troxatyl
Clinical trial activity
4 trials · 3 clinical orgs · 0 marketing orgs
Earliest trial started Oct 1, 2000 (NCT00012259)
Timeline
Indications
Mechanism of action
- DNA polymerase (alpha/delta/epsilon)INHIBITOR
DNA polymerase (alpha/delta/epsilon) inhibitor
The mode of action involves the formation of the triphosphate and incorporation into DNA causing chain termination. Because it lacks a hydroxyl group at the 3'-position, once incorporated into DNA, it causes premature termination of DNA replication and eventually leads to cell death. It is not a permeant for nucleoside transporters (cellular uptake by passive diffusion), it is resistant to deamination, it does not inhibit ribonucleotide reductase, it is activated by deoxycytidine kinase and it is phosphorylated to its triphosphate by 3-phosphoglycerate kinase instead of nucleoside diphosphate kinase.
- DNA polymerase alpha catalytic subunit (POLA1) ↗
- DNA polymerase delta subunit 4 (POLD4) ↗
- DNA polymerase delta subunit 3 (POLD3) ↗
- DNA polymerase delta catalytic subunit (POLD1) ↗
- DNA polymerase delta subunit 2 (POLD2) ↗
- DNA polymerase epsilon catalytic subunit A (POLE) ↗
- DNA polymerase alpha subunit B (POLA2) ↗
- DNA primase small subunit (PRIM1) ↗
- DNA primase large subunit (PRIM2) ↗
- DNA polymerase epsilon subunit 2 (POLE2) ↗
- DNA polymerase epsilon subunit 3 (POLE3) ↗
Chemistry & pharmacology
SMILES
Nc1ccn([C@@H]2CO[C@H](CO)O2)c(=O)n1- Mol. weight
- 213.19 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL359164 ↗
Also known as
- 1-(2-(hydroxymethyl)-1,3-dioxolan-4-yl)cytosine
- 2r(-)-cis-hmd-cytosine
- 2r(-)-trans-hmd-cytosine
- alpha-l-dioxolane-c
- bch 4556
- bch-4556
- bch-4556
- bch-4556
- beta-l-dioxolane-cytidine
- hmd-cytosine
- (-)-oddc
- (-)-oddc
- (-)-oddc
- troxacitabine
- troxacitabine
- troxacitabine
- troxacitabine
- troxacitabine
- troxacitabine
- troxacitabine
- troxacitabine
- troxacitabine, 2r(-)-cis-isomer
- troxacitabine, 2r(-)-trans-isomer
- troxacitabine, 2s(-)-trans-isomer
- troxacitabine, cis-(+-)-isomer
- troxacitabine, trans-(+-)-isomer
- troxatyl
- troxatyl
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00129948 | Phase 2 | Jul 1, 2005 | SGX Pharmaceuticals, University of Texas at Houston |
| NCT00104468 | Phase 1/Phase 2 (Phase 2) | Apr 1, 2003 | SGX Pharmaceuticals |
| NCT00104286 | Phase 1/Phase 2 (Phase 2) | Jan 1, 2003 | SGX Pharmaceuticals |
| NCT00012259 | Phase 2 | Oct 1, 2000 | Shire, University of Texas at Houston |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| SGX Pharmaceuticals | For profit | 3 | 3 | 1 | 2003 |
| University of Texas at Houston | Academic/Hospital | 2 | 0 | 1 | 2000 |
| Shire | For profit | 1 | 1 | 1 | 2000 |