CA2897672A1 - Compositions and methods for counteracting factor xa inhibition - Google Patents

Compositions and methods for counteracting factor xa inhibition Download PDF

Info

Publication number
CA2897672A1
CA2897672A1 CA2897672A CA2897672A CA2897672A1 CA 2897672 A1 CA2897672 A1 CA 2897672A1 CA 2897672 A CA2897672 A CA 2897672A CA 2897672 A CA2897672 A CA 2897672A CA 2897672 A1 CA2897672 A1 CA 2897672A1
Authority
CA
Canada
Prior art keywords
factor
variant
amino acid
seq
leu
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2897672A
Other languages
English (en)
French (fr)
Inventor
Rodney Camire
Joachim Fruebis
Debra D. Pittman
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.)
Children's Hospital of Philadelphia
Pfizer Inc
Original Assignee
Children's Hospital of Philadelphia
Pfizer 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
Application filed by Children's Hospital of Philadelphia, Pfizer Inc filed Critical Children's Hospital of Philadelphia
Publication of CA2897672A1 publication Critical patent/CA2897672A1/en
Abandoned legal-status Critical Current

Links

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
    • A61K38/43—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
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • 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)
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Biomedical Technology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Dermatology (AREA)
CA2897672A 2013-01-31 2014-01-23 Compositions and methods for counteracting factor xa inhibition Abandoned CA2897672A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361759332P 2013-01-31 2013-01-31
US61/759,332 2013-01-31
PCT/IB2014/058494 WO2014118677A1 (en) 2013-01-31 2014-01-23 Compositions and methods for counteracting factor xa inhibition

Publications (1)

Publication Number Publication Date
CA2897672A1 true CA2897672A1 (en) 2014-08-07

Family

ID=50114451

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2897672A Abandoned CA2897672A1 (en) 2013-01-31 2014-01-23 Compositions and methods for counteracting factor xa inhibition

Country Status (12)

Country Link
US (3) US20150343034A1 (cg-RX-API-DMAC10.html)
EP (1) EP2950813B1 (cg-RX-API-DMAC10.html)
JP (2) JP6437458B2 (cg-RX-API-DMAC10.html)
KR (1) KR20150103205A (cg-RX-API-DMAC10.html)
CN (1) CN104994868A (cg-RX-API-DMAC10.html)
AU (1) AU2014210830A1 (cg-RX-API-DMAC10.html)
CA (1) CA2897672A1 (cg-RX-API-DMAC10.html)
ES (1) ES2761730T3 (cg-RX-API-DMAC10.html)
HK (1) HK1215196A1 (cg-RX-API-DMAC10.html)
IL (1) IL240147A0 (cg-RX-API-DMAC10.html)
MX (1) MX2015008813A (cg-RX-API-DMAC10.html)
WO (1) WO2014118677A1 (cg-RX-API-DMAC10.html)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HK1215196A1 (zh) 2013-01-31 2016-08-19 辉瑞公司 用於抵消因子xa抑制的组合物和方法
CN112195169A (zh) 2013-09-24 2021-01-08 辉瑞大药厂 包含重组人凝血因子Xa蛋白的异质性群体的组合物
US20160235824A1 (en) * 2013-11-01 2016-08-18 The Children's Hospital Philadelphia Compositions and Methods for Increasing the Half-Life of Factor XA
CN105934250A (zh) * 2014-01-24 2016-09-07 辉瑞公司 治疗脑内出血的组合物和方法
NZ727444A (en) 2014-05-26 2021-12-24 Academisch Ziekenhuis Leiden Prohemostatic proteins for the treatment of bleeding
JP6776221B2 (ja) 2014-07-31 2020-10-28 ヘモネティクス・コーポレーションHaemonetics Corporation 凝固分析を使用した抗凝固剤の検出および分類
WO2016028872A2 (en) 2014-08-19 2016-02-25 The Children's Hospital Of Philadelphia Compositions and methods for modulating factor ix function
CN105440127B (zh) * 2015-12-30 2018-10-16 上海莱士血液制品股份有限公司 一种以人血浆Cohn组分III为原料的FEIBA的制备方法
TW201802121A (zh) 2016-05-25 2018-01-16 諾華公司 抗因子XI/XIa抗體之逆轉結合劑及其用途
KR102616666B1 (ko) 2016-12-23 2023-12-27 노파르티스 아게 인자 xi 항체 및 사용 방법
US12703762B2 (en) 2018-12-18 2026-08-11 Novartis Ag Reversal binding agents for anti-factor XI/XIa antibodies and uses thereof
WO2020163685A1 (en) * 2019-02-07 2020-08-13 Portola Pharmaceuticals, Inc. Methods for treating intracranial hemorrhage and assessing efficacy
CN114681597A (zh) * 2022-03-11 2022-07-01 兆科药业(合肥)有限公司 蝰蛇蛇毒血凝酶在制备用于逆转凝血因子Xa抑制剂的抗凝作用的药物中的应用

Family Cites Families (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5597799A (en) 1990-09-04 1997-01-28 Cor Therapeutics, Inc. Recombinant agents affecting thrombosis
US6262047B1 (en) 1996-10-11 2001-07-17 Cor Therapeutics, Inc. Selective factor Xa inhibitors
US6369080B2 (en) 1996-10-11 2002-04-09 Cor Therapeutics, Inc. Selective factor Xa inhibitors
AT405517B (de) 1997-02-27 1999-09-27 Immuno Ag Faktor x-deletionsmutanten und analoge davon
AT405516B (de) 1997-02-27 1999-09-27 Immuno Ag Faktor x-analoge mit modifizierter proteasespaltstelle
US6133256A (en) 1997-04-14 2000-10-17 Cor Therapeutics Inc Selective factor Xa inhibitors
GB9908838D0 (en) 1998-09-11 1999-06-16 Univ London Fibroblast inhibitor
AT410216B (de) 1999-08-10 2003-03-25 Baxter Ag Faktor x-analogon mit verbesserter aktivierbarkeit
AU2001249389A1 (en) 2000-03-22 2001-10-03 The Children's Hospital Of Philadelphia Modified blood clotting factors and methods of use
US6905683B2 (en) 2000-05-03 2005-06-14 Novo Nordisk Healthcare A/G Human coagulation factor VII variants
FR2831170B1 (fr) 2001-10-19 2004-03-19 Inst Nat Sante Rech Med Proteines c modifiees activables directement par la thrombine
FR2841904B1 (fr) 2002-07-03 2004-08-20 Inst Nat Sante Rech Med Analogues de facteurs x clivables par la thrombine
EP1728798A1 (en) 2005-06-01 2006-12-06 ZLB Behring GmbH Coagulation factor X polypeptides with modified activation properties
DE102005028018A1 (de) * 2005-06-16 2006-12-21 Dade Behring Marburg Gmbh Verfahren zur Standardisierung von Gerinnungstesten
MX336958B (es) 2005-11-15 2016-02-05 Philadelphia Children Hospital Metodos y composiciones para modular la hemostasia.
EP1820508A1 (en) 2006-02-21 2007-08-22 CSL Behring GmbH Coagulation factor X polypeptides with modified activation properties
EP1867660A1 (en) 2006-06-14 2007-12-19 CSL Behring GmbH Proteolytically cleavable fusion protein comprising a blood coagulation factor
KR102069498B1 (ko) 2007-09-28 2020-01-23 포톨라 파마슈티컬스, 인코포레이티드 인자 Xa 저해제에 대한 안티도트 및 그것을 사용하는 방법
WO2009061697A1 (en) 2007-11-09 2009-05-14 The Board Of Trustees Of The University Of Illinois Anticoagulant antagonist and hemophilia procoagulant
CA2743496C (en) 2008-11-14 2018-03-27 Portola Pharmaceuticals, Inc. Antidotes for factor xa inhibitors and methods of using the same in combination with blood coagulating agents
JP5833448B2 (ja) 2008-12-19 2015-12-16 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル セリンプロテアーゼ誘導体および血液凝固疾患の予防または処置における使用
PL3604510T3 (pl) 2009-03-30 2025-07-28 Alexion Pharmaceuticals, Inc. Antidota na inhibitory czynnika xa i sposoby ich stosowania
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
GB2485590A (en) 2010-11-22 2012-05-23 Univ Ruprecht Karis Heidelberg Method for detecting at least one direct factor Xa inhibitors
FR2972114B1 (fr) 2011-03-01 2013-03-15 Univ Grenoble 1 Un nouveau leurre moleculaire procoagulant pour le traitement des hemophiles a ou b avec ou sans inhibiteur
JP6514893B2 (ja) 2011-09-30 2019-05-15 ザ・チルドレンズ・ホスピタル・オブ・フィラデルフィアThe Children’S Hospital Of Philadelphia 止血を調節するための組成物および方法
WO2013123248A1 (en) 2012-02-16 2013-08-22 Portola Pharmaceuticals, Inc. MODULATION OF FACTOR Xa INHIBITOR MEDIATED BLOOD LOSS BY PARTIAL AND TRANSIENT ADMINISTRATION OF ANTIDOTE
FR3000895B1 (fr) 2013-01-11 2017-02-24 Laboratoire Francais Du Fractionnement Et Des Biotechnologies Sa Utilisation d'antidotes d'inhibiteurs de la coagulation indiques dans la prevention ou le traitement de pathologies thromboemboliques
HK1215196A1 (zh) 2013-01-31 2016-08-19 辉瑞公司 用於抵消因子xa抑制的组合物和方法
CN112195169A (zh) 2013-09-24 2021-01-08 辉瑞大药厂 包含重组人凝血因子Xa蛋白的异质性群体的组合物
US20160235824A1 (en) * 2013-11-01 2016-08-18 The Children's Hospital Philadelphia Compositions and Methods for Increasing the Half-Life of Factor XA
CN105934250A (zh) 2014-01-24 2016-09-07 辉瑞公司 治疗脑内出血的组合物和方法

Also Published As

Publication number Publication date
US20210000930A1 (en) 2021-01-07
US20150343034A1 (en) 2015-12-03
ES2761730T3 (es) 2020-05-20
AU2014210830A1 (en) 2015-07-16
IL240147A0 (en) 2015-09-24
HK1215196A1 (zh) 2016-08-19
JP2016511755A (ja) 2016-04-21
MX2015008813A (es) 2016-03-31
KR20150103205A (ko) 2015-09-09
WO2014118677A1 (en) 2014-08-07
CN104994868A (zh) 2015-10-21
US20180344819A1 (en) 2018-12-06
JP2019077677A (ja) 2019-05-23
JP6437458B2 (ja) 2018-12-12
US10588950B2 (en) 2020-03-17
EP2950813B1 (en) 2019-09-04
EP2950813A1 (en) 2015-12-09

Similar Documents

Publication Publication Date Title
US10588950B2 (en) Compositions and methods for counteracting Factor Xa inhibition
AU763466B2 (en) A pharmaceutical preparation for treating blood coagulation disorders
US10000748B2 (en) Factor IX variants with clotting activity in absence of their cofactor and/or with increased F.IX clotting activity and their use for treating bleeding disorders
EP2680876B1 (fr) Facteur xa depourvu de domaine gla pour le traitement des hemophilies a ou b avec ou sans anticorps
AU2007226566A1 (en) Use of thrombin mutants to inhibit the anticoagulation effect of thrombin inhibitors
JP6629744B2 (ja) 第Xa因子の半減期を延ばす組成物および方法
JP2025522101A (ja) 止血を促進するための薬剤
WO2005034990A1 (ja) アンチトロンビンiii含有止血用組成物

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20150709

FZDE Discontinued

Effective date: 20230906