Evidence map›Paper›PMID 37523014›Full record

ArticlePharmaceutical research2023

Evaluation of Encequidar as An Intestinal P-gp and BCRP Specific Inhibitor to Assess the Role of Intestinal P-gp and BCRP in Drug-Drug Interactions.

Jessica Chu, Erika Panfen, Linna Wang, Anthony Marino, Xue-Qing Chen, R Marcus Fancher, Raviraj Landage, Omprakash Patil, Salil Dileep Desai, Devang Shah and 3 more

Abstract read
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In one paragraph

Article in Pharmaceutical research, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
1.6field-weighted citation impact, top 14% 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

3 citing papers in PubMed, 7 citations in OpenAlex.

  1. Article
  2. Review
  3. 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

13 authors at 3 institutions in 3 countries.

Jessica Chu *Departments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Erika Panfen *Departments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Linna WangNonclinical Disposition & Bioanalysis, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Anthony MarinoDepartments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Xue-Qing ChenDiscovery Pharmaceutics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
R Marcus FancherDepartments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Raviraj LandagePharmaceutical Candidate Optimization, Biocon Bristol Myers Squibb R&D Centre (BBRC), Syngene International Ltd., Biocon Park, Bommasandra IV Phase, Bangalore, 560099, India.
Omprakash PatilPharmaceutical Candidate Optimization, Biocon Bristol Myers Squibb R&D Centre (BBRC), Syngene International Ltd., Biocon Park, Bommasandra IV Phase, Bangalore, 560099, India.
Salil Dileep DesaiPharmaceutical Candidate Optimization, Biocon Bristol Myers Squibb R&D Centre (BBRC), Syngene International Ltd., Biocon Park, Bommasandra IV Phase, Bangalore, 560099, India.
Devang ShahDepartments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Yongjun XueNonclinical Disposition & Bioanalysis, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Michael SinzDepartments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA.
Hong ShenDepartments of Drug Metabolism and Pharmacokinetics, Bristol Myers Squibb Research and Development, Princeton, NJ, 08543, USA. hong.shen1@bms.com.ORCID http://orcid.org/0000-0003-2185-4825
Bristol-Myers Squibb (United States) · USBristol-Myers Squibb (India) · INBristol-Myers Squibb (Germany) · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeThe differences between intestinal and systemic (hepatic and renal) P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) roles in drug disposition are difficult to define. Accordingly, we characterized Encequidar (ECD) as an intestinal P-gp and BCRP specific inhibitor to evaluate their role in drug disposition.

methodsWe assessed the in vitro and in vivo inhibition potential of ECD towards human and animal P-gp and BCRP.

resultsECD is a potent inhibitor with a high degree of selectivity in inhibiting human P-gp (hP-gp) over human BCRP (hBCRP) (IC

conclusionsECD may allow an in-depth appraisal of the role of intestinal efflux transporter(s) in drug disposition in animals and humans through local intestinal drug interactions.

Indexed as

ATP-Binding Cassette TransportersNeoplasm ProteinsAnimalsATP Binding Cassette Transporter, Subfamily G, Member 2Drug InteractionsHumansMacaca fascicularisPaclitaxelRatsATP-Binding Cassette TransportersATP Binding Cassette Transporter, Subfamily G, Member 2Neoplasm ProteinsPaclitaxelbreast cancer resistance proteindrug-drug interactionintestinal absorptionP-glycoprotein

Identifiers

PMID37523014
OpenAlexW4385406162

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.