tezacitabine

Small moleculeexperimental

Tezacitabine is a ribonucleotide reductase inhibitor. It is a synthetic purine nucleoside analogue with potential antineoplastic activity. It is used in synthetic DNA. — Wikipedia

Clinical trial activity

3 trials · 2 clinical orgs · 0 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Sep 1, 2001 (NCT00061620)

Timeline

2000s

Jan 1, 2001
Earliest Phase 1 Sponsor(trial)
Jan 1, 2003
Earliest Phase 2 Sponsor(trial)

Indications

Studied for

Mechanism of action

Ribonucleoside-diphosphate reductase RR1INHIBITOR
Ribonucleoside-diphosphate reductase RR1 inhibitor
Irreversible ribonucleotide reductase inhibitor and DNA chain terminator. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites.

Chemistry & pharmacology

Loading structure…

SMILES

Nc1ccn([C@@H]2O[C@H](CO)[C@@H](O)/C2=C\F)c(=O)n1.O

Mol. weight: 275.24 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Single Stereoisomer
Inorganic: No
Polymer: No

Oral

Parenteral

Topical

Sources

Also known as

2'-deoxy-2'-(fluoromethylene)cytidine
anhydrous
anhydrous
cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2e)-
fmdc
fmdc
mdl 101731
mdl 101,731
mdl-101731
mdl-101731
mdl-101731
mdl-101,731
tezacitabine
tezacitabine
tezacitabine
tezacitabine

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT00054873	Phase 2	Nov 1, 2003	Chiron
NCT00051688	Phase 2	Jun 1, 2003	Chiron
NCT00061620	Phase 1	Sep 1, 2001	Chiron, University of Texas at Houston

Showing 3 of 3 trials

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Organizations

Research & Development (2)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Chiron	For profit	3	2	2	2001
University of Texas at Houston	Academic/Hospital	1	1	1	2001

2 organizations

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