rotigaptide
Rotigaptide (ZP-123) is a drug under clinical investigation for the treatment of cardiac arrhythmias – specifically atrial fibrillation. It is a peptide analog that has been shown to increase gap junction intercellular conductance in cardiac muscle cells. Gap junctions are protein channels that are responsible for conducting electrical impulses between cells in the heart to maintain normal rhythm. Gap junction modulation is a promising and novel mechanism of action for the treatment of cardiovascular disorders. Its peptide sequence is Ac-D-Tyr-D-Pro-D-Hyp-Gly-D-Ala-Gly-NH2. — Wikipedia
Clinical trial activity
4 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Jun 1, 2005 (NCT00124891)
Timeline
2000s
- Jan 1, 2005
Earliest Phase 2 Sponsor(trial)
Indications
Studied for
Mechanism of action
- Gap junction alpha-1 proteinMODULATOR
modulator - Cx43
Chemistry & pharmacology
SMILES
CC(=O)N[C@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@@H]1C(=O)N1C[C@@H](O)C[C@@H]1C(=O)NCC(=O)N[C@H](C)C(=O)NCC(N)=O- Mol. weight
- 617.66 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaRotigaptide ↗
- ChEMBLCHEMBL450656 ↗
Also known as
- ac-d-tyr-d-pro-d-hyp-gly-d-ala-gly-nh2
- acetyl-tyrosyl-prolyl-hydroxyprolyl-glycyl-alanyl-glycinamide
- ac-tyr-pro-hyp-gly-ala-gly-nh2
- gap-486
- gap-486
- rotigaptide
- rotigaptide
- rotigaptide
- rotigaptide
- zp 123
- zp-123
- zp123 peptide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00901563 | N/A | Mar 1, 2009 | Government of Scotland, NHS Lothian, University of Edinburgh |
| NCT00137293 | Phase 2 | Nov 1, 2005 | Pfizer, Wyeth |
| NCT00137332 | Phase 2 | Nov 1, 2005 | Pfizer, Wyeth |
| NCT00124891 | Phase 2 | Jun 1, 2005 | Pfizer, Wyeth |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 3 | 3 | 1 | 2005 |
| Wyeth | For profit | 3 | 0 | 1 | 2005 |
| Government of Scotland | Government | 1 | 0 | 1 | 2009 |
| NHS Lothian | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Edinburgh | Academic/Hospital | 1 | 1 | 1 | 2009 |