EP 0961619 A4 20010926 - HYDROLYZABLE PRODRUGS FOR DELIVERY OF ANTICANCER DRUGS TO METASTATIC CELLS
Title (en)
HYDROLYZABLE PRODRUGS FOR DELIVERY OF ANTICANCER DRUGS TO METASTATIC CELLS
Title (de)
HYDROLISIERBARE PRODRUGS ZUR VERABREICHUNG VON WIRKSTOFFEN GEGEN KREBS AN METASTATISCHE ZELLEN
Title (fr)
PROMEDICAMENTS HYDROLYSABLES POUR LA LIBERATION DE MEDICAMENTS ANTICANCEREUX DANS DES CELLULES METASTATIQUES
Publication
Application
Priority
- US 9717410 W 19970925
- US 4433496 P 19960927
Abstract (en)
[origin: WO9813059A1] Hydrolyzable prodrugs according to the present invention are activated by proteases located in the cell membranes of metastatic cells to yield active anticancer drugs that can be taken up by the metastatic cells. In general, a hydrolyzable prodrug according to the present invention comprises an amino-terminal capped peptide that is a substrate for a peptidohydrolase located on the surface of a metastatic cell covalently linked to a therapeutic drug through a self-immolating spacer of sufficient length to prevent the occurrence of steric hindrance. The therapeutic drug is typically an anticancer drug. The anticancer drug is typically doxorubicin, taxol, camptothecin, mitomycin C, or esperamycin. Typically, the peptidohydrolase that hydrolyses the substrate of the hydrolyzable prodrug is cathepsin B.
IPC 1-7
IPC 8 full level
A61K 47/48 (2006.01); C07K 5/06 (2006.01); C07K 5/065 (2006.01); C07K 5/09 (2006.01); C07K 14/78 (2006.01); A61K 38/00 (2006.01)
CPC (source: EP)
A61K 47/65 (2017.07); C07K 5/06052 (2013.01); C07K 5/06078 (2013.01); C07K 5/0815 (2013.01); C07K 14/78 (2013.01); A61K 38/00 (2013.01)
Citation (search report)
- [E] WO 9819705 A1 19980514 - BRISTOL MYERS SQUIBB CO [US]
- [PX] DUBOWCHIK, GENE M. ET AL: "Monomethoxytrityl (MMT) as a versatile amino protecting group for complex prodrugs of anticancer compounds sensitive to strong acids, bases and nucleophiles", TETRAHEDRON LETT. (1997), 38(30), 5257-5260, July 1997 (1997-07-01), XP002172916
- [X] DUBOWCHIK, GENE M. ET AL: "Cathepsin B-sensitive dipeptide prodrugs. 2. Models of anticancer drugs paclitaxel (taxol), mitomycin C and doxorubicin", BIOORG. MED. CHEM. LETT. (1998), 8(23), 3347-3352, XP002172917
- [X] DUBOWCHIK, GENE M. ET AL: "Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin", BIOORG. MED. CHEM. LETT. (1998), 8(23), 3341-3346, XP002172918
- See references of WO 9813059A1
Designated contracting state (EPC)
AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9813059 A1 19980402; AU 4599597 A 19980417; AU 739028 B2 20011004; CA 2264227 A1 19980402; EP 0961619 A1 19991208; EP 0961619 A4 20010926
DOCDB simple family (application)
US 9717410 W 19970925; AU 4599597 A 19970925; CA 2264227 A 19970925; EP 97944519 A 19970925