Trial reportBritish journal of clinical pharmacology2017
Pharmacokinetics and pharmacodynamics of PF-05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects.
Trial report in British journal of clinical pharmacology, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers, 1 of them a synthesis that pooled 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.
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.
Who cites it
38 citing papers in PubMed, 1 synthesis or guideline pooled it, 55 citations in OpenAlex.
- An Overview of Appetite-Regulatory Peptides in Addiction Processes; From Bench to Bed Side.Frontiers in neuroscience · 2021Pooled it
- Pharmacokinetic and pharmacodynamic results from a randomized controlled study with the growth hormone secretagogue receptor blocker PF-5190457 in recently abstinent patients with alcohol use disorder.The international journal of neuropsychopharmacology · 2026Trial
- A randomized, double-blind, placebo-controlled study of a GHSR blocker in people with alcohol use disorder.JCI insight · 2024Trial
- Trial
- Pharmacokinetics and pharmacodynamics of PF-05190457: The first oral ghrelin receptor inverse agonist to be profiled in healthy subjects.British journal of clinical pharmacology · 2017Trial
- The Ghrelin-LEAP2 System in Obesity and Diabetes: Pathophysiological Roles and Therapeutic Potential.Current obesity reports · 2026Review
- Ghrelin's role in sleep and sleep deprivation: a narrative review.Frontiers in psychiatry · 2026Review
- Maximum likelihood estimation under the Emax model: existence, geometry and efficiency.Statistical papers (Berlin, Germany) · 2025Article
- Des-acyl ghrelin reduces alcohol intake and alcohol-induced reward in rodents.Translational psychiatry · 2024Article
- Genetic or pharmacological GHSR blockade has sexually dimorphic effects in rodents on a high-fat diet.Communications biology · 2024Article
- The intersection between ghrelin, metabolism and circadian rhythms.Nature reviews. Endocrinology · 2024Review
- Pharmacological GHSR (ghrelin receptor) blockade reduces alcohol binge-like drinking in male and female mice.Neuropharmacology · 2023Article
- Genetic or pharmacological GHSR blockade has sexually dimorphic effects in rodents on a high-fat diet.Research square · 2023Article
- Initial Pharmacological Characterization of a Major Hydroxy Metabolite of PF-5190457: Inverse Agonist Activity of PF-6870961 at the Ghrelin Receptor.The Journal of pharmacology and experimental therapeutics · 2023Article
- Pharmacotherapy for chronic obesity management: a look into the future.Internal and emergency medicine · 2023Review
- Advances in the Development of Nonpeptide Small Molecules Targeting Ghrelin Receptor.Journal of medicinal chemistry · 2022Review
- Review
- Molecular mechanism of agonism and inverse agonism in ghrelin receptor.Nature communications · 2022Article
- The Role of Ghrelin/GHS-R1A Signaling in Nonalcohol Drug Addictions.International journal of molecular sciences · 2022Review
- Off-label and investigational drugs in the treatment of alcohol use disorder: A critical review.Frontiers in pharmacology · 2022Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
aimTo evaluate safety, tolerability and pharmacokinetics of oral PF-05190457, an oral ghrelin receptor inverse agonist, in healthy adults.
methodsSingle (SAD) and multiple ascending dose (MAD) studies were randomised, placebo-controlled, double-blind studies. Thirty-five healthy men (age 38.2 ± 10.4 years; body mass index 24.8 ± 3.1 kg m
resultsPF-05190457 absorption was rapid with a T
conclusionsPF-05190457 is a well-tolerated first-in-class ghrelin receptor inverse agonist with acceptable pharmacokinetics for oral daily dosing. Blocking ghrelin receptors inhibits ghrelin-induced GH, and increases heart rate, effects that underwent tachyphylaxis with chronic dosing. PF-051940457 has the potential to treat centrally-acting disorders such as insomnia.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.