tecarfarin
Tecarfarin is a vitamin K antagonist under development for use as an anticoagulant. A Phase II/III clinical trial in 607 people, comparing it to the established vitamin K antagonist warfarin, found no difference in quality of anticoagulation or side effects between the two drugs in the overall population. Among patients taking CYP2C9 interacting drugs however, the tecarfarin patients’ TTR was 72.2% (n=92) vs 69.9% (n=87) for warfarin patients (pint=0.16); among patients who had both a CYP2C9 variant allele and taking a CYP2C9 interacting drug, TTR was 76.5% and 69.5% for the tecarfarin (n=24) and warfarin (n=31) groups, respectively (pint=0.24). This study included in 84 (14%) patients with a mechanical heart valve as an indication for anticoagulation therapy. No thrombotic or embolic events were observed in the tecarfarin treated subjects. In contrast to warfarin, tecarfarin is not affected by the cytochrome P450 inhibiting drug fluconazole, indicating a lower potential for interactions with other drugs. — Wikipedia
Clinical trial activity
5 trials · 4 clinical orgs · 0 marketing orgs
Earliest trial started Dec 1, 2006 (NCT00431782)
Timeline
Indications
Mechanism of action
- Cytochrome P450 2C9INHIBITOR
CYP2C9 inhibitor
Vitamin k epoxide reductase complex subunit 1 isoform 1 inhibitor
Chemistry & pharmacology
SMILES
CC(OC(=O)c1ccc(Cc2c(O)c3ccccc3oc2=O)cc1)(C(F)(F)F)C(F)(F)F- Mol. weight
- 460.33 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2105664 ↗
- WikipediaTecarfarin ↗
- ChEMBLCHEMBL2105676 ↗
Also known as
- 60 tis 99
- 60 tis 99
- ati5923
- ati 5923
- ati-5923
- ati-5923
- ati-5923
- ati-5923
- tecarfarin
- tecarfarin
- tecarfarin
- tecarfarin
- tecarfarin
- tecarfarin sodium
- tecarfarin sodium
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04627116 | Phase 1 | Apr 19, 2020 | Lee's Pharmaceutical |
| NCT03652779 | Phase 1 | Jun 22, 2018 | Lee's Pharmaceutical, The University of Hong Kong |
| NCT02522221 | Phase 3 | Dec 1, 2016 | Armetheon Inc |
| NCT00691470 | Phase 2/Phase 3 (Phase 3) | May 1, 2008 | ARYx Therapeutics |
| NCT00431782 | Phase 2 | Dec 1, 2006 | ARYx Therapeutics |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| ARYx Therapeutics | For profit | 2 | 2 | 2 | 2006 |
| Lee's Pharmaceutical | For profit | 2 | 2 | 1 | 2018 |
| Armetheon Inc | For profit | 1 | 1 | 1 | 2016 |
| The University of Hong Kong | Academic/Hospital | 1 | 0 | 1 | 2018 |