Evidence map›Paper›PMID 33165774›Full record

Trial reportEuropean journal of drug metabolism and pharmacokinetics2021

Comparison of the Pharmacokinetics of RIPK1 Inhibitor GSK2982772 in Healthy Western and Japanese Subjects.

Debra J Tompson, Carwyn Davies, Nicola E Scott, Edward P Cannons, Michalis Kostapanos, Annette S Gross, Marcy Powell, Hiroko Ino, Ryutaro Shimamura, Hirofumi Ogura and 3 more

2 registry-linked trialsOpen access · hybridAbstract readComparative StudyRandomized Controlled Trial
In one paragraph

Trial report in European journal of drug metabolism and pharmacokinetics, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. It is linked to 2 registered trials, which are not on this map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
0.9field-weighted citation impact, top 26% 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.

NCT03305419 phase1completednot on this map

A Single-centre, Randomized, Double-blind (Sponsor-unblinded), Placebo-controlled Study to Evaluate the Safety, Tolerability and Pharmacokinetics of GSK2982772 in Repeat Oral Doses in Healthy Subjects

TypeinterventionalSponsorGlaxoSmithKlineRan2017 to 2018Enrolled62ConditionsAutoimmune DiseasesArmsGSK2982772 capsule, Placebo capsule
NCT03590613 phase1completednot on this map

A Single-centre, Randomized, Double-blind, Dose-ascending, Placebo-controlled Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Oral TID Doses (One Day) of GSK2982772 in Japanese Healthy Male Subjects

TypeinterventionalSponsorGlaxoSmithKlineRan2018 to 2018Enrolled13ConditionsAutoimmune DiseasesArmsGSK2982772, Placebo
3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 20 citations in OpenAlex.

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  10. Small-molecule discovery through DNA-encoded libraries.Nature reviews. Drug discovery · 2023
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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

13 authors at 4 institutions in 4 countries.

Debra J TompsonClinical Pharmacology Modelling and Simulation, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK. debra.j.tompson@gsk.com.ORCID http://orcid.org/0000-0003-1030-2611
Carwyn DaviesClinical Pharmacology Modelling and Simulation, GlaxoSmithKline, Sydney, NSW, Australia.ORCID http://orcid.org/0000-0003-0363-3375
Nicola E ScottClinical Pharmacology Modelling and Simulation, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, UK.
Edward P CannonsGlobal Clinical Sciences and Delivery, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire, UK.ORCID http://orcid.org/0000-0002-7370-6018
Michalis KostapanosClinical Care Unit Cambridge, GlaxoSmithKline, and Addenbrooke's Hospital, Cambridge University Hospitals NHS Foundation Trust, Cambridge, Cambridgeshire, UK.ORCID http://orcid.org/0000-0002-7513-5319
Annette S GrossClinical Pharmacology Modelling and Simulation, GlaxoSmithKline, Sydney, NSW, Australia.ORCID http://orcid.org/0000-0001-9567-0127
Marcy PowellSafety and Medical Governance, GlaxoSmithKline, Research Triangle Park, NC, USA.ORCID http://orcid.org/0000-0001-6528-4663
Hiroko InoClinical Pharmacology, Medicines Development, GlaxoSmithKline, Tokyo, Japan.ORCID http://orcid.org/0000-0002-6793-7944
Ryutaro ShimamuraClinical Pharmacology, Medicines Development, GlaxoSmithKline, Tokyo, Japan.ORCID http://orcid.org/0000-0002-7460-7513
Hirofumi OguraClinical Pharmacology, Medicines Development, GlaxoSmithKline, Tokyo, Japan.ORCID http://orcid.org/0000-0002-8042-6495
Takashi NagakuboBiomedical Data Sciences Department, GlaxoSmithKline, Tokyo, Japan.ORCID http://orcid.org/0000-0002-8353-0968
Harue IgarashiPre-Clinical Development Department, GlaxoSmithKline, Tokyo, Japan.ORCID http://orcid.org/0000-0003-0423-128X
Atsushi NakanoMedicines Development, GlaxoSmithKline, Tokyo, Japan.ORCID http://orcid.org/0000-0002-6030-0182
GlaxoSmithKline (Japan) · JPGlaxoSmithKline (United Kingdom) · GBGlaxoSmithKline (Australia) · AUResearch Triangle Park Foundation · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

BACKGROUND AND

objectivesGSK2982772 is an oral small-molecule RIPK1 inhibitor with potential therapeutic efficacy in immune-mediated inflammatory diseases (IMIDs). An inter-ethnic comparison of GSK2982772 pharmacokinetics was conducted based on data from Western (Study 1) and Japanese subjects (Study 2).

methodsBoth studies were single-centre, randomised, double-blind, placebo-controlled studies with objectives to assess the safety and characterise the pharmacokinetics of GSK2982772. Western subjects in Study 1 (NCT03305419), Part A (N = 15), were randomly assigned to receive 120 mg three times daily (TID), 240 mg TID, or 360 mg twice daily (BID) doses of GSK2982772, or placebo (TID or BID) for 1 day. Part B subjects (N = 47) received GSK2982772 120 mg TID, 240 mg TID, or placebo TID for 14 days. Japanese subjects in Study 2 (N = 13) (NCT03590613) were randomly assigned to receive TID doses of GSK2982772 60, 120, 240 mg TID or placebo TID for 1 day.

resultsGSK2982772 was well tolerated and adverse events were generally mild. Maximum observed plasma drug concentration (C

conclusionsThe pharmacokinetics and tolerability of GSK2982772 were similar between Western and Japanese subjects, justifying inclusion of Japanese subjects in future global clinical studies to assess the therapeutic potential of RIPK1 inhibition for the treatment of IMIDs. Clinical Trials: NCT03305419 and NCT03590613 available from http://www.clinicaltrials.gov .

Indexed as

Healthy VolunteersAdultAsian PeopleDouble-Blind MethodDrug Administration ScheduleFemaleHumansJapanMaleMiddle AgedOxazepinesReceptor-Interacting Protein Serine-Threonine KinasesTriazolesUnited KingdomWhite PeopleGSK2982772OxazepinesReceptor-Interacting Protein Serine-Threonine KinasesRIPK1 protein, humanTriazoles

Identifiers

PMID33165774
PMCPMC7811991
OpenAlexW3103260642

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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Registered trials

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.