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WO2001058493A8 - Conjugates of follicle stimulating hormones - Google Patents

Conjugates of follicle stimulating hormones

Info

Publication number
WO2001058493A8
WO2001058493A8 PCT/DK2001/000090 DK0100090W WO0158493A8 WO 2001058493 A8 WO2001058493 A8 WO 2001058493A8 DK 0100090 W DK0100090 W DK 0100090W WO 0158493 A8 WO0158493 A8 WO 0158493A8
Authority
WO
WIPO (PCT)
Prior art keywords
fsh
polypeptide
subunit
conjugates
attachment group
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.)
Ceased
Application number
PCT/DK2001/000090
Other languages
French (fr)
Other versions
WO2001058493A1 (en
Inventor
Hans Thalsgaard Schambye
Kim Vilbour Andersen
Den Hazel Bart Van
Jesper Christiansen
Claus Bekker Jeppesen
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.)
Maxygen ApS
Original Assignee
Maxygen ApS
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 Maxygen ApS filed Critical Maxygen ApS
Priority to AU2001231531A priority Critical patent/AU2001231531A1/en
Priority to AU2001267337A priority patent/AU2001267337A1/en
Priority to US09/896,896 priority patent/US20030036181A1/en
Priority to JP2002507849A priority patent/JP2004504016A/en
Priority to CA002412882A priority patent/CA2412882A1/en
Priority to PCT/DK2001/000459 priority patent/WO2002002597A2/en
Priority to EP01944987A priority patent/EP1299535A2/en
Publication of WO2001058493A1 publication Critical patent/WO2001058493A1/en
Publication of WO2001058493A8 publication Critical patent/WO2001058493A8/en
Anticipated expiration legal-status Critical
Priority to US10/967,088 priority patent/US20060160177A1/en
Ceased 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
    • A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22—Hormones
    • A61K38/24—Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g. HCG; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • 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
    • A61K47/50—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—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 the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/646—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent the entire peptide or protein drug conjugate elicits an immune response, e.g. conjugate vaccines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/575—Hormones
    • C07K14/59—Follicle-stimulating hormone [FSH]; Chorionic gonadotropins, e.g.hCG [human chorionic gonadotropin]; Luteinising hormone [LH]; Thyroid-stimulating hormone [TSH]

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Zoology (AREA)
  • Reproductive Health (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Toxicology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

The invention relates to heterodimeric polypeptide conjugates exhibiting FSH activity, comprising a dimeric polypeptide comprising an FSH-α subunit and an FSH-β subunit, wherein at least one of the FSH-α and FSH-β subunits differs from the corresponding wildtype subunit in that at least one amino acid residue acid residue comprising an attachment group for a non-polypeptide moiety has been introduced or removed, and having at least one non-polypeptide moiety bound to an attachment group of at least one of said subunits. Preferably, at least one attachment group, e.g. an N- or O-glycosylation site or an attachment site for a polymer molecule such as polyethylene glycol, has been introduced, e.g. at an N-terminal. The polypeptide conjugates exhibit improved properties, in particular an increased half-life, compared to human FSH.
PCT/DK2001/000090 2000-02-11 2001-02-09 Conjugates of follicle stimulating hormones Ceased WO2001058493A1 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
AU2001231531A AU2001231531A1 (en) 2000-02-11 2001-02-09 Follicle stimulating hormones
PCT/DK2001/000459 WO2002002597A2 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
US09/896,896 US20030036181A1 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
JP2002507849A JP2004504016A (en) 2000-06-30 2001-06-29 Peptide-extended glycosylated polypeptides
CA002412882A CA2412882A1 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
AU2001267337A AU2001267337A1 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
EP01944987A EP1299535A2 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
US10/967,088 US20060160177A1 (en) 2000-06-30 2004-10-15 Peptide extended glycosylated polypeptides

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DKPA200000220 2000-02-11
DKPA200000220 2000-02-11
DKPA200001092 2000-07-14
DKPA200001092 2000-07-14

Publications (2)

Publication Number Publication Date
WO2001058493A1 WO2001058493A1 (en) 2001-08-16
WO2001058493A8 true WO2001058493A8 (en) 2001-11-08

Family

ID=26068766

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/DK2001/000090 Ceased WO2001058493A1 (en) 2000-02-11 2001-02-09 Conjugates of follicle stimulating hormones

Country Status (2)

Country Link
AU (1) AU2001231531A1 (en)
WO (1) WO2001058493A1 (en)

Families Citing this family (48)

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US7157277B2 (en) 2001-11-28 2007-01-02 Neose Technologies, Inc. Factor VIII remodeling and glycoconjugation of Factor VIII
US7173003B2 (en) 2001-10-10 2007-02-06 Neose Technologies, Inc. Granulocyte colony stimulating factor: remodeling and glycoconjugation of G-CSF
US7214660B2 (en) 2001-10-10 2007-05-08 Neose Technologies, Inc. Erythropoietin: remodeling and glycoconjugation of erythropoietin
WO2004050679A2 (en) 2001-10-22 2004-06-17 Applied Research Systems Ars Holding N.V. Mutant glycoproteins
EA007030B1 (en) * 2001-10-22 2006-06-30 Апплайд Резеч Системз Арс Холдинг Н.В. Gonadotrophines for folliculogenesis
US7553930B2 (en) 2003-01-06 2009-06-30 Xencor, Inc. BAFF variants and methods thereof
AU2004221824B2 (en) 2003-03-14 2009-08-27 Ratiopharm Gmbh Branched water-soluble polymers and their conjugates
US8791070B2 (en) 2003-04-09 2014-07-29 Novo Nordisk A/S Glycopegylated factor IX
CA2522345A1 (en) 2003-04-09 2004-11-18 Neose Technologies, Inc. Glycopegylation methods and proteins/peptides produced by the methods
JP2007523630A (en) 2003-05-09 2007-08-23 ネオス テクノロジーズ インコーポレイテッド Composition and formulation of human growth hormone glycosylation mutants
US9005625B2 (en) 2003-07-25 2015-04-14 Novo Nordisk A/S Antibody toxin conjugates
UA88879C2 (en) 2003-09-02 2009-12-10 Эплайд Рисерч Системз Эрс Холдинг Н.В. Fsh glycosylation mutant
US8633157B2 (en) 2003-11-24 2014-01-21 Novo Nordisk A/S Glycopegylated erythropoietin
US20080305992A1 (en) 2003-11-24 2008-12-11 Neose Technologies, Inc. Glycopegylated erythropoietin
US20060040856A1 (en) 2003-12-03 2006-02-23 Neose Technologies, Inc. Glycopegylated factor IX
US7259007B2 (en) * 2003-12-24 2007-08-21 Glycofi, Inc. Methods for eliminating mannosylphosphorylation of glycans in the production of glycoproteins
US8361961B2 (en) 2004-01-08 2013-01-29 Biogenerix Ag O-linked glycosylation of peptides
US20080300173A1 (en) 2004-07-13 2008-12-04 Defrees Shawn Branched Peg Remodeling and Glycosylation of Glucagon-Like Peptides-1 [Glp-1]
EP1799249A2 (en) 2004-09-10 2007-06-27 Neose Technologies, Inc. Glycopegylated interferon alpha
JP5948627B2 (en) 2004-10-29 2016-07-20 レイショファーム ゲーエムベーハー Fibroblast growth factor (FGF) remodeling and carbohydrate pegylation
ES2449195T3 (en) 2005-01-10 2014-03-18 Ratiopharm Gmbh Glycopegylated granulocyte colony stimulating factor
US20070154992A1 (en) 2005-04-08 2007-07-05 Neose Technologies, Inc. Compositions and methods for the preparation of protease resistant human growth hormone glycosylation mutants
JP5216580B2 (en) 2005-05-25 2013-06-19 ノヴォ ノルディスク アー／エス Glycopegylated factor IX
US20070105755A1 (en) 2005-10-26 2007-05-10 Neose Technologies, Inc. One pot desialylation and glycopegylation of therapeutic peptides
EA015901B1 (en) 2005-08-26 2011-12-30 Арес Трейдинг С.А. Process for the preparation of glycosylated interferon beta
WO2007031566A1 (en) 2005-09-14 2007-03-22 Ares Trading S.A. Method for the quantitative determination of poloxamers
WO2007056191A2 (en) 2005-11-03 2007-05-18 Neose Technologies, Inc. Nucleotide sugar purification using membranes
JP5199112B2 (en) * 2005-12-09 2013-05-15 アレス トレーディング ソシエテ アノニム Method for purifying FSH or FSH variants
EA013975B1 (en) 2005-12-22 2010-08-30 Мерк Сероно С.А. Fsh mutants and use thereof
US7956034B2 (en) * 2006-01-17 2011-06-07 Merck Serono Sa FSH glycosylation variant D3N
JP2009544327A (en) 2006-07-21 2009-12-17 ノヴォ ノルディスク アー／エス Glycosylation of peptides with O-linked glycosylation sequences
WO2008057683A2 (en) 2006-10-03 2008-05-15 Novo Nordisk A/S Methods for the purification of polypeptide conjugates
JP2010523582A (en) 2007-04-03 2010-07-15 バイオジェネリクス アクチェンゲゼルシャフト Treatment method using glycoPEGylated G-CSF
CA2690611C (en) 2007-06-12 2015-12-08 Novo Nordisk A/S Improved process for the production of nucleotide sugars
CA2690844C (en) * 2007-06-28 2016-05-17 Biogenerix Ag Fsh producing cell clone
US8207112B2 (en) 2007-08-29 2012-06-26 Biogenerix Ag Liquid formulation of G-CSF conjugate
RS52106B (en) 2008-02-08 2012-08-31 Biogenerix Ag Liquid formulation of fsh
JP5619630B2 (en) 2008-02-27 2014-11-05 ノボ・ノルデイスク・エー／エス Binding factor VIII molecule
ME02277B (en) 2009-04-01 2016-02-20 Ratiopharm Gmbh Method for purifying recombinant fsh
EP2325194A1 (en) 2009-11-24 2011-05-25 Glycotope GmbH Process for the purification of glycoproteins
KR20140053991A (en) 2011-07-18 2014-05-08 아츠 바이올로직스 에이/에스 Long acting luteinizing hormone (lh) compound
EP2846822A2 (en) 2012-05-11 2015-03-18 Prorec Bio AB Method for diagnosis and treatment of prolactin associated disorders
AU2016251314B2 (en) * 2015-04-24 2019-12-05 Ferring B.V. Method of production of gonadotrophin
KR101947340B1 (en) * 2017-05-05 2019-02-12 주식회사 유비프로틴 A method for extending half-life of FSH alpha
KR101947341B1 (en) * 2017-05-05 2019-02-12 주식회사 유비프로틴 A method for extending half-life of FSH beta
CL2018001347A1 (en) * 2018-05-18 2019-03-15 Centro De Biotecnologia Y Biomedicina Spa 94% Recombinant bovine stimulating follicle hormone, a composition that comprises it and a method to induce superovulation and synchronization of heat in cattle using said hormone
WO2021132957A1 (en) * 2019-12-26 2021-07-01 주식회사 엘지화학 Method for purifying follicle stimulating hormone
CN114213523B (en) * 2021-11-15 2024-07-09 广州源博医药科技有限公司 Hyperglycosylation modification sequence for recombinant protein, recombinant porcine follicle stimulating hormone and application thereof

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US5218092A (en) * 1988-09-29 1993-06-08 Kyowa Hakko Kogyo Co., Ltd. Modified granulocyte-colony stimulating factor polypeptide with added carbohydrate chains
ZA987497B (en) * 1997-09-08 1999-02-23 Akzo Nobel Nv Expression of gonadotropins in dictyostelium

Also Published As

Publication number Publication date
WO2001058493A1 (en) 2001-08-16
AU2001231531A1 (en) 2001-08-20

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