Evidence map›Paper›PMID 33543763›Full record

Trial reportPain medicine (Malden, Mass.)2021

A Phase 1, Randomized, Double-Blind, Placebo-Controlled, Crossover Study to Evaluate the Pharmacodynamic Effects of VX-150, a Highly Selective NaV1.8 Inhibitor, in Healthy Male Adults.

Hemme J Hijma, Pieter S Siebenga, Marieke L de Kam, Geert Jan Groeneveld

Open access · bronzeAbstract readClinical Trial, Phase IRandomized Controlled Trial
In one paragraph

Trial report in Pain medicine (Malden, Mass.), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 36 papers.

0numbers the graph read from it
0cells of the map it votes in
36citing papers in PubMed
2.3field-weighted citation impact, top 11% 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

36 citing papers in PubMed, 52 citations in OpenAlex.

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  10. Discovery of MK-5661, a Once-Daily Oral NaACS medicinal chemistry letters · 2026
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  13. Suzetrigine, a NaMolecules (Basel, Switzerland) · 2026
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  19. Diabetic neuropathy: cutting-edge research and future directions.Signal transduction and targeted therapy · 2025
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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

4 authors at 2 institutions in 1 country.

Hemme J HijmaCentre for Human Drug Research, Leiden, The Netherlands.ORCID 0000-0001-7298-8650
Pieter S SiebengaCentre for Human Drug Research, Leiden, The Netherlands.
Marieke L de KamCentre for Human Drug Research, Leiden, The Netherlands.
Geert Jan GroeneveldCentre for Human Drug Research, Leiden, The Netherlands.
Leiden University Medical Center · NLCentre for Human Drug Research · NL

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

objectiveTo evaluate the analgesic potential, safety, tolerability, and pharmacokinetics of VX-150, a pro-drug of a highly selective NaV1.8 inhibitor, in healthy subjects.

designThis was a randomized, double-blind, placebo-controlled, crossover study in healthy subjects. SUBJECTS: Twenty healthy male subjects with an age of 18-55 years, inclusive, were enrolled. Eligibility was based on general fitness, absence of current or previous medical conditions that could compromise subject safety, and a training assessment of pain tolerance across pain tests to exclude highly tolerant individuals whose tolerance could compromise the ability to detect analgesic responses. All dosed subjects completed the study.

methodsSubjects were randomized 1:1 to one of two sequences receiving a single VX-150 dose and subsequently placebo, or vice versa, with at least 7 days between dosing. A battery of pain tests (pressure, electrical stair, [capsaicin-induced] heat, and cold pressor) was administered before dosing and repetitively up to 10 h after dosing, with blood sampling up to 24 h after dosing. Safety was monitored throughout the study. Data were analyzed with a repeated-measures mixed-effects model.

resultsVX-150 induced analgesia in a variety of evoked pain tests, without affecting subject safety. Significant effects were reported for the cold pressor and heat pain thresholds. Maximum median concentration for the active moiety was 4.30 µg/mL at 4 h after dosing.

conclusionResults of this proof-of-mechanism study are supportive of the potential of VX-150, a highly selective NaV1.8 channel inhibitor, to treat various pain indications.

Indexed as

AnalgesicsPain ThresholdVoltage-Gated Sodium Channel BlockersAdolescentAdultCross-Over StudiesDose-Response Relationship, DrugDouble-Blind MethodHumansMaleMiddle AgedNAV1.8 Voltage-Gated Sodium ChannelYoung AdultAnalgesicsNAV1.8 Voltage-Gated Sodium ChannelVoltage-Gated Sodium Channel BlockersExperimental PainNaV1.8-Selective InhibitorVX-150

Identifiers

PMID33543763
PMCPMC8346919
OpenAlexW3128674126

What OpenQuestion holds

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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.