boelke T, Bahr V. Dose-response relationships between
`
`plasma adrenocorticotropin (ACTH), cortisol, aldosterone, and 18-
`
`AMG 1183
`
`hydroxycorticosterone after injection of ACTH-(1-39) or human
`
`corticotropin-releasing hormone in man. J Clin Endocrinol Metab
`
`1988; 66(1):181-186.
`
`22
`
`
`
`AMG 1184
`
`Schulte HM, Chrousos GP, Avgerinos P et al. The corticotropin-
`
`releasing hormone stimulation test: a possible aid in the evaluation
`
`of patients with adrenal insufficiency. J Clin Endocrinol Metab
`
`1984; 58(6):1064-1067.
`
`Grinspoon SK, Biller BM. Clinical review 62: Laboratory
`
`AMG 1185
`
`assessment of adrenal insufficiency. J Clin Endocrinol Metab 1994;
`
`79(4):923-931.
`
`AMG 1186
`
`Biglieri EG, Herron MA, Brust N. 17-hydroxylation deficiency in
`
`man. J Clin Invest 1966; 45(12):1946-1954.
`
`AMG 1187 NCT01867710 clinicaltrials.gov
`
`AMG 1188 Auchus Transcript
`
`AMG 1189 Rettig Transcript
`
`AMG 1190 Vellturo Transcript
`
`AMG 1191 McDuff Transcript of deposition held on January 18, 2017
`
`AMG 1192 Declaration of Renita Rathinam
`
`AMG 1193 Supplemental Declaration of Dr. Mark Ratain, M.D.
`
`AMG 1194 Declaration of William D. Hare
`
`AMG 1195 Declaration of Gabriela Materassi
`
`
`
`
`
`23
`
`
`
`Respectfully submitted,
`
`/William D. Hare/
`William D. Hare
`Reg. No. 44,739
`12 Roszel Road, Suite C104
`Princeton, NJ 08540
`(202) 640-1801
`bill@miplaw.com
`Counsel for Petitioner Amerigen
`
`
`
`
`
`Date: February 11, 2017
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`
`24
`
`
`
`CERTIFICATE OF SERVICE
`
`The undersigned hereby certifies that a copy of the foregoing Petitioners’
`
`
`
`
`
`Updated Exhibit List was served on counsel of record on February 11, 2017 by
`
`filing this document through the End-to-End System, as well as delivering a copy
`
`via electronic mail to counsel of record for the Patent Owner at the following
`
`addresses:
`
`Dianne B. Elderkin
`Barbara L. Mullin
`Ruben H. Munoz
`delderkin@akingump.com
`bmullin@akingump.com
`rmunoz@akingump.com
`JANS-ZYTIGA@akingump.com
`AKIN GUMP STRAUSS HAUER & FELD LLP
`
`
`
`David T. Pritikin
`Bindu Donovan
`Paul J. Zegger
`Todd Krause
`Isaac Olson
`Alyssa B. Monsen
`dpritikin@sidley.com
`bdonovan@sidley.com
`pzegger@sidley.com
`tkrause@sidley.com
`iolson@sidley.com
`amonsen@sidley.com
`ZytigaIPRTeam@sidley.com
`SIDLEY AUSTIN LLP
`
`
`
`25
`
`
`
`
`
`Jennifer H. Roscetti
`Anthony C. Tridico
`jennifer.roscetti@finnegan.com
`anthony.tridico@finnegan.com
`FINNEGAN HENDERSON FARABOW GARRETT & DUNNER
`
`Teresa Stanek Rea
`Shannon M. Lentz
`TRea@Crowell.com
`SLentz@Crowell.com
`CROWELL & MORING LLP
`
`
`
`
`Date: February 11, 2017
`
`
`
`
`
`
`
`
`
`
`
`/William D. Hare/
`William D. Hare
`
`26
`
`
Accessing this document will incur an additional charge of $.
After purchase, you can access this document again without charge.
Accept $ Charge
Still Working On It
This document is taking longer than usual to download. This can happen if we need to contact the court directly to obtain the document and their servers are running slowly.
Give it another minute or two to complete, and then try the refresh button.
A few More Minutes ... Still Working
It can take up to 5 minutes for us to download a document if the court servers are running slowly.
Thank you for your continued patience.
This document could not be displayed.
We could not find this document within its docket. Please go back to the docket page and check the link. If that does not work, go back to the docket and refresh it to pull the newest information.
Your account does not support viewing this document.
You need a Paid Account to view this document. Click here to change your account type.
Your account does not support viewing this document.
Set your membership
status to view this document.
With a Docket Alarm membership, you'll
get a whole lot more, including:
- Up-to-date information for this case.
- Email alerts whenever there is an update.
- Full text search for other cases.
- Get email alerts whenever a new case matches your search.
One Moment Please
The filing “” is large (MB) and is being downloaded.
Please refresh this page in a few minutes to see if the filing has been downloaded. The filing will also be emailed to you when the download completes.
Your document is on its way!
If you do not receive the document in five minutes, contact support at support@docketalarm.com.
Sealed Document
We are unable to display this document, it may be under a court ordered seal.
If you have proper credentials to access the file, you may proceed directly to the court's system using your government issued username and password.
Access Government Site
