List of Exhibits with Paragraph Citations
`
`Citation (Para.
`Nos.)
`
`1, 31-38, 40-45, 68,
`69, 71, 74, 76, 77,
`80, 84, 86, 92, 137,
`145, 168, 240, 241,
`242, 252, 255, 258-
`260, 281-283
`
`60, 105, 111, 195-
`217, 225, 227, 228,
`236, 237, 239, 243-
`257, 261-266, 268-
`276, 278, 279
`
`109, 218-224, 226,
`227, 232-234, 237,
`266, 267, 270-274,
`279, 280, 300-303,
`307
`
`30, 120, 158-162,
`228, 230, 231, 234,
`235, 237, 274, 276,
`278-280, 291, 292,
`296-298, 302, 303,
`305, 307
`
`100, 190-192, 194,
`228, 235, 237, 274,
`276-279, 303, 304,
`306, 307
`
`98, 116, 120, 178-
`189, 229, 230, 234,
`235, 237, 280, 284-
`287, 290, 291, 293,
`295, 297, 298, 302,
`303, 306, 307,
`
`114, 115, 172-177,
`229, 230, 234, 235,
`237, 280, 288-291,
`295, 297-298, 302,
`303, 307
`
`Exhibit Description
`
`U.S. Patent No. 8,410,131 ("the '131 patent")
`
`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-
`1
`
`Exhibit
`Name
`Number
`
`'131 Patent
`1001
`
`Wasik
`1002
`
`Navarro
`1003
`
`Crowe
`1004
`
`Luan
`1005
`
`Hidalgo
`1006
`
`Alexandre
`1007
`
`
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`
`Citation (Para.
`Nos.)
`
`Exhibit Description
`
`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")
`
`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
`
`
`2015 Orange Book,"35th Edition (2015) with
`respect to AFINITOR® ("2015 Orange
`Book")
`International Patent Application No.
`PCT/EP02/01714 ("the '714 PCT
`Application")
`AFINITOR® approval letter and prescribing
`information, as of April 26, 2012
`("AFINITOR® Apr 26, 2012 approval")
`
`AFINITOR® prescribing information, as of
`June 14, 2016 ("AFINITOR® Jun 14, 2016
`prescribing information")
`
`26, 29, 30, 104, 110,
`119, 120, 149-157,
`160, 185, 198, 228,
`230, 231, 234, 235,
`237, 276, 280, 291,
`292, 296-298, 302,
`303, 305, 307
`
`106, 163-171, 232-
`234, 237, 280, 294,
`297-299, 301-303,
`307
`
`
`N/A
`
`
`
`23 (n. 2), 109 (n. 5)
`
`16
`
`142
`
`107
`
`Schuler
`1008
`
`Neumayer
`1009
`
`
`
`Pantuck
`Declaration
`1010
`
`
`2015 Orange
`Book
`1029
`'714 PCT
`Application
`1014
`AFINITOR®
`Apr 26, 2012
`approval
`1107
`AFINITOR® Jun
`14, 2016
`prescribing
`information
`1071
`AFINITOR®
`Mar 30, 2009
`approval
`1070
`
`
`
`107, 140
`
`AFINITOR® approval letter and prescribing
`information, as of March 30, 2009
`("AFINITOR® Mar 30, 2009 approval")
`
`2
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`Alexandre and
`Raymond
`1030
`
`Citation (Para.
`Nos.)
`
`25, 27, 29, 113
`
`Bahnson
`1044
`
`88, 123, 127, 128,
`130, 132,
`
`Baker
`1047
`
`Beuvink
`1077
`
`Bissler
`1109
`
`Boni
`1031
`
`95
`
`111
`
`141
`
`29, 114, 119
`
`Breitenbach
`1060
`
`Calne
`1053
`
`100
`
`97
`
`Cantley
`1097
`
`122, 122 (n. 8), 184
`(n. 14), 186
`
`Caufield '670
`patent
`
`102, 155 (n. 9)
`
`
`
`Exhibit Description
`
`Alexandre, Raymond, et al., La rapamycine
`et le CCI-779, Bull. Cancer (1999) 86(10):
`808-811 ("Alexandre and Raymond")
`Robert R. Bahnson, Renal and Urinary Tract
`Neoplasia (371-379), In Primer on Kidney
`Diseases (Greenberg, A. et al. eds., 2nd ed.
`1998) ("Bahnson")
`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")
`Beuvink et al., Antitumor Activity of
`RAD001, an Orally Active Rapamycin
`Derivative, Proc. Amer. Assoc. Cancer Res.
`(2001) 42, 366, Abstr. No. 1972 ("Beuvink")
`Bissler et al., Sirolimus for Angiomyolipoma
`in Tuberous Sclerosis Complex or
`Lymphangioleimyomatosis, New Engl.
`Journal Med. (2008) 358(2): 140-151
`("Bissler")
`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")
`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")
`Calne et al., Rapamycin for
`Immunosuppression in Organ Allografting,
`Lancet (1989) 2(8656): 227 ("Calne")
`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")
`U.S. Patent No. 5,221,670 to Caufield
`("Caufield '670 patent")
`3
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Citation (Para.
`Nos.)
`
`Exhibit Description
`
`Choi et al., Structure of the FKBP12-
`Rapamycin Complex Interacting with the
`Binding Domain of Human FRAP, Science
`(1996) 273(5272): 239-242 ("Choi")
`Choueiri et al., Cabozantinib versus
`Everolimus in Advanced Renal-Cell
`Carcinoma, New England Journal Med.
`(2015) 373(19): 1814-1823 ("Choueiri")
`
`U.S. Patent No. 5,665,772 to Cottens et al.
`("Cottens '772 patent")
`
`Published Application No. WO 94/09010 A1,
`O-Alkylated Rapamycin Derivatives and their
`use, particularly as immunosuppressants, to
`Cottens et al. ("Cottens WO '010")
`Cowan et al., Sirolimus: Mammalian Target
`of Rapamycin Inhibitor to Prevent Kidney
`Rejection, Nephrol. Nursing Journal (2000)
`27(6): 623-625 ("Cowan")
`Dancey, J. E., Rapamycin-Sensitive Signal-
`Transduction Pathways: Protein Translation
`Control of Cell Proliferation, ASCO
`Educational Book (2000) 68-75 ("Dancey")
`DeMario et al., Oral Chemotherapy:
`Rationale and Future Directions, J. Clin.
`Oncol. (1998) 16(7): 2557-2567 ("DeMario")
`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")
`PCT Published Application No. WO
`02/40000 A2, Use of CCI-779 as an
`Antineoplastic Agent, to Dukart et al.
`("Dukart WO '000")
`U.S. Patent Application Publication No.
`2002/0091137 A1, Use of CCI-779 as an
`Antineoplastic 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
`
`4
`
`Exhibit
`Name
`Number
`1066
`
`Choi
`1057
`
`Choueiri
`1105
`
`Cottens '772
`patent
`1019
`
`Cottens WO '010
`1026
`
`Cowan
`1090
`
`Dancey
`1016
`
`DeMario
`1084
`
`Dinney
`1032
`
`98
`
`141
`
`23, 26, 27, 28, 32,
`47, 99, 100, 102,
`103, 110, 198
`
`47, 53, 54, 58, 59,
`103, 110, 198, 211,
`217, 223, 247
`
`120
`
`98, 120
`
`115
`
`39, 123, 126, 136,
`138, 214 (n. 16), 244
`(n. 21)
`
`Dukart WO '000
`1036
`
`61, 62, 63
`
`63
`
`63 and 63 (n. 3)
`
`Dukart '137
`1039
`
`Dukart
`Dukart '446
`
`
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Citation (Para.
`Nos.)
`
`Exhibit Description
`
`Exhibit
`Name
`Number
`Dukart
`Provisional
`1040
`Dukart WO '416
`1038
`
`61, 62, 63
`
`'446"), and which claims priority to U.S.
`Provisional Patent Application No.
`60/249,077 ("Dukart Provisional")
`PCT Published Application No. WO
`02/098416 A2, Antineoplastic Combinations,
`to Dukart et al. ("Dukart WO '416")
`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")
`Eng et al., Activity of Rapamycin (AY-22,989)
`against Transplanted Tumors, J. Antibiotics
`(1984) 37(10): 1231-1237 ("Eng")
`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")
`International Nonproprietary Names of
`Pharmaceutical Substances (INN), WHO
`Drug Information, (2000) 14(3): 183-209
`("Everolimus INN")
`Flowcharts for 35 U.S.C. § 102(e) Dates
`("102(e) Date Flowchart")
`Fosså et al., Survival of Patients with
`Advanced Urothelial Cancer treated with
`Cisplatin-based Chemotherapy, Brit. J.
`Cancer (1996) 74: 1655-1659 ("Fosså")
`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")
`Garber, K., Rapamycin's Resurrection: A
`New Way to Target the Cancer Cell Cycle, J
`Natl Cancer Inst. (2001) 93(2): 1517-1519
`("Garber")
`Great Britain patent application (GB
`0104072.4, "GB '072" or "the '072 priority
`application"), filed on February 19, 2001
`
`Dukart '923
`1024
`
`63
`
`Eng
`1050
`
`Escudier
`1106
`
`Everolimus INN
`1074
`
`Flowchart
`1025
`
`Fosså
`1034
`
`Freireich
`1068
`
`Garber
`1059
`
`96, 100
`
`141
`
`110
`
`63
`
`53, 55
`
`105 (n. 4), 202
`
`100
`
`GB '072 priority
`application (or
`GB '072)
`1012
`
`16, 143, 144, 147
`
`
`
`5
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`GB '957 priority
`application (or
`GB '957)
`1013
`
`Citation (Para.
`Nos.)
`
`16, 143, 144, 147
`
`Geoerger
`1087
`
`117
`
`Geoerger
`Abstract
`1086
`
`117
`
`61, 62, 63
`
`63
`
`117
`
`100
`
`142
`
`Gibbons WO
`'975
`1037
`
`Gibbons '239
`1023
`
`
`Gibbons
`Abstract
`1085
`
`Guba
`1061
`
`Henske
`1110
`
`
`
`Exhibit Description
`
`Great Britain patent application
`(GB0124957.2, "GB '957" or "the '957
`priority application"), filed on October 17,
`2001
`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")
`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")
`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")
`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")
`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")
`Guba et al, Rapamycin inhibits Tumor
`Growth and Metastasis by Antiangiogenesis,
`Chirugicshes Forum 2001 für experimentelle
`und klinsche Forschung (2001) 30: 37-39
`("Guba")
`Henske et al., Tuberous Sclerosis Complex,
`mTOR, and the Kidney: Report of an
`NIDDK-sponsored Workshop, Am J Physiol
`
`6
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`
`Citation (Para.
`Nos.)
`
`Hidalgo ESMO
`Abstract
`1080
`
`114, 115
`
`Hidalgo NCI
`Abstract
`1082
`
`Hosoi
`1062
`
`Hu '300 patent
`1065
`Huang
`1076
`
`Hutchinson
`1081
`
`114
`
`101
`
`102, 155 (n. 9)
`
`110, 111, 117, 120
`
`114, 115, 122, 186
`
`IPR Final Rules
`1015
`
`N/A
`
`Jennings
`1043
`
`73, 88, 123, 125,
`127-129, 131, 134,
`146,
`
`Kenerson
`1108
`
`142
`
`Exhibit Description
`
`Renal Physiol. (2014) 306(3): F279-F283
`("Henske")
`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")
`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")
`Hosoi et al., Studies on the Mechanism of
`Resistance to Rapamycin in Human Cancer
`Cells, Mol. Pharmacol., (1998) 54 815-824
`("Hosoi")
`U.S. Patent No. 5,260,300 to Hu ("Hu '300
`patent")
`Huang et al., Mechanisms of Resistance to
`Rapamycin, Drug Resistance Updates, (2001)
`4: 378-392 ("Huang")
`December 1, 2000 issue of The Lancet
`Oncology, CCI-779: A New Targeted
`Anticancer Agent, by Ezzie Hutchinson
`("Hutchinson")
`IPR Final Rules
`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")
`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")
`
`
`
`7
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`
`Citation (Para.
`Nos.)
`
`Kingswood
`1111
`
`142
`
`Kondo
`1098
`
`Langreth
`1079
`
`186, 122
`
`114, 115, 229 (n. 19)
`
`Majewski
`1075
`
`110, 111
`
`96
`
`46, 47, 211, 217,
`247
`
`101
`
`122, 186
`
`97
`
`97
`
`Martel
`1049
`
`May 10, 2010
`Amendment
`1027
`Merck Index
`1064
`
`Morita
`1099
`
`Morris 1989
`1054
`
`Morris 1992
`1055
`
`
`
`Exhibit Description
`
`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")
`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")
`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")
`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")
`Martel et al. Inhibition of the Immune
`Response by Rapamycin, a New Antifungal
`Antibiotic, Can. J. Physiol. Pharmacol. (1977)
`55(1): 48-51 ("Martel")
`Selected portions of Prosecution History
`Documents ("May 10, 2010 Amendment re.
`Cottens WO '010")
`Monograph 8288 of The Merck Index, 12th
`Ed. (2006) ("Merck Index")
`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")
`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,
`
`8
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`
`Citation (Para.
`Nos.)
`
`Motzer
`1101
`
`123, 134
`
`Motzer et al.
`1035
`
`Navarro '703
`patent
`1073
`
`Neshat
`1093
`
`NEXAVAR®
`approval letter
`1102
`Pantuck C.V.
`1028
`
`57
`
`109
`
`122, 186
`
`140
`
`8
`
`Perez-Atayde
`1041
`
`72, 123
`
`Podsypanina
`1094
`
`122, 186
`
`Press Release
`1069
`
`106, 110, 164 (n.
`10),
`
`Quinn
`1104
`
`141
`
`RAPAMUNE®
`(sirolimus) Oral
`Solution
`
`24, 95, 99, 181 (n.
`13), 230,
`
`
`
`Exhibit Description
`
`Transplantation Reviews (1992) 6(1): 39-87
`("Morris 1992")
`Motzer et al., Chemotherapy for Renal Cell
`Carcinoma (885-896) in Principles and
`Practice of Genitourinary Oncology
`(Raghavan et al. eds., 1997) ("Motzer")
`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.")
`U.S. Patent No. 7,297,703 to Navarro et al.
`("Navarro '703 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")
`NEXAVAR® approval letter and prescribing
`information as of December 1, 2005
`("NEXAVAR® approval letter")
`Curriculum Vitae of Allan J. Pantuck, M.D.
`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")
`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")
`PRNewswire, August 30, 2000 press release,
`Novartis Announces Positive Trial Results for
`Two Novel Transplantation Drugs ("Press
`Release")
`Quinn et al., Renal-Cell Cancer ― Targeting
`an Immune Checkpoint or Multiple Kinases,
`New England J. Med. (2015) 373(19): 1872-
`1874 ("Quinn")
`RAPAMUNE® (sirolimus) Oral Solution
`RAPAMUNE® Approval Letter and
`approved labeling
`
`9
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Citation (Para.
`Nos.)
`
`Exhibit Description
`
`Exhibit
`Name
`Number
`1011
`
`Raymond NCI
`Abstract
`1083
`
`114
`
`Sedrani
`1020
`
`Sehgal
`1046
`
`Sehgal '018
`patent
`1052
`Sehgal '493
`patent
`1051
`Sehgal '992
`patent
`1048
`
`Serkova
`1091
`
`26, 30, 104, 106,
`120, 156, 185, 198
`
`95
`
`96, 100
`
`96, 100
`
`95
`
`120
`
`Shi
`1033
`
`Skotnicki '260
`patent
`1067
`
`53, 54, 58, 59
`
`102, 155 (n. 9)
`
`Raymond et al., CCI-779, an ester analogue
`of rapamycin that interacts with PTEN/PI3
`Kinase Pathways: 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")
`Sedrani et al., Chemical Modification of
`Rapamycin: The Discovery of SDZ RAD,
`Transplantation Proc. (1998) 30(5): 2192-
`2194 ("Sedrani")
`Sehgal et al., Rapamycin (AY-22,989), a New
`Antifungal Antibiotic II. Fermentation,
`Isolation, and Characterization, J.
`Antibiotics (1975) 28(10): 727-732
`("Sehgal")
`U.S. Patent No. 5,206,018 to Sehgal et al.
`("Sehgal '018 patent")
`
`U.S. Patent No. 5,066,493 to Sehgal et al.
`("Sehgal '493 patent")
`
`U.S. Patent No. 3,929,992 to Sehgal ("Sehgal
`'992 patent")
`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")
`Shi et al., Rapamycin enhances Apoptosis
`and Increases Sensitivity to Cisplatin in
`Vitro, Cancer Research (1995) 55(9): 1982-
`1988 ("Shi")
`U.S. Patent No. 5,434,260 to Skotnicki et al.
`("Skotnicki '260 patent")
`
`10
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`Skotnicki '718
`patent
`1018
`
`Citation (Para.
`Nos.)
`
`36, 102, 112, 155 (n.
`9)
`
`Sokoloff
`1100
`
`123, 134
`
`Sorbera
`1017
`SUTENT®
`approval letter
`1103
`Temsirolimus
`INN
`1078
`TORISEL®
`Approval (2007)
`1088
`TORISEL®
`prescribing
`information, as
`of July 27, 2016
`1089
`
`26, 27, 30, 102, 110,
`120
`
`140
`
`113
`
`118, 140
`
`118
`
`True
`1042
`
`72, 123, 124, 126,
`128-130, 146
`
`Van Duyne
`1056
`
`98, 141
`
`Vézina
`1045
`
`Weckbecker
`1021
`
`95
`
`105
`
`
`
`Exhibit Description
`
`U.S. Patent No. 5,362,718, to Skotnicki et al.
`("Skotnicki '718 patent")
`Sokoloff et al., Systemic Immunotherapy for
`Genitourinary Neoplasms (869-883), in
`Principles and Practice of Genitourinary
`Oncology (Raghavan et al. eds., 1997)
`("Sokoloff")
`Sorbera et al, SDZ-RAD, Drugs of the Future
`(1999) 24(1): 22-29 ("Sorbera")
`SUTENT® approval letter and prescribing
`information as of January 26, 2006
`("SUTENT® approval letter")
`International Nonproprietary Names of
`Pharmaceutical Substances (INN), WHO
`Drug Information, (2005) 19(3): 243-270
`("Temsirolimus INN")
`TORISEL® approval letter and prescribing
`information, as of May 30, 2007
`("TORISEL® Approval")
`
`TORISEL® prescribing information, as of
`July 27, 2016
`
`True et al., Pathology of Renal Cancers (799-
`811), in Principles and Practice of
`Genitourinary Oncology (Raghavan et al.
`eds., 1997) ("True")
`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")
`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")
`PCT Published Application No. WO
`97/47317 A1, Combination of a Somatostatin
`Analogue and a Rapamycin, to G.
`Weckbecker ("Weckbecker")
`
`11
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`

`

`List of Exhibits with Paragraph Citations
`
`Exhibit
`Name
`Number
`
`Citation (Para.
`Nos.)
`
`Wen
`1096
`
`Yu
`1095
`
`122, 186
`
`122, 186
`
`Zhang
`1063
`
`101, 111, 199
`
`Zhu '547 patent
`1022
`
`121
`
`Zhu '973 patent
`1092
`
`121
`
`ZORTRESS®
`approval
`1072
`
`
`108
`
`Exhibit Description
`
`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")
`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")
`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")
`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 No. 6,432,973, Water Soluble
`Rapamycin Esters, which issued to Zhu et al.
`on August 13, 2002 from U.S. Provisional
`Patent Application No. 60/233,776, filed on
`September 19, 2000 ("Zhu '973 patent")
`ZORTRESS® approval letter and prescribing
`information, as of April 20, 2010
`("ZORTRESS® approval")
`
`
`
`12
`
`Breckenridge Exhibit 1120
`List of Exhibits with Paragraph Citations to Dr. Pantuck's Declaration
`Breckenridge v. Novartis IPR2017-01592
`
`