Evidence map›Paper›PMID 29915999›Full record

ArticlePharmaceutical research2018

Fampridine is a Substrate and Inhibitor of Human OCT2, but not of Human MATE1, or MATE2K.

Guangqing Xiao, Christopher Rowbottom, Carri Boiselle, Liang-Shang Gan

Abstract read
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Article in Pharmaceutical research, 2018. 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
0.5field-weighted citation impact, top 32% 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, 10 citations in OpenAlex.

  1. Trial
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  3. Review
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  5. 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

4 authors at 3 institutions in 1 country.

Guangqing XiaoDepartment of Drug Metabolism and Pharmacokinetics, Takeda, 35 Landsdowne St, Cambridge, Massachusetts, 02139, USA. guangqing.xiao@takeda.com.ORCID http://orcid.org/0000-0002-1471-3955
Christopher RowbottomDepartment of Drug Metabolism and Pharmacokinetics, Biogen, Cambridge, Massachusetts, 02142, USA.
Carri BoiselleBDPK, Intellia Therapeutics, Cambridge, Massachusetts, 02139, USA.
Liang-Shang GanForesee Pharmaceuticals Co., LTD, Taipei City, Taiwan, 22180, Republic of China.
Biogen (United States) · USIntellia Therapeutics (United States) · USTakeda (United States) · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

purposeThe renal clearance of fampridine (Fampyra®, or Ampyra®) significantly exceeds the glomerular filtration rate, suggesting active renal secretion is likely the major elimination pathway. The goal of this study was to identify the renal transporters that are involved in the renal active secretion, and elucidate the active renal secretion mechanism of fampridine.

methodsThe uptake of fampridine to HEK-293 cells overexpressing human OCT2, MATE1 or MATE2K was determined in the absence and presence of Cimetidine, the prototypical inhibitor of the transporters. The inhibition potential of fampridine on the renal transporters was evaluated by determining the uptake of TEA and Metformin, the probe substrates of the transporters of OCT2 and MATEs, respectively, in the absence or presence of fampridine.

resultsSignificant time- and concentration-dependent uptake of fampridine by human OCT2 was observed. The K

conclusionThe studies indicated fampridine is a substrate and inhibitor of OCT2, but not MATE1 or MATE2K. Results from the study suggested the active renal secretion of fampridine is mediated by human OCT2 but not MATE1 or MATE2K. To our knowledge, fampridine is the first reported substrate specific to OCT2 but not to MATE1 or MATE2K.

Indexed as

4-AminopyridineBiological TransportHEK293 CellsHumansHypoglycemic AgentsMetforminOrganic Cation Transporter 2Organic Cation Transport ProteinsPotassium Channel Blockers4-AminopyridineHypoglycemic AgentsMetforminOrganic Cation Transporter 2Organic Cation Transport ProteinsPotassium Channel BlockersSLC22A2 protein, humanSLC47A1 protein, humanSLC47A2 protein, humandrug-drug interactionsfampridinemultidrug and toxin extrusion 1multidrug and toxin extrusion 2 Korganic cation transporter 2

Identifiers

PMID29915999
OpenAlexW2809250350

What OpenQuestion holds

Textmetadata
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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.