EP 1765403 A4 20110330 - COMBINED ACTIVE AND PASSIVE TARGETING OF BIOLOGICALLY ACTIVE AGENTS
Title (en)
COMBINED ACTIVE AND PASSIVE TARGETING OF BIOLOGICALLY ACTIVE AGENTS
Title (de)
KOMBINIERTES AKTIVES UND PASSIVES TARGETING VON BIOLOGISCH AKTIVEN WIRKSTOFFEN
Title (fr)
CIBLAGE ACTIF ET PASSIF COMBINES D'AGENTS BIOLOGIQUEMENT ACTIFS
Publication
Application
Priority
- US 2005015681 W 20050505
- US 56977004 P 20040510
Abstract (en)
[origin: WO2005115457A2] Disclosed is a conjugate comprising a biologically active agent (drug) linked to a subcellular targeting moiety that targets a drug specifically to the nucleus. Targeting is achieved by attaching a steroid hormone (or an analog) to the drug. The steroid hormone attached to the drug binds its corresponding receptor; the formation of the receptor-ligand complex results in the internalization of the complex into the nucleus, thus resulting in nuclear translocation of the drug. Also disclosed is a conjugate (comprising the complex of the drug and the steroid hormone) bound to a polymer by spacers allowing for concurrent passive targeting to the tumor cell (afforded by attachment to the polymer by the EPR effect) and nuclear targeting of the conjugate (due to the presence of the steroid). Using a suitable degradable spacer allows for the release of free drug in the tumor and enhances nuclear targeting efficacy. The polymer can be further linked to a cellular targeting molecule, where the targeting molecule directs the polymer to specific cells. One may thus be able to effectively target drugs to the nucleus of tumor cells. With little or modifications, several therapeutic agents can be targeted using the invention.
IPC 8 full level
C07K 14/00 (2006.01); A61K 39/40 (2006.01); A61K 47/48 (2006.01); C07K 16/00 (2006.01); C07K 16/30 (2006.01)
CPC (source: EP)
A61K 41/0071 (2013.01); A61K 47/554 (2017.07); A61K 47/58 (2017.07); A61K 47/65 (2017.07); A61K 47/6869 (2017.07); C07K 16/3069 (2013.01); C07K 2319/09 (2013.01)
Citation (search report)
- [XI] US 2002099041 A1 20020725 - GALLOP MARK A [US], et al
- [XI] US 5853713 A 19981229 - COOPER EUGENE R [US], et al
- [XI] WO 2004009136 A2 20040129 - PSIMEI PHARMACEUTICALS PLC [GB], et al
- [XI] WO 03046185 A1 20030605 - SALUS THERAPEUTICS [US]
- [XYI] WO 0191798 A2 20011206 - UNIV CATHOLIQUE LOUVAIN [BE], et al
- [XYI] WO 03070982 A1 20030828 - AVARIS AB [SE], et al
- [XYI] WO 9929303 A1 19990617 - EXPRESSION GENETICS INC [US]
- See references of WO 2005115457A2
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU MC NL PL PT RO SE SI SK TR
DOCDB simple family (publication)
WO 2005115457 A2 20051208; WO 2005115457 A3 20090409; EP 1765403 A2 20070328; EP 1765403 A4 20110330
DOCDB simple family (application)
US 2005015681 W 20050505; EP 05780057 A 20050505