Evidence map›Paper›PMID 27858108›Full record

Trial reportEuropean journal of clinical pharmacology2017

Effects of ranitidine (antacid), food, and formulation on the pharmacokinetics of fostamatinib: results from five phase I clinical studies.

Talia Flanagan, Paul Martin, Michael Gillen, David Mathews, Eleanor Lisbon, Martin Kruusmägi

Abstract readClinical Trial, Phase IRandomized Controlled Trial
PubMed Publisher
In one paragraph

Trial report in European journal of clinical pharmacology, 2017. 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
–field-weighted citation impact
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.

  1. Review
  2. Article
  3. Review
  4. Review
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

6 authors.

Talia FlanaganAstraZeneca Pharmaceuticals, Alderley Park, Macclesfield, Cheshire, SK10 4TF, UK.
Paul MartinSandoz, Industriestrasse 25, Holzkirchen, Germany. paul-1.martin@sandoz.com.
Michael GillenAstraZeneca, One MedImmune Way, Gaithersburg, MD, USA.
David MathewsQuintiles Inc., 6700 W. 115th St, Overland Park, KS, 66211, USA.
Eleanor LisbonQuintiles Inc., 6700 W. 115th St, Overland Park, KS, 66211, USA.
Martin KruusmägiLEO Pharma, Industriparken 55, 2750, Ballerup, Denmark.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeFostamatinib is an orally dosed phosphate prodrug that is cleaved by intestinal alkaline phosphatase to the active metabolite R406. Clinical studies were performed to assess the effect of food and ranitidine on exposure, to support in vitro-in vivo relationships (IVIVR) understanding and formulation transitions and to investigate absolute oral bioavailability.

methodsA series of in vitro dissolution and clinical pharmacokinetic studies were performed to support the design and introduction of a new formulation, understand the impact of changes in in vitro dissolution on in vivo performance for two fostamatinib formulations, to characterize the effects of food and ranitidine on exposure, and determine the absolute oral bioavailability.

resultsThe in vivo performance of fostamatinib was generally insensitive to changes in in vitro dissolution performance, although marked slowing of the dissolution rate did impact exposures. Food and ranitidine had minor effects on R406 exposure that were not considered clinically relevant. The absolute oral bioavailability of fostamatinib was 54.6 %.

conclusionsThe absolute oral bioavailability of fostamatinib was ~55 %. Food and ranitidine had minor effects on R406 exposure. An in vitro dissolution versus clinical performance relationship was determined that supported formulation transitions.

Indexed as

Administration, OralAdolescentAdultAminopyridinesAntacidsAnti-Ulcer AgentsBiological AvailabilityCelluloseChemistry, PharmaceuticalCross-Over StudiesDrug InteractionsFemaleFoodHumansMaleMiddle AgedAminopyridinesAntacidsAnti-Ulcer AgentsCellulosefostamatinibmicrocrystalline celluloseMorpholinesOxazinesProdrugsPyridinesPyrimidinesRanitidineSyk KinaseAbsolute bioavailabilityFood effectFostamatinibPharmacokineticsRanitidine DDISYK inhibitor

Identifiers

PMID27858108

What OpenQuestion holds

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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.