CA2961739C - Lyophilized formulations for factor xa antidote - Google Patents

Lyophilized formulations for factor xa antidote Download PDF

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Publication number
CA2961739C
CA2961739C CA2961739A CA2961739A CA2961739C CA 2961739 C CA2961739 C CA 2961739C CA 2961739 A CA2961739 A CA 2961739A CA 2961739 A CA2961739 A CA 2961739A CA 2961739 C CA2961739 C CA 2961739C
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CA
Canada
Prior art keywords
seq
formulation
arginine
mannitol
sucrose
Prior art date
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Active
Application number
CA2961739A
Other languages
English (en)
French (fr)
Other versions
CA2961739A1 (en
Inventor
Juan Wang
Gregory A. Sacha
Phuong M. Nguyen
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Alexion Pharmaceuticals Inc
Original Assignee
Alexion Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
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Publication of CA2961739A1 publication Critical patent/CA2961739A1/en
Application granted granted Critical
Publication of CA2961739C publication Critical patent/CA2961739C/en
Active legal-status Critical Current
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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/36—Blood coagulation or fibrinolysis factors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C12N9/6424—Serine endopeptidases (3.4.21)
    • C12N9/6432—Coagulation factor Xa (3.4.21.6)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/43—Enzymes; Proenzymes; Derivatives thereof
    • A61K38/46—Hydrolases (3)
    • A61K38/48—Hydrolases (3) acting on peptide bonds (3.4)
    • A61K38/482—Serine endopeptidases (3.4.21)
    • A61K38/4846—Factor VII (3.4.21.21); Factor IX (3.4.21.22); Factor Xa (3.4.21.6); Factor XI (3.4.21.27); Factor XII (3.4.21.38)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/21—Serine endopeptidases (3.4.21)
    • C12Y304/21006—Coagulation factor Xa (3.4.21.6)

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
CA2961739A 2014-08-20 2015-08-20 Lyophilized formulations for factor xa antidote Active CA2961739C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462039809P 2014-08-20 2014-08-20
US62/039,809 2014-08-20
PCT/US2015/046173 WO2016029061A1 (en) 2014-08-20 2015-08-20 Lyophilized formulations for factor xa antidote

Publications (2)

Publication Number Publication Date
CA2961739A1 CA2961739A1 (en) 2016-02-25
CA2961739C true CA2961739C (en) 2024-04-30

Family

ID=55351266

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2961739A Active CA2961739C (en) 2014-08-20 2015-08-20 Lyophilized formulations for factor xa antidote

Country Status (14)

Country Link
US (6) US20160237420A1 (cg-RX-API-DMAC7.html)
EP (2) EP3182993B1 (cg-RX-API-DMAC7.html)
JP (4) JP6742986B2 (cg-RX-API-DMAC7.html)
KR (3) KR102867491B1 (cg-RX-API-DMAC7.html)
CN (2) CN107073082B (cg-RX-API-DMAC7.html)
AU (3) AU2015305413B2 (cg-RX-API-DMAC7.html)
CA (1) CA2961739C (cg-RX-API-DMAC7.html)
DK (1) DK3182993T3 (cg-RX-API-DMAC7.html)
EA (2) EA202091385A3 (cg-RX-API-DMAC7.html)
ES (1) ES2814157T3 (cg-RX-API-DMAC7.html)
IL (2) IL250413B (cg-RX-API-DMAC7.html)
SG (1) SG11201701247RA (cg-RX-API-DMAC7.html)
WO (1) WO2016029061A1 (cg-RX-API-DMAC7.html)
ZA (1) ZA201701764B (cg-RX-API-DMAC7.html)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010117729A1 (en) * 2009-03-30 2010-10-14 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
CA2961739C (en) 2014-08-20 2024-04-30 Portola Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
US20190046450A1 (en) 2016-02-24 2019-02-14 Portola Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote
PE20190661A1 (es) 2016-06-17 2019-05-08 Portola Pharm Inc Preparacion de derivados del factor xa
EP3624828B1 (en) * 2017-05-18 2024-08-07 Merck Sharp & Dohme LLC Pharmaceutical formulation comprising incretin-insulin conjugates
US20210196568A1 (en) * 2018-05-21 2021-07-01 Chugai Seiyaku Kabushiki Kaisha Lyophilized formulation sealed in glass container
CN110760479A (zh) * 2019-05-17 2020-02-07 上海交通大学医学院附属瑞金医院 靶向血小板表达的凝血因子Xa及其应用

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE177752T1 (de) 1992-12-15 1999-04-15 Corvas Int Inc Neue inhibitoren von faktor xa
CN100553678C (zh) 1999-02-22 2009-10-28 巴克斯特国际有限公司 新的无白蛋白的因子ⅷ制剂
US6586574B1 (en) * 1999-08-17 2003-07-01 Nn A/S Stabilization of freeze-dried cake
ES2254385T3 (es) 2000-02-29 2006-06-16 Millennium Pharmaceuticals, Inc. Benzamidas e inhibidores relacionados del factor xa.
US6586584B2 (en) * 2001-01-29 2003-07-01 Becton, Dickinson And Company Sequences and methods for detection of Hepatitis C virus
CA2512680A1 (en) * 2003-01-08 2004-07-29 Chiron Corporation Stabilized lyophilized compositions comprising tissue factor pathway inhibitor or tissue factor pathway inhibitor variants
ATE549317T1 (de) 2005-11-08 2012-03-15 Millennium Pharm Inc Pharmazeutische salze und polymorphe aus n-(5- chloro-2-pyridinyl)-2-ää4- ä(dimethylamino)iminomethylübenzoylüaminoü-5- methoxy-benzamid, einem faktor-xa-hemmer
JO3324B1 (ar) * 2006-04-21 2019-03-13 Amgen Inc مركبات علاجية مجففة بالتبريد تتعلق بالعصارة الهضمية
DK2915564T3 (da) * 2007-09-28 2021-02-08 Alexion Pharma Inc Antidoter mod faktor XA-inhibitorer og fremgangsmåder til anvendelse deraf
CN107050437A (zh) 2008-09-03 2017-08-18 奥克塔法马股份有限公司 重组制备的因子viii的新型保护组合物
JP5709316B2 (ja) 2008-11-14 2015-04-30 ポートラ ファーマシューティカルズ， インコーポレイテッド 第Ｘａ因子阻害剤のための解毒剤および血液凝固剤と組み合わせて該解毒剤を使用する方法
WO2010117729A1 (en) 2009-03-30 2010-10-14 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same
EP2453910B1 (en) 2009-07-15 2016-08-31 Portola Pharmaceuticals, Inc. Unit dose formulation of antidote for factor xa inhibitors for use in preventing bleeding
US20120121580A1 (en) * 2009-07-28 2012-05-17 Merck Sharp & Dohme Corp. Methods for producing high concentration lyophilized pharmaceutical formulations
US20130165459A1 (en) * 2010-01-12 2013-06-27 Norvartis Pharma Ag Pharmaceutical composition and dosage forms of elinogrel and methods of use thereof
KR102049254B1 (ko) * 2010-04-20 2019-11-28 옥타파마 아게 약학 단백질을 위한 신규한 안정화제
US8987285B2 (en) * 2010-12-03 2015-03-24 Portola Pharmaceuticals, Inc. Pharmaceutical compositions, dosage forms and new forms of the compound of formula (I), and methods of use thereof
US9683020B2 (en) * 2011-08-01 2017-06-20 Emory University VLPS containing ligands and methods related thereto
AU2012315516B2 (en) * 2011-09-30 2017-05-04 The Children's Hospital Of Philadelphia Compositions and methods for modulating hemostasis
GB201310946D0 (en) * 2013-06-19 2013-07-31 Cambridge Entpr Ltd Antidote
CA2961739C (en) * 2014-08-20 2024-04-30 Portola Pharmaceuticals, Inc. Lyophilized formulations for factor xa antidote

Also Published As

Publication number Publication date
ZA201701764B (en) 2020-10-28
EP3182993A1 (en) 2017-06-28
ES2814157T3 (es) 2021-03-26
AU2015305413A1 (en) 2017-03-23
AU2015305413B2 (en) 2020-09-24
IL276960A (en) 2020-10-29
JP2023158199A (ja) 2023-10-26
JP7416549B2 (ja) 2024-01-17
US20200299668A1 (en) 2020-09-24
EP3750556A1 (en) 2020-12-16
EA201790415A1 (ru) 2017-08-31
US20210284986A1 (en) 2021-09-16
US11028382B2 (en) 2021-06-08
KR102867491B1 (ko) 2025-10-01
US20160237420A1 (en) 2016-08-18
KR20250150675A (ko) 2025-10-20
EA202091385A3 (ru) 2021-06-30
EA036091B1 (ru) 2020-09-25
EP3182993B1 (en) 2020-07-01
AU2020289768A1 (en) 2021-01-21
JP2022003101A (ja) 2022-01-11
US20250163399A1 (en) 2025-05-22
JP2017525704A (ja) 2017-09-07
KR20230007550A (ko) 2023-01-12
CN113171447B (zh) 2024-05-17
JP2019206595A (ja) 2019-12-05
CN113171447A (zh) 2021-07-27
KR20170042776A (ko) 2017-04-19
EP3182993A4 (en) 2018-01-17
AU2020289768B2 (en) 2024-06-13
KR102482517B1 (ko) 2022-12-28
CN107073082A (zh) 2017-08-18
CN107073082B (zh) 2021-04-30
WO2016029061A1 (en) 2016-02-25
US20180320160A1 (en) 2018-11-08
SG11201701247RA (en) 2017-03-30
IL250413B (en) 2020-09-30
JP6742986B2 (ja) 2020-08-19
IL250413A0 (en) 2017-03-30
EA202091385A2 (ru) 2021-03-31
CA2961739A1 (en) 2016-02-25
US20200299667A1 (en) 2020-09-24
AU2024219698A1 (en) 2024-10-03
DK3182993T3 (da) 2020-09-21
IL276960B (en) 2022-04-01

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