tedizolid phosphate
Trade name: sivextro
Small moleculeapproved
Approved
Jun 20, 2014
Tedizolid phosphate is an oxazolidinone prodrug which in the body is dephosphorylated to the active compound tedizolid. The antibacterial activity of tedizolid is mediated by binding to the 50S subunit of the bacterial ribosome resulting in inhibition of protein synthesis. Tedizolid inhibits bacterial protein synthesis through a mechanism of action different from that of other non-oxazolidinone class antibacterial drugs; therefore, cross-resistance between tedizolid and other classes of antibacterial drugs is unlikely. Tedizolid is bacteriostatic against Gram Positive bacteria such as enterococci, staphylococci, and streptococci. No drug-drug interactions were identified with tedizolid. — NCATS
Clinical trial activity
35 trials · 16 clinical orgs · 1 marketing orgs
Phase 1
19
Phase 2
11
Phase 3
7
Phase 4
4
Earliest trial started Jan 1, 2008 (NCT00671814)
Timeline
Indications
Approved for
Studied for
- Abscess · Phase 2
- Bacterial Infections · Phase 3
- Bone Diseases, Infectious · Phase 2
- Cellulitis · Phase 2
- Cystic Fibrosis · Phase 4
- Diabetes Mellitus · Phase 1
- Endocarditis · Phase 4
- Erysipelas · Phase 2
- Gram-Positive Bacteria · Phase 1
- Gram-Positive Bacterial Infections · Phase 1
- Healthy Volunteers · Phase 1
- Kidney Failure, Chronic · Phase 1
- Liver Diseases · Phase 1
- Obesity · Phase 4
- Pneumonia · Phase 3
- Prosthesis-Related Infections · Phase 4
- Skin Diseases, Bacterial · Phase 3
- Skin Diseases, Infectious · Phase 3
- Tuberculosis · Phase 2
- Tuberculosis, Multidrug-Resistant · Phase 2
- Wound Infection · Phase 1
Mechanism of action
- 50S ribosomal protein L2ANTAGONIST
rplB antagonist
Approval history
- approvedPriority reviewJun 20, 2014
Chemistry & pharmacology
Loading structure…
SMILES
CN1N=NC(=N1)C2=NC=C(C=C2)C3=CC=C(C=C3F)N4C[C@H](CO)OC4=O- Mol. weight
- 370.3378 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Availability
- Prescription Only
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTedizolid ↗
- NCATS97HLQ82NGL ↗
- ChEMBLCHEMBL2105669 ↗
- ChEMBLCHEMBL1257051 ↗
Also known as
- 3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-(hydroxymethyl)oxazolidin-2-one
- 3-(3-fluoro-4-(6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl)phenyl)-5-hydroxymethyloxazolidin-2-one
- [(5r)-3-{3-fluoro-4-[6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl]phenyl}-2-oxo-1,3-oxazolidin-5-yl]methyl dihydrogen phosphate
- [(5r)-3-{3-fluoro-4-[6-(2-methyl-2h-tetrazol-5-yl)pyridin-3-yl]phenyl}-2-oxo-1,3-oxazolidin-5-yl]methyl dihydrogen phosphate
- da7218
- da 7218
- da-7218
- da-7218
- da-7218
- sivextro
- sivextro
- sivextro
- sivextro
- sivextro
- tedizolid
- tedizolid
- tedizolid
- tedizolid
- tedizolid
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- tedizolid phosphate
- torezolid
- torezolid
- torezolid
- torezolid phosphate
- torezolid phosphate
- torezolid phosphate
- torezolid phosphate
- torezolid phosphate
- tr 700
- tr-700
- tr-700
- tr-700
- tr-700
- tr701
- tr701
- tr 701
- tr-701
- tr-701
- tr701 cpd
- tr-701-fa
- tr-701-fa
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05534750 | Phase 2 | Sep 30, 2022 | Assistance Publique - Hôpitaux de Paris |
| NCT05398679 | Phase 4 | Jun 1, 2022 | University of Barcelona |
| NCT03746327 | Phase 4 | Jun 1, 2019 | University of Barcelona |
| NCT03217565 | Phase 1 | Mar 11, 2019 | Merck |
| NCT03378427 | N/A | Aug 28, 2018 | Centre Hospitalier de Tourcoing |
| NCT03176134 | Phase 3 | Jan 17, 2018 | Merck |
| NCT03009045 | Phase 2 | Feb 6, 2017 | Los Angeles Biomedical Research Institute |
| NCT02750761 | Phase 1 | May 2, 2016 | Merck |
| NCT02620787 | Phase 1 | Feb 23, 2016 | Merck, University of Connecticut |
| NCT02444234 | Phase 4 | Jul 1, 2015 | Merck, University of Southern California |
| NCT02477514 | Phase 1 | Jun 1, 2015 | Merck |
| NCT02276482 | Phase 3 | Mar 25, 2015 | Cubist, Merck |
| NCT02342418 | Phase 4 | Mar 1, 2015 | Albany College of Pharmacy and Health Sciences, Merck, University of Michigan |
| NCT02097043 | Phase 1 | May 1, 2014 | Dong-A Pharmaceutical, Seoul National University |
| NCT02066402 | Phase 3 | Mar 4, 2014 | Bayer, Merck |
| NCT02019420 | Phase 3 | Jan 6, 2014 | Cubist, Merck |
| NCT01967225 | Phase 3 | Nov 1, 2013 | Bayer |
| NCT01623401 | Phase 1 | May 1, 2012 | Trius Therapeutics |
| NCT01577459 | Phase 1 | Apr 1, 2012 | Trius Therapeutics |
| NCT01539473 | Phase 1 | Feb 1, 2012 | Trius Therapeutics |
Showing 20 of 35 trials
Page 1 / 2
Organizations
Research & Development (16)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Trius Therapeutics | For profit | 18 | 18 | 3 | 2008 |
| Merck | For profit | 11 | 4 | 3 | 2010 |
| Covance | For profit | 4 | 0 | 1 | 2008 |
| Bayer | For profit | 3 | 2 | 2 | 2012 |
| Cubist | For profit | 2 | 2 | 1 | 2014 |
| University of Barcelona | Academic/Hospital | 2 | 2 | 1 | 2019 |
| Albany College of Pharmacy and Health Sciences | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Assistance Publique - Hôpitaux de Paris | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Centre Hospitalier de Tourcoing | Academic/Hospital | 1 | 1 | 1 | 2018 |
| Dong-A Pharmaceutical | For profit | 1 | 1 | 1 | 2014 |
| Los Angeles Biomedical Research Institute | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Seoul National University | Academic/Hospital | 1 | 0 | 1 | 2014 |
| University of Connecticut | Academic/Hospital | 1 | 1 | 1 | 2016 |
| University of Florida | Academic/Hospital | 1 | 0 | 1 | 2008 |
| University of Michigan | Academic/Hospital | 1 | 0 | 1 | 2015 |
| University of Southern California | Academic/Hospital | 1 | 1 | 1 | 2015 |
16 organizations
Page 1 / 1
Marketing (1)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Cubist | For profit | NDA | Jun 20, 2014 |