WO2005021043A3 - High-molecular-mass prodrugs - Google Patents

High-molecular-mass prodrugs Download PDF

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Publication number
WO2005021043A3
WO2005021043A3 PCT/FR2004/002162 FR2004002162W WO2005021043A3 WO 2005021043 A3 WO2005021043 A3 WO 2005021043A3 FR 2004002162 W FR2004002162 W FR 2004002162W WO 2005021043 A3 WO2005021043 A3 WO 2005021043A3
Authority
WO
WIPO (PCT)
Prior art keywords
prodrugs
molecular
mass
spacer
prodrug form
Prior art date
Application number
PCT/FR2004/002162
Other languages
French (fr)
Other versions
WO2005021043A2 (en
Inventor
Andre Trouet
Vincent Dubois
Original Assignee
Diatos
Andre Trouet
Vincent Dubois
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 Diatos, Andre Trouet, Vincent Dubois filed Critical Diatos
Priority to AU2004268405A priority Critical patent/AU2004268405A1/en
Priority to BRPI0413843-0A priority patent/BRPI0413843A/en
Priority to JP2006523656A priority patent/JP2007503382A/en
Priority to CA002536442A priority patent/CA2536442A1/en
Priority to EP04786328A priority patent/EP1701743A2/en
Publication of WO2005021043A2 publication Critical patent/WO2005021043A2/en
Priority to IL173760A priority patent/IL173760A0/en
Priority to US11/357,966 priority patent/US20060281897A1/en
Publication of WO2005021043A3 publication Critical patent/WO2005021043A3/en

Links

Classifications

    • 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
    • A61K47/643—Albumins, e.g. HSA, BSA, ovalbumin or a Keyhole Limpet Hemocyanin [KHL]
    • 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
    • A61K47/56—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—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 an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • 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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Peptides Or Proteins (AREA)

Abstract

The invention relates to a modified prodrug form. According to the invention, a typical prodrug form comprises a bulky group, a spacer, a cleavable structure in the circulatory system and a therapeutic agent or a marker, said spacer enabling or facilitating the cleavage of the cleavable structure.
PCT/FR2004/002162 2003-08-22 2004-08-19 High-molecular-mass prodrugs WO2005021043A2 (en)

Priority Applications (7)

Application Number Priority Date Filing Date Title
AU2004268405A AU2004268405A1 (en) 2003-08-22 2004-08-19 Potentiation of the activation of high-molecular-mass prodrugs
BRPI0413843-0A BRPI0413843A (en) 2003-08-22 2004-08-19 enhancement of activation of high molecular weight prodrugs
JP2006523656A JP2007503382A (en) 2003-08-22 2004-08-19 Possible activation of high molecular weight prodrugs
CA002536442A CA2536442A1 (en) 2003-08-22 2004-08-19 Potentiation of the activation of high-molecular-mass prodrugs
EP04786328A EP1701743A2 (en) 2003-08-22 2004-08-19 Potentiation of the activation of high-molecular-mass prodrugs
IL173760A IL173760A0 (en) 2003-08-22 2006-02-16 Potentialization of the activation of high-molecular-mass prodrugs
US11/357,966 US20060281897A1 (en) 2003-08-22 2006-02-22 Potentialization of the activation of high molecular weight prodrugs

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FR0310114A FR2858936A1 (en) 2003-08-22 2003-08-22 New active compound precursor, useful as therapeutic or diagnostic agent or tracer, includes cleavable component that increases half-life in the circulation, attached through hydrophilic spacer
FR0310114 2003-08-22

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/357,966 Continuation-In-Part US20060281897A1 (en) 2003-08-22 2006-02-22 Potentialization of the activation of high molecular weight prodrugs

Publications (2)

Publication Number Publication Date
WO2005021043A2 WO2005021043A2 (en) 2005-03-10
WO2005021043A3 true WO2005021043A3 (en) 2006-06-15

Family

ID=34112859

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/FR2004/002162 WO2005021043A2 (en) 2003-08-22 2004-08-19 High-molecular-mass prodrugs

Country Status (8)

Country Link
EP (1) EP1701743A2 (en)
JP (1) JP2007503382A (en)
AU (1) AU2004268405A1 (en)
BR (1) BRPI0413843A (en)
CA (1) CA2536442A1 (en)
FR (1) FR2858936A1 (en)
IL (1) IL173760A0 (en)
WO (1) WO2005021043A2 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2560289A1 (en) * 2004-03-23 2005-10-13 Amgen Inc. Chemically modified protein compositions and methods
WO2007073597A1 (en) * 2005-12-27 2007-07-05 Mcmaster University Enzyme measurement assay using a modified substrate comprising a substrate attached to a macromolecule via a spacer
EP1993608A1 (en) * 2006-03-10 2008-11-26 Diatos Anticancer drugs conjugated to antibody via an enzyme cleavable linker
CA2739757C (en) * 2008-10-07 2016-07-05 Rexahn Pharmaceuticals, Inc. Hpma - docetaxel or gemcitabine conjugates and uses therefore
KR20100083632A (en) * 2009-01-14 2010-07-22 울산대학교 산학협력단 Anticancer prodrug sensitive to target protease
MX2012004416A (en) 2009-10-13 2012-05-08 Rexahn Pharmaceuticals Inc Polymeric systems for the delivery of anticancer agents.
GB201700557D0 (en) * 2017-01-12 2017-03-01 Peptinnovate Ltd Novel peptides

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996005863A1 (en) * 1994-08-19 1996-02-29 La Region Wallonne Compounds, pharmaceutical composition and diagnostic device comprising same and their use
WO2001091798A2 (en) * 2000-06-01 2001-12-06 Universite Catholique De Louvain Tumor activated prodrug compounds
WO2001095945A2 (en) * 2000-06-14 2001-12-20 Medarex, Inc. Prodrug compounds cleavable by thimet oligopeptidase

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996005863A1 (en) * 1994-08-19 1996-02-29 La Region Wallonne Compounds, pharmaceutical composition and diagnostic device comprising same and their use
WO2001091798A2 (en) * 2000-06-01 2001-12-06 Universite Catholique De Louvain Tumor activated prodrug compounds
WO2001095945A2 (en) * 2000-06-14 2001-12-20 Medarex, Inc. Prodrug compounds cleavable by thimet oligopeptidase

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
GREENWALD R B ET AL: "Effective drug delivery by PEGylated drug conjugates", ADVANCED DRUG DELIVERY REVIEWS 10 FEB 2003 NETHERLANDS, vol. 55, no. 2, 10 February 2003 (2003-02-10), pages 217 - 250, XP002275066, ISSN: 0169-409X *
KRATZ FELIX ET AL: "Development and in vitro efficacy of novel MMP2 and MMP9 specific doxorubicin albumin conjugates", BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS, vol. 11, no. 15, 6 August 2001 (2001-08-06), pages 2001 - 2006, XP002360788, ISSN: 0960-894X *
MANSOUR AHMED M ET AL: "A new approach for the treatment of malignant melanoma: Enhanced antitumor efficacy of an albumin-binding doxorubicin prodrug that is cleaved by matrix metalloproteinase 2.", CANCER RESEARCH, vol. 63, no. 14, 15 July 2003 (2003-07-15), pages 4062 - 4066, XP002360787, ISSN: 0008-5472 *

Also Published As

Publication number Publication date
JP2007503382A (en) 2007-02-22
EP1701743A2 (en) 2006-09-20
FR2858936A1 (en) 2005-02-25
BRPI0413843A (en) 2006-10-24
IL173760A0 (en) 2006-07-05
AU2004268405A1 (en) 2005-03-10
CA2536442A1 (en) 2005-03-10
WO2005021043A2 (en) 2005-03-10

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