zoptarelin doxorubicin
Zoptarelin doxorubicin consists of doxorubicin linked to a small peptide agonist to the luteinizing hormone-releasing hormone (LHRH) receptor. It has been developed as a potential treatment for a number of human cancers. The LHRH receptor is aberrantly present on the cell surface of approximately 80% of endometrial and ovarian cancers, 86% of prostate cancers and about 50% of breast cancers. Whereas in normal tissues, expression of this receptor is mainly confined to the pituitary gland, reproductive organs and hematopoietic stem cells. To a lesser extent the LHRH receptor is also found on the surface of bladder, colorectal, and pancreatic cancers, sarcomas, lymphomas, melanomas, and renal cell carcinomas. — Wikipedia
Clinical trial activity
5 trials · 8 clinical orgs · 0 marketing orgs
Earliest trial started Dec 1, 2007 (NCT00569257)
Timeline
Indications
Mechanism of action
GNRHR agonist
- Unspecified targetUnclear
unclear
Chemistry & pharmacology
SMILES
COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)COC(=O)CCCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1- Mol. weight
- 1893.04 g/mol
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaZoptarelin doxorubicin ↗
- ChEMBLCHEMBL3544954 ↗
Also known as
- aezs-108
- aezs-108
- aezs-108
- aezs-108
- an-152
- an-152
- an-152
- lhrh, lysine(6)-doxorubicin
- luteinizing hormone-releasing factor (pig), 6-(n6-(5-(2-(4- ((3-amino-2,3,6-trideoxy-alpha-l-lyxo-hexopyranosyl)oxy)- 1,2,3,4,6,11-hexahydro-2,5,12-trihydroxy-7-methoxy-6,11- dioxo-2-naphthacenyl)-2-oxoethoxy)-1,5-dioxopentyl)-d- lysine)-, (2s-cis)-
- lys(6)-lhrh-doxorubicin
- zen-008
- zoptarelin
- zoptarelin
- zoptarelin doxorubicin
- zoptarelin doxorubicin
- zoptarelin doxorubicin
- zoptarelin doxorubicin
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01767155 | Phase 3 | Apr 1, 2013 | AEterna Zentaris, The University of Texas, Dallas, University of London |
| NCT01698281 | Phase 2 | Dec 1, 2012 | AEterna Zentaris, University of Miami |
| NCT01240629 | Phase 1/Phase 2 (Phase 2) | Nov 2, 2010 | AEterna Zentaris, National Cancer Institute (NCI), University of Southern California |
| NCT01234519 | Phase 1/Phase 2 (Phase 2) | Nov 1, 2010 | AEterna Zentaris, Department of Veteran Affairs, University of Miami |
| NCT00569257 | Phase 2 | Dec 1, 2007 | AEterna Zentaris, AGO Germany |
Organizations
Research & Development (8)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| AEterna Zentaris | For profit | 5 | 4 | 2 | 2007 |
| University of Miami | Academic/Hospital | 2 | 0 | 1 | 2010 |
| AGO Germany | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Department of Veteran Affairs | Government | 1 | 0 | 1 | 2010 |
| National Cancer Institute (NCI) | Government | 1 | 0 | 1 | 2010 |
| The University of Texas, Dallas | Academic/Hospital | 1 | 0 | 1 | 2013 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2013 |
| University of Southern California | Academic/Hospital | 1 | 1 | 1 | 2010 |