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
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
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 CA002412882A priority patent/CA2412882A1/en
Priority to PCT/DK2001/000459 priority patent/WO2002002597A2/en
Priority to AU2001267337A priority patent/AU2001267337A1/en
Priority to US09/896,896 priority patent/US20030036181A1/en
Priority to EP01944987A priority patent/EP1299535A2/en
Priority to JP2002507849A priority patent/JP2004504016A/en
Publication of WO2001058493A1 publication Critical patent/WO2001058493A1/en
Publication of WO2001058493A8 publication Critical patent/WO2001058493A8/en
Priority to US10/967,088 priority patent/US20060160177A1/en

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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Medicinal Chemistry (AREA)
  • Endocrinology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Reproductive Health (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Virology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Toxicology (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 WO2001058493A1 (en)

Priority Applications (8)

Application Number Priority Date Filing Date Title
AU2001231531A AU2001231531A1 (en) 2000-02-11 2001-02-09 Follicle stimulating hormones
CA002412882A CA2412882A1 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
PCT/DK2001/000459 WO2002002597A2 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
AU2001267337A AU2001267337A1 (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
EP01944987A EP1299535A2 (en) 2000-06-30 2001-06-29 Peptide extended glycosylated polypeptides
JP2002507849A JP2004504016A (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 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 (47)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7157277B2 (en) 2001-11-28 2007-01-02 Neose Technologies, Inc. Factor VIII remodeling and glycoconjugation of Factor VIII
US7214660B2 (en) 2001-10-10 2007-05-08 Neose Technologies, Inc. Erythropoietin: remodeling and glycoconjugation of erythropoietin
US7173003B2 (en) 2001-10-10 2007-02-06 Neose Technologies, Inc. Granulocyte colony stimulating factor: remodeling and glycoconjugation of G-CSF
AU2002340562B2 (en) * 2001-10-22 2008-10-23 Merck Serono Sa Compositions of FSH with high sialylation degree and their use for the preparation of medicaments
IL161541A0 (en) 2001-10-22 2004-09-27 Applied Research Systems Mutant glycoproteins
US7553930B2 (en) 2003-01-06 2009-06-30 Xencor, Inc. BAFF variants and methods thereof
KR20060003862A (en) 2003-03-14 2006-01-11 네오스 테크놀로지스, 인크. Branched water-soluble polymers and their eonjugates
US8791070B2 (en) 2003-04-09 2014-07-29 Novo Nordisk A/S Glycopegylated factor IX
MXPA05010773A (en) 2003-04-09 2005-12-12 Neose Technologies Inc Glycopegylation methods and proteins/peptides produced by the methods.
WO2005012484A2 (en) 2003-07-25 2005-02-10 Neose Technologies, Inc. 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
BRPI0506741A (en) 2004-01-08 2007-05-15 Neose Technologies Inc glycosylation of peptides linked to the
US20080300173A1 (en) 2004-07-13 2008-12-04 Defrees Shawn Branched Peg Remodeling and Glycosylation of Glucagon-Like Peptides-1 [Glp-1]
US8268967B2 (en) 2004-09-10 2012-09-18 Novo Nordisk A/S Glycopegylated interferon α
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
EP1858543B1 (en) 2005-01-10 2013-11-27 BioGeneriX AG 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
CA2612613A1 (en) 2005-09-14 2007-03-22 Mara Rossi Method for the determination of poloxamers
US20090048440A1 (en) 2005-11-03 2009-02-19 Neose Technologies, Inc. Nucleotide Sugar Purification Using Membranes
US8604175B2 (en) 2005-12-09 2013-12-10 Ares Trading S.A. Method for purifying FSH or a FSH mutant
JP5249044B2 (en) 2005-12-22 2013-07-31 メルク セローノ ソシエテ アノニム FSH mutant
ATE487738T1 (en) * 2006-01-17 2010-11-15 Merck Serono Sa NEW FSH GLYCOSYLATION VARIANT D3N
CN101516388B (en) 2006-07-21 2012-10-31 诺和诺德公司 Glycosylation of peptides via O-linked glycosylation sequences
EP2054521A4 (en) 2006-10-03 2012-12-19 Novo Nordisk As Methods for the purification of polypeptide conjugates
RS52845B (en) 2007-04-03 2013-12-31 Biogenerix Ag Methods of treatment using glycopegylated g-csf
US9493499B2 (en) 2007-06-12 2016-11-15 Novo Nordisk A/S Process for the production of purified cytidinemonophosphate-sialic acid-polyalkylene oxide (CMP-SA-PEG) as modified nucleotide sugars via anion exchange chromatography
UA103598C2 (en) * 2007-06-28 2013-11-11 Биодженерикс Аг Fsh producing cell clone
US8207112B2 (en) 2007-08-29 2012-06-26 Biogenerix Ag Liquid formulation of G-CSF conjugate
NZ586588A (en) 2008-02-08 2012-10-26 Biogenerix Ag Formulation of ( follice stimulating hormone) fsh and varients with benzalkonium chloride and benzyl alcohol
EP2257311B1 (en) 2008-02-27 2014-04-16 Novo Nordisk A/S Conjugated factor viii molecules
UA106369C2 (en) 2009-04-01 2014-08-26 Рациофарм Гмбх 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
DK3286209T3 (en) * 2015-04-24 2020-12-21 Ferring Bv GONADOTROPHINE PRODUCTION PROCEDURE
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
KR20210083174A (en) * 2019-12-26 2021-07-06 주식회사 엘지화학 Method for Purifying Follicle stimulating hormone
CN114213523A (en) * 2021-11-15 2022-03-22 广州源博医药科技有限公司 High glycosylation modified sequence for recombinant protein, recombinant porcine follicle-stimulating hormone and application thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4904584A (en) * 1987-12-23 1990-02-27 Genetics Institute, Inc. Site-specific homogeneous modification of polypeptides
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
AU2001231531A1 (en) 2001-08-20
WO2001058493A1 (en) 2001-08-16

Similar Documents

Publication Publication Date Title
WO2001058493A8 (en) Conjugates of follicle stimulating hormones
WO2001051510A3 (en) G-csf conjugates
YU48703A (en) New interferon beta-like molecules
PH12019501613A1 (en) Site-directed modification of fviii
WO2005056760A3 (en) Glycopegylated follicle stimulating hormone
WO2001036001A3 (en) Interferon gamma conjugates
CN102958533B (en) The medicament that dipeptides connects
HK1205193A1 (en) Recombinant n-glycosylated proteins from procaryotic cells n-
IL195338A (en) Antibody comprising an fc variant comprising d or e amino acid substitution at position 239 and pharmaceutical composition and use thereof
HUP0401591A2 (en) Novel receptor nucleic acids and polypeptides
EP2573109A3 (en) Peptide vaccines comprising Seq Id 101, 80 or 100 for cancers expressing tumor-associated antigens
WO2007056362A3 (en) Glucagon analogs exhibiting physiological solubility and stability
EP2476698A3 (en) Peptide vaccines for cancers expressing MPHOSPH1 or DEPDC1 polypeptides
WO2002055532A3 (en) Variant growth hormone molecules conjugated with macromolecular compounds
WO2007030519A3 (en) Stabilized glp-1 analogs
WO2004027064A3 (en) Ghrh analogues
DE69637535D1 (en) BASED ON RADIOMARKED PEPTIDES FOR LOCAL ADMINISTRATION
WO2001015736A3 (en) Interferon-beta conjugates
DE60324406D1 (en) MODIFIED FACTOR VIII
PT2289533E (en) Epitope peptides derived from vascular endothelial growth factor receptor 1 and vaccines containing these peptides
YU32402A (en) Interferon gamma conjugates
EP1279677A4 (en) Gd3-mimetic peptides
WO2005075021A3 (en) Chemically-modified human growth hormone receptor antagonist conjugates
GB0001712D0 (en) Therapeutic peptides
EP3219720A3 (en) Wdrpuh epitope peptides and vaccines containing the same

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
121 Ep: the epo has been informed by wipo that ep was designated in this application
AK Designated states

Kind code of ref document: C1

Designated state(s): AE AG AL AM AT AU AZ BA BB BG BR BY BZ CA CH CN CR CU CZ DE DK DM DZ EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MA MD MG MK MN MW MX MZ NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT TZ UA UG UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: C1

Designated state(s): GH GM KE LS MW MZ SD SL SZ TZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE TR BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

CFP Corrected version of a pamphlet front page

Free format text: REVISED TITLE RECEIVED BY THE INTERNATIONAL BUREAU AFTER COMPLETION OF THE TECHNICAL PREPARATIONS FOR INTERNATIONAL PUBLICATION

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase in:

Ref country code: JP