Evidence map›Paper›PMID 36365202›Full record

ArticlePharmaceutics2022

Ileocolonic-Targeted JAK Inhibitor: A Safer and More Effective Treatment for Inflammatory Bowel Disease.

Vipul Yadav, Aileen House, Silvia Matiz, Laura E McCoubrey, Kimberly A Bettano, Leena Bhave, Meiyao Wang, Peter Fan, Siqun Zhou, Janice D Woodhouse and 7 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
3.0field-weighted citation impact, top 8% 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

5 citing papers in PubMed, 16 citations in OpenAlex.

  1. From triggers to interfaces: polymer-stabilized nano-co-crystals for robust mesalazine delivery in UC.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2026
    Review
  2. Colon-targeted pH-responsive tofacitinib beads improve ulcerative colitis outcomes with lower systemic exposure.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2026
    Article
  3. Article
  4. Article
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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

17 authors at 4 institutions in 3 countries.

Vipul YadavIntract Pharma Ltd., London Bioscience Innovation Centre, 2 Royal College Street, London NW1 0NH, UK.
Aileen HouseMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Silvia MatizIntract Pharma Ltd., London Bioscience Innovation Centre, 2 Royal College Street, London NW1 0NH, UK.
Laura E McCoubreyUCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.
Kimberly A BettanoMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Leena BhaveMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Meiyao WangMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Peter FanMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Siqun ZhouMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Janice D WoodhouseMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Eirini Poimenidou90TEN, Battersea Studios, 80 Silverthorne Road, London SW8 3HE, UK.
Liu DouSchool of Pharmaceutical Sciences (Shenzhen), Sun Yat-Sen University, Guangzhou 510275, China.
Abdul W BasitUCL School of Pharmacy, University College London, 29-39 Brunswick Square, London WC1N 1AX, UK.ORCID 0000-0002-5368-6603
Lily Y MoyMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Robert SaklatvalaMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.ORCID 0000-0002-4548-3398
Laxminarayan G HegdeMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Hongshi YuMerck & Co., Inc., 126 East Lincoln Avenue, P.O. Box 2000, Rahway, NJ 07065, USA.
Merck & Co., Inc., Rahway, NJ, USA (United States) · USUniversity College London · GBBattersea Arts Centre · GBSun Yat-sen University · CN

Funding

Intract Pharma Ltd. EP/S023054/1Merck & Co., Inc. EP/S023054/1The Engineering and Physical Sciences Research Council EP/S023054/1
6 · The paper itself

Abstract

Janus kinase (JAK) inhibitors, such as tofacitinib (Xeljanz) and filgotinib (Jyseleca), have been approved for treatment of ulcerative colitis with several other JAK inhibitors in late-stage clinical trials for inflammatory bowel disease (IBD). Despite their impressive efficacy, the risk of adverse effects accompanying the use of JAK inhibitors has brought the entire class under scrutiny, leading to them receiving an FDA black box warning. In this study we investigated whether ileocolonic-targeted delivery of a pan-JAK inhibitor, tofacitinib, can lead to increased tissue exposure and reduced systemic exposure compared to untargeted formulations. The stability of tofacitinib in the presence of rat colonic microbiota was first confirmed. Next, in vivo computed tomography imaging was performed in rats to determine the transit time and disintegration site of ileocolonic-targeted capsules compared to gastric release capsules. Pharmacokinetic studies demonstrated that systemic drug exposure was significantly decreased, and colonic tissue exposure increased at 10 mg/kg tofacitinib dosed in ileocolonic-targeted capsules compared to gastric release capsules and an oral solution. Finally, in a rat model of LPS-induced colonic inflammation, targeted tofacitinib capsules significantly reduced concentrations of proinflammatory interleukin 6 in colonic tissue compared to a vehicle-treated control (

Indexed as

anti-inflammatorycolonic drug deliveryCrohn’s diseasedrug stabilityJAK inhibitorsPhloral film coating technologytargeting the large intestineulcerative colitis

Identifiers

PMID36365202
PMCPMC9698010
OpenAlexW4308548248

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.