IPR2021-00816
`U.S. Patent No. 9,220,631
`
`UNITED STATES PATENT AND TRADEMARK OFFICE
`______________________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`______________________
`
`REGENERON PHARMACEUTICALS, INC.,
`Petitioner,
`
`v.
`
`NOVARTIS PHARMA AG,
`NOVARTIS TECHNOLOGY LLC,
`NOVARTIS PHARMACEUTICALS CORPORATION,
`Patent Owner.
`______________________
`
`Case No. IPR2021-00816
`U.S. Patent No. 9,220,631
`______________________
`
`PETITIONER’S FIRST SUPPLEMENTAL EXHIBIT LIST
`
`
`
`
`
`
`
`

`

`Petitioner Regeneron Pharmaceuticals, Inc. submits this First Supplemental
`
`IPR2021-00816
`U.S. Patent No. 9,220,631
`
`
`
`
`Exhibit List with Petitioner’s Notice of Supplemental Evidence pursuant to 37
`
`C.F.R. § 42.63(e):
`
`Ex.
`1001
`
`Ex.
`1002
`
`Ex.
`1003
`
`Ex.
`1004
`
`Ex.
`1005
`
`Ex.
`1006
`
`U.S. Patent No. 9,220,631 (“the ’631 Patent”)
`
`Prosecution File History of U.S. Patent No. 9,220,631
`
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`
`Curriculum Vitae of Horst Koller
`
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`
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`
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`
`Ex.
`1010
`
`ITC Investigation No. 337-TA-1207, Initial Determination Terminating
`the Investigation
`
`
`
`1
`
`

`

`IPR2021-00816
`U.S. Patent No. 9,220,631
`
`Ex.
`1011
`
`Ex.
`1012
`
`Ex.
`1013
`
`Ex.
`1014
`
`Ex.
`1015
`
`Ex.
`1016
`
`Ex.
`1017
`
`Ex.
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`
`Ex.
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`
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`
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`
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`
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`
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`
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`
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`
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`
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`
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`
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`
`
`
`2
`
`

`

`IPR2021-00816
`U.S. Patent No. 9,220,631
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`Ex.
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`
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`1026
`
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`
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`
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`
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`
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`Prescribing Information, (June 2010) (“Lucentis Label”)
`
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`
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`
`Declaration of Dr. Szilard Kiss under 37 C.F.R. § 1.68.
`
`Curriculum Vitae of Dr. Szilard Kiss
`
`Declaration of James L. Mullins, Ph.D.
`
`Dow Corning® 365 35% Dimethicone NF Emulsion – Frequently
`Asked Questions (2002) (“DC365 FAQ”)
`
`3
`
`Ex.
`1031
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`Ex.
`1032
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`Ex.
`1033
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`Ex.
`1034
`
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`

`

`IPR2021-00816
`U.S. Patent No. 9,220,631
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`European Patent Application No. 12174860 to Novartis AG
`
`U.S. Food and Drug Administration, Guidance for Industry: Sterile
`Drug Products Produced by Aseptic Processing—Current Good
`Manufacturing Practice (September 2004)
`
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`
`Internet Archive WayBack Machine, March 8, 2011 Record of
`Drugs.com, Welcome to Drugs.com, available at
`https://web.archive.org/web/20110308203650/http://www.drugs.com:
`80/
`
`Internet Archive WayBack Machine, February 25, 2011 Record of
`Drugs.com, FDA Professional Drug Information, available at
`https://web.archive.org/web/20110225193929/http://www.drugs.com:
`80/pro/
`
`U.S. Food and Drug Administration, Eylea® Highlights of the
`Prescribing Information, (November 2011) (“Eylea label”)
`
`U.S. Food and Drug Administration, Guidance for Industry: Container
`Closure Systems for Packaging Human and Biologics – Chemistry,
`Manufacturing, and Controls Documentation (May 1999), available at
`https://www.fda.gov/downloads/drugs/guidances/ucm070551.pdf
`International Standard ISO-7864, Sterile hypodermic needles for single
`use, ISO 7864:1993(E) (“ISO-7864”)
`
`International Standard ISO-9626, Stainless steel needle tubing for the
`manufacture of medical devices – Amendment 1, ISO
`9626:1991/Amd.1:2001(E) (“ISO-9626”)
`Advait Badkar, et al. Development of Biotechnology Products in Pre-
`filled Syringes: Technical Considerations and Approaches, American
`Association of Pharmaceutical Sciences, June 2011, 12(2): 564-572
`(“Badkar”)
`William Leventon, “Medical Device Sterilization: What Manufacturers
`Need to Know” (MDDI online, Sept. 1, 2002), available at
`https://www.mddionline.com/medical-device-sterilization-what-
`manufacturers-need-know (“Leventon”)
`4
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`Ex.
`1035
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`Ex.
`1036
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`Ex.
`1037
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`Ex.
`1038
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`Ex.
`1039
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`Ex.
`1040
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`Ex.
`1041
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`Ex.
`1042
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`Ex.
`1043
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`Ex.
`1044
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`Ex.
`1045
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`

`

`IPR2021-00816
`U.S. Patent No. 9,220,631
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`Ex.
`1046
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`Ex.
`1047
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`Ex.
`1048
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`Ex.
`1049
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`Ex.
`1050
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`Ex.
`1051
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`Ex.
`1052
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`Ex.
`1053
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`Ex.
`1054
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`Ex.
`1055
`
`Ex.
`1056
`
`Pamela Carter, et al. The lowdown on low temperature sterilization for
`packaged devices, Healthcare Purchasing News, July 2008, 42-45.
`(“Carter”)
`U.S. Patent Publication No. 2005/0182370 to Hato (“Hato”)
`
`U.S. Department of Labor, Occupational Safety & Health
`Administration, Ethylene Oxide (EtO): Understanding OSHA’s
`Exposure monitoring Requirements, 2007 OSHA3325-01N (2007),
`available at https://www.osha.gov/Publications/ethylene_oxide.html
`(“OSHA Guidelines”)
`Bryon Lambert, et al. Radiation and Ethylene Oxide Terminal
`Sterilization Experiences with Drug Eluting Stent Products, American
`Association of Pharmaceutical Sciences, December 2011, 12(4):1116-
`1126 (“Lambert”)
`IPR2020-1317, Paper No. 10, Patent Owner’s Preliminary Response
`
`IPR2020-1317, Paper No. 14, Patent Owner’s Sur-Reply
`
`
`John R. Gillis & Gregg Mosley, Validation of Pharmaceutical
`Processes, Chapter 16 – Validation of Ethylene Oxide Sterilization
`Processes (2011), pp.241-262 (“Gillis”)
`FDA Pesticide Analytical Manual Vol. 1, Chapter 6 - HPLC, available
`at
`https://www.fda.gov/downloads/Food/FoodScienceResearch/
`ucm113651.pdf
`Kim, Leo & D’Amore, Patricia, ASIP Centennial Commentary – A
`Brief History of Anti-VEGF for the Treatment of Ocular Angiogenesis,
`The American Journal of Pathology, August 2012 182(2):376-379,
`available at (note: published online July 2, 2012
`https://ajp.amjpathol.org/article/S0002-9440(12)00442-7/fulltext )
`J.S. Penn, et al. Vascular Endothelial Growth Factor in Eye Disease,
`Prog. Retin Eye Res., July 2008, 27(4):331-371. (“Penn2008”)
`
`U.S. Food and Drug Administration, Trivaris ® Highlights of the
`Prescribing Information, (May 2008) (“Trivaris label”)
`
`
`
`5
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`

`IPR2021-00816
`U.S. Patent No. 9,220,631
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`Ex.
`1057
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`Ex.
`1058
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`Ex.
`1059
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`Ex.
`1060
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`Ex.
`1061
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`Ex.
`1062
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`Ex.
`1063
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`Ex.
`1064
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`Ex.
`1065
`
`Ex.
`1066
`
`Ex.
`1067
`
`Internet Archive WayBack Machine, May 17, 2011 Record of U.S.
`Pharmacopeia, Understanding USP–NF, available at
`https://web.archive.org/web/20110517215303/http://www.usp.org/
`USPNF/understandingUSPNF.html
`Christine I. Falkner-Radler, et al. Needle Size in Intravitreal Injections-
`Preliminary Results of a Randomized Clinical Trial, AVRO Annual
`Meeting Abstract, March 2012, 54(884), available at
`https://iovs.arvojournals.org/article.aspx?articleid=2350271 (“ARVO
`abstract”)
`Carsten H. Meyer, et al. Steps for a Safe Intravitreal Injection
`Technique – A look at how European and American approaches
`compare, Retinal Physician (July 1, 2009), available at
`https://www.retinalphysician.com/issues/2009/july-aug/steps-for-a-
`safe-intravitreal-injection-technique (“Meyer”)
`Curriculum Vitae of James L. Mullins, Ph.D.
`
`DUPONT™ TYVEK® COMPLIANCE TO ISO 11607-1:2006 (2011)
`
`Center for Drug Evaluation and Research, Application Number: 21-
`756, Approved Labeling, Macugen® (pegaptanib sodium injection)
`(December 17, 2004) (“2004 Macugen Label”)
`Evangelos S. Gragoudas, et al. Pegaptanib for Neovascular Age-
`Related Macular Degeneration, New England Journal of Medicine
`2004; 351:2805-16, with Supplementary Appendix.
`IPR2020-1317, Paper No. 15, Institution Decision
`
`Anita M. Leys, et al. Neovascular Growth Following Photodynamic
`Therapy for Choroidal Hemangioma and Neovascular Regression after
`Intravitreous Injection of Triamcinolone, Retina 2006; 26(6):693-7,
`available at https://pubmed.ncbi.nlm.nih.gov/16829815/ (“Leys”)
`Australian Government, Department of Health and Ageing, Australian
`Public Assessment Report for Aflibercept, (July 2012)
`
`Sophie J. Bakri and Noha S. Ekdawi, Intravitreal Silicone Oil Droplets
`after Intravitreal Drug Injections, Retina 2008; 20:996-1001, available
`at https://pubmed.ncbi.nlm.nih.gov/18698303/ (“Bakri”)
`
`
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`6
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`IPR2021-00816
`U.S. Patent No. 9,220,631
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`Jared S. Bee, et al. Effects of Surfaces and Leachables on the Stability
`of Biopharmaceuticals, Journal of Pharmaceutical Science (Oct. 2011),
`available at https://pubmed.ncbi.nlm.nih.gov/21523787/ (“Bee”)
`Michael Colucciello, Prefilled Syringe Delivery of Intravitreal Anti-
`VEGF Medications: Advantages for Patients and Physicians, Retinal
`Physician (Mar. 1, 2019), available at
`https://www.retinalphysician.com/issues/2019/march-2019/prefilled-
`syringe-delivery-of-intravitreal-anti-ve (“Colucciello”)
`Declaration of Juergen Sigg (“Sigg Declaration”)
`
`Department of Health & Human Services, Macugen Approval Letter
`(Dec. 18, 2004)
`
`Lonny Wolgemuth, Challenges with Prefilled Syringes: The Parylene
`Solution, ONdrugDelivery (Oct. 2012), available at
`https://ondrugdelivery.com/wp-content/uploads/2018/11/Oct2012.pdf
`Therese M. Sassalos, Prefilled Syringes for Intravitreal Drug Delivery,
`Clinical Ophthalmology 2019:13 701-706, available at
`https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6485318/
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`https://www.physics.rutgers.edu/~podzorov/parylene%20properties.pdf
`(“SCS”)
`Lonny Wolgemuth, Assessing the Effects of Sterilization Methods on
`Parylene Coating, Medical Device & Diagnostic Industry, (Aug. 2002)
`
`David E. Overcashier, et al. Technical Considerations in the
`Development of Pre-filled Syringes for Protein Products, Am. Pharm.
`Rev. 2006;9(7): 77-83 (“Overcashier”)
`SDNY 20-5502 Docket
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`Federal Court Statistics
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`Novartis Letter to NDNY Court
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`Ex.
`1068
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`Ex.
`1069
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`Ex.
`1070
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`Ex.
`1071
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`Ex.
`1072
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`Ex.
`1073
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`Ex.
`1074
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`Ex.
`1075
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`Ex.
`1076
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`Ex.
`1077
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`Ex.
`1078
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`Ex.
`1079
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`IPR2021-00816
`U.S. Patent No. 9,220,631
`
`Mehmet S. Kocabora, et al. Intravitreal Silicone Oil Droplets
`Following Pegaptanib Injection, Acta Ophthalmologica 2010, available
`at https://onlinelibrary.wiley.com/doi/full/10.1111/j.1755-
`3768.2008.01336.x (“Kocabora”)
`Macugen Label (2008)
`
`U.S. Pharmacopeia, USP 789, Particulate Matter in Ophthalmic
`Solutions, USP 32 NF 27 (2009)
`
`Novartis NDNY Complaint
`
`Novartis Letter to SDNY Court
`
`ITC Investigation No. 337-TA-1207, Statement on the Public Interest
`by Proposed Respondent Regeneron Pharmaceuticals, Inc.
`
`ITC Investigation No. 337-TA-1207, Statement on the Public Interest
`by Szilard Kiss
`
`Ex.
`1080
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`Ex.
`1081
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`Ex.
`1082
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`Ex.
`1083
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`Ex.
`1084
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`Ex.
`1085
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`Ex.
`1086
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`Ex.
`1087
`
`Nitin Rathore, et al. Variability in Syringe Components and its Impact
`on Functionality of Delivery Systems, PDA Journal of Pharmaceutical
`Science and Technology 2011, 65 468-480 (“Rathore”)
`Ex.
`1088 PCT Patent Publication No. WO 2007/084765 to Deschatelets et al.
`PCT Patent Publication No. WO 97/44068 to Tack et al.
`Ex.
`1089
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`Text Minute Entry re Rule 16 Conference held on August 18, 2021,
`Novartis Pharma AG et al v. Regeneron Pharma., Inc., No. 1:20-cv-
`00690 (N.D.N.Y. Aug. 18, 2021)
`Declaration of Juergen Sigg
`
`Supplemental Declaration of Horst Koller under 37 C.F.R. § 1.68
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`8
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`Ex.
`1090
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`Ex.
`1091
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`Ex.
`1092
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`IPR2021-00816
`U.S. Patent No. 9,220,631
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`Supplemental Declaration of Szilard Kiss under 37 C.F.R. § 1.68
`
`ONDrugDelivery, Prefilled Syringe, available at
`https://ondrugdelivery.com/magazines/prefilled-syringes-the-rise-of-
`the-delivery-device-portfolio/
`
`Ex.
`1093
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`Ex.
`1094
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`Date: November 23, 2021
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`Respectfully submitted,
`
`
`/s/ Elizabeth Stotland Weiswasser
`Elizabeth S. Weiswasser (Reg. No. 73,760)
`Anish R. Desai (Reg. No. 73,760)
`Natalie Kennedy (Reg. No. 68,511)
`Andrew Gesior (Reg. No. 76,588)
`Weil, Gotshal & Manges LLP
`767 Fifth Avenue
`New York, NY 10153
`T: 212-310-8000
`F: 212-310-8007
`E: Regeneron.IPR.Service@weil.com
`
`Brian E. Ferguson (Reg. No. 36,801)
`Christopher Pepe (Reg. No. 73,851)
`Weil, Gotshal & Manges LLP
`2001 M Street NW, Suite 600
`Washington, DC 20036
`T: 202-682-7000
`F: 202-857-0940
`E: Regeneron.IPR.Service@weil.com
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`IPR2021-00816
`U.S. Patent No. 9,220,631
`
`CERTIFICATE OF SERVICE
`
`
`
`I hereby certify that on November 23, 2021, copies of the foregoing
`
`PETITIONER’S FIRST SUPPLEMENTAL EXHIBIT LIST was served via
`
`electronic mail, upon the following:
`
`Elizabeth J. Holland
`Linnea Cipriano
`Goodwin Procter LLP
`620 Eighth Avenue
`New York, NY 10018
`EHolland@goodwinlaw.com
`LCipriano@goodwinlaw.com
`
`William G. James
`Goodwin Procter LLP
`1900 N Street, N.W.
`Washington, D.C. 20036
`WJames@goodwinlaw.com
`
`Joshua Weinger
`Goodwin Procter LLP
`100 Northern Avenue
`Boston, MA 02210
`JWeinger@goodwinlaw.com
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`DG-NovartisPFS@goodwinlaw.com
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`/Lauren McDuffie/
`Lauren McDuffie
`IP Paralegal
`Weil, Gotshal & Manges LLP
`2001 M Street N.W., Suite 600
`Washington, D.C. 20036
`
`202-682-7000
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`lauren.mcduffie@weil.com
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