`________________
`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 Reserved
`
`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
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`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,
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`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
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`Prostate Cancer and Prostatic Diseases (2016) 00, pp 1–5.
`Zaferiou et al. in Balaji, Chapter 9, Abiraterone for the Treatment of
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`mCRPC, pp 125-155.
`Zaferiou et al., Managing Metastatic Castration-Resistant Prostate
`
`AMG 1135
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`Cancer in the Pre-chemotherapy Setting: A Changing Approach in
`
`the Era of New Targeted Agents, Drugs, 76:421–430 (2016).
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`Richards et al., Interactions of Abiraterone, Eplerenone, and
`
`AMG 1136
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`Prednisolone with Wild-type and Mutant Androgen Receptor: A
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`Rationale for Increasing Abiraterone Exposure or Combining with
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`MDV31002012, Cancer Res; 72(9) pp 2176-2182, May 1, 2012.
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`Arora et al., Glucocorticoid Receptor Confers Resistance to Anti-
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`AMG 1137
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`Androgens by Bypassing Androgen Receptor Blockade, Cell. 2013
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`December 5; 155(6): 1309–1322.
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`16
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`Zhao XY, Malloy PJ, Krishnan AV, Swami S, Navone NM, Peehl
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`AMG 1138
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`DM, Feldman D 2000 Glucocorticoids can promote androgen-
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`independent growth of prostate cancer cells through a mutated
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`androgen receptor. Nat Med 6: 703–706
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`AMG 1139 NCT02025010, Clinicaltrials.gov
`
`Zustovich 2016 Therapeutic management of bone metastasis in
`
`AMG 1140
`
`prostate cancer: an update, Expert Review of Anticancer Therapy,
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`http://dx.doi.org/10.1080/14737140.2016.1241148 (2016).
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`Crawford et al., Treating Patients with Metastatic Castration
`
`AMG 1141
`
`Resistant Prostate Cancer: A Comprehensive Review of Available
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`Therapies, The Journal of Urology, Vol. 194, 1537-1547 (2015).
`
`AMG 1142
`
`AMG 1143
`
`AMG 1144
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`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
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`Intravenous Therapy, The Oncologist 2001;6(suppl 4):12-16.
`
`Fallowfield et al., Patients’ preference for administration of
`
`AMG 1145
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`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 -
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`Supplement n. 4 (7-12) 2004.
`
`AMG 1148 Deposition transcript of Gerald W. Chodak
`
`17
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`
`
`
`
`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 Declaration of DeForest McDuff, Ph.D. dated January 16, 2017.
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`Attard G, Reid AH, Auchus RJ et al. Clinical and biochemical
`
`consequences of CYP17A1 inhibition with abiraterone given with
`
`AMG 1153
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`and without exogenous glucocorticoids in castrate men with
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`advanced prostate cancer. J Clin Endocrinol Metab 2012; 97(2):507-
`
`516.
`
`Yanase T, Simpson ER, Waterman MR. 17 alpha-
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`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
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`inhibition of 17alpha-hydroxylase and 17,20-lyase activities by three
`
`AMG 1155
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`novel missense CYP17 mutations identified in patients with
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`P450c17 deficiency. J Clin Endocrinol Metab 2002; 87(12):5714-
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`5721.
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`18
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`
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`Yanase T, Kagimoto M, Suzuki S, Hashiba K, Simpson ER,
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`Waterman MR. Deletion of a phenylalanine in the N-terminal region
`
`AMG 1156
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`of human cytochrome P-450(17 alpha) results in partial combined
`
`17 alpha-hydroxylase/17,20-lyase deficiency. J Biol Chem 1989;
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`264(30):18076-18082.
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`AMG 1157 Reserved
`
`AMG 1158 Reserved
`
`AMG 1159 Reserved
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`AMG 1160
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`Dorin RI, Qualls CR, Crapo LM. Diagnosis of adrenal insufficiency.
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`Ann Intern Med 2003; 139(3):194-204.
`
`Grinspoon SK, Biller BM. Clinical review 62: Laboratory
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`AMG 1161
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`assessment of adrenal insufficiency. J Clin Endocrinol Metab 1994;
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`79(4):923-931.
`
`AMG 1162
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`Oelkers W. Adrenal insufficiency. N Engl J Med 1996;
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`335(16):1206-1212.
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`MELBY JC, SPINK WW. Comparative studies on adrenal cortical
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`AMG 1163
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`function and cortisol metabolism in healthy adults and in patients
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`with shock due to infection. J Clin Invest 1958; 37(12):1791-1798.
`
`AMG 1164
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`MELBY JC, Egdhal RH, SPINK WW. Secretion and metabolism of
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`cortisol after injection of endotoxin. J Lab Clin Med 1960; 56:50-62.
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`19
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`Marik PE, Pastores SM, Annane D et al. Recommendations for the
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`diagnosis and management of corticosteroid insufficiency in
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`AMG 1165
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`critically ill adult patients: consensus statements from an
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`international task force by the American College of Critical Care
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`Medicine. Crit Care Med 2008; 36(6):1937-1949.
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`Abad L, Parrilla JJ, Marcos J, Gimeno F, Lopez BA. Male
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`AMG 1166
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`pseudohermaphroditism with 17 alpha-hydroxylase deficiency. A
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`case report. Br J Obstet Gynaecol 1980; 87(12):1162-1165.
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`Heremans GF, Moolenaar AJ, van Gelderen HH. Female phenotype
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`AMG 1167
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`in a male child due to 17-alpha-hydroxylase deficiency. Arch Dis
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`Child 1976; 51(9):721-723.
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`Auchus RJ. Steroid 17-hydroxylase and 17,20-lyase deficiencies,
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`AMG 1168
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`genetic and pharmacologic. J Steroid Biochem Mol Biol 2017;
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`165(Pt A):71-78.
`
`AMG 1169
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`New MI. Male pseudohermaphroditism due to 17 alpha-hydroxylase
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`deficiency. J Clin Invest 1970; 49(10):1930-1941.
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`Ryan CJ, Smith MR, Fong L et al. Phase I clinical trial of the
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`AMG 1170
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`CYP17 inhibitor abiraterone acetate demonstrating clinical activity
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`in patients with castration-resistant prostate cancer who received
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`prior ketoconazole therapy. J Clin Oncol 2010; 28(9):1481-1488.
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`Therasse P, Arbuck SG, Eisenhauer EA et al. New guidelines to
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`evaluate the response to treatment in solid tumors. European
`
`AMG 1171
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`Organization for Research and Treatment of Cancer, National
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`Cancer Institute of the United States, National Cancer Institute of
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`Canada. J Natl Cancer Inst 2000; 92(3):205-216.
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`20
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`Osoba D, Tannock IF, Ernst DS, Neville AJ. Health-related quality
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`AMG 1172
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`of life in men with metastatic prostate cancer treated with
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`prednisone alone or mitoxantrone and prednisone. J Clin Oncol
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`1999; 17(6):1654-1663.
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`Auchus RJ, Yu MK, Nguyen S, Mundle SD. Use of prednisone with
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`AMG 1173
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`abiraterone acetate in metastatic castration-resistant prostate cancer.
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`Oncologist 2014; 19(12):1231-1240.
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`Annane D, Sebille V, Charpentier C et al. Effect of treatment with
`
`AMG 1174
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`low doses of hydrocortisone and fludrocortisone on mortality in
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`patients with septic shock. JAMA 2002; 288(7):862-871.
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`Dickstein G, Spigel D, Arad E, Shechner C. One microgram is the
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`lowest ACTH dose to cause a maximal cortisol response. There is
`
`no diurnal variation of cortisol response to submaximal ACTH
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`AMG 1175
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`stimulation. Eur J Endocrinol 1997; 137(2):172-175.
`
`AMG 1176
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`Clark PM, Neylon I, Raggatt PR, Sheppard MC, Stewart PM.
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`Defining the normal cortisol response to the short Synacthen test:
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`implications for the investigation of hypothalamic-pituitary
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`disorders. Clin Endocrinol (Oxf) 1998; 49(3):287-292.
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`Endert E, Ouwehand A, Fliers E, Prummel MF, Wiersinga WM.
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`AMG 1177
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`Establishment of reference values for endocrine tests. Part IV:
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`Adrenal insufficiency. Neth J Med 2005; 63(11):435-443.
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`21
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`Gonzalbez J, Villabona C, Ramon J et al. Establishment of reference
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`values for standard dose short synacthen test (250 microgram), low
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`AMG 1178
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`dose short synacthen test (1 microgram) and insulin tolerance test
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`for assessment of the hypothalamo-pituitary-adrenal axis in normal
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`subjects. Clin Endocrinol (Oxf) 2000; 53(2):199-204.
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`Brooke AM, Taylor NF, Shepherd JH et al. A novel point mutation
`
`AMG 1179
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`in P450c17 (CYP17) causing combined 17alpha-hydroxylase/17,20-
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`lyase deficiency. J Clin Endocrinol Metab 2006; 91(6):2428-2431.
`
`Di Cerbo, Biason-Lauber A, Savino M et al. Combined 17alpha-
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`AMG 1180
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`Hydroxylase/17,20-lyase deficiency caused by Phe93Cys mutation
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`in the CYP17 gene. J Clin Endocrinol Metab 2002; 87(2):898-905.
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`Ospina NS, Al NA, Bancos I et al. ACTH Stimulation Tests for the
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`AMG 1181
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`Diagnosis of Adrenal Insufficiency: Systematic Review and Meta-
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`Analysis. J Clin Endocrinol Metab 2016; 101(2):427-434.
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`Dickstein G, Shechner C. Low dose ACTH test--a word of caution
`
`AMG 1182
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`to the word of caution: when and how to use it. J Clin Endocrinol
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`Metab 1997; 82(1):322.
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`Oelkers W, Boelke T, Bahr V. Dose-response relationships between
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`plasma adrenocorticotropin (ACTH), cortisol, aldosterone, and 18-
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`AMG 1183
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`hydroxycorticosterone after injection of ACTH-(1-39) or human
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`corticotropin-releasing hormone in man. J Clin Endocrinol Metab
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`1988; 66(1):181-186.
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`22
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`AMG 1184
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`Schulte HM, Chrousos GP, Avgerinos P et al. The corticotropin-
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`releasing hormone stimulation test: a possible aid in the evaluation
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`of patients with adrenal insufficiency. J Clin Endocrinol Metab
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`1984; 58(6):1064-1067.
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`Grinspoon SK, Biller BM. Clinical review 62: Laboratory
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`AMG 1185
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`assessment of adrenal insufficiency. J Clin Endocrinol Metab 1994;
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`79(4):923-931.
`
`AMG 1186
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`Biglieri EG, Herron MA, Brust N. 17-hydroxylation deficiency in
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`man. J Clin Invest 1966; 45(12):1946-1954.
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`AMG 1187 NCT01867710 clinicaltrials.gov
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`AMG 1188 Auchus Transcript
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`AMG 1189 Rettig Transcript
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`AMG 1190 Vellturo Transcript
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`AMG 1191 McDuff Transcript of deposition held on January 18, 2017
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`
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`Date: February 3, 2017
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`
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`Respectfully submitted,
`
`/william d. hare/
`William D. Hare
`Reg. No. 44,739
`Counsel for Petitioner
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`23
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`CERTIFICATE OF SERVICE
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`The undersigned hereby certifies that a copy of the foregoing Petitioners’
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`
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`Updated Exhibit List was served on counsel of record on February 3, 2017 by
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`filing this document through the End-to-End System, as well as delivering a copy
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`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
`
`
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`24
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`
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`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
`
`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
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`25
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`Date: February 3, 2017
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