Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 1 of 17
`
`IN THE UNITED STATES DISTRICT COURT
`FOR THE DISTRICT OF MASSACHUSETTS
`
`TEVA PHARMACEUTICALS
`INTERNATIONAL GMBH and
`TEVA PHARMACEUTICALS USA, INC.,
`
`Plaintiffs,
`
`v.
`
`ELI LILLY AND COMPANY,
`
`Defendant.
`
`)
`)
`)
`)
`)
`)
`)
`)
`)
`)
`)
`)
`
`Case No. 1:18-cv-12029-ADB
`
`DEFENDANT ELI LILLY AND COMPANY’S SECTION 282 NOTICE
`
`Pursuant to 35 U.S.C. § 282, Defendant Eli Lilly and Company (“Lilly”), by and through
`
`its undersigned counsel, hereby provides the following identification of patents and publications
`
`to be relied upon as showing the state of the art and/or showing evidence of knowledge of one of
`
`ordinary skill in the art with regard to U.S. Patent Nos. 8,586,045 (“the ’045 patent”); 9,884,907
`
`(“the ’907 patent”); and 9,884,908 (“the ’908 patent”; collectively, “the patents-in-suit”).
`
`Lilly hereby incorporates by reference all pleadings and prior communications that identify
`
`any patents or publications that Lilly cites to show that any claim(s) of the patents-in-suit are
`
`invalid for one or more of the reasons under 35 U.S.C. § 101, et. seq., including but not limited to
`
`the following documents, all appendices and exhibits thereto, as well as all materials cited therein:
`
` Opening Expert Report of Dr. Andrew Charles Regarding Invalidity of U.S. Patent Nos.
`
`8,586,045, 9,884,907, and 9,884,908, served September 16, 2021;
`
` Opening Expert Report of James M. McDonnell, Ph.D., Regarding Invalidity of U.S.
`
`Patent Nos. 8,586,045, 9,884,907, and 9,884,908, served September 16, 2021;
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 2 of 17
`
` Opening Expert Report of Diane R. Mould, Ph.D., FCP, FAAPS, served September 16,
`
`2021;
`
` Rebuttal Expert Report of Dr. Andrew Charles Regarding Noninfringement, served
`
`November 1, 2021;
`
` Rebuttal Expert Report of James M. McDonnell, Ph.D., Regarding Noninfringement of
`
`U.S. Patent Nos. 8,586,045, 9,884,907, and 9,884,908, served November 1, 2021;
`
` Rebuttal Expert Report of Egilius Spierings, M.D., Ph.D., served November 1, 2021;
`
` Reply Expert Report of Dr. Andrew Charles Regarding Invalidity of U.S. Patent Nos.
`
`8,586,045, 9,884,907, and 9,884,908, served December 7, 2021;
`
` Reply Expert Report of James M. McDonnell, Ph.D., Regarding Invalidity of U.S. Patent
`
`Nos. 8,586,045, 9,884,907, and 9,884,908, served December 7, 2021;
`
` Reply Expert Report of Dr. Diane R. Mould, Ph.D., served December 7, 2021;
`
` Lilly’s Initial Disclosure Statement Pursuant to Fed. R. Civ. P. 26(a)(1), served May 1,
`
`2020;
`
` Lilly’s First Supplemental Initial Disclosure Statement Pursuant to Fed. R. Civ. P.
`
`26(a)(1), served May 29, 2020;
`
` Lilly’s Preliminary Disclosures Pursuant to Local Rule 16.6(d)(4), served July 10, 2020;
`
` Lilly’s First Supplemental Disclosures Pursuant to Local Rule 16.6(d)(4), served April
`
`28, 2021;
`
` All prior art cited on the face of the patents-in-suit;
`
` All materials identified in the record of inter partes review proceeding nos. IPR2018-
`
`01422, IPR2018-01423, IPR2018-01424, IPR2018-01425, IPR2018-01426, IPR2018-
`
`01427, IPR2018-01710, IPR2018-01711, and IPR2018-01712;
`
`2
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 3 of 17
`
` All materials identified in the appellate record of case nos. 20-1747, 20-1748, 20-1749,
`
`20-1750, 20-1751, 20-1752, 20-1876, 20-1877, and 20-1878, including briefs and the
`
`Federal Circuit’s decision rendered in each appeal;
`
` All other materials identified to and/or exchanged with Plaintiffs from Lilly during the
`
`course of fact and expert discovery in the above-captioned matter; and
`
` All materials listed in Lilly’s Trial Exhibit List and identified by Lilly in the Joint Pretrial
`
`Memorandum, including all amendments and supplements thereto.
`
`Lilly provides the following list of patents, publications, persons, products, and other
`
`information out of an abundance of caution to satisfy 35 U.S.C. § 282. The fact that Lilly lists
`
`these patents, publications, persons, products, and other information does not reflect that all, more,
`
`or any number of these patents, publications, persons, products, and other information will
`
`ultimately be used by Lilly in the presentation of evidence at trial. Therefore, no implication
`
`should be taken that reliance on all of the identified patents, publications, persons, products, and
`
`other information are necessary to support any of Lilly’s invalidity defenses.
`
`PATENTS
`
`DATE
`
`DESCRIPTION
`
`2/3/1998
`
`U.S. Patent No. 5,714,468 to Binder
`
`1/30/2001 U.S. Patent No. 6,180,370 to Queen et al.
`
`4/22/2003 U.S. Patent No. 6,552,041 B1 to Patchett et al.
`
`4/22/2003 U.S. Patent No. 6,552,043 B1 to Patchett et al.
`
`2/10/2010 U.S. Patent No. 7,655,244 B2 to Blumenfeld
`
`3
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 4 of 17
`
`PUBLICATIONS, PRODUCTS, AND OTHER INFORMATION
`
`DATE
`
`3/11/2004
`
`12/1/1995
`
`3/9/1994
`
`5/1/1992
`
`7/30/2004
`9/16/2004
`5/1/2005
`3/1/2004
`10/1/2004
`
`9/1/2005
`
`5/1/2004
`10/1/2004
`11/1/2001
`
`8/1/2002
`
`1/1/1998
`
`6/1/2004
`
`2/17/2000
`
`8/1/2004
`
`3/1/2005
`
`10/1/1993
`
`DESCRIPTION
`J. Olesen et al., Calcitonin Gene-Related Peptide Receptor Antagonist BIBN
`4096 BS tor the Acute Treatment of Migraine, The New England Journal of
`Medicine, 350:1104-110 (2004)
`K. Tan et al., Calcitonin Gene-Related Peptide as an Endogenous Vasodilator:
`Immunoblockade Studies In Vivo with an Anti-Calcitonin Gene-Related Peptide
`Monoclonal Antibody and Its Fab' Fragment, Clinical Science 89:565-73 (1995)
`Application of monoclonal antibodies to the investigation of the role of
`calcitonin gene-related peptide as a vasodilatory neurotransmitter. Dissertation
`by K. Tan submitted to University of Cambridge for Ph.D. Degree
`N. Shaw et al., The Effect of Monoclonal antibodies to Calcitonin Gene-Related
`Peptide (CGRP) on CGRP-Induced Vasodilatation in Pig Coronary Artery Rings,
`Br. J. Pharmacol. 106:196-98 (1992)
`Highlights of Prescribing Information, Humira (July 30, 2004)
`Highlights of Prescribing Information, Remicade (September 16, 2004)
`A. Ahn and A. Basbaum, Where do triptans act in the treatment of migraine?,
`Pain 115(1-2):1–4 (2005)
`N. Araki, Migraine, JMAJ 47(3):124-129 (2004)
`U. Arulmani et al., Calcitonin Gene-Related Peptide and its Role in Migraine
`Pathophysiology, European Journal of Pharmacology 500:315-30 (2004)
`D. Arulmozhi et al., Migraine: Current Concepts and Emerging Therapies,
`Vascular Pharmacol, 43:176-87 (2005)
`W. Banks, Are the Extracelluar Pathways a Conduit for the Delivery of
`Therapeutics to the Brain?, Current Pharmaceutical Design, 10:1365-70 (2004)
`G. Bussone, Pathophysiology of Migraine, Neurol Sci 25:S239–S241(2004)
`P. Carter, Improving the Efficacy of Antibody-Based Cancer Therapies, Nature
`Revs. Cancer 1:118-29 (2001)
`A. Conner et al., Interaction of Calcitonin-Gene-Related Peptide with Its
`Receptors, Biochemistry Society Transactions 30(4):451-55 (2002)
`F. Cutrer et al., Perfusion-weighted imaging defects during spontaneous
`migrainous aura, Ann Neurol. 43(1):25-31 (1998)
`D. Dodick and V. Martin, Triptans and CNS Side-Effects: Pharmacokinetic and
`Metabolic Mechanisms, Cephalalgia 24:417-24 (2004)
`H. Doods et al., Pharmacological Profile of BIBN4096BS, the First Selective
`Small Molecule CGRP Antagonist, Br. J. Pharmacol. 129:420-23 (2000)
`I. Edvinsson, Blockade of CGRP Receptors in the Intracranial Vasculature: A
`New Target in the Treatment of Headache, Cephalalgia 24:611-22 (2004)
`L. Edvinsson, Clinical Data on the CGRP Antagonist BIBN4096BS for
`Treatment of Migraine Attacks, CNS Drug Revs. 11:69-76 (2005)
`K. Escott and S. Brain, Effect of a Calcitonin Gene-Related Peptide Antagonist
`(CGRP8-37) on Skin Vasodilatation and Oedema Induced by Stimulation of the
`Rat Saphenous Nerve, Br. J. Pharmacol. 110:772-776 (1993)
`
`4
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 5 of 17
`
`3/13/1992
`
`6/22/2005
`
`2/1/1999
`
`6/1/1994
`
`1/1/2002
`
`9/1/2005
`
`3/1/2005
`
`1/1/2004
`1/1/2004
`7/1/1993
`
`8/31/2005
`
`2/1/2002
`
`11/1/2005
`
`11/1/2004
`
`4/1/2001
`
`8/1/2000
`
`1/1/2005
`
`3/1/1993
`
`12/1/1990
`
`M. Ferrari and P. Saxena, Clinical Effects and Mechanism of Action of
`Sumatriptan in Migraine, Clinical Neurology and Neurosurgery 94 Supp.:S73-
`S77 (1992)
`M. Fischer et al., The Nonpeptide Calcitonin Gene-Related Peptide Receptor
`Antagonist BIBN4096BS Lowers the Activity of Neurons with Meningeal Input
`in the Rat Spinal Trigeminal Nucleus, The Journal of Neuroscience 25(25):5877–
`883 (2005)
`Y. Frobert et al., A Sensitive Sandwich Enzyme Immunoassay for Calcitonin
`Gene-Related Peptide (CGRP): Characterization and Application, Peptides
`20:275-84 (1998)
`P. Goadsby and L. Edvinsson, Human in vivo Evidence for Trigeminovascular
`Activation in Cluster Headache: Neuropeptide Changes and Effects of Acute
`Attacks Therapies, Brain 117:427-34 (1994)
`P. Goadsby et al., Migraine — Current Understanding and Treatment, N. Engl. J.
`Med. 346:257-270 (2002)
`P. Goadsby, Can We Develop Neurally Acting Drugs for the Treatment of
`Migraine?, Nature Revs. Drug Disc. 4:741-750 (2005)
`D. Hay and D. Poyner, The Preclinical Pharmacology of BIBN4096BS, a CGRP
`Antagonist, Cardiovascular Drug Rev. 23(1):31-42 (2005)
`The International Classification of Headache Disorders, Cephalalgia 24(1):1-151
`(2004)
`Physicians' Desk Reference, Imitrex® Prescribing Information (2004)
`H. Kaube et al., Inhibition by Sumatriptan of Central Trigeminal Neurones Only
`After Blood-Brain Barrier Disruption, Br. J. Pharmacol. 109:788-92 (1993)
`S. Kim et al., Antibody Engineering for the Development of Therapeutic
`Antibodies, Mol. Cell (20)1:17-29 (2005)
`L. Lassen et al., CGRP May Play a Causative Role in Migraine, Cephalagia
`22:54-61 (2002)
`D. Levy et al., Calcitonin Gene–Related Peptide Does Not Excite or Sensitize
`Meningeal Nociceptors: Implications for the Pathophysiology of Migraine, Ann.
`Neurol. 58: 698-705 (2005)
`E. Lobo et al., Antibody Pharmacokinetics and Pharmacodynamics, J.
`Pharmaceutical Sciences 93: 2645-68 (2004)
`A. May & P. Goadsby, Substance P Receptor Antagonists in the Therapy of
`Migraine, Exp. Opin. Invest. Drugs10:673-78 (2001)
`J. Maynard and G. Georgiou, Antibody Engineering, Annu. Rev. Biomed. Eng.
`2:339-76 (2000)
`K. Messlinger et al., Inhibition of Neurogenic Blood Flow Increases in the Rat
`Cranial Dura Mater by a CGRP-Binding Spiegelmer, Cephalalgia 25(10):923
`(2005)
`M. Moskowitz et al., Neocortical Spreading Depression Provokes the Expression
`of C-fos Protein-like lmmunoreactivity within Trigeminal Nucleus Caudalis via
`Trigeminovascular Mechanisms, J. Neurosci.13:1167-177 (1993)
`J. Olesen et al., Timing and topography of cerebral blood flow, aura, and
`headache during migraine attacks, Ann Neurol. 28(6):791-98 (1990)
`
`5
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 6 of 17
`
`3/1/2005
`
`8/1/2005
`
`9/1/2005
`
`1/1/1998
`
`1/1/2004
`
`12/1/1997
`
`8/1/2004
`
`K. Petersen et al., BIBN4096BS Antagonizes Human Calcitonin Gene Related
`Peptide-Induced Headache and Extracerebral Artery Dilation, Clinical
`Pharmacology & Therapeutics 77(3):202-13 (2005)
`D. Pietrobon, Migraine: New Molecular Mechanisms, The Neuroscientist
`11:373-86 (2005)
`J. Reichert et al., Monoclonal Antibody Successes in the Clinic, Nature
`Biotechnol. 23:1073-078 (2005)
`B. Rist et al., From Micromolar to Nanomolar Affinity: A Systematic Approach
`to Identify the Binding Site of CGRP at the Human Calcitonin Gene-Related
`Peptide 1 Receptor, J. Med. Chem. 41:117-23 (1998)
`Sigma-Aldrich, Biochemicals & Reagents for Life Science Research, 350-352
`(2004)
`R. Storer and P. Goadsby, Microiontophoretic Application of Serotonin
`(5HT)1B/1D Agonists Inhibits Trigeminal Cell Firing in the Cat, Brain 120:
`2171-177 (1997)
`R. Storer et al., Calcitonin Gene-Related Peptide (CGRP) Modulates Nociceptive
`Trigeminovascular Transmission in the Cat, Br. J. Pharmacol. 142:1171-181
`(2004)
`I. Tomlinson, Next-Generation Protein Drugs, Nature Biotechnology 22(5):521-
`5/1/2004
`22 (2004)
`8/20/1999 W. Wang, Instability, Stabilization, and Formulation of Liquid Protein
`Pharmaceuticals, Int'l J. of Pharmaceutics 185:129-188 (1999)
`D. Williamson et al., Intravital Microscope Studies on then Effects of Neurokinin
`Agonists and Calcitonin Gene-Related Peptide on Dural Vessel Diameter in the
`Anaesthetized Rat, Cephalalgia 17:518-524 (1997)
`S. Wimalawansa, Calcitonin Gene-Related Peptide and Its Receptors: Molecular
`Genetics, Physiology, Pathophysiology, and Therapeutic Potentials, Endocrine
`Revs. 17(5):533-85 (1996)
`H. Wong et al., Monoclonal Antibody to Rat CGRP: Production,
`Characterization, and in vivo Immunoneutralization Activity, Hybridoma 12:93-
`106 (1993)
`C. Zwetsloot et al., Lack of Asymmetry of Middle Cerebral Artery Blood
`Velocity in Unilateral Migraine, Stroke 24:1335-338 (1993)
`E. Beck et al., Management of Cluster Headache, (2005) 71:717-24
`G. Lichtenstein, Approach to Steroid-Dependent and Steroid- Refractory Crohn’s
`Disease, J. Pediatric Gastroenterology & Nutrition (2001) 33:S27-S35 (2001)
`L. Djavadi-Ohaniance et al., Chapter 4, Measuring Antibody Affinity in
`Solution. Antibody Engineering: A Practical Approach (1996) and L. Hefta et al.,
`Chapter 5, Measuring Antibody Affinity Using Biosensors, Antibody
`Engineering: A Practical Approach (1996)
`S. Ozyalcin et al., The Efficacy and Safety of Venlafaxine in the Prophylaxis of
`2/10/2005
`Migraine, Headache 45:144-52 (2005)
`11/1/2001 W. Sandborn et al., Etanercept for Active Crohn’s Disease: A Randomized,
`Double-Blind, Placebo-Controlled Trial, Gastroenterology 121:1088-94 (2001)
`8/20/2003
`S. Bowers, Celltech hit by failure of Crohn's disease drug, The Guardian (2003)
`
`9/1/1993
`2/15/2005
`9/1/2001
`
`6/24/1997
`
`10/1/1996
`
`2/1/1993
`
`1/1/1996
`
`6
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 7 of 17
`
`9/1/2002
`
`2/1/1993
`
`7/1/2000
`
`8/1/2004
`
`5/1/2003
`
`12/1/1999
`
`4/1/1997
`
`3/1/1994
`
`9/1/1997
`
`6/1/1997
`
`S. Akerman et al., Nitric Oxide Synthase Inhibitors Can Antagonize Neurogenic
`and Calcitonin Gene-Related Peptide Induced Dilation of Dural Meningeal
`Vessels, British J. of Pharmacology 137:62-68 (2002)
`M. Gawel et al., Subcutaneous Sumatriptan in the Treatment of Acute Episodes
`of Posttraumatic Headache 33:96 (1993)
`R. Hill, NK1 (Substance P) Receptor Antagonists – Why Are They Not
`Analgesic in Humans? TiPS 21:244-46 (2000)
`M. Iovino et al., Safety, Tolerability and Pharmacokinetics of BIBN 4096 BS,
`the First Selective Small Molecule Calcitonin Gene-Related Peptide Receptor
`Antagonist, Following Single Intravenous Administration in Healthy Volunteers,
`Cephalalgia 24:645-56 (2004)
`D. Pietrobon and J. Striessnig, Neurobiology of Migraine, Nat. Rev. Neurosci.
`4:386-98 (2003)
`S. Shepheard et al., Possible Antimigraine Mechanisms of Action of the 5HT1F
`Receptor Agonist LY334370, Cephalalgia 19:851-58 (1999)
`S. Shepherd et al., Differential Effects of 5-HT1B/1D Receptor Agonists on
`Neurogenic Dural Plasma Extravasation and Vasodilation in Anaesthetized Rats,
`Neuropharmacol. 36(4/5):525-33 (1997)
`K. Tan et al., Demonstration of the neurotransmitter role of calcitonin gene-
`related peptides (CGRP) by immunoblockade with anti-CGRP monoclonal
`antibodies, Br. J. Pharmacol. 111:703-10 (1994)
`D. Williamson et al., The Novel Anti-Migraine Agent Rizatriptan Inhibits
`Neurogenic Dural Vasodilation and Extravasation, Eur. J. Pharmacol. 328:61-64
`(1997)
`D. Williamson et al., Sumatriptan Inhibits Neurogenic Vasodilation of Dural
`Blood Vessels in the Anaesthetized Rat-Intravital Microscope Studies,
`Cephalalgia 17(4):525-31 (1997)
`D. Williamson et al., Role of Opioid Receptors in Neurogenic Dural
`Vasodilation and Sensitization of Trigeminal Neurones in Anaesthetized Rats,
`Br. J. Pharmacol. 133:807-14 (2001)
`D. Williamson and R. Hargreaves, Neurogenic Inflammation in the Context of
`Migraine, Microscopy Res. & Tech. 53:167-78 (2001)
`D. Williamson et al., The Anti-Migraine 5-HT1B/1D Agonist Rizatriptan
`Inhibits Neurogenic Dural Vasodilation in Anaesthetized Guinea-Pigs, Br. J.
`Pharmacol. 133:1029-034 (2001)
`S. Tepper et al., Prevalence and Diagnosis of Migraine in Patients Consulting
`Their Physician with a Complaint of Headache: Data from the Landmark Study,
`Headache 44: 865-64 (2004)
`10/11/2003 P. Torelli, et al. Pain and behaviour in cluster headache. A prospective study and
`review of the literature, Functional Neurology 18(4):205-210 (2003)
`K. Petersen et al., Inhibitory effect of BIBN4096BS on cephalic vasodilatation
`induced by CGRP or transcranial electrical stimulation in the rat, British Journal
`of Pharmacology 143:697-704 (2004)
`S. Akerman et al., The effect of adrenergic compounds on neurogenic dural
`vasodilatation, European Journal of Pharmacology 424:53–58 (2001)
`
`10/25/2004
`
`7/1/2001
`
`5/1/2001
`
`8/1/2001
`
`10/1/2004
`
`7/13/2001
`
`7
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 8 of 17
`
`1/1/1991
`
`1/1/2004
`
`1/1/2004
`
`1/1/2004
`
`1/1/2005
`
`1/1/1999
`
`3/11/2004
`
`3/24/1988
`
`11/1/1995
`
`1/1/2000
`
`11/6/1990
`
`10/7/2002
`
`4/1/2004
`
`9/1/2004
`
`7/1/2005
`
`2/1/1995
`
`1/1/2001
`
`2/1/2004
`
`12/1/2001
`
`R. Hill, Criteria for the Development of Analgesic Drugs: A Personal View from
`the Perspective of the Pharmaceutical Industry, Towards a New
`Pharmacotherapy of Pain, 293- 296 (1991)
`R. Hill et al., Chapter 28, New possibilities for antimigraine therapy via 5-HT
`receptors?, Preventive Pharmacotherapy of Headache Disorders,189-193 (2004)
`R. Hill, Chapter 41, New targets II: discussion summary, Preventive
`Pharmacotherapy of Headache Disorders, 271-272 (2004)
`R. Hill, Chapter 14, Can the Evaluation of Drugs in Animal Pain Models
`Reliably Predict the Ability to Produce Clinical Analgesia?, The Pain System in
`Normal and Pathological States: A Primer for Clinicians. Progress in Pain
`Research and Management, 3(1):247-58 (2004)
`R. Hill, Ch. 35, Analgesic drugs in development, Wall and Melzack’s Textbook
`of Pain (5th Edition), 541-552 (2005)
`J. Longmore et al., Advances in migraine therapy-5-HT receptor subtype-specific
`agonist drugs, Current Opinion in CPNS Investigational Drugs 1(1):39-53 (1999)
`P. Durham, CGRP-Receptor Antagonists -A Fresh Approach to Migraine
`Therapy?, N ENGL J MED (350) 11:1073-75 (2004)
`L. Riechmann et al., Reshaping human antibodies for therapy, Nature 332:323-
`27 (1988)
`G. Hale and J. Phillips, Clinical trials with CAMPATH- I and other monoclonal
`antibodies, Therapeutic Monoclonals 23:1057-063 (1995)
`G. Hale and H. Waldmann, From Laboratory to Clinic, The Story of
`CAMPATH-1, Methods in Molecular Medicine, Vol. 40: Diagnostic and
`Therapeutic Antibodies, 243-267 (2000)
`D. Andrew et al., Monoclonal antibodies distinguishing α and β forms of
`calcitonin gene-related peptide, Journal of Immunological Methods, 154:87-94
`(1990)
`Time Magazine, Preventing Headaches, The latest research offers new hope for
`all of us (2002)
`A. Blumenfeld et al., Botulinum neurotoxin for the treatment of migraine and
`other primary headache disorders, Dermatol Clin 22:167–175 (2004)
`A. Blumenfeld, Botulinum Toxin Type A for the Treatment of Headache: Pro,
`Headache 44:825-30 (2004)
`Guidance for Industry Estimating the Maximum Safe Starting Dose in Initial
`Clinical Trials for Therapeutics in Adult Healthy Volunteers, U.S. Department of
`Health and Human Services, Food and Drug Administration, Center for Drug
`Evaluation and Research (CDER) (July 2005)
`L. Lacey et al., Single dose pharmacokinetics of sumatriptan in healthy
`volunteers, Eur J Clin Pharmacol 47:543-548 (1995)
`C. Janeway, Appendix I, Immunologists' Toolbox, Immunobiology: The Immune
`System in Health and Disease, 5th Edition 613-59 (2001)
`P. Hinton et al., Engineered Human IgG Antibodies with Longer Serum Half-
`lives in Primates. Journal of Biological Chemistry 279(8):6213-16 (2004)
`R. Ober et al., Differences in promiscuity for antibody-FcRn interactions across
`species: Implications for therapeutic antibodies, International Immunology,
`13:1551–59 (2001)
`
`8
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 9 of 17
`
`10/1/2005
`
`9/1/2004
`
`2/1/2002
`
`6/1/2002
`
`1/1/2002
`
`1/1/1986
`
`10/1/2005
`
`11/1/1997
`
`2/1/1999
`
`7/1/2001
`
`1/1/1998
`
`4/1/2001
`
`9/1/2001
`
`12/7/1998
`
`2/28/1997
`
`7/1/2000
`
`11/30/1993
`
`11/1/1993
`
`1/1/2004
`
`L. Presta, Selection, design, and engineering of therapeutic antibodies, J. Allergy
`Clin. Immunol. 116:731-36 (2005)
`L. Tang et al., Pharmacokinetic Aspects of Biotechnology Products, J.Pharm.
`Sci. 93:2184-204 (2004)
`S. Brain et al., CGRP receptors: a headache to study, but will antagonists prove
`therapeutic in migraine? TRENDS in Pharmcol. Scr. 23(2):51-53 (2002)
`J. Cavagnaro, Preclinical safety evaluation of biotechnology-derived
`pharmaceuticals, Drug Discovery 1:469-475 (2002)
`L. Mitscher, Chapter 1, Drug Design and Discovery: an Overview, Textbook of
`Drug Design and Discovery, 3rd Edition, Ed., Taylor & Francis, New York, NY
`(2002)
`P. Willner, Validation criteria for animal models of human mental disorders:
`learned helplessness as a paradigm case, Prog. Neuro-
`Neuropsychopharmacology & Biological Psychiatry, 10:677-90 (1986)
`P. Goadsby, Advances in the understanding of headache, British Medical
`Bulletin 73 and 74:83–92 (2005)
`D. Goldstein et al., Ineffectiveness of neurokinin-1 antagonist in acute migraine:
`a crossover study, Cephalalgia 17:785-90 (1997)
`D. Goldstein et al., Lanepitant, An NK-1 Antagonist, in Migraine Prophylaxis,
`Clinical Pharmacology & Therapist 65(3):129 (1999)
`R. Lipton et al., Prevalence and Burden of Migraine in the United States: Data
`From the American Migraine Study II, Headache 41:646-57 (2001)
`B. Norman and D. Panebianco, A placebo-controlled, in-clinic study to explore
`the preliminary safety and efficacy of intravenous L-758,298 (a prodrug of the
`NK1 receptor antagonist L-754,030) in the acute treatment of migraine,
`Cephalalgia 18:407 (1998)
`M-P Lefranc, Nomenclature of the Human lmmunoglobulin Heavy (IGH) Genes,
`Exp. Clin. lmmunogenet. 18:100-116 (2001)
`M-P Lefranc, Nomenclature of the Human lmmunoglobulin Kappa (IGK) Genes,
`Exp. Clin. lmmunogenet. 18:161-174 (2001)
`F. Matsuda et al., The Complete Nucleotide Sequence of the Human
`Immunoglobulin Heavy Chain Variable Region Locus, J. Exp. Med. 188:2151–
`2162 (1998)
`FDA Center for Biologics Evaluation and Research, Points to Consider in the
`Manufacture and Testing of Monoclonal Antibody Products for Human Use
`J. Xu and M. Davis, Diversity in the CDR3 Region of VH Is Sufficient for Most
`Antibody Specificities, Immunity, 13:37-45, (July 2000)
`B. Peskar et al., A monoclonal antibody to calcitonin gene-related peptide
`abolishes capsaicin-induced gastroprotection, European Journal of
`Pharmacology, 250: 201-03 (1993)
`V. Plourde et al., CGRP Antagonists and Capsaicin on Celiac Ganglia Partly
`Prevent Postoperative Gastric Ileus, Peptides 14:1225-229 (1993)
`M. Bigal & R. Lipton, Overview on the prevalence and impact of migraine. J
`Headache Pain 5:S88–S91 (2004)
`
`9
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 10 of 17
`
`12/1/2000
`
`5/30/2002
`
`2/1/1997
`
`7/1/1997
`
`8/1/2000
`
`1/1/1988
`
`8/1/2005
`5/1/2005
`
`4/1/2005
`
`W. Binder et al., Botulinum toxin type A (BOTOX) for treatment of migraine
`headaches: An open-label study. Otolaryngology–Head and Neck Surgery,
`123:669-76 (2000)
`L. Edvinsson, Calcitonin Gene-Related Peptide (CGRP) in Cerebrovascular
`Disease. The Scientific World Journal 2:1484-90 (2002)
`M. Fanciullacci et al., Responsiveness of the trigeminovascular system to
`nitroglycerine in cluster headache patients, Brain 120:283-288 (1997)
`Guidance for Industry, M3 Nonclinical Safety Studies for the Conduct of Human
`Clinical Trials for Pharmaceuticals, U.S. Department of Health and Human
`Services, Food and Drug Administration, Center for Drug Evaluation and
`Research (CDER), Center for Biologics Evaluation and Research (CBER), (July
`1997)
`H. Havanka et al., Efficacy of Naratriptan Tablets in the Acute Treatment of
`Migraine: A Dose-Ranging Study, Clinical Therapeutics 22(8):970- 980 (2000)
`Headache Classification Committee of the International Headache Society, The
`International Classification of Headache Disorders, 1st Edition, Cephalalgia 8(7)
`(1988)
`J. Joubert, Diagnosing headache, Headache 34(8):621-625 (2005)
`G. Manzoni and P. Torelli, Epidemiology of typical and atypical craniofacial
`neuralgias, Neurol Sci 26:S65-S67 (2005)
`N. Mathew et al., Botulinum Toxin Type A (BOTOX®) for the Prophylactic
`Treatment of Chronic Daily Headache: A Randomized, Double-Blind, Placebo-
`Controlled Trial, Headache 45:293-307 (2005)
`A. May, Cluster headache: pathogenesis, diagnosis, and management, Lancet
`9/3/2005
`366:843-55 (2005)
`10/15/2000 S. Morey, Guidelines on Migraine: Part 2, General Principles of Drug Therapy,
`Am Fam Physician 62(8):1915-17 (2000)
`S. Morey, Guidelines on Migraine: Part 3, Recommendations for Individual
`11/1/2000
`Drugs, Am Fam Physician 62(9):2145-51 (2000)
`11/15/2000 S. Morey, Guidelines on Migraine: Part 4, General Principles of Preventive
`Therapy, Am Fam Physician 62(10):2359-62 (2000)
`S. Morey, Guidelines on Migraine: Part Part 5, Recommendations for Specific
`Prophylactic Drugs, Am Fam Physician 62(11):2535-39 (2000)
`A. Rapoport et al., Optimizing the dose of zolmitriptan (Zomig, 311C90) for the
`acute treatment of migraine, A multicenter, double-blind, placebo-controlled,
`dose-range-finding study, The 017 Clinical Trial Study Group, Neurology
`49:1210-218 (1997)
`A. Rapoport et al., Dose Range-Finding Studies With Frovatriptan in the Acute
`Treatment of Migraine, Headache 42:S74-S83 (2002)
`A. Shah et al., The Pharmacokinetics and Safety of Single Escalating Oral Doses
`of Eletriptan, J. Clin Pharmacol 42:520-27 (2002)
`S. Silberstein et al., Botulinum Toxin Type A as a Migraine Preventive
`Treatment, Headache 40:445-50 (2000)
`S. Silberstein et al., Topiramate in Migraine Prevention: Results of a Large
`Controlled Trial, Arch Neurol 61:490-95 (2004)
`S. Silberstein, Chronic Daily Headache, JAOA Supp. 2 105(4):S23-S29 (2005)
`
`4/1/2004
`4/1/2005
`
`12/1/2000
`
`11/1/1997
`
`4/1/2002
`
`5/1/2002
`
`6/1/2000
`
`10
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 11 of 17
`
`1/1/1998
`
`7/26/2005
`
`5/6/2005
`
`7/1/1998
`
`8/1/1996
`
`7/1/1997
`
`7/21/2003
`
`J. van Vliet et al., Features involved in the diagnostic delay of cluster headache, J
`Neurol Neurosurg Psychiatry 74:1123-125 (2003)
`H. Connor et al., Clinical evaluation of a novel, potent, CNS penetrating NK
`receptor antagonist in the acute treatment of migraine, Cephalalgia 18:392 (1998)
`P. Deng et al., Role of calcitonin gene-related peptide in the phenol-induced
`7/15/2004
`neurogenic hypertension in rats, Regulatory Peptides 119:155– 61 (2004)
`8/19/2004 W. Li et al., Interleukin-1β induces β-calcitonin gene-related peptide secretion in
`human type II alveolar epithelial cells, The FASEB Journal 1–26 (2004)
`X. Qin et al., CCL2 and CXCL1 Trigger Calcitonin Gene-Related Peptide
`Release by Exciting Primary Nociceptive Neurons, Journal of Neuroscience
`Research 82:51–62 (2005)
`S. Supowit et al., Calcitonin gene-related peptide and substance P contribute to
`reduced blood pressure in sympathectomized rats, Am J Physiol Heart Circ
`Physiol 289:H1169–H1175 (2005)
`A. Taylor et al., Suppression of Nitric Oxide Generated by Inflammatory
`Microphages by Calcitonin Gene-Related Peptide in Aqueous Humor,
`Investigative Ophthalmology & Visual Science 39:1372–1378 (1998)
`X. Wang et al., Rapid nitric oxide- and prostaglandin-dependent release of
`calcitonin gene-related peptide (CGRP) triggered by endotoxin in rat mesenteric
`arterial bed, British Journal of Pharmacology 118:2164–170 (1996)
`X. Wang and R. Fiscus, Lactic acid potentiates bradykinin- and low-pH-induced
`release of CGRP from rat spinal cord slices, The American Physiological Society
`(1997)
`H. Wang et al., Production and secretion of calcitonin gene-related peptide from
`9/1/2002
`human lymphocytes, Journal of Neuroimmunology 130:155–162 (2002)
`10/15/2000 L. Xing et al., Induction and Expression of β-Calcitonin Gene-Related Peptide in
`Rat T Lymphocytes and Its Significance, J Immunol 165:4359–366 (2000)
`C. Maggi et al., Biological activity of N-terminal fragments of calcitonin gene-
`related peptide, European Journal of Pharmacology, 179:217-219 (1990)
`S. Akerman te al., The Role of Histamine in Dural Vessel Dilation, Brain
`Research 956: 96-102 (2002)
`J. Buscaglia and A. Tokayer, Migraine Headache and Its Association with
`Emesis and Gastric Motility: A Brief Review, Practical Gastroenterology 28(3)
`66-72 (2004)
`ICH Topic E4, Dose Response Information to Support Drug Registration
`(European Medicines Agency, Nov. 1994)
`C. Barbas et al., Semisynthetic Combinatorial Antibody Libraries: A Chemical
`Solution to the Diversity Problem, Proc. Natl. Acad. Sci. 89: 4457-61 (1992)
`Y. Barrios et al., Length of the Antibody Heavy Chain Complementarity
`Determining Region 3 as a Specificity-Determining Factor, J. Molecular
`Recognition 17:332-38 (2004)
`D. Bylund and M. Toews, Radioligand Binding Methods; Practical Guide and
`Tips, Am. J. Physiology 265(5): L421-29 (1993)
`D. Chelius et al., Identification and Characterization of Deamidation Sites in the
`Conserved Regions of Human Immunoglobulin Gamma Antibodies, Anal.
`Chem. 77(18): 6004-11 (2005)
`
`4/1/1990
`
`11/1/2002
`
`3/1/2004
`
`11/1/1994
`
`5/15/1992
`
`5/14/2004
`
`11/1/1993
`
`9/15/2005
`
`11
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 12 of 17
`
`5/1/2004
`
`3/1/2005
`
`4/1/1998
`
`4/1/2001
`
`12/1/1995
`
`8/1/2001
`
`5/1/1993
`
`9/1/1999
`
`1/1/1999
`
`8/21/1995
`
`10/8/1999
`
`6/1/2004
`
`1/1/2004
`
`1/1/1999
`
`1/7/1994
`
`1/1/2001
`1/1/2002
`8/1/1986
`
`3/1/1982
`1/1/2002
`
`10/15/2000
`
`F. Gala and S. Morrison, V Region Carbohydrate and Antibody Expression, J.
`Immunology 172: 5489-94 (2004)
`L. Huang et al., In Vivo Deamidation Characterization of Monoclonal Antibody
`by LC/MS/MS, Anal. Chem. 77(5): 1432-39 (2005)
`A. Jakobovits, The Long-Awaited Magic Bullets: Therapeutic Human
`Monoclonal Antibodies from Transgenic Mice, Exp. Opin. Invest. Drugs 7(4):
`607-14 (1998)
`M.-P. Lefranc, Nomenclature of the Human Immunoglobulin Lambda (IGL)
`Genes, Exp. Clin. Immunogenet. 18: 242-254 (2001)
`S. Li et al., Chemical Instability of Protein Pharmaceuticals: Mechanisms of
`Oxidation and Strategies for Stabilization, Biotechnology & Bioengineering 48:
`490-500 (1995)
`M. van Dijk and J. van de Winkel, Human Antibodies as Next Generation
`Therapeutics, Current Opinion in Chemical Biology 5:368-74 (2001)
`G. Winter and W. Harris, Antibody-Based Therapy - Humanized Antibodies,
`TIPS 14:139-143 (1993)
`F. Wisskirchen et al., Receptors Mediating CGRP-Induced Relaxation in the Rat
`Isolated Thoracic Aorta and Porcine Isolated Coronary Artery Differentiated by
`hα CGRP8-37, British J. of Pharmacology 128:283-292 (1999)
`L. Gilliland et al., Elimination of the Immunogenicity of Therapeutic Antibodies.
`J. Immunology 162: 3663-71 (1999)
`G. Hale, Synthetic Peptide Mimotope of the CAMPATH-1 (CD52) Antigen, a
`Small Glycosylphosphatidylinositol-Anchored Glycoprotein. Immunotechnology
`1:175-87 (1995)
`L. James et al., 1.9 A Structure of the Therapeutic Antibody CAMPATH-1H Fab
`in Complex with a Synthetic Peptide Antigen. J. Mol. Biol. 289: 293-301 (1999)
`W. Martanto et al., Transdermal Delivery of Insulin Using Microneedles In Vivo.
`Pharmaceutical Research 21(6): 947-52 (2004)
`M. Prausnitz, Microneedles for Transdermal Drug Delivery. Advanced Drug
`Delivery Reviews 56: 581-87 (2004)
`M. Co et al., Properties and Pharmacokinetics of Two Humanized Antibodies
`Specific for L-Selectin. Immunotechnology 4: 253-66 (1999)
`M. Sun et al., Antigen Recognition by an Antibody Light Chain. J. Biol. Chem.
`269(1): 734-38 (1994)
`Goodman & Gilman's The Pharmacological Basis of Therapeutics (10th ed.
`2001), Section 1 - General Principles pp. 1-2
`R. Aalberse et al., IgG4 breaking the rules, Immunology 105: 9-19 (2002)
`D. Covell et al., Pharmacokinetics of Monoclonal Immunoglobulin G1, F(ab')2,
`and Fab' in Mice, Cancer Research 46(8): 3969-3978 (August 1986)
`S. Rudikoff et al., Single amino acid substitution altering antigen-binding
`specificity, Proc. Natl. Acad. Sci. USA, 79:1979-1983, (1982)
`J. Berg et al., Chapter 3, Protein Structure and Function, BioChemistry, (2002)
`K. Winkler et al., Changing the Antigen Binding Specificity by Single Point
`Mutations of an Anti-p24 (HIV-1) Antibody, The Journal of Immunology,
`165:4505-14 (2000)
`
`12
`
`

`

`Case 1:18-cv-12029-ADB Document 490 Filed 09/19/22 Page 13 of 17
`
`4/1/1982
`
`2/1/2003
`
`1/1/2