WO2002055097A3 - Conjugates of nucleosides with lactosaminated human albumine - Google Patents

Conjugates of nucleosides with lactosaminated human albumine Download PDF

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Publication number
WO2002055097A3
WO2002055097A3 PCT/EP2002/000435 EP0200435W WO02055097A3 WO 2002055097 A3 WO2002055097 A3 WO 2002055097A3 EP 0200435 W EP0200435 W EP 0200435W WO 02055097 A3 WO02055097 A3 WO 02055097A3
Authority
WO
WIPO (PCT)
Prior art keywords
nucleosides
antiblastic
conjugates
analogs
lactosaminated
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/EP2002/000435
Other languages
French (fr)
Other versions
WO2002055097A2 (en
Inventor
Luigi Fiume
Stefano Giuseppina Di
Corrado Busi
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.)
University of Bologna
Original Assignee
University of Bologna
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 University of Bologna filed Critical University of Bologna
Priority to AU2002242680A priority Critical patent/AU2002242680A1/en
Priority to EP02708297A priority patent/EP1351700B1/en
Priority to AT02708297T priority patent/ATE284218T1/en
Priority to DE60202193T priority patent/DE60202193T2/en
Priority to US10/250,875 priority patent/US20040044178A1/en
Publication of WO2002055097A2 publication Critical patent/WO2002055097A2/en
Publication of WO2002055097A3 publication Critical patent/WO2002055097A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)

Abstract

Pharmaceutical compositions containing as active compound conjugates of lactosaminated albumin with antiblastic nucleosides (and their analogs) are here described. These compositions are particularly useful to increase the efficacy of the antiblastic nucleosides (and their analogs) on liver micrometastases. They preferably consist of aqueous solutions administered by parenteral route, preferably by intravenous injection. The antiblastic nucleoside of choice is 5-fluoro-2'-deoxyuridine (FUdR).
PCT/EP2002/000435 2001-01-10 2002-01-07 Conjugates of nucleosides with lactosaminated human albumine Ceased WO2002055097A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
AU2002242680A AU2002242680A1 (en) 2001-01-10 2002-01-07 Conjugates of nucleosides with lactosaminated human albumine
EP02708297A EP1351700B1 (en) 2001-01-10 2002-01-07 Conjugates of nucleosides with lactosaminated human albumine
AT02708297T ATE284218T1 (en) 2001-01-10 2002-01-07 NUCLEOSIDES CONJUGATED WITH HUMAN LACTOSAMINATED ALBUMINE
DE60202193T DE60202193T2 (en) 2001-01-10 2002-01-07 NUCLEOSIDE CONJUGATES WITH HUMAN LACTOSAMINATED ALBUMIN
US10/250,875 US20040044178A1 (en) 2001-01-10 2002-01-07 Hepatotropic conjugates of antiblastic drugs accomplishing a loco-regional chemotherapy of liver micrometastases after adminstration by peripheral venous route

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT2001MI000027A ITMI20010027A1 (en) 2001-01-10 2001-01-10 THERAPUTIC COMPOSITIONS FOR A NON-INVASIVE LOCOREGIONAL CHEMOTHERAPY OF HEPATIC MICROMETASTASIS
ITMI2001A000027 2001-01-10

Publications (2)

Publication Number Publication Date
WO2002055097A2 WO2002055097A2 (en) 2002-07-18
WO2002055097A3 true WO2002055097A3 (en) 2002-10-03

Family

ID=11446415

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/000435 Ceased WO2002055097A2 (en) 2001-01-10 2002-01-07 Conjugates of nucleosides with lactosaminated human albumine

Country Status (7)

Country Link
US (1) US20040044178A1 (en)
EP (1) EP1351700B1 (en)
AT (1) ATE284218T1 (en)
AU (1) AU2002242680A1 (en)
DE (1) DE60202193T2 (en)
IT (1) ITMI20010027A1 (en)
WO (1) WO2002055097A2 (en)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080219939A1 (en) * 2007-03-07 2008-09-11 Grune Guerry L Sunblock formulations

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5594110A (en) * 1992-11-23 1997-01-14 Laboratori Baldacci Spa Process of conjugation of antiviral nucleosides with lactosaminated human albumin

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1177381B (en) * 1984-12-11 1987-08-26 Baldacci Lab Spa METHOD FOR THE PREPARATION OF ADENINE-9-BETA-D-ARABINO FURANO-SIDE 5 'CONJUGATES MONOPHOSPHATE WITH HUMAN LACTOSAMINATED ALBUMIN, RESULTING CONJUGATES AND RELATED THERAPEUTICALLY ACTIVE COMPOSITIONS
IT1207507B (en) * 1985-10-21 1989-05-25 Baldacci Lab Spa CONJUGATE OF 9- (2-HYDROXYETHOXYMETHYL) GUANINE WITH LACTOSAMINATED HUMAN ALBUMIN, PROCEDURE FOR ITS PREPARATION AND PHARMACEUTICAL COMPOSITIONS THAT CONTAIN IT.
US6291638B1 (en) * 1993-05-26 2001-09-18 Laboratori Balducci S.P.A. Hepatotropic conjugates of antiviral drugs carriers thereof and pharmaceutical compositions containing them
US5959077A (en) * 1993-05-26 1999-09-28 Laboratori Balducci S.P.A. Hepatotropic conjugates of antiviral drugs carriers thereof and pharmaceutical compositions containing them

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5594110A (en) * 1992-11-23 1997-01-14 Laboratori Baldacci Spa Process of conjugation of antiviral nucleosides with lactosaminated human albumin

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
DI STEFANO G ET AL: "Enhanced liver blood concentrations of adenine arabinoside accomplished by lactosaminated poly-L-lysine coupling: implications for regional chemotherapy of hepatic micrometastases.", BIOCHEMICAL PHARMACOLOGY. ENGLAND 1 FEB 2000, vol. 59, no. 3, 1 February 2000 (2000-02-01), pages 301 - 304, XP001074753, ISSN: 0006-2952 *
FIUME L ET AL: "Coupling of antiviral nucleoside analogs to lactosaminated human albumin by using the imidazolides of their phosphoric esters.", ANALYTICAL BIOCHEMISTRY. UNITED STATES 1 AUG 1993, vol. 212, no. 2, 1 August 1993 (1993-08-01), pages 407 - 411, XP000371938, ISSN: 0003-2697 *
FIUME L ET AL: "Liver targeting of antiviral nucleoside analogues through the asialoglycoprotein receptor.", JOURNAL OF VIRAL HEPATITIS. ENGLAND 1997, vol. 4, no. 6, 1997, pages 363 - 370, XP008004173, ISSN: 1352-0504 *
FIUME L ET AL: "Liver targeting of nucleoside analogues coupled to galactosyl terminating macromolecules: a new approach to the treatment of a chronic viral hepatitis.", ITALIAN JOURNAL OF GASTROENTEROLOGY AND HEPATOLOGY. ITALY JUN 1997, vol. 29, no. 3, June 1997 (1997-06-01), pages 275 - 280, XP008004174, ISSN: 1125-8055 *
FIUME L ET AL: "The pathogenesis of vacuoles produced in rat and mouse liver cells by a conjugate of adenine arabinoside monophosphate with lactosaminated albumin.", JOURNAL OF HEPATOLOGY, vol. 15, no. 3, 1992, pages 314 - 322, XP008004165, ISSN: 0168-8278 *
PONZETTO A ET AL: "ARA AMP AND ACYCLOVIR MONOPHOSPHATE COUPLED TO LACTOSAMINATED ALBUMIN REDUCE WOODCHUCK HEPATITIS VIRUS VIREMIA AT DOSES LOWER THAN DO THE UNCONJUGATED DRUGS", HEPATOLOGY, vol. 14, no. 1, 1991, pages 16 - 24, XP000800471, ISSN: 0270-9139 *

Also Published As

Publication number Publication date
US20040044178A1 (en) 2004-03-04
ATE284218T1 (en) 2004-12-15
WO2002055097A2 (en) 2002-07-18
EP1351700A2 (en) 2003-10-15
DE60202193T2 (en) 2005-05-04
DE60202193D1 (en) 2005-01-13
AU2002242680A1 (en) 2002-07-24
ITMI20010027A1 (en) 2002-07-10
EP1351700B1 (en) 2004-12-08

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