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`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`UNITED STATES PATENT AND TRADEMARK OFFICE PATENT
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`
`WEST-WARD PHARMACEUTICALS INTERNATIONAL LIMITED,
`
`Petitioner,
`
`v.
`
`NOVARTIS PHARMACEUTICALS CORPORATION
`
`Patent Owner.
`
`Case: IPR2017-015921
`Patent No. 8,410,131
`
`PETITIONER’S UPDATED EXHIBIT LIST DATED AUGUST 10, 2018
`
`
`
`1 IPR2018-0007 has been joined to this proceeding and the proceeding has been
`terminated as to Petitioner Breckenridge Pharmaceutical Inc.
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1001
`
`U.S. Patent No. 8,410,131 (“the ‘131 patent”)
`
`1002
`
`1003
`
`1004
`
`1005
`
`1006
`
`1007
`
`1008
`
`PCT Published Application No. WO 01/51049 A1, O-
`Methylated Rapamycin Derivatives for Alleviation and
`Inhibition of Lymphoproliferative Disorders, to Wasik
`et al. (“Wasik”)
`
`PCT Published Application No. WO 00/33878
`A2,Macrolides, to Navarro et al. (“Navarro”)
`
`Crowe et al., Absorption and Intestinal Metabolism of
`SDZ-RAD and Rapamycin in Rats, Drug Metab. Disp.
`(1999), 27(5): 627-632 (“Crowe”)
`
`Luan et al., Sirolimus Prevents Tumor Progression:
`mTOR Targeting for the Inhibition of Neoplastic
`Progression, Am. J. Transplant. (2001) 1 Suppl 1,243
`(Abstr. No. 428) (“Luan”)
`
`Hidalgo et al., The Rapamycin-sensitive Signal
`Transduction Pathway as a Target for Cancer Therapy,
`Oncogene (2000) 19(56): 6680-6686 (“Hidalgo”)
`
`Alexandre et al., CCI-779, A new Rapamycin Analog,
`Has Antitumor Activity at Doses Including Only Mild
`Cutaneous Effects and Mucositis: Early Results of an
`Ongoing Phase I Study, Clin. Cancer Res. Suppl.
`(1999) 5: 3730s, Abstr. No. 7 (AACR- NCI-EORTC
`International Conference, November 16-19, 1999 held
`in Washington, DC) (“Alexandre”)
`
`Schuler et al., SDZ RAD, A New Rapamycin Derivative,
`Transplantation (1997) 64(1): 36-42 (“Schuler”)
`
`1
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1009
`
`1010
`
`1011
`
`1012
`
`1013
`
`1014
`
`1015
`
`1016
`
`1017
`
`1018
`
`1019
`
`Neumayer et al., Entry-into-human Study with the
`Novel Immunosuppressant SDZ RAD in Stable Renal
`Transplant Patients, Br. J. Clin. Pharmacol. (1999)
`48(5): 694-703 (“Neumayer”)
`
`Declaration of Allan J. Pantuck, M.D. in Support of
`Petition for Inter Partes Review of U.S. Patent No.
`8,410,131
`RAPAMUNE® (sirolimus) Oral Solution
`RAPAMUNE® Approval Letter and approved labeling
`
`Great Britain patent application (GB 0104072.4, “GB
`‘072” or “the ‘072 priority application”)
`
`Great Britain patent application (GB0124957.2, “GB
`‘957” or “the ‘957 priority application”)
`
`International Patent Application No. PCT/EP02/01714
`(“the ‘714 PCT Application”)
`
`IPR Final Rules
`
`Dancey, J. E., Rapamycin-Sensitive Signal-
`Transduction Pathways: Protein Translation Control of
`Cell Proliferation, ASCO Educational Book (2000) 68-
`75 (“Dancey”)
`
`Sorbera et al, SDZ-RAD, Drugs of the Future (1999)
`24(1): 22-29 (“Sorbera”)
`
`U.S. Patent No. 5,362,718, to Skotnicki et al.
`(“Skotnichi ‘718”)
`
`U.S. Patent No. 5,665,772 to Cottens et al. (“Cottens
`‘772 patent”)
`
`2
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1020
`
`1021
`
`1022
`
`1023
`
`1024
`
`1025
`
`1026
`
`1027
`
`1028
`
`Sedrani et al., Chemical Modification of Rapamycin:
`The Discovery of SDZ RAD, Transplantation
`Proc.(1998) 30(5): 2192-2194 (“Sedrani”)
`
`PCT Published Application No. WO 97/47317 A1,
`Combination of a Somatostatin Analogue and a
`Rapamycin, to G. Weckbecker (“Weckbecker”)
`
`U.S. Patent No. 6,331,547, Water Soluble SDZ RAD
`Esters, which issued to Zhu et al. on December 18,
`2001 from U.S. Provisional Patent Application No.
`60/183,035 filed on August 18, 1999 to Zhu (“Zhu ‘547
`patent”)
`
`U.S. Patent Application Publication No. 2002/0183239
`A1, Antineoplastic Combinations, which published on
`December 5, 2002 from an application filed on April 6,
`2001, to Gibbons (“Gibbons US ‘239”)
`
`U.S. Patent Application Publication No. 2003/0008923
`A1, Antineoplastic Combinations, which published on
`January 9, 2003 from an application filed on June 1,
`2001 to Dukart (“Dukart US ‘923”)
`
`Flowcharts for 35 U.S.C. § 102(e) Dates (“102(e) Date
`Flowchart”)
`
`Published Application No. WO 94/09010 A1, O-
`Alkylated Rapamycin Derivatives and their use,
`particularly as immunosuppressants, to Cottens et al.
`(“Cottens WO ‘010”)
`
`Selected portions of Prosecution History Documents
`(“May 10, 2010 Amendment re. Cottens WO ‘010”)
`
`Curriculum Vitae of Allan J. Pantuck, M.D.
`
`3
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`
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`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1029
`
`1030
`
`1031
`
`1032
`
`1033
`
`1034
`
`1035
`
`1036
`
`2015 Orange Book,”35th Edition (2015) with respect to
`AFINITOR® (“2015 Orange Book “)
`
`Alexandre, Raymond, et al., La rapamycine et le CCI-
`779, Bull. Cancer (1999) 86(10): 808-811(“Alexandre”
`and Raymond”)
`
`Boni et al., Pharmacokinetics of escalating doses of
`CCI-779 in Combination with 5-Fluorouracil and
`Leucovorin in Patients with Advanced Solid Tumors,
`Eur. J. Cancer (2001) 37(Suppl. 6): S68 (Abstr. No.
`242) (The 11th ECCO October 21-25, 2001 meeting
`held in Lisbon, Portugal) (“Boni”)
`
`Dinney et al., Biology of Metastasis: Studies in Renal
`Cancer (17-24), in Principles and Practice of
`Genitourinary Oncology (Raghavan et al. eds., 1997)
`(“Dinney”)
`
`Shi et al., Rapamycin enhances Apoptosis and
`Increases Sensitivity to Cisplatin in Vitro, Cancer
`Research (1995) 55(9): 1982-1988 (“Shi”)
`
`Fosså et al., Survival of Patients with Advanced
`Urothelial Cancer
`treated with Cisplatin-based
`Chemotherapy, Brit. J. Cancer (1996) 74: 1655-1659
`(“Fosså”)
`
`Motzer et al., Survival and Prognostic Stratification of
`670 Patients with Advanced Renal Cell Carcinoma, J.
`Clin. Oncol. (1999) 17(8): 2530-2540 (“Motzer et al.”)
`
`PCT Published Application No. WO 02/40000 A2, Use
`of CCI-779 as an Antineoplastic Agent, to Dukart et al.
`(“Dukart WO ‘000”)
`
`4
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1037
`
`1038
`
`1039
`
`1040
`
`1041
`
`1042
`
`1043
`
`PCT Published Application No. WO 02/080975 A1,
`Antineoplastic Combinations such as Rapamycin
`together with Gemcitabine or Fluorouracil, to Gibbons
`et al. (“Gibbons WO ‘975”)
`
`PCT Published Application No. WO 02/098416 A2,
`Antineoplastic Combinations, to Dukart et al. (“Dukart
`WO ‘416”)
`
`U.S. Patent Application Publication No. 2002/0091137
`A1, Use of CCI-779 as anAntineoplastic Agent, which
`published on July 11, 2002, to Dukart (“Dukart ‘137”)
`
`U.S. Patent No. 7,781,446, Use of CCI-779 as an
`Antineoplastic Agent, which issued to Dukart et al. on
`August 24, 2010 (“Dukart ‘446”), and which claims
`priority to U.S. Provisional Patent Application No.
`60/249,077 (“Dukart”)
`
`Perez-Atayde et al., Spectrum of Tumor Angiogenesis
`in the Bone Marrow of Children with Acute
`Lymphoblastic Leukemia, Am. J. Pathol. (1997) 150(3):
`815-821 (“Perez-Atayde”)
`
`True et al., Pathology of Renal Cancers (799-811), in
`Principles and Practice of Genitourinary Oncology
`(Raghavan et al. eds., 1997) (“True”)
`
`Jennings et al., Renal, Perirenal and Ureteral
`Neoplasms (643-694), In Adult and Pediatric Urology;
`Third Edition. (Gillenwater et al. eds., 3rd ed. 1996,
`Volume 1), Grayhack, Howards, and Duckett Eds.
`Mosby-Year Book, Inc. 1996 (“Jennings”)
`
`5
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1044
`
`1045
`
`1046
`
`1047
`
`1048
`
`1049
`
`1050
`
`1051
`
`1052
`
`Robert R. Bahnson, Renal and Urinary Tract
`Neoplasia (371-379), In Primer on Kidney Diseases
`(Greenberg, A. et al. eds., 2nd ed. 1998) (“Bahnson”)
`
`Vézina et al., Rapamycin (AY-22,989), A New
`Antifungal Antibiotic I. Taxonomy of the Producing
`Streptomycete and Isolation of the Active Principle, J.
`Antibiot. (1975) 28 (10): 721-726 (“Vézina”)
`
`Sehgal et al., Rapamycin (AY-22,989), a New
`Antifungal Antibiotic II. Fermentation, Isolation, and
`Characterization, J. Antibiotics (1975) 28(10):727-
`
`Baker et al., Rapamycin (AY-22,989), A New
`Antifungal Antibiotic III. In Vitro and In Vivo
`Evaluation, J. Antibiotics (1978) 31(6): 539-545
`(“Baker”)
`
`U.S. Patent No. 3,929,992 to Sehgal (“Sehgal ‘992
`patent”)
`
`Martel et al. Inhibition of the Immune Response by
`Rapamycin, a New Antifungal Antibiotic, Can. J.
`Physiol. Pharmacol. (1977) 55(1): 48-51 (“Martel”)
`
`Eng et al., Activity of Rapamycin (AY-22,989) against
`Transplanted Tumors, J. Antibiotics (1984) 37(10):
`1231-1237 (“Eng”)
`
`U.S. Patent No. 5,066,493 to Sehgal et al. (“Sehgal
`‘493 patent”)
`
`U.S. Patent No. 5,206,018 to Sehgal et al. (“Sehgal
`‘018 patent”)
`
`6
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1053
`
`1054
`
`1055
`
`1056
`
`1057
`
`1058
`
`1059
`
`1060
`
`Calne et al., Rapamycin for Immunosuppression in
`Organ Allografting, Lancet (1989) 2(8656):227
`(“Calne”)
`
`Morris et al., Identification of a New Pharmacological
`Action for an Old Compound, Med. Sci. Res. (1989)
`17(14): 609-610610 (“Morris 1989”)
`
`Morris, R. N., Rapamycins: Antifungal, Antitumor,
`Antiproliferative, and Immunosuppressive Macrolides,
`Transplantation Reviews (1992) 6(1): 39-87 (“Morris
`1992”)
`
`Van Duyne et al., Atomic Structure of the Rapamycin
`Human Immunophilin FKBP-12 Complex, J. Am.
`Chem. Soc. (1991) 113(19): 7433-7434 (“Van Duyne”)
`
`Choi et al., Structure of the FKBP12-Rapamycin
`Complex Interacting with the Binding Domain of
`Human FRAP, Science (1996) 273(5272): 239-242
`(“Choi”)
`
`Rapamune prescribing information as of August 2000
`
`Garber, K., Rapamycin’s Resurrection: A New Way to
`Target the Cancer Cell Cycle, J Natl Cancer Inst.
`(2001) 93(2): 1517-1519 (“Garber”)
`
`Breitenbach et al., Rapamycin Inhibits Tumor Growth
`and Metastasis in Mice by Antiangiogenesis, Am. J.
`Transplant. (2001) 1 Suppl 1, 250 (Abstr. No.459)
`(“Breitenbach”)
`
`7
`
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`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1061
`
`1062
`
`1063
`
`1064
`
`1065
`
`1066
`
`1067
`
`1068
`
`1069
`
`Guba et al, Rapamycin inhibits Tumor Growth and
`Metastasis by Antiangiogenesis, Chirugicshes Forum
`2001 für experimentelle und klinsche Forschung (2001)
`30: 37-39 (“Guba”)
`
`Hosoi et al., Studies on the Mechanism of Resistance to
`Rapamycin in Human Cancer Cells, Mol. Pharmacol.,
`(1998) 54 815-824 (“Hosoi”)
`
`Zhang et al., Differences in Phosphorylation of the IL-
`2R Associated JAK/STAT Proteins between HTLV-I
`(+), IL-2-independent and IL-2-dependent Cell Lines
`and Uncultured Leukemic Cells from Patients with
`Adult T-cell Lymphoma/Leukemia, Leukemia Res.
`(1999) 23(4): 373-384 (“Zhang”)
`
`Monograph 8288 of The Merck Index, 12th Ed. (2006)
`(“Merck Index”)
`
`U.S. Patent No. 5,260,300 to Hu (“Hu ‘300 patent”)
`
`U.S. Patent No. 5,221,670 to Caufield (“Caufield ‘670
`patent”)
`
`U.S. Patent No. 5,434,260 to Skotnicki et al.
`(“Skotnicki ‘260 patent”)
`
`Freireich et al., Quantitative Comparison of Toxicity of
`Anticancer Agents in Mouse, Rat, Hamster, Dog,
`Monkey, and Man, Cancer Chemotherapy Reports
`(1966) 50(4): 219-244 (“Freireich”)
`
`PRNewswire, August 30, 2000 press release, Novartis
`Announces Positive Trial Results for Two Novel
`Transplantation Drugs (“Press Release”)
`
`8
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`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1070
`
`1071
`
`1072
`
`1073
`
`1074
`
`1075
`
`1076
`
`1077
`
`AFINITOR® approval letter and prescribing
`information, as of March 30, 2009 (“AFINITOR® Mar
`30, 2009 approval”)
`AFINITOR® prescribing information, as of June 14,
`2016 (“AFINITOR® Jun 14, 2016 prescribing
`information”)
`ZORTRESS® approval letter and prescribing
`information, as of April 20, 2010 (“ZORTRESS®
`approval”)
`
`U.S. Patent No. 7,297,703 to Navarro et al. (“Navarro
`‘703 patent”)
`
`International Nonproprietary Names of Pharmaceutical
`Substances (INN), WHO Drug Information, (2000)
`14(3): 183-209 (“Everolimus INN”)
`
`Majewski et al., The Immunosuppresive Macrolide
`RAD inhibits Growth of Human Epstein-Barr Virus-
`transformed B Lymphocytes in vitro and in vivo: A
`Potential Approach to Prevention and Treatment of
`Postrransplant Lymphoproliferative Disorders, Proc.
`Natl. Acad. Sci. (2000) 97(8): 4285-4290 (“Majewski”)
`
`Huang et al., Mechanisms of Resistance to Rapamycin,
`Drug Resistance Updates, (2001) 4: 378-392 (“Huang”)
`
`Beuvink et al., Antitumor Activity of RAD001, an
`Orally Active Rapamycin Derivative, Proc. Amer.
`Assoc. Cancer Res. (2001) 42, 366, Abstr. No. 1972
`(“Beuvink”)
`
`9
`
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`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1078
`
`1079
`
`1080
`
`1081
`
`1082
`
`1083
`
`International Nonproprietary Names of Pharmaceutical
`Substances (INN), WHO Drug Information, (2005)
`19(3): 243-270 (“Temsirolimus INN”)
`
`Wall Street Journal, Drug Progress on Hard-to- Treat
`Cancers is Cited, by Robert Langreth and Michael
`Waldholz in the November 17, 1999 edition
`(“Langreth”)
`
`Hidalgo et al., A Phase I and Pharmacological Study of
`CCI-779, a Rapamycin Ester Cell Cycle Inhibitor, Ann.
`Oncol. (2000) 11 (Suppl. 4) 133, Abstr. No. 606O
`(25th ESMO Congress, October 13-17, 2000 held in
`Hamburg, DE) (“Hidalgo ESMO Abstract”)
`
`December 1, 2000 issue of The Lancet Oncology,CCI-
`779: A New Targeted Anticancer Agent, by Ezzie
`Hutchinson (“Hutchinson”)
`
`Hidalgo et al., Phase I and Pharmacological Study of
`CCI-779, a Cell Cycle Inhibitor, Clinical Cancer
`Research (2000), Supplement 6: 4548s-4549s, Abstr.
`No. 413 (11th NCI-EORTC-AACR November 7-10,
`2000 meeting held in Amsterdam, NL) (“Hidalgo NCI
`Abstract”)
`
`Raymond et al., CCI-779, an ester analogue of
`rapamycin that interacts with PTEN/PI3
`KinasePathways: A Phase I Study utilizing a Weekly
`Intravenous Schedule, Clinical Cancer Res. (2000)
`Supplement 6: 4549s, Abstr. No. 414 (11th NCI-
`EORTC-AACR November 7-10, 2000 meeting held in
`Amsterdam, The Netherlands) (“Raymond NCI
`Abstract”)
`
`10
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`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1084
`
`1085
`
`1086
`
`1087
`
`1088
`
`1089
`
`1090
`
`DeMario et al., Oral Chemotherapy: Rationale and
`Future Directions, J. Clin. Oncol. (1998) 16(7): 2557-
`2567 (“DeMario”)
`
`Gibbons et al., The Effect of CCI-779, a Novel
`Macrolide Anti-Tumor Agent, on the Growth of
`Human Tumor Cells In Vitro and in Nude Mouse
`Xenographs In Vivo, Proc. Amer. Assoc. Cancer Res.
`(1999) 40: 301, Abstr. No. 2000 (“Gibbons Abstract”)
`
`Geoerger et al., Rapamycin analog CCI 779 inhibits
`growth of Human Medulloblastoma Xenographs, Proc.
`Amer. Assoc. Cancer Res. (1999) 40: 603a, Abstr. No.
`3978 (90th Annual Meeting of the AACR, April 10-14,
`1999 held in Philadelphia, PA) (“Geoerger Abstract”)
`
`Geoerger et al., Antitumor Activity of the Rapamycin
`Analog CCI-779 in Human Primitive Neuroectodermal
`Tumor/Medulloblastoma Models as Single Agent and
`in Combination Chemotherapy, Cancer Res. (2001)
`61(4): 1527-1532 (“Geoerger”)
`TORISEL® approval letter and prescribing information,
`as of May 30, 2007 (“TORISEL® Approval”)
`TORISEL® prescribing information, as of July 27,
`2016
`
`Cowan et al., Sirolimus: Mammalian Target of
`Rapamycin Inhibitor to Prevent Kidney Rejection,
`Nephrol. Nursing Journal (2000) 27(6): 623-625
`(“Cowan”)
`
`11
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`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1091
`
`1092
`
`1093
`
`1094
`
`1095
`
`1096
`
`1097
`
`Serkova et al., Tissue Distribution and Clinical
`Monitoring of the Novel Macrolide
`Immunosuppressant SDZ-RAD and its Metabolites in
`Monkey Lung Transplant Recipient: Interaction with
`Cyclosporine, J. Pharmacol. Exper. Therap. (2000)
`294(1): 323-332 (“Serkova”)
`
`U.S. Patent No. 6,432,973, to Zhu et al. (“Zhu ‘973
`patent”)
`
`Neshat et al., Enhanced Sensitivity of PTEN-deficient
`Tumors to Inhibition of FRAP/mTOR, Proc. Natl.
`Acad. Sci. USA (2001) 98(18) 10314-10319
`(“Neshat”)
`
`Podsypanina et al., An Inhibitor of mTOR reduces
`Neoplasia and Normalizes p70/S6 Kinase Activity in
`PTEN+/- Mice, Proc. Natl. Acad. Sci. (2001) 98(18):
`10320-10325 (“Podsypanina”)
`
`Yu et al., Deregulated P13k/AKT/TOR Pathway in
`PTEN-Deficient Tumor Cells Correlates with an
`Increased Growth Inhibition Sensitivity to a TOR
`Kinase Inhibitor CCI-779, Proc. Amer. Assoc. Cancer
`Res. (2001) 42: 802 (Abstr. No. 4305) (“Yu”)
`
`Wen et al., PTEN controls Tumor-induced
`Angiogenesis, Proc. Natl. Acad. Sci. USA (2001)
`98(8): 4622-4627 (92nd Annual Meeting of the AACR,
`March 24-28, 2001 held in New Orleans, LA) (“Wen”)
`
`Cantley et al., New Insights into Tumor Suppression:
`PTEN suppresses Tumor Formation by restraining the
`Phosphoinositide 3-Kinase / AKT Pathway, Proc. Natl.
`Acad. Sci. USA, (1999) 96 (8): 4240-4245 (“Cantley”)
`
`12
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`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1098
`
`1099
`
`1100
`
`1101
`
`1102
`
`1103
`
`1104
`
`1105
`
`Kondo et al., PTEN/MMAC1/TEP1 Mutations in
`Human Primary Renal-Cell Carcinomas and Renal
`Carcinoma Cell Lines, Intl. J. Cancer (2001) 91(2):
`219–224 (“Kondo”)
`
`Morita et al., Common Regions of Deletion on
`Chromosomes 5q, 6q, and 10q in Renal Cell
`Carcinoma, Cancer Res. (1991) 51(21): 5817-5820
`(“Morita”)
`
`Sokoloff et al., Systemic Immunotherapy for
`Genitourinary Neoplasms (869-883), in Principles and
`Practice of Genitourinary Oncology (Raghavan et al.
`eds., 1997) (“Sokoloff”)
`
`Motzer et al., Chemotherapy for Renal Cell Carcinoma
`(885-896) in Principles and Practice of Genitourinary
`Oncology (Raghavan et al. eds., 1997) (“Motzer”)
`NEXAVAR® approval letter and prescribing
`information as of December 1, 2005 (“NEXAVAR®
`approval letter”)
`SUTENT® approval letter and prescribing information
`as of January 26, 2006 (“SUTENT®approval letter”)
`Quinn et al., Renal-Cell Cancer ― Targeting an
`Immune Checkpoint or Multiple Kinases, New England
`J. Med. (2015) 373(19): 1872-1874 (“Quinn”)
`
`Choueiri et al., Cabozantinib versus Everolimus in
`Advanced Renal-Cell Carcinoma, New England
`Journal Med. (2015) 373(19): 1814-1823(“Choueiri”)
`
`13
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`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1106
`
`1107
`
`1108
`
`1109
`
`1110
`
`1111
`
`1112
`
`1113
`
`1114
`
`R. J. Motzer, B. Escudier et al., Nivolumab versus
`Everolimus in Advanced Renal-Cell Carcinoma, New
`England Journal Med. (2015) 373(19): 1803-1813
`(“Escudier”)
`AFINITOR® approval letter and prescribing
`information, as of April 26, 2012 (“AFINITOR® Apr
`26, 2012 approval”)
`
`Kenerson et al., Activated Mammalian Target of
`Rapamycin Pathway in the Pathogenesis of Tuberous
`Sclerosis Complex Renal Tumors, Cancer Research
`(2002) 62(2): 5645-5650 (“Kenerson”)
`
`Bissler et al., Sirolimus for Angiomyolipoma in
`Tuberous Sclerosis Complex or
`Lymphangioleimyomatosis, New Engl. Journal Med.
`(2008) 358(2): 140-151 (“Bissler”)
`
`Henske et al., Tuberous Sclerosis Complex, mTOR,
`and the Kidney: Report of an NIDDK-sponsored
`Workshop, Am J Physiol Renal Physiol. (2014) 306(3):
`F279-F283 (“Henske”)
`
`Kingswood et al., Review of the Tuberous Sclerosis
`Renal Guidelines from the 2012 Consensus
`Conference: Current Data and Future Study, Nephron.
`Clin. Pract. (2016) 134(2) (“Kingswood”)
`
`Declaration of Daniel R. Evans dated January 18, 2018
`
`Morel, Inhibitors of mTOR and FTY 720, Special
`Transcript 2001 (“Morel”)
`
`Program Book for Joint American Transplant Meeting,
`May 11-16, 2001 (“Transplant 2001 Program Book”)
`
`14
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1115
`
`1116
`
`1117
`
`1118
`
`1119
`
`1120
`
`1121
`
`1122
`
`Luan et al., Sirolimus Prevents Tumor Progressions:
`mTOR Targeting for the Inhibition of Neapolastic
`Progression, American Journal of Transplantation,
`Sup. 1, Vol.1, Abstract 428, Chicago, May 11-16,2001
`(“Luan Abstract”)
`
`ISO 26324, Information and documentation – Digital
`object identifier system, 1st Ed. 2012-05-01 (“ISO
`26324”)
`
`The DOI Foundation and Wiley Online Library
`webpages
`
`Declaration of Terrence L. Stokke dated January 18,
`2018
`
`Declaration of Fu L. Luan, M.D., dated January 19,
`2018
`
`List of exhibits with paragraph citations
`
`Shrinkage table showing results of the Weckbecker in
`vivo assay (page 128 from Ex. 2092 marked as Burris
`Depo Ex. 1121) (“Shrinkage Table”)
`
`O’Donnell et al., Phase I Pharmacokinetic and
`Pharmacodynamic Study of the Oral Mammalian
`Target of Rapamycin Inhibitor Everolimus in Patients
`with Advanced Solid Tumors, Journal of Clinical
`Ongology, 2:6(10)1588-1595, April 1, 2008 (marked as
`Burris Depo Ex. 1122) (“O’Donnell”)
`
`15
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1123
`
`1124
`
`1125
`
`1126
`
`1127
`
`1128
`
`1129
`
`1130
`
`1131
`
`O’Reilly et al., In vivo activity of RAD001, an orally
`active rapamycin derivative, in experimental tumor
`models, Proceedings AACR, 93rd Annual Meeting,
`43:71 Abstract #359, March 2002 (marked as Burris
`Depo Ex. 1123) (“O’Reilly”)
`
`Pages from US Patent 6,432,973 Zhu (pages from
`Exhibit 1092 marked as Burris Depo Ex. 1124)
`
`Pages from Zhu ‘973 patent provisional application
`(pages from Exhibit 1092 marked as Burris Depo Ex.
`1125)
`
`Transcript (updated) of deposition of Howard A. Burris
`taken May 24, 2018 in this action (“Burris Tr.”)
`
`Transcript (updated) of deposition of Krishna V.
`Komanduri taken June 5, 2018 in this action
`(“Komanduri Tr.”)
`
`Burris Trial Demonstratives (“Burris First Trial
`Demonstratives”)
`
`Dr. Burris’ First Everolimus Trial Testimony, Novartis
`v. Breckenridge, 14cv1043, Trial Transcript, DI No.
`166 (“Burris First Trial Testimony”)
`
`Dr. Burris Second Trial Testimony, Novartis v. West-
`Ward, 15cv-474, Trial Transcript, DI No. 98 (“Burris
`Second Trial Testimony”)
`
`Alexandre et al., Phase I Study of CCI-779, a novel
`rapamycin analog: preliminary results, Proc. Am.
`Assoc. Cancer Res. (2000) 41: 613 (Abst. No. 3897).
`(“Alexandre AACR Abstract”)
`
`16
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1132
`
`1133
`
`1134
`
`1135
`
`1136
`
`1137
`
`1138
`
`1139
`
`Alley et al., Feasability of Drug Screening with Panels
`of Human Tumor Cell Lines Using a Microculture
`Tetrazolium Assay, Cancer Res. (1988) 45(3): 589-601
`(“Alley”)
`
`WO 93/19752 A1, Inhibition of P70 S6 Kinase, to
`Beirer et al. (“Beirer”)
`
`Boyd et al., Some Practical Considerations and
`Applications of the National Cancer Institute In Vitro
`Anticancer Drug Discovery Screen, Drug. Dev. Res.
`(1995) 34(2): 91-109 (“Boyd”)
`
`Fairlamb et al., Spontaneous Regression of Metastases
`of Renal Cancer, Cancer (1981) 47(8): 2102-2106
`(“Fairlamb”)
`
`Fiebig et al., In vitro and in vivo evaluation of US- NCI
`compounds in human tumor xenografts, Cancer
`Treatment Reviews (1990) 17(2-3): 109-117 (“Fiebig”)
`
`Gonzalez-Angulo, Weekly nab-Rapamycin in Patients
`with Advanced Nonhematologic Malignancies: Final
`Results of a Phase I Trial, Clin. Cancer Res. (2013)
`19(19): 5474-5484 (“Gonzalez- Angulo”)
`
`European Patent Application EP 0 525 960 A1, Use of
`rapamycin for the treatment of adult T-cell leukemia,
`which published on February 3, 1993 to Miller et al.
`(“Miller EP ‘960”)
`
`Monks et al., Feasibility of a High-Flux Anticancer
`Drug Screen Using a Diverse Panel of Cultured
`Human Tumor Cell Lines, J. Natl. Cancer Inst. (1991)
`83(11): 757-766 (“Monks”)
`
`17
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1140
`
`1141
`
`1142
`
`1143
`
`1144
`
`1145
`
`1146
`
`1147
`
`1148
`
`Pantuck et al., Prognostic Relevance of the mTOR
`Pathway in Renal Cell Carcinoma, Cancer (2007)
`109(11): 2257-2267 (“Pantuck 2007”)
`
`Paull et al., Identification of Novel Antimitotic Agents
`Acting at the Tubulin Level by Computer- assisted
`Evaluation of Differential Cytotoxic Data, Cancer Res.
`(1992) 52(14): 3892-3900 (“Paull”)
`
`Price et al., Rapamycin-Induced Inhibition of the 70-
`Kilodalton S6 Protein Kinase, Science (1992)
`257(5072): 973-977 (“Price”)
`
`PTE Request for Cottens ‘772 Patent (“PTE Request”)
`
`Raymond et al., Safety and Pharmacokinetics of
`Escalated Doses of Weekly Intravenous Infusion of
`CCI-779, a Novel mTOR Inhibitor, in Patients With
`Cancer, J. Clin. Oncol. (2004) 22(12): 2336-
`2347(“Raymond 2004”)
`
`Raymond et al., CCI-779, a Rapamycin Analog with
`Antitumor Activity: A Phase I Study Utilizing a Weekly
`Schedule, Proc. Amer. Soc. Clin. Oncol. (2000) 19:
`187a (Abst. No. 728) (“Raymond ASCO Abstract”)
`
`Retain, M.J., Phase II Oncology Trials: Let’s Be
`Positive, Clin. Cancer Res. (2005) 11(16): 5661-5663
`(“Retain”)
`
`Ribomustin (2001) Product Monograph (“Ribomustin
`Label”)
`
`Robins, P., Poster Highlights I, Drugs (1999) 2(6):
`534-537 (“Robins”)
`
`18
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1149
`
`1150
`
`1151
`
`1152
`
`1153
`
`1154
`
`1155
`
`1156
`
`1157
`
`Sausville, E. A., New Agents – Noncytotoxins,
`Antiangiogenesis, ASCO Educational Book (1998)
`112-117 (“Sausville”)
`
`Rapamycin_Tumor or Cancer (1980-2002) (“SciFinder
`Search Results”)
`
`Stinson et al., Morphological and Immunocytochemical
`Characteristics of Human Tumor Cell Lines for Use in
`a Disease-Oriented Anticancer Drug Screen,
`Anticancer Res. (1992) 12(4): 1035-1053 (“Stinson”)
`
`U.S. Patent No. 6,362,164, Combination of a
`Somatostatin Analogue and a Rapamycin,
`to
`Weckbecker (“Weckbecker ‘164 patent”)
`
`U.S. Patent Application No. 09/194,957 file wrapper
`(“Weckbecker application”)
`
`Wyeth’s EP 0 763 039 A1, which is a European
`counterpart of the Skotnicki ‘718 patent related to
`rapamycin hydroxyesters, i.e., temsirolimus (“Wyeth’s
`EP ‘039”)
`
`Wyeth’s May 11, 2000 letter filed in the EP ‘671
`application by Wyeth in European Patent Application
`No. 95915671.2 (“Wyeth’s May 11, 2000 letter filed in
`the EP ‘671 application”)
`A-498 ATCC® HTB-44 (human kidney cell line)
`(“HTB-44-A498”)
`
`December 15, 2000, press release by Caprius
`(“December 15, 2000 press release”)
`
`19
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`Exhibit Number
`
`Exhibit Description
`
`1158
`
`1159
`
`1160
`
`1161
`
`1162
`
`ACHN ATCC ® CRL-1611 (human kidney cell line)
`(“CRL-1611-ACHN”)
`
`Second Declaration of Allan J. Pantuck, M.D. in
`support of Inter Partes Review of U.S. Patent
`8,410,131
`
`File history of U.S. Patent Application No. 13/546,686
`(“13/546,686 file history”)
`
`MPEP 2136.003.III (“MPEP 2136.003.III”)
`
`Declaration In Support Of Petitioner West-Ward’s
`Motion For Pro Hac Vice Admission Of Michael B.
`Cottler Under 37 C.F.R. § 42.10
`
`
`
`
`
`
`
`
`
`
`20
`
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`
`
`
`
`
`
`
`
`
`
`Case No. IPR2017-01592
`U.S. Patent No. 8,410,131
`
`CERTIFICATE OF SERVICE
`
`The undersigned hereby certifies that the foregoing Petitioner’s Updated
`
`Exhibit List Dated August 10, 2018 was served on August 10, 2018, upon the
`
`following parties via email:
`
`Nicholas N. Kallas
`Laura K. Fishwick
`Fitzpatrick, Cella, Harper & Scinto
`nkallas@fchs.com
`lfishwick@fchs.com
`ZortressAfinitorIPR@fchs.com
`
`
`
`
`
`
`
`
`
`Dated: August 10, 2018
`
`
`
`
`Respectfully submitted,
`
`By: /Marta E. Delsignore/
`
`Marta E. Delsignore (Reg. No. 32,689)
`GOODWIN PROCTER LLP
`620 Eighth Avenue
`New York, NY 10018
`212-813-8822
`mdelsignore@goodwinprocter.com
`
`Counsel for Petitioner West-Ward
`Pharmaceuticals International Limited
`
`
`
`
`21
`
`
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