Evidence map›Paper›PMID 15980324›Full record

ArticleAntimicrobial agents and chemotherapy2005

Pharmacology and pharmacokinetics of the antiviral agent beta-D-2',3'-dideoxy-3'-oxa-5-fluorocytidine in cells and rhesus monkeys.

Brenda I Hernandez-Santiago, Huachun Chen, Ghazia Asif, Thierry Beltran, Shuli Mao, Selwyn J Hurwitz, Jason Grier, Harold M McClure, Chung K Chu, Dennis C Liotta and 1 more

Abstract read
In one paragraph

Article in Antimicrobial agents and chemotherapy, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.5field-weighted citation impact, top 36% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed, 7 citations in OpenAlex.

  1. Review
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4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

11 authors at 3 institutions in 1 country.

Brenda I Hernandez-SantiagoDepartment of Pediatrics, Emory School of Medicine/Veterans Affairs Medical Center, Medical Research 151H, 1670 Clairmont Rd., Decatur, Georgia 30033, SUA.
Huachun Chen
Ghazia Asif
Thierry Beltran
Shuli Mao
Selwyn J Hurwitz
Jason Grier
Harold M McClure
Chung K Chu
Dennis C Liotta
Raymond F Schinazi
University of Georgia · USCentro Nacional de PrimatasEmory University · US

Funding

YNPRC NHP CLINICAL MEDICINE RESIDENCY PROGRAM - SUPPLEMENTP51RR000165 · NCRR · EMORY UNIVERSITY · PI JOHNS, MICHAEL M · 1985 to 2011
$114.0M
Virology and Molecular Biomarkers CoreP30AI050409 · NIAID · EMORY UNIVERSITY · PI Hannah LF Cooper · 2002 to 2026
$74.0M
NUCLEOSIDES WITH DUAL ANTI-HIV AND HBV ACTIVITYR37AI041980 · NIAID · EMORY UNIVERSITY · PI SCHINAZI, RAYMOND FELIX · 2000 to 2009
$2.1M
SYNTHESIS &EVALUATION OF ANTI-HIV NUCLEOSIDESR01AI032351 · NIAID · UNIVERSITY OF GEORGIA (UGA) · PI CHU, CHUNG K · 1992 to 2005
$1.7M
NCRR NIH HHS P51 RR000165NCRR NIH HHS RR00165NIAID NIH HHS 2P30-AI-50409NIAID NIH HHS AI-32351NIAID NIH HHS P30 AI050409NIAID NIH HHS R01 AI032351NIAID NIH HHS R37 AI041980NIAID NIH HHS R37-AI-41980
6 · The paper itself

Abstract

Beta-D-2',3'-dideoxy-3'-oxa-5-fluorocytidine (D-FDOC) is an effective inhibitor of human immunodeficiency virus 1 (HIV-1) and HIV-2, simian immunodeficiency virus, and hepatitis B virus (HBV) in vitro. The purpose of this study was to evaluate the intracellular metabolism of d-FDOC in human hepatoma (HepG2), human T-cell lymphoma (CEM), and primary human peripheral blood mononuclear (PBM) cells by using tritiated compound. By 24 h, the levels of D-FDOC-triphosphate (D-FDOC-TP) were 2.8 +/- 0.4, 6.7 +/- 2.3, and 2.0 +/- 0.1 pmol/10(6) cells in HepG2, CEM, and primary human PBM cells, respectively. Intracellular D-FDOC-TP concentrations remained greater than the 50% inhibitory concentration for HIV-1 reverse transcriptase for up to 24 h after removal of the drug from cell cultures. In addition to d-FDOC-monophosphate (D-FDOC-MP), -diphosphate (D-FDOC-DP), and -TP, D-FDOC-DP-ethanolamine and d-FDOC-DP-choline were detected in all cell extracts as major intracellular metabolites. D-FDOC was not a substrate for Escherichia coli thymidine phosphorylase. No toxicity was observed in mice given D-FDOC intraperitoneally for 6 days up to a dose of 100 mg/kg per day. Pharmacokinetic studies in rhesus monkeys indicated that D-FDOC has a t(1/2) of 2.1 h in plasma and an oral bioavailability of 38%. The nucleoside was excreted unchanged primary in the urine, and no metabolites were detected in plasma or urine. These results suggest that further safety and pharmacological studies are warranted to assess the potential of this nucleoside for the treatment of HIV- and HBV-infected individuals.

Indexed as

Antiviral AgentsCytidineAnimalsCell Line, TumorEscherichia coliFemaleHumansLeukocytes, MononuclearMacaca mulattaMaleMiceThymidine Phosphorylase2',3'-dideoxy-5-fluoro-oxacytidineAntiviral AgentsCytidineThymidine Phosphorylase

Identifiers

PMID15980324
PMCPMC1168701
OpenAlexW2138427032

What OpenQuestion holds

Textmetadata
Read underepoch 390

Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.