zotarolimus
Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of sirolimus (rapamycin). It was designed for use in stents with phosphorylcholine as a carrier. Zotarolimus, or ABT-578, was originally used on Abbott's coronary stent platforms to reduce early inflammation and restenosis; however, Zotarolimus failed Abbott's primary endpoint to bring their stent/drug delivery system to market. The drug was sold/distributed to Medtronic for use on their stent platforms, which is the same drug they use today. Coronary stents reduce early complications and improve late clinical outcomes in patients needing interventional cardiology. The first human coronary stent implantation was first performed in 1986 by Puel et al. However, there are complications associated with stent use, development of thrombosis which impedes the efficiency of coronary stents, haemorrhagic and restenosis complications are problems associated with stents. — Wikipedia
Clinical trial activity
6 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Dec 1, 2006 (NCT00611286)
Timeline
No events for the selected filters.
Indications
Approved for
Mechanism of action
- RyR1/FKBP12INHIBITOR
RyR1/FKBP12 inhibitor
- FK506-binding protein 1AINHIBITOR
FK506-binding protein 1A inhibitor
Chemistry & pharmacology
SMILES
CO[C@H]1C[C@@H]2CC[C@@H](C)[C@@](O)(O2)C(=O)C(=O)N2CCCC[C@H]2C(=O)O[C@H]([C@H](C)C[C@@H]2CC[C@H](n3cnnn3)[C@H](OC)C2)CC(=O)[C@H](C)/C=C(\C)[C@@H](O)[C@@H](OC)C(=O)[C@H](C)C[C@H](C)/C=C/C=C/C=C/1C- Mol. weight
- 966.23 g/mol
- Lipinski Ro5
- 3 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL219410 ↗
- WikipediaZotarolimus ↗
- ChEMBLCHEMBL1614661 ↗
Also known as
- abt578
- abt578
- abt 578
- abt-578
- abt-578
- abt-578
- abt-578
- abt-578
- zotalolimus
- zotarilumus
- zotarolimus
- zotarolimus
- zotarolimus
- zotarolimus
- zotarolimus
- zotarolimus
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03056118 | Phase 4 | May 2, 2011 | Yonsei University |
| NCT01508663 | Phase 4 | Aug 1, 2010 | Yonsei University |
| NCT01267734 | Phase 4 | Jun 1, 2010 | Boston Scientific Corporation, Seoul National University |
| NCT01887704 | N/A | Jan 1, 2010 | Capital Medical University |
| NCT01857843 | Phase 4 | Nov 1, 2009 | Yonsei University |
| NCT00611286 | Phase 4 | Dec 1, 2006 | University of Ferrara |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Yonsei University | Academic/Hospital | 3 | 3 | 1 | 2009 |
| Boston Scientific Corporation | For profit | 1 | 0 | 1 | 2010 |
| Capital Medical University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| Seoul National University | Academic/Hospital | 1 | 1 | 1 | 2010 |
| University of Ferrara | Academic/Hospital | 1 | 1 | 1 | 2006 |