Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 1 of 16 PageID #: 12589
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`IN THE UNITED STATES DISTRICT COURT
`FOR THE EASTERN DISTRICT OF TEXAS
`MARSHALL DIVISION
`
`SEAGEN INC.,
`
`Plaintiff,
`
`v.
`
`DAIICHI SANKYO CO., LTD.,
`
`Defendant,
`
`ASTRAZENECA PHARMACEUTICALS LP,
`AND ASTRAZENECA UK LTD.,
`
`
`Intervenor-Defendants.
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`Case No. 2:20-cv-00337-JRG
`
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`
`
`DEFENDANTS’ NOTICE PURSUANT TO 35 U.S.C. § 282
`
`Pursuant to 35 U.S.C. § 282, Defendant Daiichi Sankyo Company, Limited (“Daiichi
`
`Sankyo Japan”) and Intervenor-Defendants AstraZeneca Pharmaceuticals LP and AstraZeneca UK
`
`Ltd. (“AstraZeneca”) (collectively, “Defendants”), hereby identify the following materials that
`
`may be relied upon to invalidate U.S. Patent No. 10,808,039 (“the ’039 patent”) and/or show the
`
`state of the art relative to the asserted patent.
`
`Defendants have already provided notice to Plaintiff Seagen Inc. (“Seagen”) of the identity
`
`of certain publications, patents, and persons within the ambit of 35 U.S.C. § 282, through the
`
`pleadings and correspondence in this case, including but not limited to, invalidity contentions;
`
`expert witness reports; deposition testimony provided by party and non-party witnesses; exhibits
`
`introduced at deposition taken by the parties; Defendants’ response to interrogatories, request for
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`admission, and requests for production; documents produced in the litigation; Defendants’
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`disclosures under Rule 26; Defendants’ motion for summary judgment of anticipation; the parties’
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`1
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`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 2 of 16 PageID #: 12590
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`motions in limine and motions to strike briefing; the materials disclosed in Defendants’ trial exhibit
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`list; and/or the joint pre-trial order. Defendants expressly incorporate herein by reference all of
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`the publications, patents, patent applications, and specifications of persons within the ambit of 35
`
`U.S.C. § 282 previously cited in these pleadings, testimony, correspondence, and other materials.
`
`To the extent not listed above, Defendants also incorporate by reference all art listed on the face
`
`of the ’039 patent or identified in the prosecution history of that patent.
`
`Defendants may also rely on the patentees/authors of the patents and publications listed
`
`below. Pursuant to the statutory provisions of 35 U.S.C. § 282, Defendants further refer to the list
`
`of identified patents, publications, materials, and persons below. The inclusion of the references
`
`listed below in this notice should not be construed as a representation that Defendants will use
`
`every one of the references in its presentation of evidence at trial. Nor should it be understood or
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`taken as implied that reliance upon all of these materials is necessary to Defendants’ defenses.
`
`Additionally, Defendants reserve the right to amend and/or supplement this notice to add items to
`
`this statement that were inadvertently omitted.
`
`A.
`
`Patents, Patent Applications, and File Histories
`
`Exhibit No.
`
`Patent / Application No.
`
`DX-0073
`
`U.S. Patent Application Publication No.
`2016/0303254
`
`DX-0156
`
`U.S. Patent No. 11,116,847
`
`DX-0144
`
`U.S. Patent No. 8,871,720
`
`DX-0153
`
`U.S. Patent Application Publication No.
`2017/0247412
`
`DX-0209
`
`United States Patent No. 8,592,576
`
`DX-0238
`
`United States Patent No. 4,981,979
`
`Production No.
`DSC_ENHERTU_00015719
`DSC_ENHERTU_00015835
`
`DSC_ENHERTU_00390746
`DSC_ENHERTU_00390859
`
`DSC_ENHERTU_00390259
`DSC_ENHERTU_00390347
`
`DSC_ENHERTU_00390478
`DSC_ENHERTU_00390713
`
`DSC_ENHERTU_00391536
`DSC_ENHERTU_00391574
`
`DSC_ENHERTU_00395244
`DSC_ENHERTU_00395260
`
`2
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`

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`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 3 of 16 PageID #: 12591
`
`DX-0240
`
`United States Patent No. 5,525,338
`
`DX-0239
`
`United States Patent No. 5,024,834
`
`DX-0071
`
`DX-0208
`
`Excerpt from File History of U.S. Patent
`Application No. 12/016,978
`
`Excerpt from File History of U.S. Patent
`Application No. 12/016,978
`
`DSC_ENHERTU_00395271
`DSC_ENHERTU_00395284
`
`DSC_ENHERTU_00395261
`DSC_ENHERTU_00395270
`
`DSC_ENHERTU_00015710
`DSC_ENHERTU_00015714
`
`DSC_ENHERTU_00391528
`DSC_ENHERTU_00391535
`
`
`
`B.
`
`Publications
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0109
`
`
`DX-
`0110
`
`
`DX-
`0111
`
`
`DX-
`0078
`
`DX-
`0077
`
`DX-
`0082
`
`DX-
`0166
`
`Y. Ogitani et al., DS-8201a, A Novel HER2-
`Targeting ADC with a Novel DNA Topoisomerase I
`Inhibitor, Demonstrates a Promising Antitumor
`Efficacy with Differentiation from T-DM1, 22 CLIN.
`CANCER RES. 5097 (2016)
`Y. Ogitani et al., Bystander Killing Effect of DS-
`8201a, a Novel Anti-Human Epidermal Growth
`Factor Receptor 2 Antibody-Drug Conjugate, in
`Tumors with Human Epidermal Growth Factor
`Receptor 2 Heterogeneity, 107 CANCER SCI. 1039
`(2016)
`Y. Abe et al., Development of New ADC Technology
`with Topoisomerase I Inhibitor, in Antibody
`Engineering & Therapeutics 2015 (San Diego, CA)
`J. Lambert & C. Morris, Antibody-Drug Conjugates
`(ADCs) for
`Personalized Treatment of Solid Tumors: A Review,
`34 ADV. THER. 1015 (2017),
`A. Beck et al., Strategies and Challenges for the Next
`Generation of Antibody-Drug
`Conjugates, 16 NAT. REV. DRUG DISCOV. 315
`(2017),
`J. McCombs & S. Owen, Antibody Drug
`Conjugates: Design and Selection of Linker, Payload
`and Conjugation Chemistry, 17(2)
`AAPS J. 339 (2015),
`J. Tong et al., An Insight into FDA Approved
`Antibody-Drug Conjugates for Cancer Therapy, 26
`Molecules 5847 (2021)
`
`DSC_ENHERTU_00025303
`DSC_ENHERTU_00025315
`
`DSC_ENHERTU_00025316
`DSC_ENHERTU_00025326
`
`DSC_ENHERTU_00025327
`DSC_ENHERTU_00025327
`
`DSC_ENHERTU_00015910
`DSC_ENHERTU_00015930
`
`DSC_ENHERTU_00015887
`DSC_ENHERTU_00015909
`
`DSC_ENHERTU_00016046
`DSC_ENHERTU_00016058
`
`DSC_ENHERTU_00390993
`DSC_ENHERTU_00391015
`
`3
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 4 of 16 PageID #: 12592
`
`Exhibit
`No.
`
`DX-
`0186
`
`DX-
`0064
`
`DX-
`0204
`
`DX-
`0084
`
`DX-
`0083
`
`DX-
`0088
`
`DX-
`0072
`
`DX-
`0087
`
`DX-
`0093
`
`DX-
`0094
`
`DX-
`0104
`
`DX-
`0095
`
`Publication
`
`Production No.
`
`ADC Drugs with New Targets Clinical Pipeline
`Review, Biopharma PEG,
`https://www.biochempeg.com/article/202.html
`T. Nakada et al., The Latest Research and
`Development into the Antibody-Drug Conjugate,
`[fam-] Trastuzumab Deruxtecan (DS-8201a), for
`HER2 Cancer Therapy, 67 Chem. Pharm. Bull. 173
`(2019)
`L. Gauzy-Lazo et al., Advances in Antibody-Drug
`Conjugate Design: Current Clinical Landscape and
`Future Innovations, 25 SLAS Discovery 843 (2020)
`B. Nolting, Linker Technologies for Antibody-Drug
`Conjugates, 1045 Antibody-Drug Conjugates 71
`(2013)
`D. Leung et al., Antibody Conjugates-Recent
`Advances and Future Innovations, 9 Antibodies 2
`(2020)
`J. Lambert, Design Factors Important for Antibody-
`Drug Conjugate (ADC) Payloads, 71 Drug
`Discoveries 31 (2019)
`R. Kolakowski et al., The Methylene Alkoxy
`Carbamate Self-Immolative Unit: Utilization for the
`Targeted Delivery of Alcohol-Containing Payloads
`with Antibody-Drug Conjugates, 55 Angew. Chem.
`Int. Ed. 7948 (2016)
`J. Lambert, Drug-Conjugated Monoclonal Antibodies
`for the Treatment of Cancer, 5 Current Opinion
`Pharmacology 543 (2005)
`M. Dorywalska et al., Molecular Basis of Valine-
`Citrulline-PABC Linker Instability in Site-Specific
`ADCs and Its Mitigation by Linker Design, 15
`Molecular Cancer Therapeutics 958 (2016)
`Y. Anami, Glutamic Acid-Valine-Citrulline Linkers
`Ensure Stability and Efficacy of Antibody-Drug
`Conjugates in Mice, 9 Nature Communications 2512
`(2018)
`N. Caculitan et al., Cathepsin B is Dispensable for
`Cellular Processing of Cathepsin B-Cleavable
`Antibody-Drug Conjugates, 77 Cancer Research
`7027 (2017)
`M. Ritchie et al., Implications of Receptor-Mediated
`Endocytosis and Intracellular Trafficking Dynamics
`in the Development of Antibody Drug Conjugates, 5
`Landes Bioscience mAbs 13 (2013)
`
`DSC_ENHERTU_00391277
`DSC_ENHERTU_00391284
`
`DSC_ENHERTU_00011871
`DSC_ENHERTU_00011883
`
`DSC_ENHERTU_00391475
`DSC_ENHERTU_00391500
`
`DSC_ENHERTU_00016088
`
`DSC_ENHERTU_00016117
`
`DSC_ENHERTU_00016061
`DSC_ENHERTU_00016087
`
`DSC_ENHERTU_00016180
`DSC_ENHERTU_00016205
`
`DSC_ENHERTU_00015715
`DSC_ENHERTU_00015718
`
`DSC_ENHERTU_00016173
`DSC_ENHERTU_00016179
`
`DSC_ENHERTU_00016237
`DSC_ENHERTU_00016250
`
`DSC_ENHERTU_00016251
`DSC_ENHERTU_00016259
`
`DSC_ENHERTU_00016368
`DSC_ENHERTU_00016379
`
`DSC_ENHERTU_00016260
`DSC_ENHERTU_00016268
`
`4
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 5 of 16 PageID #: 12593
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0089
`
`DX-
`0085
`
`DX-
`0160
`
`DX-
`0096
`
`DX-
`0098
`
`DX-
`0099
`
`DX-
`0100
`
`DX-
`0097
`
`DX-
`0101
`
`DX-
`0102
`
`DX-
`0103
`
`DX-
`0196
`
`DX-
`0189
`
`DX-
`0151
`
`H. Tang et al., The Analysis of Key Factors Related
`to ADCs Structural Design, 10(373) Frontiers
`Pharmacology Art. (2019)
`W. Widdison et al., Factors Involved in the Design of
`Cytotoxic Payloads for Antibody-Drug Conjugates,
`Antibody-Drug Conjugates and Immunotoxins 93
`(2013)
`H. Donaghy, Effects of Antibody, Drug and Linker on
`the Preclinical and Clinical Toxicities of Antibody-
`Drug Conjugates, 8 mAbs 659 (2016)
`S. Yan et al., Molecular Regulation of Human
`Cathepsin B: Implication in Pathologies, 384 Biol.
`Chem. 845 (2003)
`S. Gao et al., Cathepsin G and Its Role in
`Inflammation and Autoimmune Diseases, 33 Arch.
`Rheumatol. 498 (2018)
`J. Reiser et al., Specialized Roles for Cysteine
`Cathepsins in Health and Disease, 120 J. Clin.
`Invest. 3421 (2010)
`H. Ruan et al., Targeting Cathepsin B for Cancer
`Therapies, 56 Horiz. Cancer Res. 23 (2015)
`
`E. Vidak et al., Cysteine Cathepsins and Their
`Extracellular Roles: Shaping the Microenvironment,
`8 Cells 264 (2019)
`Y. Kato et al., Acidic Extracellular
`Microenvironment and Cancer, 13 Cancer Cell Int.
`89 (2013)
`S. Kumari et al., New Insight on the Role of
`Plasminogen Receptor in Cancer Progression, 8
`Cancer Growth & Metastasis 35 (2015)
`Y. Cantres-Rosario et al., HIV Infection Induces
`Extracellular Cathepsin B Uptake and Damage to
`Neurons, 9 Scientific Reports (2019)
`Solid Tumor, NIH National Cancer Institute,
`https://www.cancer.gov/publications/dictionaries/can
`cer-terms/def/solid-tumor
`Definition of blood cancer, Cancer.gov,
`https://www.cancer.gov/publications/dictionaries/can
`cer-terms/def/blood-cancer
`A. Dean et al., Targeting Cancer with Antibody-Drug
`Conjugates: Promises and Challenges, 13(1) mAbs
`(2021)
`
`DSC_ENHERTU_00016206
`DSC_ENHERTU_00016216
`
`DSC_ENHERTU_00016118
`DSC_ENHERTU_00016140
`
`DSC_ENHERTU_00390929
`DSC_ENHERTU_00390942
`
`DSC_ENHERTU_00016269
`DSC_ENHERTU_00016278
`
`DSC_ENHERTU_00016303
`DSC_ENHERTU_00016309
`
`DSC_ENHERTU_00016310
`DSC_ENHERTU_00016321
`
`DSC_ENHERTU_00016322
`DSC_ENHERTU_00016333
`
`DSC_ENHERTU_00016279
`DSC_ENHERTU_00016302
`
`DSC_ENHERTU_00016339
`DSC_ENHERTU_00016346
`
`DSC_ENHERTU_00016347
`DSC_ENHERTU_00016354
`
`DSC_ENHERTU_00016355
`DSC_ENHERTU_00016367
`
`DSC_ENHERTU_00391404
`DSC_ENHERTU_00391404
`
`DSC_ENHERTU_00391315
`DSC_ENHERTU_00391315
`
`DSC_ENHERTU_00390449
`DSC_ENHERTU_00390472
`
`5
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 6 of 16 PageID #: 12594
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0183
`
`DX-
`0143
`
`DX-
`0171
`
`DX-
`0188
`
`DX-
`0148
`
`DX-
`0203
`
`DX-
`0150
`
`DX-
`0213
`
`DX-
`0215
`
`DX-
`0164
`
`DX-
`0140
`
`DX-
`0145
`
`J. Masters et al., Clinical Toxicity of Antibody Drug
`Conjugates: A Meta-Analysis of Payloads, 36 Invest
`New Drugs 121 (2018)
`S. Chuprakov et al., Tandem-Cleavage Linkers
`Improve the In Vivo Stability and Tolerability of
`Antibody-Drug Conjugates, 32 Bioconjugate Chem.
`746 (2021)
`O. Trédan et al., Drug Resistance and the Solid
`Tumor Microenvironment, 99 J. Nat'l Cancer Inst.
`1441 (2007)
`K. Fenn et al., Sacituzumab Govitecan: Antibody-
`Drug Conjugate in Triple Negative Breast Cancer
`and Other Solid Tumors, 55 Drugs Today 575 (2019)
`S. Kaur et al., Bioanalytical Assay Strategies for the
`Development of Antibody-Drug Conjugate
`Biotherapeutics, 5 Bioanalysis 201 (2013)
`O. Saad et al., Bioanalytical Approaches for
`Characterizing Catabolism of Antibody-Drug
`Conjugates, 7(13) Bioanalysis 1583 (2015)
`D. Su et al., Linker Design Impacts Antibody-Drug
`Conjugate Pharmacokinetics and Efficacy via
`Modulating the Stability and Payload Release
`Efficiency, 12 Frontiers in Pharmacology (2021)
`G. Dubowchik et al., Cathepsin B-Sensitive Dipeptide
`Prodrugs. 2. Models of Anticancer Drugs Paclitaxel
`(Taxol®), Mitomycin C and Doxorubicin, 8
`Bioorganic Medicinal Chemistry Letters 3347 (1998)
`G. Dubowchik et al., Cathepsin B-Sensitive Dipeptide
`Prodrugs. 1. A Model Study of Structural
`Requirements for Efficient Release of Doxorubicin, 8
`Bioorganic Medicinal Chemistry Letters 3341 (1998)
`S. Doronina et al., Development of Potent
`Monoclonal Antibody Auristatin Conjugates for
`Cancer Therapy, 21 Nature Biotechnology 778
`(2003)
`S. Jordans et al., Monitoring Compartment-Specific
`Substrate Cleavage by Cathepsins B, K, L, and S at
`Physiological pH and Redox Conditions, 10 BMC
`Biochemistry 23 (2009)
`T. Kaillunki et al., Cancer-Associated Lysosomal
`Changes: Friends or Foes?, 32 Oncogene 1995
`(2013)
`
`DSC_ENHERTU_00391231
`DSC_ENHERTU_00391245
`
`DSC_ENHERTU_00390250
`DSC_ENHERTU_00390258
`
`DSC_ENHERTU_00391073
`DSC_ENHERTU_00391086
`
`DSC_ENHERTU_00391301
`DSC_ENHERTU_00391314
`
`DSC_ENHERTU_00390405
`DSC_ENHERTU_00390430
`
`DSC_ENHERTU_00391453
`DSC_ENHERTU_00391474
`
`DSC_ENHERTU_00390441
`DSC_ENHERTU_00390448
`
`DSC_ENHERTU_00391625
`DSC_ENHERTU_00391630
`
`DSC_ENHERTU_00391635
`DSC_ENHERTU_00391640
`
`DSC_ENHERTU_00390971
`DSC_ENHERTU_00390978
`
`DSC_ENHERTU_00390223
`DSC_ENHERTU_00390237
`
`DSC_ENHERTU_00390348
`DSC_ENHERTU_00390357
`
`6
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 7 of 16 PageID #: 12595
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0185
`
`DX-
`0155
`
`DX-
`0074
`
`DX-
`0207
`
`DX-
`0175
`
`DX-
`0158
`
`DX-
`0070
`
`DX-
`0179
`
`DX-
`0205
`
`DX-
`0079
`
`DX-
`0176
`
`DX-
`0202
`
`M. Barok et al., Trastuzumab Emtansine:
`Mechanisms of Action and Drug Resistance, 16
`Breast Cancer Research 209 (2014)
`Y. Tai et al., Novel Anti-B-Cell Maturation Antigen
`Antibody-Drug Conjugate (GSK2857916) Selectively
`Induces Killing of Multiple Myeloma, 123 Blood
`3128 (2014)
`R. Singh et al., A New Triglycyl Peptide Linker for
`Antibody-Drug Conjugates (ADCs) with Improved
`Targeted Killing of Cancer Cells, 15 Mol. Cancer
`Ther. 1311 (2016)
`B. Gorovits et al., Bioanalysis of Antibody-Drug
`Conjugates: American Association of
`Pharmaceutical Scientists Antibody-Drug Conjugate
`Working Group Position Paper, 5 Bioanalysis 997
`(2013)
`J. Atzrodt et al., Synthesis of Radiolabelled
`Compounds for Clinical Studies, Drug Discovery and
`Evaluation: Methods in Clinical Pharmacology 807
`(2020)
`V. Kostova et al., The Chemistry Behind ADCs, 14
`Pharmaceuticals 442 (2021)
`
`J. Lambert et al., Ado-trastuzumab Emtansine (T-
`DM1): An Antibody-Drug Conjugate (ADC) for
`HER2-Positive Breast Cancer, 57 J. Med. Chem.
`6949 (2014)
`C. Liu et al., Eradication of Large Colon Tumor
`Xenografts by Targeted Delivery of Maytansinoids,
`93 Proc. Natl. Acad. Sci. 8618 (1996)
`R. Chari et al., Immunoconjugates Containing Novel
`Maytansinoids: Promising Anticancer Drugs, 52
`Cancer Research 127 (1992)
`V. Goldmacher et al., Immunotoxins and Antibody-
`Drug Conjugates for Cancer Treatment, Biomedical
`Aspects of Drug Targeting 291 (2002)
`G. Phillips et al., Targeting HER2-Positive Breast
`Cancer with Trastuzumab-DM1, an Antibody-
`Cytotoxic Drug Conjugate, 68 Cancer Res. 9280
`(2008)
`J. Cassady et al., Recent Developments in the
`Maytansinoid Antitumor Agents, 52 Chem. Pharm.
`Bull. (2004)
`
`DSC_ENHERTU_00391253
`DSC_ENHERTU_00391264
`
`DSC_ENHERTU_00390735
`DSC_ENHERTU_00390745
`
`DSC_ENHERTU_00015845
`DSC_ENHERTU_00015855
`
`DSC_ENHERTU_00391518
`DSC_ENHERTU_00391527
`
`DSC_ENHERTU_00391128
`DSC_ENHERTU_00391146
`
`DSC_ENHERTU_00390866
`DSC_ENHERTU_00390911
`
`DSC_ENHERTU_00015694
`DSC_ENHERTU_00015709
`
`DSC_ENHERTU_00391178
`DSC_ENHERTU_00391183
`
`DSC_ENHERTU_00391501
`DSC_ENHERTU_00391507
`
`DSC_ENHERTU_00015931
`DSC_ENHERTU_00015949
`
`DSC_ENHERTU_00391147
`DSC_ENHERTU_00391158
`
`DSC_ENHERTU_00391427
`DSC_ENHERTU_00391452
`
`7
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 8 of 16 PageID #: 12596
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0069
`
`DX-
`0182
`
`DX-
`0174
`
`DX-
`0193
`
`DX-
`0187
`
`DX-
`0192
`
`DX-
`0198
`
`DX-
`0138
`
`DX-
`0130
`
`DX-
`0178
`
`DX-
`0201
`
`DX-
`0142
`
`DX-
`0177
`
`A. Tolcher, Antibody Drug Conjugates: Lessons from
`20 Years of Clinical Experience, 27(12) Ann. Oncol.
`2168 (2016)
`J. Wright et al., Summary of Results with Triethylene
`Thiophosphoramide, 68 Annals. N.Y. Acad. Sci. 937
`(1958)
`G. Vassal et al., Dose-Dependent Neurotoxicity of
`High-Dose Busulfan in Children: A Clinical and
`Pharmacological Study, 50 Cancer Research 6203
`(1990)
`A. Reese et al., Treatment of Retinoblastoma by
`Radiation and Triethylenemelamine, 53 A.M.A.
`Archives of Ophthalmology 505 (1954)
`A. Pardee et al., Cancer Therapy with ß-Lapachone,
`2(3) Current Cancer Drug Targets 227 (2002)
`
`National Cancer Institute, CHOP regimen,
`https://www.cancer.gov/publications/dictionaries/can
`cer-terms/def/chop-regimen
`FOLFOX, NIH National Cancer Institute,
`https://www.cancer.gov/about cancer/
`treatment/drugs/folfox
`C. Chitambar, Gallium Nitrate Revisited, 30(2)
`Seminars in Oncology (2003)
`
`L. Hansen et al., Altretamine, 25 Annals of
`Pharmacotherapy 146 (1991)
`
`M. Wall et al., The Effects of Some Steroidal
`Alkylating Agents on Experimental Animal Mammary
`Tumor and Leukemia Systems, J. Med. Chem.,
`12:810 (1969)
`Paclitaxel Albumin-stabilized Nanoparticle
`Formulation, National Cancer Institute,
`https://www.cancer.gov/about-
`cancer/treatment/drugs/nanoparticlepaclitaxel
`M. Studer et al., Influence of a Peptide Linker on
`Biodistribution and Metabolism of Antibody-
`Conjugated Benzyl-EDTA. Comparison of Enzymatic
`Digestion in Vitro and in Vivo, 3 Bioconjugate Chem.
`424 (1992)
`R. Duncan et al., Anticancer agents coupled to N-(2-
`hydroxypropyl)methacrylamide copolymers. II.
`Evaluation of daunomycin conjugates in vivo against
`L1210 leukaemia, 57 Br. J. Cancer 147 (1988)
`
`DSC_ENHERTU_00015689
`DSC_ENHERTU_00015693
`
`DSC_ENHERTU_00391201
`DSC_ENHERTU_00391230
`
`DSC_ENHERTU_00391122
`DSC_ENHERTU_00391127
`
`DSC_ENHERTU_00391349
`DSC_ENHERTU_00391361
`
`DSC_ENHERTU_00391285
`DSC_ENHERTU_00391300
`
`DSC_ENHERTU_00391348
`DSC_ENHERTU_00391348
`
`DSC_ENHERTU_00391417
`DSC_ENHERTU_00391417
`
`DSC_ENHERTU_00390207
`DSC_ENHERTU_00390211
`
`DSC_ENHERTU_00390140
`DSC_ENHERTU_00390146
`
`DSC_ENHERTU_00391169
`DSC_ENHERTU_00391177
`
`DSC_ENHERTU_00391425
`DSC_ENHERTU_00391426
`
`DSC_ENHERTU_00390244
`DSC_ENHERTU_00390249
`
`DSC_ENHERTU_00391159
`DSC_ENHERTU_00391168
`
`8
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 9 of 16 PageID #: 12597
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0214
`
`DX-
`0090
`
`DX-
`0068
`
`DX-
`0091
`
`DX-
`0092
`
`DX-
`0199
`
`DX-
`0157
`
`DX-
`0163
`
`DX-
`0131
`
`DX-
`0168
`
`DX-
`0133
`
`DX-
`0200
`
`G. Dubowchik et al., Doxorubicin Immunoconjugates
`Containing Bivalent, Lysosomally-Cleavable
`Dipeptide Linkages, 12 Bioorganic Medicinal
`Chemistry Letters 1529 (2002)
`M. Akaiwa et al., Antibody-Drug Conjugate
`Payloads; Study of Auristatin Derivatives, 68(3)
`Chem. Pharm. Bull. 201 (2020)
`N. Joubert et al., Antibody-Drug Conjugates: The
`Last Decade, 13(9) Pharmaceuticals 245 (2020)
`
`K. Norsworthy et al., FDA Approval Summary:
`Mylotarg for Treatment of Patients with Relapsed or
`Refractory CD33-Positive Acute Myeloid Leukemia,
`23 Oncologist 1103 (2018)
`R. Chari, Expanding the Reach of Antibody-Drug
`Conjugates, 7 ACS Medicinal Chemistry Letters 974
`(2016)
`P. Carl et al., Communications to the Editor: A Novel
`Connector Linkage Applicable in Prodrug Design, 24
`J. Med. Chem. 479 (1981)
`B. Teicher et al., Nitrobenzyl Halides and
`Carbamates as Prototype Bioreductive Alkylating
`Agents, 23 J. Med. Chem. 955 (1980)
`B. Toki et al., Protease-Mediated Fragmentation of
`p-Amidobenzyl Ethers: A New Strategy for the
`Activation of Anticancer Prodrugs, 67 J. Organic
`Chem. 1866 (2002)
`R. Chari et al., Enhancement of the Selectivity and
`Antitumor Efficacy of a CC-1065 Analogue through
`Immunoconjugate Formation, 55 Cancer Research
`4079 (1995)
`S. Doronina et al., Enhanced Activity of
`Monomethylauristatin F Through Monoclonal
`Antibody Delivery: Effects of Linker Technology on
`Efficacy and Toxicity, 17 Bioconjugate Chem. 114
`(2006)
`M. Hay et al., A 2-Nitroimidazole Carbamate
`Prodrug of 5-Amino-1-(Chloromethyl)-3-[(5,6,7-
`Trimethoxyindol-2-yl)carbonyl]-1,2-Dihydro-3H-
`Benz[e]indole (Amino-seco-cbi-tmi)
`for use with ADEPT and GDEPT, 9 Bioorganic &
`Medicinal Chemistry Letters 2237 (1999)
`M. Rodrigues et al., Synthesis and ß-lactamase-
`mediated activation of a cephalosporin-taxol
`prodrug, 2 Chemistry & Biology 223 (1995)
`
`DSC_ENHERTU_00391631
`DSC_ENHERTU_00391634
`
`DSC_ENHERTU_00016217
`DSC_ENHERTU_00016227
`
`DSC_ENHERTU_00015637
`DSC_ENHERTU_00015667
`
`DSC_ENHERTU_00016228
`DSC_ENHERTU_00016233
`
`DSC_ENHERTU_00016234
`DSC_ENHERTU_00016236
`
`DSC_ENHERTU_00391418
`DSC_ENHERTU_00391419
`
`DSC_ENHERTU_00390860
`DSC_ENHERTU_00390865
`
`DSC_ENHERTU_00390962
`DSC_ENHERTU_00390970
`
`DSC_ENHERTU_00390147
`DSC_ENHERTU_00390153
`
`DSC_ENHERTU_00391036
`DSC_ENHERTU_00391056
`
`DSC_ENHERTU_00390159
`DSC_ENHERTU_00390164
`
`DSC_ENHERTU_00391420
`DSC_ENHERTU_00391424
`
`9
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 10 of 16 PageID #: 12598
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0139
`
`DX-
`0170
`
`DX-
`0152
`
`DX-
`0219
`
`DX-
`0141
`
`DX-
`0137
`
`DX-
`0128
`
`DX-
`0149
`
`DX-
`0135
`
`DX-
`0132
`
`D. Storm et al., Effect of Small Changes in
`Orientation on Reaction Rate, 94 J. Amer. Chem.
`Soc. 5815 (1972)
`K. Amsberry et al., The Lactonization of 2’-
`Hydroxyhydrocinnamic Acid Amides: A Potential
`Prodrug for Amines, 55 J. Org. Chem. 5867 (1990)
`W. Kingsbury et al., A Novel Peptide Delivery System
`Involving Peptidase Activated Prodrugs as
`Antimicrobial Agents. Synthesis and Biological
`Activity of Peptidyl Derivatives of 5-Fluorouracil, 26
`J. Med. Chem. 1447 (1984)
`W. Widdison et al., Development of Anilino-
`Maytansinoid ADCs that Efficiently Release
`Cytotoxic Metabolites in Cancer Cells and Induce
`High Levels of Bystander Killing, 26 Bioconjugate
`Chemistry 2261 (2015)
`Y. Ueda et al., Novel, Water-Soluble Phosphate
`Derivatives of 2’-Ethoxy Carbonylpaclitaxel as
`Potential Prodrugs of Paclitaxel: Synthesis and
`Antitumor Evaluation, 5(3) Bioorganic & Medicinal
`Chemistry Letters 247 (1995)
`P. Senter et al., The Role of Rat Serum
`Carboxylesterase in the Activation of Paclitaxel and
`Camptothecin Prodrugs, 56 Cancer Research 1471
`(1996)
`P. Burke et al., Development of Novel Quarternary
`Ammonium Linkers for Antibody-Drug Conjugates,
`15(5) Molecular Cancer Therapeutics 938 (2016)
`
`H. Xie et al., Pharmacokinetics and Biodistribution
`of the Antitumor Immunoconjugate, Cantuzumab
`Mertansine (huC242-DM1), and Its Two Components
`in Mice, 308(3) J. Pharmacology & Experimental
`Therapeutics 1073 (2004)
`S. Jeffrey et al., A Potent Anti-CD70 Antibody-Drug
`Conjugate Combining a Dimeric
`Pyrrolobenzodiazepine Drug with Site-Specific
`Conjugation Technology, 24 Bioconjugate Chemistry
`1256 (2013)
`A. Tiberghien et al., Design and Synthesis of
`Tesirine, A Clinical Antibody-Drug Conjugate
`Pyrrolobenzodiazepine Dimer Payload, 7 ACS
`Medicinal Chemistry Letters 983 (2016)
`
`DSC_ENHERTU_00390212
`DSC_ENHERTU_00390222
`
`DSC_ENHERTU_00391062
`DSC_ENHERTU_00391072
`
`DSC_ENHERTU_00390473
`DSC_ENHERTU_00390477
`
`DSC_ENHERTU_00391673
`DSC_ENHERTU_00391690
`
`DSC_ENHERTU_00390238
`DSC_ENHERTU_00390243
`
`DSC_ENHERTU_00390202
`DSC_ENHERTU_00390206
`
`DSC_ENHERTU_00390124
`DSC_ENHERTU_00390132
`
`DSC_ENHERTU_00390431
`DSC_ENHERTU_00390440
`
`DSC_ENHERTU_00390187
`DSC_ENHERTU_00390194
`
`DSC_ENHERTU_00390154
`DSC_ENHERTU_00390158
`
`10
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 11 of 16 PageID #: 12599
`
`Exhibit
`No.
`
`Publication
`
`Production No.
`
`DX-
`0194
`
`DX-
`0220
`
`DX-
`0216
`
`DX-
`0169
`
`DX-
`0075
`
`DX-
`0136
`
`DX-
`0195
`
`DX-
`0191
`
`DX-
`0161
`
`DX-
`0197
`
`DX-
`0206
`
`A. Bharadwaj et al., Plasmin and Plasminogen
`System in the Tumor Microenvironment: Implications
`for Cancer Diagnosis, Prognosis, and Therapy, 13
`Cancers 1838 (2021)
`R. Lyon et al., Reducing Hydrophobicity of
`Homogeneous Antibody-Drug Conjugates Improves
`Pharmacokinetics and Therapeutic Index, 33 Nature
`Biotechnology 733 (2015)
`K. Hamblett et al., SLC46A3 Is Require to Transport
`Catabolites of Noncleavable Antibody Maytansine
`Conjugates from the Lysosome to the Cytoplasm, 75
`Cancer Research 5329 (2015)
`J. Lambert, Drug-Conjugated Antibodies for the
`Treatment of Cancer, 76(2) British J. Clinical
`Pharmacology 248 (2012)
`E. Kraynov et al., Current Approaches for
`Absorption, Distribution, Metabolism, and Excretion
`Characterization of Antibody-Drug Conjugates: An
`Industry White Paper, 44 Drug Metab. Dispos. 617
`(2016)
`A. Staudacher et al., Antibody Drug Conjugates and
`Bystander Killing: Is Antigen-Dependent
`Internalisation Required? 117 Brit. J. Cancer 1736
`(2017)
`J. Francisco et al., cAC10-vcMMAE, an Anti-CD30-
`Monomethyl Auristatin E Conjugate with Potent and
`Selective Antitumor Activity, 102(4) Blood 1458
`(2003)
`C. Fennelly et al., Lysosomal Biology in Cancer,
`1594 Methods Mol. Biol. 293 (2017)
`
`Y. Kovtun et al., Antibody-Drug Conjugates
`Designed to Eradicate Tumors with Homogeneous
`and Heterogeneous Expression of the Target Antigen,
`66 Cancer Res. 3214 (2006)
`M. Birrer et al., Antibody-Drug Conjugate-Based
`Therapeutics: State of the Science, 111(6) J. Natl.
`Cancer Inst. 538 (2019)
`D. Goldenberg et al., Antibody-Drug Conjugates
`Targeting TROP-2 and Incorporating SN-38: A Case
`Study of Anti-TROP-2 Sacituzumab Govitecan, 11(6)
`mAbs 987 (2019)
`
`DSC_ENHERTU_00391362
`DSC_ENHERTU_00391395
`
`DSC_ENHERTU_00391691
`DSC_ENHERTU_00391694
`
`DSC_ENHERTU_00391641
`DSC_ENHERTU_00391653
`
`DSC_ENHERTU_00391047
`DSC_ENHERTU_00391061
`
`DSC_ENHERTU_00015856
`DSC_ENHERTU_00015862
`
`DSC_ENHERTU_00390195
`DSC_ENHERTU_00390201
`
`DSC_ENHERTU_00391396
`DSC_ENHERTU_00391403
`
`DSC_ENHERTU_00391332
`DSC_ENHERTU_00391347
`
`DSC_ENHERTU_00390943
`DSC_ENHERTU_00390951
`
`DSC_ENHERTU_00391405
`DSC_ENHERTU_00391416
`
`DSC_ENHERTU_00391508
`DSC_ENHERTU_00391517
`
`11
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 12 of 16 PageID #: 12600
`
`Exhibit
`No.
`
`DX-
`0181
`
`DX-
`0134
`
`DX-
`0154
`
`DX-
`0076
`
`DX-
`0080
`
`DX-
`0081
`
`DX-
`0184
`
`DX-
`0086
`
`DX-
`0146
`
`DX-
`0147
`
`DX-
`0190
`
`
`
`Publication
`
`Production No.
`
`H. Erickson et al., The Effect of Different Linkers on
`Target Cell Catabolism and
`Pharmacokinetics/Pharmacodynamics of
`Trastuzumab Maytansinoid Conjugates, 11
`Molecular Cancer Therapy 1133 (2012)
`R. Chari, Targeted Delivery of Chemotherapeutics:
`Tumor-Activated Prodrug
`Therapy, 31 ADV. DRUG DELIVERY REV. 89
`(1998)
`W. Dokter et al., Preclinical Profile of the HER2-
`Targeting ADC SYD983/SYD985:
`Introduction of a New Duocarmycin-Based Linker-
`Drug Platform, 13 MOL. CANCER
`THER. (2014)
`P. Carter & P. Senter, Antibody-Drug Conjugates for
`Cancer Therapy, 14 CANCER J. 154 (2008)
`
`M. Chiu et al., Antibody Structure and Function: The
`Basis for Engineering Therapeutics, 8 Antibodies 55
`(2019)
`Y. Houzong, Methods to Design and Synthesize
`Antibody-Drug Conjugates (ADCs), 17 Int. J. Mol.
`Sci. 194 (2016)
`S. Fargion et al., Heterogeneity of Cell Surface
`Antigen Expression of Human Small Cell Lung
`Cancer Detected by Monoclonal Antibodies, 46
`Cancer Research 2633 (1986)
`R. Chari et al., Antibody-Drug Conjugates: An
`Emerging Concept in Cancer Therapy, 53 Angew.
`Chem. Int. Ed. 3796 (2014)
`T. Stylianopoulos et al., Reengineering the Physical
`Microenvironment of Tumors to Improve Drug
`Delivery and Efficacy: From Mathematical Modeling
`to Bench to Bedside, 4(4) Trends in Cancer 292
`(2018)
`E. Cruz et al., Monoclonal Antibody Therapy of Solid
`Tumors: Clinical Limitations and Novel Strategies to
`Enhance Treatment Efficacy, 13 Biologics Targets &
`Therapy 33 (2019)
`K. Poon et al., Preclinical Safety Profile of
`Trastuzumab Emtansine (T-DM1): Mechanism of
`Action of its Cytotoxic Component Retained with
`Improved Tolerability, 273 Toxicology & Applied
`Pharmacology 298 (2013)
`
`DSC_ENHERTU_00391190
`DSC_ENHERTU_00391200
`
`DSC_ENHERTU_00390171
`DSC_ENHERTU_00390186
`
`DSC_ENHERTU_00390714
`DSC_ENHERTU_00390726
`
`DSC_ENHERTU_00015871
`DSC_ENHERTU_00015886
`
`DSC_ENHERTU_00015950
`DSC_ENHERTU_00016029
`
`DSC_ENHERTU_00016030
`DSC_ENHERTU_00016045
`
`DSC_ENHERTU_00391246
`DSC_ENHERTU_00391252
`
`DSC_ENHERTU_00016141
`DSC_ENHERTU_00016172
`
`DSC_ENHERTU_00390358
`DSC_ENHERTU_00390385
`
`
`DSC_ENHERTU_00390386
`DSC_ENHERTU_00390404
`
`DSC_ENHERTU_00391316
`DSC_ENHERTU_00391331
`
`12
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 13 of 16 PageID #: 12601
`
`Exhibit
`No.
`DX-
`0172
`
`DX-
`0167
`
`DX-
`0212
`
`DX-
`0129
`
`DX-
`0173
`
`DX-
`0180
`
`DX-
`0217
`
`
`
`Publication
`
`Production No.
`
`J. Lambert, Typical Antibody-Drug Conjugates, 13
`Antibody-Drug Conjugates 3 (2017)
`
`DSC_ENHERTU_00391087
`DSC_ENHERTU_00391117
`
`J. Lambert & A. Berkenblit, Antibody-Drug
`Conjugates for Cancer Treatment, 69 Ann. Rev.
`Med. 191 (2018)
`S. Ponziani et al., Antibody-Drug Conjugates: The
`New Frontier of Chemotherapy, 21 Int. J. Mol. Sci.
`5510 (2020)
`P. Senter et al., The Discovery and Development of
`Brentuximab Vedotin for Use in Relapsed Hodgkin
`Lymphoma and Systemic Anaplastic Large Cell
`Lymphoma, 30(7) Nature Biotechnology 631 (2012)
`S. Doronina et al., Novel Peptide Linkers for Highly
`Potent Antibody-Auristatin Conjugate, 19
`Bioconjugate Chem. 1960 (2008)
`J. Bargh et al., Sulfatase-Cleavable Linkers for
`Antibody-Drug Conjugates, 11 Chem. Sci. 2375
`(2020)
`J. Peterson & C. Meares, Enzymatic Cleavage of
`Peptide-Linked Radiolabels from
`Immunoconjugates,10(4) Bioconjugate Chem. 618
`(1998)
`
`DSC_ENHERTU_00391016
`DSC_ENHERTU_00391035
`
`DSC_ENHERTU_00391599
`DSC_ENHERTU_00391624
`
`DSC_ENHERTU_00390133
`DSC_ENHERTU_00390139
`
`DSC_ENHERTU_00391118
`DSC_ENHERTU_00391121
`
`DSC_ENHERTU_00391184
`DSC_ENHERTU_00391189
`
`DSC_ENHERTU_00391664
`DSC_ENHERTU_00391668
`
`C.
`
`Persons Upon Whom Defendants May Rely
`
`All patentees, applicants, and authors of the patents and publications listed above.
`
`
`
`13
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 14 of 16 PageID #: 12602
`
`Dated: March 4, 2022
`
`
`Respectfully submitted,
`
`/s/ Deron R. Dacus
`(with permission by Jennifer P. Ainsworth)
`Deron R. Dacus
`State Bar No. 00790553
`The Dacus Firm, P.C.
`821 ESE Loop 323, Suite 430
`Tyler, Texas, 75701
`+1 (903) 705-1117
`+1 (903) 581-2543 facsimile
`ddacus@dacusfirm.com
`
`J. Mark Mann
`State Bar No. 12926150
`mark@themannfirm.com
`MANN | TINDEL | THOMPSON
`300 West Main Street
`Henderson, Texas 75652
`(903) 657-8540
`(903) 657-6003 (fax)
`
`Attorneys for Defendant Daiichi Sankyo Company,
`Limited
`
`Of Counsel:
`
`Preston K. Ratliff II
`Ashley N. Mays-Williams
`Paul Hastings LLP
`200 Park Avenue
`New York, NY 10166
`(212) 318-6000
`
`Jeffrey A. Pade
`Paul Hastings LLP
`2050 M Street NW
`Washington, DC 20036
`(202) 551-1700
`
`Attorneys for Defendant Daiichi Sankyo Company,
`Limited
`
`
`
`
`
`
`14
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 15 of 16 PageID #: 12603
`
`/s/ Jennifer Parker Ainsworth
`Jennifer Parker Ainsworth
`Texas State Bar No. 00784720
`WILSON, ROBERTSON & CORNELIUS, P.C.
`909 ESE Loop 323, Suite 400
`Tyler, Texas 75701
`Phone: (903) 509-5000
`Facsimile: (903) 509-5092
`
`Attorneys for Intervenor-Defendants AstraZeneca
`Pharmaceuticals LP and AstraZeneca UK Ltd
`
`Of Counsel:
`
`David I. Berl
`Thomas S. Fletcher
`Jessamyn Berniker
`Jessica L. Pahl
`Kathryn Kayali
`Kevin Hoagland-Hanson
`Angela X. Gao
`WILLIAMS & CONNOLLY LLP
`725 Twelfth Street, N.W.
`Washington, DC 20005
`Phone: (202) 434-5000
`Facsimile: (202) 434-5029
`
`Attorneys for Intervenor-Defendants AstraZeneca
`Pharmaceuticals LP and AstraZeneca UK Ltd
`
`
`
`15
`
`

`

`Case 2:20-cv-00337-JRG Document 346 Filed 03/04/22 Page 16 of 16 PageID #: 12604
`
`CERTIFICATE OF SERVICE
`
`I hereby certify that a true and correct copy of the foregoing document was filed
`
`electronically in compliance with L.R. CV-5 on March 4, 2022. As of this date, all counsel of
`
`record had consented to electronic service and are being served with a copy of this document
`
`through the Court’s CM/ECF system under L.R. CV-5(a)(3)(A).
`
`
`
`
`
`
`
`
`
`
`
`/s/ Jennifer