In the United States Patent and Trademark Office
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`
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`
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`
`
`
`
`Before the Patent Trial and Appeal Board
`
`AMERIGEN PHARMACEUTICALS LIMITED,
`
`Petitioner
`
`v.
`
`JANSSEN ONCOLOGY, INC.,
`
`Patent Owner
`
`
`
`
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`
`
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`
`
`
`U.S. Patent No. 8,822,438 to Auerbach et al.
`Issue Date: September 2, 2014
`Title: Methods and Compositions for Treating Cancer
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`Inter Partes Review No. Unassigned
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`
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438 Under
`35 U.S.C. §§ 311-319 and 37 C.F.R. §§ 42.1-42.80, 42.100-42.123
`
`
`
`Mail Stop “PATENT BOARD”
`Patent Trial and Appeal Board
`U.S. Patent and Trademark Office
`P.O. Box 1450
`Alexandria, Virginia 22313–1450
`
`Submitted Electronically via the Patent Review Processing System
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`
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`

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`Page
`
`TABLE OF CONTENTS
`TABLE OF CONTENTS .................................................................................................................. i
`
`LISTING OF EXHIBITS PURSUANT TO 37 C.F.R. § 42.63(e) AND TABLE OF
`ABBREVIATIONS ............................................................................................................... iii
`
`TABLE OF ABBREVIATIONS ....................................................................................................... x
`
`CHALLENGED CLAIMS OF U.S. PATENT NO. 8,822,438 ......................................................... xi
`
`I.
`
`II.
`
`III.
`
`IV.
`
`V.
`
`INTRODUCTION ................................................................................................................. 1
`
`MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1)) ............................................................ 1
`
`A.
`
`B.
`
`C.
`
`D.
`
`E.
`
`Real Party-In-Interest Under 37 C.F.R. § 42.8(b)(1) ---------------------------------------- 1
`
`Related Matters Under 37 C.F.R. § 42.8(b)(2) ----------------------------------------------- 1
`
`Lead And Back-Up Counsel Under 37 C.F.R. § 42.8(b)(3) --------------------------------- 2
`
`Service Information Under 37 C.F.R. § 42.8(b)(4) ------------------------------------------ 2
`
`Service on Patent Owner Under 37 C.F.R. § 42.106(a) and 42.105(a) ------------------- 2
`
`GROUNDS FOR STANDING (37 C.F.R. §§ 42.101 and 42.104) ........................................ 3
`
`PAYMENT OF FEES (37 C.F.R. § 42.103) ......................................................................... 4
`
`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE REASONS
`THEREFOR (37 C.F.R. § 42.22(a)) ...................................................................................... 4
`
`VI.
`
`IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(b)) ......................................... 4
`
`VII.
`
`INTRODUCTION AND SUMMARY OF ARGUMENT .................................................... 5
`
`VIII. LEVEL OF ORDINARY SKILL IN THE ART ................................................................... 7
`
`IX.
`
`U.S. PATENT NO. 8,822,438 AND ITS FILE HISTORY................................................... 8
`
`A.
`
`B.
`
`Specification of the ‘438 Patent ----------------------------------------------------------------- 8
`
`File History of the ‘438 Patent ------------------------------------------------------------------ 11
`
`X.
`
`CLAIM CONSTRUCTION (37 C.F.R. §§ 42.100(b), 42.104(b)(3)) ................................... 17
`
`XI.
`
`SCOPE AND CONTENT OF THE PRIOR ART ................................................................. 19
`
`A.
`
`B.
`
`C.
`
`1.
`
`2.
`
`Overview ------------------------------------------------------------------------------------------- 19
`
`Background of Prostate Cancer and Its Treatment ------------------------------------------ 23
`
`Prior Art References ------------------------------------------------------------------------------ 28
`
`IN 2004, O’DONNELL DESCRIBED THE ADMINISTRATION OF ABIRATERONE ACETATE
`AS MORE EFFECTIVE FOR TREATING METASTATIC REFRACTORY PROSTATE CANCER
`THAN KETOCONAZOLE, AND POSSIBLY REQUIRING CONCOMITANT GLUCOCORTICOID
`REPLACEMENT THERAPY ....................................................................................................................... 28
`
`IN 1990, GERBER DISCLOSED THE USE OF KETOCONAZOLE WITH PREDNISONE, A
`GLUCOCORTICOID,
`IN PATIENTS WITH HORMONE REFRACTORY METASTATIC
`PROSTATE CANCER ................................................................................................................................ 31
`
`i
`
`ii
`
`v
`
`

`
`3.
`
`IN 1997, THE ‘213 PATENT DISCLOSED ABIRATERONE ACETATE, AND ITS
`SUPERIORITY OVER KETOCONAZOLE IN THE TREATMENT OF PROSTATE CANCER ................................. 33
`
`XII. EXPLANATION OF GROUNDS FOR UNPATENTABILITY .......................................... 36
`
`A.
`
`B.
`
`C.
`
`D.
`
`E.
`
`F.
`
`G.
`
`H.
`
`I.
`
`J.
`
`K.
`
`L.
`
`Claim 1 --------------------------------------------------------------------------------------------- 36
`
`Claims 2 and 3------------------------------------------------------------------------------------- 40
`
`Claim 4 --------------------------------------------------------------------------------------------- 41
`
`Claim 5 --------------------------------------------------------------------------------------------- 42
`
`Claims 6-9 ------------------------------------------------------------------------------------------ 43
`
`Claim 10 -------------------------------------------------------------------------------------------- 44
`
`Claim 11 -------------------------------------------------------------------------------------------- 44
`
`Claims 12-16--------------------------------------------------------------------------------------- 45
`
`Claim 17 -------------------------------------------------------------------------------------------- 46
`
`Claim 18 -------------------------------------------------------------------------------------------- 47
`
`Claim 19 -------------------------------------------------------------------------------------------- 47
`
`Claim 20 -------------------------------------------------------------------------------------------- 48
`
`XIII. SECONDARY CONSIDERATIONS DO NOT INDICATE THAT THE CLAIMS
`OF THE ‘438 PATENT ARE NON-OBVIOUS ................................................................... 48
`
`A.
`
`B.
`
`C.
`
`D.
`
`E.
`
`Applicants Did Not Offer Relevant Evidence of Commercial Success and the
`Examiner Issued the ‘438 Patent Based on the Erroneous Conclusion that the
`Asserted Commercial Success of Zytiga® Overcame the Obviousness of the
`Claimed Invention. -------------------------------------------------------------------------------- 48
`
`One of Skill Would Not Anticipate Unexpected Benefits from the Claimed
`Invention and Applicants Did Not Offer Any Evidence of Relevant Unexpected
`Results ---------------------------------------------------------------------------------------------- 52
`
`The ‘438 Patent Satisfied No Long-Felt But Unmet Need ---------------------------------- 56
`
`The '213 is a Blocking Patent that Limits the Applicability of Commercial Success --- 57
`
`Copying By Generic Drug Makers Is Irrelevant --------------------------------------------- 59
`
`XIV. CONCLUSION ..................................................................................................................... 59
`
`CERTIFICATE OF SERVICE .......................................................................................................... 60
`
`
`
`
`
`ii
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`ii
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`v
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`

`
`LISTING OF EXHIBITS PURSUANT TO 37 C.F.R. § 42.63(e) AND
`TABLE OF ABBREVIATIONS
`
`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 (“Serels Decl.")
`
`O’Donnell, A. et al., “Hormonal impact of the 17α-hydroxylase/C17-
`
`AMG 1003
`
`20-lyase inhibitor abiraterone acetate (CB7630) in patients with
`
`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)
`
`(“Gerber”)
`
`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
`
`cancer: a Canadian randomized trial with palliative end points,” The
`
`Journal of Clinical Oncology, 14:1756-1764 (1996) (“Tannock”)
`
`February 3, 2012 Office Action (excerpt from prosecution history of
`
`'438 patent)
`
`July 3, 2012 Response (excerpt from prosecution history of ’438
`
`patent)
`
`AMG 1004
`
`AMG 1005
`
`AMG 1006
`
`AMG 1007
`
`AMG 1008
`
`iii
`
`ii
`
`v
`
`

`
`Ryan et al., “Abiraterone in metastatic prostate cancer without
`
`AMG 1009
`
`previous chemotherapy,” The New England Journal of Medicine,
`
`368:138-148 (2012).
`
`AMG 1010
`
`AMG 1011
`
`AMG 1012
`
`AMG 1013
`
`AMG 1014
`
`AMG 1015
`
`AMG 1016
`
`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
`
`of ’438 patent)
`
`AMG 1017 Declaration of Dr. DeForest McDuff, PhD (“McDuff Declaration”)
`
`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)
`
`iv
`
`ii
`
`v
`
`

`
`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).
`
`Kasper, D.L. et al. (Eds.), Harrison's Principles of Internal
`
`Medicine, 16th Edition (2005), p. 549.
`
`AMG 1024
`
`AMG 1025
`
`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
`60 (2004)
`
`AMG 1028
`
`hormone refractory metastatic prostate carcinoma,” J. Urol.,
`
`142(1):89-901 (1989)
`
`U.S. Patent 5,688,977, Sisti, N.J. et al., “Method for Docetaxel
`
`Synthesis”
`
`AMG 1029
`
`U.S. Food and Drug Administration ("FDA") FDA News Release
`
`AMG 1030
`
`dated May 19, 2004, “FDA Approves New Indication for Taxotere-
`
`Prostate Cancer”
`
`v
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`ii
`
`v
`
`

`
`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).
`
`vi
`
`ii
`
`v
`
`

`
`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
`
`Chemo Approval,” 12/11/2012.
`
`FDA News Release, “FDA expands Zytiga’s use for late-stage
`
`AMG 1045
`
`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
`
`seaction=Search.DrugDetails (accessed 7/23/2015).
`FDA Website, Orange Book, Zytiga (NDA 202379),
`
`AMG 1047
`
`AMG 1048
`
`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.
`
`vii
`
`ii
`
`v
`
`

`
`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
`
`7.
`Merck & Co., Inc. v. Teva Pharmaceuticals USA, Inc., 395 F.3d
`
`AMG 1053
`
`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
`
`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
`
`AMG 1056
`
`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
`
`AMG 1057
`
`AMG 1058
`
`AMG 1059
`
`Prostate Cancer,” 2/3/2014.
`
`viii
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`ii
`
`v
`
`

`
`AMG 1060
`
`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.
`
`AMG 1062
`
`AMG 1063
`
`William Blair, “Biotechnology – Zytiga Fourth-Quarter Sales Imply
`
`Xtandi Strength,” 1/22/2013.
`
`William Blair, “Medivation, Inc. – Looking into Recent
`
`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®
`
`
`
`
`
`ix
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`ii
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`v
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`

`
`TABLE OF ABBREVIATIONS
`
`Abbreviation
`
`Definition
`
`ACTH
`
`AR
`
`CRPC
`
`mCRPC
`
`CYP17
`
`DHT
`
`Adrenocorticotropic hormone
`
`Androgen receptor
`
`Castration-resistant prostate cancer
`
`Metastatic Castration-resistant prostate cancer
`
`17 α-hydroxylase/C17,20-lyase
`
`Dihydrotestosterone
`
`HWT mice
`
`Human wild type mice
`
`Information Disclosure Statement
`
`Luteinizing hormone
`
`New Drug Application
`
`Person of Ordinary Skill in the Art
`
`Prostate-specific antigen
`
`Request for Continued Examination
`
`
`
`IDS
`
`LH
`
`NDA
`
`POSA
`
`PSA
`
`RCE
`
`
`
`x
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`ii
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`

`
`CHALLENGED CLAIMS OF U.S. PATENT NO. 8,822,438
`
`1. A method for the treatment of a prostate cancer in a human comprising
`
`administering to said human a therapeutically effective amount of abiraterone acetate
`
`or a pharmaceutically acceptable salt thereof and a therapeutically effective amount of
`
`prednisone.
`
`2. The method of claim 1, wherein the therapeutically effective amount of
`
`abiraterone acetate or pharmaceutically acceptable salt thereof is from about 50
`
`mg/day to about 2000 mg/day.
`
`3. The method of claim 2, wherein the therapeutically effective amount of
`
`abiraterone acetate or pharmaceutically acceptable salt thereof is from about 500
`
`mg/day to about 1500 mg/day.
`
`4. The method of claim 3, wherein the therapeutically effective amount of
`
`abiraterone acetate or pharmaceutically acceptable salt thereof is about 1000 mg/day.
`
`5. The method of claim 1, wherein the therapeutically effective amount of the
`
`abiraterone acetate or a pharmaceutically acceptable salt thereof is administered in at
`
`least one dosage form comprising about 250 mg of abiraterone acetate or a
`
`pharmaceutically acceptable salt thereof.
`
`6. The method of claim 1, wherein therapeutically effective amount of
`
`prednisone is from about 0.01 mg/day to about 500 mg/day.
`
`xi
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`
`7. The method of claim 6, wherein therapeutically effective amount of
`
`prednisone is from about 10 mg/day to about 250 mg/day.
`
`8. The method of claim 7, wherein therapeutically effective amount of
`
`prednisone is about 10 mg/day.
`
`9. The method of claim 1, wherein the therapeutically effective amount of
`
`prednisone is administered in at least one dosage form comprising about 5 mg of
`
`prednisone.
`
`10. The method of claim 1, comprising administering to said human about 500
`
`mg/day to about 1500 mg/day of abiraterone acetate or a pharmaceutically acceptable
`
`salt thereof and about 0.01 mg/day to about 500 mg/day of prednisone.
`
`11. The method of claim 10, comprising administering to said human about
`
`1000 mg/day of abiraterone acetate or a pharmaceutically acceptable salt thereof and
`
`about 10 mg/day of prednisone.
`
`12. The method of claim 1, wherein said prostate cancer is refractory prostate
`
`cancer.
`
`13. The method of claim 2, wherein refractory prostate cancer is not responding
`
`to at least one anti-cancer agent.
`
`14. The method of claim 13, wherein at least one anti-cancer agent comprises a
`
`hormonal ablation agent, an anti-androgen agent, or anti-neoplastic agent.
`
`xii
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`
`15. The method of claim 14, wherein the hormonal ablation agent comprises
`
`deslorelin, leuprolide, goserelin, or triptorelin.
`
`16. The method of claim 14, wherein the anti-androgen agent comprises
`
`bicalutamide, flutamide, or nilutamide.
`
`17. The method of claim 14, wherein the antineoplastic agent comprises
`
`docetaxel.
`
`18. The method of claim 12, comprising administering to said human about 500
`
`mg/day to about 1500 mg/day of abiraterone acetate or a pharmaceutically acceptable
`
`salt thereof and about 0.01 mg/day to about 500 mg/day of prednisone.
`
`19. The method of claim 18, comprising administering to said human about
`
`1000 mg/day of abiraterone acetate or a pharmaceutically acceptable salt thereof and
`
`about 10 mg/day of prednisone.
`
`20. The method of claim 17, comprising administering to said human about
`
`1000 mg/day of abiraterone acetate or a pharmaceutically acceptable salt thereof and
`
`about 10 mg/day of prednisone.
`
`xiii
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`
`
`
`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
`
`I.
`
`INTRODUCTION
`
`(IPR2015-TBD)
`
`Amerigen Pharmaceuticals, Ltd. ("Petitioner") petitions for Inter Partes
`
`
`Review of claims 1 - 20 of U.S. Patent No. 8,822,438 to Auerbach et al. (“the ’438
`
`patent”) (AMG Ex. 1001), which is assigned to Janssen Oncology, Inc.
`
`(“Janssen”), under 35 U.S.C. §§ 311-319 and 37 C.F.R. Part 42 and a
`
`determination that all claims (1-20) of the ’438 patent be canceled as unpatentable.
`
`II. MANDATORY NOTICES (37 C.F.R. § 42.8(a)(1))
`
`Petitioner provides the following mandatory notices under 37 C.F.R. §§
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`42.8(a)(1) and 42.8(b).
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`A. Real Party-In-Interest Under 37 C.F.R. § 42.8(b)(1)
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`Petitioner Amerigen Pharmaceuticals, Ltd. is the real party-in-interest.
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`B. Related Matters Under 37 C.F.R. § 42.8(b)(2)
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`To the best of Petitioner’s knowledge, the following litigations or other
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`related matters related to the ’438 patent that would affect, or be affected by, a
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`decision in this proceeding are pending:
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`BTG International Limited et al. v. Actavis Laboratories FL, Inc. et al., 15 cv
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`81079-DMM (Southern District of Florida).
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`BTG INTERNATIONAL LIMITED et al. v. Actavis Laboratories FL, Inc.,
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`Amneal Pharmaceuticals LLC,, Amneal Pharmaceuticals of New York, LLC.,
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`
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`Apotex Corp., Apotex Inc., Citron Pharma LLC,, Dr. Reddy's Laboratories, Inc., Dr.
`(IPR2015-TBD)
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`Reddy's Laboratories, Ltd., Hikma Pharmaceuticals, LLC., Mylan Pharmaceuticals
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`Inc., Mylan, Inc., Par Pharmaceuticals Companies, Inc., Par Pharmaceuticals, Inc.,
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`Sun Pharmaceuticals Industries, Inc., Sun Pharmaceuticals Industries, Ltd, Teva
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`Pharmaceuticals USA, Inc., West-Ward Pharmaceuticals Corp., Wockhardt BIO
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`AG, Wockhardt Ltd., Wockhardt USA LLC, 15 cv 5909-KM-JBC (District of New
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`Jersey)
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`C.
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`Lead And Back-Up Counsel Under 37 C.F.R. § 42.8(b)(3)
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`Lead Counsel
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`Back-Up Counsel
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`William Hare (Reg. No. 44,739)
`McNeely Hare & War LLP
`12 Roszel Road, Suite C104,
`Princeton, NJ 08540
`Telephone: (202) 640-1801
`Fax: (202) 478-1813
`bill@miplaw.com
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`Gabriela Materassi (Reg. No. 47,774)
`McNeely Hare & War LLP
`12 Roszel Road, Suite C104,
`Princeton, NJ 08540
`Telephone: (347) 684-4154
`Fax: (202) 478-1813
`materassi@miplaw.com
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`D.
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`Service Information Under 37 C.F.R. § 42.8(b)(4)
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`Documents may be delivered by hand to the addresses of lead and back-up
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`counsel above. Petitioner consents to electronic service by e-mail at the above
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`listed email addresses of Lead and Back-Up Counsel (bill@miplaw.com and
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`materassi@miplaw.com).
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`E.
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`Service on Patent Owner Under 37 C.F.R. § 42.106(a) and
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`42.105(a)
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`2
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`
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`This petition is being served by Express Mail on Janssen Oncology, Inc.,
`(IPR2015-TBD)
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`owners of the ‘438 Patent, at their addresses of record according to the USPTO
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`PAIR database: Janssen Oncology, Inc., 10990 Wilshire Blvd., Suite 1200, Los
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`Angeles, CA 90024; and Johnson & Johnson, One Johnson & Johnson Plaza, New
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`Brunswick, NJ 08933-7003.
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`III. GROUNDS FOR STANDING (37 C.F.R. §§ 42.101 and 42.104)
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`Petitioner is eligible under 37 C.F.R. § 42.101 to file a petition to initiate an
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`inter partes review of the ‘438 patent because: (1) the Petitioner does not own the
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`‘438 patent; (2) prior to the date this Petition was filed, neither the Petitioner nor
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`any real party-in-interest filed a civil action challenging the validity of a claim of
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`the ‘438 patent; (3) this Petition has been filed less than one year after the date on
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`which Petitioner, a real party-in-interest, or a privy of the Petitioner were served
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`with a complaint alleging infringement of the ‘438 patent; and (4) neither
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`Petitioner, any real party-in-interest, nor any privies of Petitioner, are estopped
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`from challenging the claims on the grounds identified in this Petition.
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`Petitioner certifies under 37 C.F.R. § 42.104 that the ‘438 patent is available
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`for inter partes review and that the Petitioner is not barred or estopped from
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`requesting an inter partes review challenging the patent claims on the grounds
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`identified in the petition.
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`This Petition is filed in accordance with 37 CFR § 42.106(a). Concurrently
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`3
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`filed herewith is a Power of Attorney and an Exhibit List per § 42.10(b) and §
`(IPR2015-TBD)
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`42.63(e), respectively.
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`
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`IV. PAYMENT OF FEES (37 C.F.R. § 42.103)
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`The required fee is paid via online credit card payment. The Office is
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`authorized to charge any fee deficiencies and credit overpayments to Deposit Acct.
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`No. 502923, Customer ID No. 32687.
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`V.
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`STATEMENT OF THE PRECISE RELIEF REQUESTED AND THE
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`REASONS THEREFOR (37 C.F.R. § 42.22(a))
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`Petitioner requests inter partes review and cancellation of claims 1-20.
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`Petitioner’s full statement of the reasons for the relief requested is set forth in
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`detail in Section XI-XIII below.
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`VI.
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`IDENTIFICATION OF CHALLENGE (37 C.F.R. § 42.104(b))
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`Petitioner respectfully requests inter partes review and cancellation of
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`claims 1-20 of the ‘438 Patent based on the grounds set forth in the table below:
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`Ground Challenged Claims
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`Statutory Basis
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`References
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`1
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`2
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`1-20
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`§ 103
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`O’Donnell in view of Gerber
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`1-4 and 6-11
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`§ 103
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`'213 patent in view of Gerber
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`Sections XI-XIII below explain how the ‘438 patent claims are unpatentable
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`on the grounds listed above. See Graham v. John Deere Co., 383 U.S. 1, 17-18
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`4
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`(1966) (obviousness analysis evaluates the level of ordinary skill in the art; the
`(IPR2015-TBD)
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`scope and content of the prior art; whether any differences between the prior art
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`and the claims would have been obvious to the skilled artisan; and secondary
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`considerations).
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`In support of these grounds for unpatentability, Petitioner submits the expert
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`declaration of Dr. Scott Serels, M.D., (AMG Ex. 1002 (“Serels Declaration”)) to
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`discuss the relevant field and art in general, and the factual and opinion bases
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`underlying Petitioner’s Grounds 1 and 2 for the Graham factors other than
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`commercial success. Petitioner also submits the expert declaration of economics
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`expert Dr. DeForest McDuff, PhD (AMG Ex. 1017 (“McDuff Declaration”)) on
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`the secondary considerations of the Graham factors.
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`Petitioner also relies on the other Exhibits set forth in the concurrently filed
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`Listing of Exhibits.
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`VII. INTRODUCTION AND SUMMARY OF ARGUMENT
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`The claims of the ‘438 patent are directed to treating prostate cancer by
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`administering therapeutically effective amounts of abiraterone acetate, a 17 α-
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`hydroxylase/C17,20-lyase inhibitor ("CYP17 inhibitor"), in combination with
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`prednisone, a glucocorticoid. The prior art taught use of abiraterone acetate as an
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`effective anti-cancer agent which suppresses testosterone synthesis in prostate
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`cancer patients. AMG Ex. 1002, Serels Decl. ¶¶ 26, 45, 56, 58. It was known that
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`testosterone promoted prostate cancer proliferation and progress so that to treat
`(IPR2015-TBD)
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`prostate cancer, testosterone synthesis must be suppressed.
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`However, it was known that in using a CYP17 inhibitor to reduce
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`testosterone synthesis, the CYP17 inhibitor also undesirably suppressed the
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`production of cortisol, a glucocorticoid, which is necessary for other biochemical
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`cycles in the body and its reduced production caused adverse effects, including
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`hypertension, hypokalemia (decrease in circulating potassium levels), and fluid
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`retention. To address the suppressed synthesis of cortisol, the prior art also taught
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`that concomitant glucocorticoid replacement therapy might be necessary when
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`administering abiraterone to treat prostate cancer in a patient, and that this was
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`common practice in the treatment of prostate cancer with ketoconazole, another
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`CYP17 inhibitor. AMG Ex. 1002, Serels Decl. ¶¶ 32, 34, 48.
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`The prior art also taught that abiraterone was a more effective CYP17
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`inhibitor than ketoconazole. For example, the prior art taught that abiraterone
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`acetate was more effective in decreasing testosterone levels in a mammal than
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`ketoconazole. AMG Ex. 1002, Serels Decl. ¶¶36, 45. The prior art also taught that
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`the combination of ketoconazole and prednisone was a safe and effective treatment
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`for refractory metastatic prostate cancer. AMG Ex. 1002, Serels Decl. ¶48.
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`One of skill in the art would have combined abiraterone acetate and
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`prednisone based on teachings of O’Donnell in view of Gerber and/or the '213
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`6
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`patent in view of Gerber for a safe and effective treatment of prostate cancer with a
`(IPR2015-TBD)
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`reasonable expectation of success because the prior art taught abiraterone acetate
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`as a more effective CYP17 inhibitor than ketoconazole and the combination of
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`ketoconazole and prednisone as safe and effective to treat patients with hormone
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`refractory metastatic prostate cancer. AMG Ex. 1002, Serels Decl. ¶¶45-49.
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`There are no secondary considerations of commercial success that overcome
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`obviousness. The claims of the application resulting in the ‘438 patent were
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`repeatedly rejected for obviousness until the Examiner allowed the claims based on
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`the purported "unexpected commercial success" of Zytiga®, the brand name under
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`which abiraterone acetate is marketed in the United States by the Assignee. In
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`particular, the Examiner's allowance of the claims based on secondary
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`considerations of commercial success of Zytiga® was in error because Applicants
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`failed to show the necessary nexus between the claimed invention (which is
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`directed to method of treating prostate cancer by administering abiraterone acetate
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`and prednisone) and any commercial success of the drug Zytiga®.
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`VIII. LEVEL OF ORDINARY SKILL IN THE ART
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`A person of ordinary skill in the art is presumed to be aware of all pertinent
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`art, thinks along conventional wisdom in the art, and is a person of ordinary
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`creativity. With respect to the '438 patent, the scientific field relevant is oncology
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`or urology. AMG Ex. 1002, Serels Decl. ¶8. A person of ordinary skill in the art
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`7
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`Petition for Inter Partes Review of U.S. Patent No. 8,822,438
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`would be a physician specializing in urology or oncology, or holding a Ph.D. in
`(IPR2015-TBD)
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`pharmacology, biochemistry or a related discipline. AMG Ex. 1002, Serels Decl.
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`¶8. Additional experience could substitute for the advanced degree. AMG Ex.
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`1002, Serels Decl. ¶8. To the extent necessary, one of skill in the art may
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`collaborate with one or more other persons of skill in the art for one or more
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`aspects with which the other person may have expertise, experience and/or
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`knowledge that was obtained through his or her education, industrial or academic
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`experiences. AMG Ex. 1002, Serels Decl. ¶9. For example, one of skill may
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`consult with an enzymologist and/or molecular biologist and thus may rely on the
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`opinions of such specialists in evaluating the claims. AMG Ex. 1002, Serels Decl.
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`¶10.
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`IX. U.S. PATENT NO. 8,822,438 AND ITS FILE HISTORY
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`A.
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`Specification of the ‘438 Patent
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`The “Background” section describes prostatectomy and radiotherapy, a
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`primary course of treatment for patients diagnosed with organ-confined prostate
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`cancer, as being highly invasive and ineffective on metastasized prostate cancer.
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`In addition, the specification states that these localized treatments are not effective
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`on prostate cancer after it has metastasized; and that, moreover, a large percent of
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`individuals who receive such localized treatments will suffer from “recurring
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`cancer.” The specification states that another treatment option for prostate cancer,
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`8
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`Petition for Inte