WO2001000240A2 - Compose antitumoral - Google Patents

Compose antitumoral Download PDF

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Publication number
WO2001000240A2
WO2001000240A2 PCT/EP2000/005348 EP0005348W WO0100240A2 WO 2001000240 A2 WO2001000240 A2 WO 2001000240A2 EP 0005348 W EP0005348 W EP 0005348W WO 0100240 A2 WO0100240 A2 WO 0100240A2
Authority
WO
WIPO (PCT)
Prior art keywords
formula
camptothecin
compound
tumor
mole
Prior art date
Application number
PCT/EP2000/005348
Other languages
English (en)
Other versions
WO2001000240A3 (fr
Inventor
Antonino Suarato
Francesco Angelucci
Mariella Farao
Valeria Caiolfa
Original Assignee
Pharmacia & Upjohn Spa
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 Pharmacia & Upjohn Spa filed Critical Pharmacia & Upjohn Spa
Priority to AU50775/00A priority Critical patent/AU5077500A/en
Publication of WO2001000240A2 publication Critical patent/WO2001000240A2/fr
Publication of WO2001000240A3 publication Critical patent/WO2001000240A3/fr

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
    • A61K47/65—Peptidic linkers, binders or spacers, e.g. peptidic enzyme-labile linkers

Definitions

  • the polymer-bound conjugates of formula 1 were described and claimed in our international patent application EP98/06048, filed on September 22, 1998.
  • the polymer-bound conjugates of formula 1 are random polymer, i.e. above formula does not indicate the exact monomer sequence, and have a molecular weight preferably in the range of from 10,000 to 45,000, more preferably from 18,000 to 35,000.
  • the conjugates of formula 1 are unexpectedly endowed with remarkable antitumor activity against pancreatic malignancies, which are known to be not sensitive to the other known anticancer agents.
  • the polymeric conjugates of the formula 1 contain the N- (2-hydroxypropyl) methacryloyl amide units in a proportion of 90 % or more; more preferably x is 90%.
  • the course of therapy generally employed is from about 1 to about 1000 mg/m 2 of captothecin of camptothecin equivalent per m 2 body surface area for one to about three days. More preferably, the course therapy employed is from about 100 to about 500 mg/nr of body surface area per day for one to five consecutive days.
  • the present invention is directed to the preparation of a pharmaceutical composition contaning an effective amount of a compound of formula 1 in the therapy of pancreatic tumor in mammals, including humans, as well as to the use of a compound of formula 1 for the treatment of pancreatic tumors.
  • the following biological examples illustrate the invention. Antitumor Activity

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne l'utilisation d'un composé correspondant à la formule (1) dans la préparation d'un médicament destiné au traitement de tumeurs du pancréas.
PCT/EP2000/005348 1999-06-29 2000-06-08 Compose antitumoral WO2001000240A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU50775/00A AU5077500A (en) 1999-06-29 2000-06-08 Antitumor compound

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9915180.5A GB9915180D0 (en) 1999-06-29 1999-06-29 Antitumour compound
GB9915180.5 1999-06-29

Publications (2)

Publication Number Publication Date
WO2001000240A2 true WO2001000240A2 (fr) 2001-01-04
WO2001000240A3 WO2001000240A3 (fr) 2001-03-15

Family

ID=10856268

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/005348 WO2001000240A2 (fr) 1999-06-29 2000-06-08 Compose antitumoral

Country Status (3)

Country Link
AU (1) AU5077500A (fr)
GB (1) GB9915180D0 (fr)
WO (1) WO2001000240A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001076597A2 (fr) * 2000-04-11 2001-10-18 Pharmacia & Upjohn Spa Methode d'administration d'un compose antitumoral

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995010304A1 (fr) * 1993-10-08 1995-04-20 Pharmacia S.P.A Derives de camptothecine lies a des polymeres
WO1999017804A1 (fr) * 1997-10-03 1999-04-15 Pharmacia & Upjohn S.P.A. Derives polymeres de camptothecines

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995010304A1 (fr) * 1993-10-08 1995-04-20 Pharmacia S.P.A Derives de camptothecine lies a des polymeres
WO1999017804A1 (fr) * 1997-10-03 1999-04-15 Pharmacia & Upjohn S.P.A. Derives polymeres de camptothecines

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
DATABASE MEDLINE [Online] US NATIONAL LIBRARY OF MEDICINE (NLM), BETHESDA, MD, US; CAIOLFA V R ET AL: "Polymer -bound camptothecin: initial biodistribution and antitumour activity studies." retrieved from STN Database accession no. 2000165376 XP002156326 & JOURNAL OF CONTROLLED RELEASE, (2000 MAR 1) 65 (1-2) 105-19. , *
FRAIER D ET AL: "Determination of MAG- camptothecin, a new polymer -boun camptothecin derivative, and free camptothecin in dog plasma by HPLC with fluorimetric detection." JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS, (2000 APR) 22 (3) 505-14. , XP000971260 *
LERCHEN H.-G.: "Camptothecin antitumor agents." IDRUGS, (1999) 2/9 (896-906). , XP000971262 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001076597A2 (fr) * 2000-04-11 2001-10-18 Pharmacia & Upjohn Spa Methode d'administration d'un compose antitumoral
WO2001076597A3 (fr) * 2000-04-11 2002-05-16 Pharmacia & Upjohn Spa Methode d'administration d'un compose antitumoral

Also Published As

Publication number Publication date
GB9915180D0 (en) 1999-09-01
WO2001000240A3 (fr) 2001-03-15
AU5077500A (en) 2001-01-31

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