PF-05190457 / Pfizer 
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 5 Diseases   0 Trials   0 Trials   33 News 
  • ||||||||||  PF-05190457 / Pfizer
    Preclinical, Journal:  Pharmacological GHSR (ghrelin receptor) blockade reduces alcohol binge-like drinking in male and female mice. (Pubmed Central) -  Aug 7, 2023   
    Systemic administration of the GHSR antagonists JMV2959, PF-5190457, PF-6870961, and HM-04 reduced alcohol intake in both male and female mice...These findings suggest that central GHSR mediates binge-like alcohol intake. These data reveal novel pharmacological compounds with translational potential in the treatment of AUD and provide further evidence of the GHSR as a potential treatment target for AUD.
  • ||||||||||  PF-05190457 / Pfizer
    Trial termination:  A Novel Compound for Alcoholism Treatment: A Translational Strategy - Part II (clinicaltrials.gov) -  Mar 16, 2022   
    P2,  N=42, Terminated, 
    Effective, patient-tailored treatment will require greater understanding provided by many more preclinical and clinical studies. Completed --> Terminated; Early termination of the study due to the COVID-19 pandemic
  • ||||||||||  ondansetron / Generic mfg., gabapentin / Generic mfg., disulfiram / Generic mfg.
    Review, Journal:  Novel Agents for the Pharmacological Treatment of Alcohol Use Disorder. (Pubmed Central) -  Mar 4, 2022   
    Importantly, these medications also offer potential improvements towards the advancement of precision medicine and personalized treatment for the heterogeneous AUD population. However, there remains a great need to improve access to treatment, increase the menu of approved pharmacological treatments, and de-stigmatize and increase treatment-seeking for AUD.
  • ||||||||||  PF-05190457 / Pfizer
    Journal:  Molecular mechanism of agonism and inverse agonism in ghrelin receptor. (Pubmed Central) -  Feb 15, 2022   
    Here, we report a crystal structure of the ghrelin receptor bound to the inverse agonist PF-05190457 and a cryo-electron microscopy structure of the active ghrelin receptor-Go complex bound to the endogenous agonist ghrelin...Combining the structural comparisons and cellular function assays, we find that a polar network and a notable hydrophobic cluster are required for receptor activation and constitutive activity. Together, our study provides insights into the detailed mechanism of ghrelin receptor binding to agonists and inverse agonists, and paves the way to design specific ligands targeting ghrelin receptors.
  • ||||||||||  PF-05190457 / Pfizer
    Trial completion, Trial completion date, Trial primary completion date:  A Novel Compound for Alcoholism Treatment: A Translational Strategy - Part II (clinicaltrials.gov) -  Sep 11, 2020   
    P2,  N=42, Completed, 
    PK/PD/behavioral findings support continued research of PF-5190457 as a potential pharmacological agent to treat alcohol use disorder. Recruiting --> Completed | Trial completion date: Dec 2020 --> Sep 2020 | Trial primary completion date: Dec 2020 --> Feb 2020
  • ||||||||||  PF-05190457 / Pfizer
    Review, Journal:  Ghrelin: From a gut hormone to a potential therapeutic target for alcohol use disorder. (Pubmed Central) -  May 7, 2020   
    PF-5190457, a GHS-R1a blocker, has been shown to be safe and tolerable when co-administered with alcohol...Collectively, the existing literature supports further examination of the ghrelin system as a therapeutic target for AUD. More research is also needed to understand the biobehavioral and molecular mechanisms underlying ghrelin's functions and to examine different interventional approaches to target the ghrelin system for AUD treatment.
  • ||||||||||  PF-05190457 / Pfizer
    Review, Journal:  Pharmacological Modulation of Ghrelin to Induce Weight Loss: Successes and Challenges. (Pubmed Central) -  Apr 15, 2020   
    PF-05190457 is the first inverse agonist of the ghrelin receptor tested in humans shown to inhibit growth hormone secretion, gastric emptying, and reduce postprandial glucose levels...Although various highly promising agents targeting ghrelin signaling exist, so far, they were mostly only tested in vitro or in animal models. Further research in humans is thus needed to further assess the effects of ghrelin antagonism on body weight especially under conditions of obesity.
  • ||||||||||  PF-05190457 / Pfizer
    Trial completion date, Trial primary completion date:  A Novel Compound for Alcoholism Treatment: A Translational Strategy - Part II (clinicaltrials.gov) -  Sep 26, 2019   
    P2,  N=55, Recruiting, 
    Further, the application of the method was demonstrated by measuring the concentration of PF-5190457 and its hydroxy metabolite in patient plasma samples from 100 mg dose. Trial completion date: Dec 2019 --> Dec 2020 | Trial primary completion date: Dec 2019 --> Dec 2020
  • ||||||||||  PF-05190457 / Pfizer
    Trial initiation date, Trial primary completion date:  A Novel Compound for Alcoholism Treatment: A Translational Strategy - Part II (clinicaltrials.gov) -  Oct 22, 2018   
    P2,  N=55, Recruiting, 
    Future research should investigate the potential mechanism(s) underlying this effect. Initiation date: Mar 2016 --> Jun 2016 | Trial primary completion date: Dec 2018 --> Dec 2019
  • ||||||||||  PF-05190457 / Pfizer
    Trial completion, Enrollment change, Trial primary completion date:  A Novel Compound for Alcoholism Treatment (clinicaltrials.gov) -  Oct 5, 2015   
    P1,  N=14, Completed, 
    Initiation date: Mar 2016 --> Jun 2016 | Trial primary completion date: Dec 2018 --> Dec 2019 Recruiting --> Completed | N=20 --> 14 | Trial primary completion date: Jun 2017 --> Oct 2015
  • ||||||||||  PF-05190457 / Pfizer
    Enrollment change:  A Novel Compound for Alcoholism Treatment (clinicaltrials.gov) -  Dec 7, 2014   
    P1,  N=20, Recruiting, 
    Recruiting --> Completed | N=20 --> 14 | Trial primary completion date: Jun 2017 --> Oct 2015 N=15 --> 20
  • ||||||||||  PF-05190457 / Pfizer
    New P1 trial:  A Novel Compound for Alcoholism Treatment (clinicaltrials.gov) -  Jan 15, 2014   
    P1,  N=15, Recruiting, 
  • ||||||||||  PF-05190457 / Pfizer
    Trial termination:  A Study Of PF-05190457 In Healthy Volunteers And Type-2 Diabetic Patients (clinicaltrials.gov) -  May 15, 2012   
    P1,  N=35, Terminated, 
    N=15 --> 20 Recruiting --> Terminated; B3301002 was discontinued on 18 April 2012 for strategic reasons.There were no safety concerns leading to discontinuation of this study.
  • ||||||||||  PF-05190457 / Pfizer
    Enrollment change:  A Study Of PF-05190457 In Healthy Volunteers And Type-2 Diabetic Patients (clinicaltrials.gov) -  May 15, 2012   
    P1,  N=35, Terminated, 
    Recruiting --> Terminated; B3301002 was discontinued on 18 April 2012 for strategic reasons.There were no safety concerns leading to discontinuation of this study. N=69 --> 35