Page last updated: 2024-12-11

tezacitabine

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

tezacitabine: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6435808
CHEMBL ID2105467
SCHEMBL ID18724
SCHEMBL ID18725
MeSH IDM0383847

Synonyms (39)

Synonym
mdl-101731
kw-2331
tezacitabine
mdl 101731
fmdc cpd
2'-deoxy-2'-(fluoromethylene)cytidine
cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2e)-
mdl 101,731
4-amino-1-[(2r,3e,4s,5r)-3-(fluoromethylidene)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
(e)-2'-deoxy-2'-(fluoromethylene)cytidine
tezacitabine, anhydrous
130306-02-4
unii-7607y95n9s
tezacitabine [inn]
tezacitabine, anhydrous [inn]
7607y95n9s ,
fmd-c
CHEMBL2105467
cytidine, 2'-deoxy-2'-(fluoromethylene)-
171233-40-2
(2'e)-2'-deoxy-2'-(fluoromethylene)cytidine
cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2'e)-
tezacitabine [who-dd]
2'-deoxy-2'-((e)-fluoromethylene)cytidine
tezacitabine anhydrous
GFFXZLZWLOBBLO-ASKVSEFXSA-N
SCHEMBL18724
SCHEMBL18725
(e)-2'-deoxy-2'-(fluoromethylene) cytidine
DTXSID10156446
4-amino-1-((2r,4s,5r,e)-3-(fluoromethylene)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1h)-one
Q383775
mfcd00893181
DB06433
fmdc; kw 2331; mdl 101731
4-amino-1-((2r,4s,5r)-3-(fluoromethylene)-4-hydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1h)-one
MS-23621
CS-0024626
HY-106014

Research Excerpts

Overview

Tezacitabine (FMdC) is a new cytostatic/cytotoxic agent widely investigated in clinical trials and on the cellular level. It is a nucleoside analogue characterized by a dual mechanism of action.

ExcerptReferenceRelevance
"Tezacitabine (FMdC) is a new cytostatic/cytotoxic agent widely investigated in clinical trials and on the cellular level. "( Tezacitabine blocks tumor cells in G1 and S phases of the cell cycle and induces apoptotic cell death.
Grieb, P; Koronkiewicz, M; Skierski, JS,
)
3.02
"Tezacitabine is a nucleoside analogue characterized by a dual mechanism of action. "( Tezacitabine enhances the DNA-directed effects of fluoropyrimidines in human colon cancer cells and tumor xenografts.
Aardalen, K; Doyle, L; Hibner, B; Jekic-McMullen, D; Moler, E; Rendahl, K; Salangsang, F; Shao, Y; Taverna, P, 2007
)
3.23

Toxicity

ExcerptReferenceRelevance
" After 24 h incubation tezacitabine was equally or less toxic compared to cladribine."( Cytotoxic effects of cladribine and tezacitabine toward HL-60.
Grieb, P; Skierski, JS; Stachnik, K, 2005
)
0.91

Compound-Compound Interactions

ExcerptReferenceRelevance
"Tezacitabine at a dose of 200 mg/m(2) in combination with CI 5-FU at a dose of 200 mg/m(2) per day was relatively well tolerated and had clinical activity in patients with advanced solid tumors, particularly in patients with esophageal and other gastrointestinal carcinomas."( Phase I dose-escalation study of tezacitabine in combination with 5-fluorouracil in patients with advanced solid tumors.
Bendell, JC; Clark, JW; Eder, JP; Fidias, P; Lynch, TJ; Ryan, DP; Seiden, MV, 2005
)
2.05

Dosage Studied

ExcerptRelevanceReference
" Studies were performed to optimize dosing schedule and route of administration."( Response of human colon and prostate tumor xenografts to (E)-2'-deoxy-2'-(fluoromethylene) cytidine, an inhibitor of ribonucleotide reductase.
Bitonti, AJ; Bush, TL; Lewis, MT; Sunkara, PS,
)
0.13
"5 mg/kg MDL 101,731 following the same dosing regimen."( Regression of human breast tumor xenografts in response to (E)-2'-deoxy-2'-(fluoromethylene)cytidine, an inhibitor of ribonucleoside diphosphate reductase.
Bitonti, AJ; Bush, TL; Cashman, EA; Cross-Doersen, DE; Dumont, JA; Kaplan, DA; Matthews, DP; McCarthy, JR; Wright, PS, 1994
)
0.29
" Further investigations are necessary to establish optimal dosing schedules and routes for the administration of FMdC."( Phase I and pharmacologic study of oral (E)-2'-deoxy-2'-(fluoromethylene) cytidine: on a daily x 5-day schedule.
Fukuoka, M; Hirashima, T; Kobayashi, S; Kudoh, S; Kurata, N; Kuwabara, T; Masuda, N; Matsui, K; Negoro, S; Takada, M; Takeda, K; Takifuji, N; Yana, T,
)
0.13
" Preclinical tests have shown antiproliferative activity in various human tumor xenograft models and have also indicated that efficacy is greatest with frequent dosing schedules."( A phase I study of the antimetabolite (E)-2'-fluoromethylene-2'-deoxycytidine (MDL 101,731) administered as a twice-weekly infusion.
Belker, M; Burtness, B; Chmael, SE; Clark, MB; DeVita, VT; Lamb, LA; Marsh, JC; McKeon, A; Peccerillo, KM; Pizzorno, G; Stoltz, M; Winship, J,
)
0.13
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's15 (60.00)18.2507
2000's10 (40.00)29.6817
2010's0 (0.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 18.24

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index18.24 (24.57)
Research Supply Index3.64 (2.92)
Research Growth Index4.25 (4.65)
Search Engine Demand Index15.26 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (18.24)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials6 (19.35%)5.53%
Reviews4 (12.90%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other21 (67.74%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (3)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
[NCT00051688]Phase 20 participants Interventional2003-06-30Terminated
[NCT00054873]Phase 20 participants Interventional2003-11-30Completed
Phase I Study of Continuous Infusion Schedule of (E)-2'-Deoxy-2'-(Fluoromethylene) Cytidine (Tezacitabine, FMdC) in Hematologic Malignancies [NCT00061620]Phase 119 participants (Actual)Interventional2001-09-06Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]