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A first-in-human, double-blind, placebo-controlled, randomized, dose escalation study of DWP05195, a novel TRPV1 antagonist, in healthy volunteers

Overview of attention for article published in Drug Design, Development and Therapy, April 2017
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Title
A first-in-human, double-blind, placebo-controlled, randomized, dose escalation study of DWP05195, a novel TRPV1 antagonist, in healthy volunteers
Published in
Drug Design, Development and Therapy, April 2017
DOI 10.2147/dddt.s128727
Pubmed ID
Authors

Jieon Lee, Bo-Hyung Kim, Kyung-Sang Yu, Hee Sun Kim, Ji Duck Kim, Joo-Youn Cho, SeungHwan Lee, Namyi Gu

Abstract

DWP05195 is a transient receptor potential vanilloid 1 (TRPV1) antagonist developed for managing pain. The purpose of this study was to evaluate the pharmacodynamics pharmacokinetics, safety, and tolerability of DWP05195 in healthy subjects. This was a first-in-human randomized, double-blinded, placebo-controlled, dose escalation study. DWP05195 or placebo was administered as a single dose of 10-600 mg in the single-dose study and as 100-400 mg once daily for 8 days in the multiple-dose studies. Each study group consisted of 10 subjects (study drug-to-placebo ratio was 8:2). For pharmacodynamics assessment, the heat pain threshold (HPtr), heat pain tolerance (HPtol), perfusion intensity, and flare area ratio of cutaneous blood flow were measured. Safety and tolerability were evaluated throughout the study. The maximum plasma concentrations and area under the plasma concentration-time curve from zero to the last measurable time dose-dependently increased. HPtr and HPtol tended to increase more after DWP05195 administration than after placebo administration. HPtr and HPtol tended to dose-dependently increase after administration of DWP05195. Cutaneous blood flow was reduced as the dose of DWP05195 increased during the multiple-dose study. DWP05195 was well tolerated up to 600 and 400 mg single- and multiple-dose administrations, respectively. The pharmacological activity of DWP05195, measured using HPtr and HPtol, increased as expected in a dose-dependent manner owing to increased systemic exposure, indicating that DWP05195 can be used as a TRPV1 antagonist for pain management.

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Mendeley readers

Mendeley readers

The data shown below were compiled from readership statistics for 34 Mendeley readers of this research output. Click here to see the associated Mendeley record.

Geographical breakdown

Country Count As %
Unknown 34 100%

Demographic breakdown

Readers by professional status Count As %
Researcher 5 15%
Student > Bachelor 3 9%
Student > Master 3 9%
Lecturer 2 6%
Unspecified 2 6%
Other 5 15%
Unknown 14 41%
Readers by discipline Count As %
Neuroscience 4 12%
Agricultural and Biological Sciences 4 12%
Pharmacology, Toxicology and Pharmaceutical Science 3 9%
Biochemistry, Genetics and Molecular Biology 2 6%
Unspecified 2 6%
Other 6 18%
Unknown 13 38%
Attention Score in Context

Attention Score in Context

This research output has an Altmetric Attention Score of 1. This is our high-level measure of the quality and quantity of online attention that it has received. This Attention Score, as well as the ranking and number of research outputs shown below, was calculated when the research output was last mentioned on 24 February 2018.
All research outputs
#20,472,455
of 26,032,395 outputs
Outputs from Drug Design, Development and Therapy
#1,337
of 2,289 outputs
Outputs of similar age
#238,293
of 326,968 outputs
Outputs of similar age from Drug Design, Development and Therapy
#42
of 60 outputs
Altmetric has tracked 26,032,395 research outputs across all sources so far. This one is in the 18th percentile – i.e., 18% of other outputs scored the same or lower than it.
So far Altmetric has tracked 2,289 research outputs from this source. They typically receive a little more attention than average, with a mean Attention Score of 7.4. This one is in the 35th percentile – i.e., 35% of its peers scored the same or lower than it.
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We're also able to compare this research output to 60 others from the same source and published within six weeks on either side of this one. This one is in the 26th percentile – i.e., 26% of its contemporaries scored the same or lower than it.