Evidence map›Paper›PMID 15655513›Full record

ArticleBritish journal of pharmacology2005

Preclinical pharmacology of lumiracoxib: a novel selective inhibitor of cyclooxygenase-2.

Ronald Esser, Carol Berry, Zhengming Du, Janet Dawson, Alyson Fox, Roger A Fujimoto, William Haston, Earl F Kimble, Julie Koehler, Jane Peppard and 8 more

Open access · greenAbstract read
In one paragraph

Article in British journal of pharmacology, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.

0numbers the graph read from it
0cells of the map it votes in
25citing papers in PubMed
11.0field-weighted citation impact, top 1% 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

25 citing papers in PubMed, 123 citations in OpenAlex.

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  16. Selective COX-2 Inhibitors: A Review of Their Structure-Activity Relationships.Iranian journal of pharmaceutical research : IJPR · 2011
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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

18 authors at 1 institution in 1 country.

Ronald EsserArthritis Bone Metabolism at Novartis Institute for Biomedical Research, East Hanover, NJ, USA.
Carol Berry
Zhengming Du
Janet Dawson
Alyson Fox
Roger A Fujimoto
William Haston
Earl F Kimble
Julie Koehler
Jane Peppard
Elizabeth Quadros
Joseph Quintavalla
Karen Toscano
Laszlo Urban
John van Duzer
Xiaoli Zhang
Siyuan Zhou
Paul J Marshall
Novartis (Switzerland) · CH

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

1. This manuscript presents the preclinical profile of lumiracoxib, a novel cyclooxygenase-2 (COX-2) selective inhibitor. 2. Lumiracoxib inhibited purified COX-1 and COX-2 with K(i) values of 3 and 0.06 microM, respectively. In cellular assays, lumiracoxib had an IC(50) of 0.14 microM in COX-2-expressing dermal fibroblasts, but caused no inhibition of COX-1 at concentrations up to 30 microM (HEK 293 cells transfected with human COX-1). 3. In a human whole blood assay, IC(50) values for lumiracoxib were 0.13 microM for COX-2 and 67 microM for COX-1 (COX-1/COX-2 selectivity ratio 515). 4. Lumiracoxib was rapidly absorbed following oral administration in rats with peak plasma levels being reached between 0.5 and 1 h. 5. Ex vivo, lumiracoxib inhibited COX-1-derived thromboxane B(2) (TxB(2)) generation with an ID(50) of 33 mg kg(-1), whereas COX-2-derived production of prostaglandin E(2) (PGE(2)) in the lipopolysaccharide-stimulated rat air pouch was inhibited with an ID(50) value of 0.24 mg kg(-1). 6. Efficacy of lumiracoxib in rat models of hyperalgesia, oedema, pyresis and arthritis was dose-dependent and similar to diclofenac. However, consistent with its low COX-1 inhibitory activity, lumiracoxib at a dose of 100 mg kg(-1) orally caused no ulcers and was significantly less ulcerogenic than diclofenac (P<0.05). 7. Lumiracoxib is a highly selective COX-2 inhibitor with anti-inflammatory, analgesic and antipyretic activities comparable with diclofenac, the reference NSAID, but with much improved gastrointestinal safety.

Indexed as

AnimalsAnti-Inflammatory Agents, Non-SteroidalArthritis, ExperimentalBiological AvailabilityBlood PlateletsCell LineCyclooxygenase 2Cyclooxygenase 2 InhibitorsCyclooxygenase InhibitorsDiclofenacDinoprostoneDisease Models, AnimalDrug Evaluation, PreclinicalEdemaFemaleFeverAnti-Inflammatory Agents, Non-SteroidalCyclooxygenase 2Cyclooxygenase 2 InhibitorsCyclooxygenase InhibitorsDiclofenacDinoprostonelumiracoxibMembrane ProteinsOrganic ChemicalsProstaglandin-Endoperoxide SynthasesPTGS2 protein, humanThromboxane B2

Identifiers

PMID15655513
PMCPMC1576032
OpenAlexW1978504750

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.