`Yancopoulos
`
`US 11,253,572 B2
`( 10 ) Patent No .:
`( 45 ) Date of Patent :
`* Feb . 22 , 2022
`
`US011253572B2
`
`( 54 ) USE OF A VEGF ANTAGONIST TO TREAT
`ANGIOGENIC EYE DISORDERS
`( 71 ) Applicant : REGENERON
`PHARMACEUTICALS , INC . ,
`Tarrytown , NY ( US )
`( 72 ) Inventor : George Yancopoulos , Yorktown
`Heights , NY ( US )
`( 73 ) Assignee : REGENERON
`PHARMACEUTICALS , INC . ,
`Tarrytown , NY ( US )
`Subject to any disclaimer , the term of this
`patent is extended or adjusted under 35
`U.S.C. 154 ( b ) by 0 days .
`This patent is subject to a terminal dis
`claimer .
`( 21 ) Appl . No .: 17 / 352,892
`( 22 ) Filed :
`Jun . 21 , 2021
`( 65 )
`Prior Publication Data
`Oct. 7 , 2021
`US 2021/0308217 A1
`Related U.S. Application Data
`Continuation of application No. 17 / 350,958 , filed on
`Jun . 17 , 2021 , which is a continuation of application
`No. 17 / 112,404 , filed on Dec. 4 , 2020 , which is a
`continuation of application No. 17 / 072,417 , filed on
`Oct. 16 , 2020 , which is a continuation of application
`No. 16 / 055,847 , filed on Aug. 6 , 2018 , now Pat . No.
`10,857,205 , and a continuation of application No.
`16 / 397,267 , filed on Apr. 29 , 2019 , now Pat . No.
`10,888,601 , which is a continuation of application
`No. 16 / 159,282 , filed on Oct. 12 , 2018 , now Pat . No.
`10,828,345 , which is a continuation of application
`No. 15 / 471,506 , filed on Mar. 28 , 2017 , now Pat . No.
`10,130,681 , which is a continuation of application
`No. 14 / 972,560 , filed on Dec. 17 , 2015 , now Pat . No.
`9,669,069 , which is a continuation of application No.
`a
`13 / 940,370 , filed on Jul . 12 , 2013 , now Pat . No.
`9,254,338 , which is a continuation - in - part of
`application No. PCT / US2012 / 020855 , filed on Jan.
`11 , 2012 .
`Provisional application No. 61 / 432,245 , filed on Jan.
`13 , 2011 , provisional application No. 61 / 434,836 ,
`filed on Jan. 21 , 2011 , provisional application No.
`61 / 561,957 , filed on Nov. 21 , 2011 .
`( 51 ) Int . Cl .
`( 2006.01 )
`A61K 38/17
`( 2006.01 )
`COZK 14/71
`( 2006.01 )
`COZK 19/00
`( 2006.01 )
`CO7K 16/22
`( 2006.01 )
`A61K 9/00
`( 2006.01 )
`A61K 39/00
`U.S. Cl .
`A61K 38/179 ( 2013.01 ) ; A61K 9/0048
`CPC
`( 2013.01 ) ; C07K 14/71 ( 2013.01 ) ; C07K 16/22
`
`( 63 )
`
`.
`
`( * ) Notice :
`
`( 60 )
`
`( 52 )
`
`( 2013.01 ) ; A61K 2039/505 ( 2013.01 ) ; COOK
`2319/30 ( 2013.01 ) ; CO7K 2319/32 ( 2013.01 )
`( 58 ) Field of Classification Search
`None
`See application file for complete search history .
`
`( 56 )
`
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`
`( Continued )
`
`Primary Examiner Christine J Saoud
`Assistant Examiner - Jon M Lockard
`( 74 ) Attorney , Agent , or Firm — Thomas Triolo ; Karl
`Bozicevic
`
`( 57 )
`ABSTRACT
`The present invention provides methods for treating angio
`genic eye disorders by sequentially administering multiple
`doses of a VEGF antagonist to a patient . The methods of the
`present invention include the administration of multiple
`doses of a VEGF antagonist to a patient at a frequency of
`a
`once every 8 or more weeks . The methods of the present
`invention are useful for the treatment of angiogenic eye
`disorders such as age related macular degeneration , diabetic
`retinopathy , diabetic macular edema , central retinal vein
`occlusion , branch retinal vein occlusion , and corneal neo
`vascularization .
`
`30 Claims , 1 Drawing Sheet
`Specification includes a Sequence Listing .
`
`Samsung Bioepis Exhibit 1001 Page 1
`Biocon Exhibit 1001 Page 1
`
`
`
`US 11,253,572 B2
`Page 2
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`Biocon Exhibit 1001 Page 2
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`
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`istration of VEGF Trap in Patients With Neovascular Age - Related
`Macular Degeneration ” 70 pages , Latest version submitted Jun . 8 ,
`2011 on ClinicalTrials.gov ( NCT00320775_2006-2011 ) .
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`Study : NCT00320775 " Safety and Tolerability of Intravitreal Admin
`istration of VEGF Trap in Patients With Neovascular Age - Related
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`Study : NCT00320788 “ Safety and Efficacy of Repeated Intravitreal
`Administration of Vascular Endothelial Growth Factor ( VEGF )
`Trap in Patients With Wet Age - Related Macular Degeneration
`( AMD ) ” 71 pages , Latest version submitted Dec. 1 , 2011 on
`ClinicalTrials.gov ( NCT00320788_2006-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00320788 “ Safety and Efficacy of Repeated Intravitreal
`Administration of Vascular Endothelial Growth Factor ( VEGF )
`Trap in Patients With Wet Age - Related Macular Degeneration
`( AMD ) ” 31 pages , Latest version submitted Jan. 27 , 2012 on
`ClinicalTrials.gov ( NCT00320788_2012 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00320814 “ Phase 1 Study of VEGF Trap in Patients
`With Diabetic Macular Edema ” 30 pages , Latest version submitted
`Jun . 8 , 2011 on Clinical Trials.gov ( NCT00320814_2006-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00509795 “ Double - Masked Study of Efficacy and Safety
`of IVT VEGF Trap - Eye in Subjects With Wet AMD ( VIEW 1 ) ” 318
`pages , Latest version submitted Dec. 1 , 2011 on ClinicalTrials.gov
`( NCT00509795_2007-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00509795 “ Double - Masked Study of Efficacy and Safety
`of IVT VEGF Trap - Eye in Subjects With Wet AMD ( VIEW 1 ) " 200
`pages , Latest version submitted Dec. 20 , 2012 on ClinicalTrials.gov
`( NCT00509795_2012 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00527423 “ Randomized , Single - Masked , Long - Term ,
`
`*
`
`Samsung Bioepis Exhibit 1001 Page 3
`Biocon Exhibit 1001 Page 3
`
`
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`US 11,253,572 B2
`Page 4
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`( 56 )
`
`References Cited
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`pages , Latest version submitted Nov. 1 , 2011 on Clinical Trials.gov
`( NCT00527423_2007-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00527423 “ Randomized , Single - Masked , Long - Term ,
`Safety and Tolerability Study of VEGF Trap - Eye in AMD ” 42
`pages , Latest version submitted Jun . 10 , 2013 on Clinical Trials.gov
`( NCT00527423_2012-2013 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00637377 “ Vascular Endothelial Growth Factor ( VEGF )
`Trap - Eye : Investigation of Efficacy and Safety in Wet Age - Related
`Macular Degeneration ( AMD ) ( VIEW 2 ) ” 667 pages , Latest version
`submitted Dec. 16 , 2011 on ClinicalTrials.gov ( NCT00637377_
`2008-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00637377 “ Vascular Endothelial Growth Factor ( VEGF )
`Trap - Eye : Investigation of Efficacy and Safety in Wet Age - Related
`Macular Degeneration ( AMD ) ( VIEW 2 ) ” 289 pages , Latest version
`submitted Nov. 28 , 2014 on ClinicalTrials.gov ( NCT00637377_
`2012-2014 ) .
`Information from Clinical Trials.gov archive History of Changes for
`Study : NCT00789477 “ DME And VEGF Trap - Eye [ Intravitreal
`Aflibercept Injection ( IAI ; EYLEA® ; BAY86-5321 ) ] INvestigation
`of Clinical Impact ( DA VINCI ) ” 135 pages , Latest version submit
`ted May 2 , 2011 on Clinical Trials.gov ( NCT00789477_2008-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00789477 “ DME And VEGF Trap - Eye [ Intravitreal
`Aflibercept Injection ( IAI ; EYLEA® ; BAY86-5321 ) ] INvestigation
`of Clinical Impact ( DA VINCI ) " 53 pages , Latest version submitted
`Aug. 28 , 2014 on Clinical Trials.gov ( NCT00789477_2013-2014 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00943072 “ Vascular Endothelial Growth Factor ( VEGF )
`Trap - Eye : Investigation of Efficacy and Safety in Central Retinal
`Vein Occlusion ( CRVO ) ” 98 pages , Latest version submitted May
`9 , 2011 on ClinicalTrials.gov ( NCT00943072_2009-2011 ) .
`Information from ClinicalTrials.gov archive History of Changes for
`Study : NCT00943072 “ Vascular Endothelial Growth Factor ( VEGF )
`Trap - Eye : Investigation of Efficacy and Safety in Central Retinal
`Vein Occlusion ( CRVO ) ” 64 pages , Latest version submitted Apr.
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`
`2
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