`_______________
`
`BEFORE THE PATENT TRIAL AND APPEAL BOARD
`_______________
`
`SUN PHARMACEUTICAL INDUSTRIES LTD.
`AND SUN PHARMACEUTICAL INDUSTRIES, INC.,
`Petitioners,
`v.
`NOVO NORDISK A/S,
`Patent Owner.
`_______________________________
`U.S. Patent No. 10,335,462 to Jensen
`Issue Date: July 2, 2019
`Title: Use of Long-Acting GLP-1 Peptides
`_______________________________
`Inter Partes Review IPR2024-00107
`_______________
`PETITIONER’S UPDATED EXHIBIT LIST AS OF MAY 16, 2024
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`TABLE OF EXHIBITS
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`EXHIBIT
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`DESCRIPTION
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`1001
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`1002
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`1003
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`1004
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`1005
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`1006
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`1007
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`1008
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`1009
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`1010
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`U.S. Patent No. 10,335,462
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`Prosecution history excerpts for U.S. Patent No. 10,335,462
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`Declaration of John Bantle, MD
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`CV of John Bantle MD
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`Declaration of William J. Jusko, Ph.D.
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`CV of William J. Jusko, Ph.D.
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`Declaration of Paul Dalby, Ph.D.
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`CV of Paul Dalby, Ph.D.
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`Intentionally Left Blank
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`Intentionally Left Blank
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`1011 WO 2011/138421
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`1012
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`1013
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`1014
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`Lovshin, Incretin-Based Therapies for Type 2 Diabetes Mellitus, 5
`NATURE REV. ENDOCRINOLOGY 262 (2009)
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`Clinical Trial No. NCT00696657
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`Clinical Trial No. NCT00851773
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`1015 WO 2006/097537
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`1016
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`1017
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`1018
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`U.S. Patent Application Pub. No. US2007/0010424
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`U.S. Patent No. 5,512,549
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`Banting, The Internal Secretion of the Pancreas, 7 J. LAB.
`CLINICAL MED. 251 (1922)
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`ii
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`EXHIBIT
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`DESCRIPTION
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`1019
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`1020
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`1021
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`1022
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`1023
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`1024
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`1025
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`1026
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`1027
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`1028
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`1029
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`and Two Related Peptides, 302 NATURE 716 (1983)
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`Current Status and Future Prospects, 30 PHARMACOTHERAPY
`609 (2010)
`
`Drucker, Enhancing Incretin Action for the Treatment of Type 2
`Diabetes, 26 DIABETES CARE 2929 (2003)
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`Drucker, The Incretin System: Glucagon-Like Peptide-1 Receptor
`Agonists and Dipeptidyl Peptidase-4 Inhibitors in Type 2 Diabetes, 368
`LANCET 1696 (2006)
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`Glaesner, Engineering and Characterization of the Long-Acting
`Glucagon-Like Peptide-1 Analogue LY2189265, an Fc Fusion
`Protein, 26 DIABETES/METABOLISM RSCH. & REV. 287
`(2010)
`
`HARRISON’S PRINCIPLES OF INTERNAL MED., Chapter 338
`(Fauci et al. eds. 17th ed. 2008)
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`Holst, Truncated Glucagon-like Peptide I, an Insulin-Releasing
`Hormone from the Distal Gut, 211 (2) FEBS LETTERS 169 (1987)
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`Holst, Glucagon-Like Peptide 1 and Inhibitors of Dipeptidyl
`Peptidase IV in the Treatment of Type 2 Diabetes Mellitus, 4
`CURRENT OP. IN PHARMACOLOGY 589 (2004)
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`Jimenez-Solem, Dulaglutide, a Long-Acting GLP-1 Analog Fused
`with an Fc Antibody Fragment for the Potential Treatment of Type 2
`Diabetes, 12 CURRENT OP. IN MOLECULAR THERAPEUTICS
`790 (2010)
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`iii
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`EXHIBIT
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`1030
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`1031
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`1032
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`1033
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`DESCRIPTION
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`Kim, Effects of Once-Weekly Dosing of a Long-Acting Release
`Formulation of Exenatide on Glucose Control and Body Weight in
`Subjects with Type 2 Diabetes, 30 DIABETES CARE 1487 (2007)
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`Knudsen, GLP-1 Derivatives as Novel Compounds for the Treatment
`of Type 2 Diabetes: Selection of NN2211 for Clinical Development,
`26 DRUGS OF THE FUTURE 677 (2001)
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`Knudsen, Glucagon-like Peptide-1: The Basis of a New Class of
`Treatment for Type 2 Diabetes, 47 J. MED. CHEMISTRY 4128
`(2004)
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`Knudsen, Liraglutide, a GLP-1 Analogue to Treat Diabetes, in
`ANALOGUE-BASED DRUG DISCOVERY II (Fischer & Ganellin
`eds. 2010)
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`1034
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`1035
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`Lund, Emerging GLP-1 Receptor Agonists, 16 EXPERT OP. ON
`EMERGING DRUGS 607 (2011)
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`1036
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`1037
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`1038
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`Mojsov, Insulinotropin: Glucagon-like Peptide I (7-37) Co-encoded
`in the Glucagon Gene is a Potent Simulator of Insulin Release in the
`Perfused Rat Pancreas, 79 J. CLINICAL INVESTIGATION 616
`(1987)
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`Nielsen, Pharmacology of Exenatide (Synthetic Exendin-4): A
`Potential Therapeutic for Improved Glycemic Control of Type 2
`Diabetes, 117 REGUL. PEPTIDES 77 (2004)
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`Seino, Dose-Dependent Improvement in Glycemia with Once-Daily
`Liraglutide without Hypoglycemia or Weight Gain: A Double-Blind,
`Randomized, Controlled Trial in Japanese Patients with Type 2
`Diabetes, 81 DIABETES RSCH. & CLINICAL PRACTICE 161
`(2008)
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`1039
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`Victoza, PHYSICIANS’ DESK REFERENCE (65th ed. 2010)
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`EXHIBIT
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`DESCRIPTION
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`1040
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`Vilsbøll, Glucagon-Like Peptide-1 and Diabetes Treatment, 21 INT’L
`DIABETES MONITOR 1 (2009)
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`1041 WO 03/002136
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`1042 WO 91/11457
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`1043
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`U.S. Patent App. Pub. 2004/0102486
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`1044
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`1045
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`1046
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`1047
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`1048
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`1049
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`1050
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`1051
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`Rohatagi, Model-Based Development of a PPARγ Agonist,
`Rivoglitazone, to Aid Dose Selection and Optimize Clinical Trial
`Designs, 48 J. CLINICAL PHARMACOLOGY 1420 (2008)
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`Shargel, APPLIED BIOPHARMACEUTICS &
`PHARMACOKINETICS (5th ed. 2005)
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`Yun, Pharmacokinetic and Pharmacodynamic Modelling of the
`Effects of Glimepiride on Insulin Secretion and Glucose Lowering in
`Healthy Humans, 31 J. CLINICAL PHARMACY &
`THERAPEUTICS 469 (2006)
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`Tamimi, Drug Development: From Concept to Marketing!, 113
`NEPHRON CLINICAL PRACTICE c125 (2009)
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`FDA Guidance for Industry, Exposure-Response Relationships -
`Study Design, Data, Analysis, and Regulatory Applications (Apr.
`2003)
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`International Conference on Harmonisation; Dose-Response
`Information to Support Drug Registration; Guideline; Availability,
`59 Fed. Reg. 55972 (Nov. 9, 1994) (“ICH 1994”)
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`Garber, Efficacy of Metformin in Type II Diabetes: Results of a
`Double-Blind, Placebo-Controlled, Dose-Response Trial, 102 AM.
`J. MED. 491 (1997)
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`Landersdorfer, Pharmacokinetic/Pharmacodynamic Modelling in
`Diabetes Mellitus, 47(7) CLINICAL PHARMACOKINETICS 417
`(2008)
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`DESCRIPTION
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`1052
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`1053
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`1054
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`1055
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`Madsbad, An Overview of Once-Weekly Glucagon-Like Peptide-1
`Receptor Agonists—Available Efficacy and Safety Data and
`Perspectives for the Future, 13 DIABETES, OBESITY &
`METABOLISM 394 (2011)
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`Møller, Mechanism-Based Population Modelling for Assessment of
`L-Cell Function Based on Total GLP-1 Response Following an Oral
`Glucose Tolerance Test, 38 J. PHARMACOKINETICS &
`PHARMACODYNAMICS 713 (2011)
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`Landersdorfer, Mechanism-Based Population Pharmacokinetic
`Modelling in Diabetes: Vildagliptin as a Tight Binding Inhibitor and
`Substrate of Dipeptidyl Peptidase IV, 73 BRIT. J. CLINICAL
`PHARMACOLOGY 391 (2011) (“Landersdorfer 2011a”)
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`Landersdorfer, Mechanism-Based Population Modelling of the Effects
`of Vildagliptin on GLP-1, Glucose and Insulin in Patients with Type 2
`Diabetes, 73 BRIT. J. CLINICAL PHARMACOLOGY
`373 (2011) “(Landersdorfer 2011b”)
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`1056
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`U.S. Patent No. 5,118,666
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`1057 WO 2011/073328
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`1058
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`1059
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`Blonde, Comparison of Liraglutide Versus Other Incretin-Related
`Anti-Hyperglycaemic Agents, 14 (suppl. 2) DIABETES, OBESITY
`& METABOLISM 20 (2012)
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`Murphy, Review of the Safety and Efficacy of Exenatide Once
`Weekly for the Treatment of Type 2 Diabetes Mellitus, 46 ANNALS
`OF PHARMACOTHERAPY 812 (2012)
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`1060 WO 2011/058193
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`1061
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`U.S. Patent App. Pub. No. 2011/0166321
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`1062
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`Zarin, The ClinicalTrials.gov Results Database—Update and Key
`Issues, 364 NEW ENGL. J. MED. 852 (2011)
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`DESCRIPTION
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`1071
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`1072
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`1073
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`Kirillova, Results and Outcome Reporting in ClinicalTrials.gov,
`What Makes it Happen?, 7(6) PLOS ONE 1 (2012)
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`Monami, Effects of Glucagon-Like Peptide-1 Receptor Agonists on
`Body Weight: A Meta-Analysis, 2012 EXPERIMENTAL
`DIABETES RSCH. 1 (2012)
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`Tasneem, The Database for Aggregate Analysis of ClinicalTrials.gov
`(AACT) and Subsequent Regrouping by Clinical Specialty, 7(3) PLOS
`ONE 1(2012)
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`Knudsen, Liraglutide: The Therapeutic Promise from Animal Models,
`64(suppl 167) INT’L J. CLINICAL PRACTICE 4 (2010)
`(“Knudsen 2010b”)
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`U.S. Patent No. 8,536,122
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`U.S. Patent No. 8,129,343
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`REMINGTON: THE SCIENCE AND PRACTICE OF
`PHARMACY (Alfonso R. Gennaro ed., 20th ed. 2000)
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`Boylan, Parenteral Products, in MODERN PHARMACEUTICS
`(Gilbert S. Banker et al. eds., 3d ed. 1996)
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`U.S. Patent No. 6,284,727
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`U.S. Patent No. 5,164,366
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`U.S. Patent No. 6,458,924
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`1074 WO 00/37098
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`1075
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`U.S. Patent No. 7,022,674
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`ClinicalTrials.gov Background, CLINICALTRIALS.GOV,
`https://clinicaltrials.gov/ct2/about-site/background (last visited Mar.
`10, 2023)
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`EXHIBIT
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`DESCRIPTION
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`Award: ClinicalTrials.gov,
`https://ash.harvard.edu/news/clinicaltrials.gov (last visited Mar. 10,
`2023)
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`U.S. Patent App. Pub. No. 2004/0102486
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`1079
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`https://www.clinicaltrials.gov/ct2/show/NCT01933490 (last visited
`Mar. 10, 2023)
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`1081
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`Ozempic prescribing information (Oct. 2022)
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`1082
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`1084
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`1085
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`1086
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`Scheduling Order, Novo Nordisk Inc. v. Rio Biopharmaceuticals
`Inc., No. 22-294 (CFC) (D. Del. June 30, 2022), ECF No. 22
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`Transfer Order, In re: Ozempic (Semaglutide) Patent Litigation, No.
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`Prosecution history excerpts for U.S. Patent No. 9,764,003
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`Intentionally Left Blank
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`Intentionally Left Blank
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`Intentionally Left Blank
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`EXHIBIT
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`DESCRIPTION
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`1091
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`1092
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`1093
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`1094
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`1095
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`Declaration of Melissa Weinberg, MD
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`CV of Melissa Weinberg, MD
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`Declaration of Craig Dyar, Ph.D.
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`CV of Craig Dyar, Ph.D.
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`Declaration of Alekha Dash, Ph.D.
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`1098
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`CV of Alekha Dash, Ph.D.
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`Inc. v. Rio Biopharmaceuticals Inc., (D. Del. May 1, 2024), ECF
`No. 333
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`1099
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`Dated: May 16, 2024
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`IPR2024-00107
`U.S. Patent No. 10,335,462
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`Respectfully submitted,
`
`
`
` /s/ Brian Sodikoff
`Brian Sodikoff
`Reg No. 54,697
`KATTEN MUCHIN ROSENMAN LLP
`525 West Monroe Street
`Chicago, IL 60661
`
`Counsel for Petitioners
`Sun Pharmaceutical Industries Ltd. and
`Sun Pharmaceutical Industries Inc.
`
`1
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`
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`IPR2024-00107
`U.S. Patent No. 10,335,462
`CERTIFICATE OF SERVICE
`Pursuant to 37 C.F.R. § 42.6(e), I hereby certify that on this 16th day of May
`
`2024, I caused to be served a true and correct copy of the foregoing by electronic
`
`delivery to Patent Owner’s counsel of record:
`
`J. Steven Baughman - steve.baughman@groombridgewu.com
`Megan Raymond - megan.raymond@groombridgewu.com
`Novo-Semaglutide-IPR@groombridgewu.com
`GROOMBRIDGE, WU, BAUGHMAN & STONE LLP
`
`
`
`Dated: May 16, 2024
`
`
`
` /s/ Brian Sodikoff
`Brian Sodikoff
`
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`2
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